SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
He, Qinyang
Cheng, Yan
Zhuang, Guanglei
Abstract
The present invention provides a cyclin-dependent kinase degrader, a preparation method therefor and the use thereof. Particularly, the present invention provides compounds shown as formula I, the definition of each group being as described in the description. The compounds have excellent inhibitory activity on cyclin-dependent kinases (CDKs), and therefore can be used for preparing a pharmaceutical composition for treating blood cancer or solid tumor cancer.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Qiang
Huang, Gang
Sun, Jing
Abstract
A thermally curable modified polymer having high frequency and low dielectric constant, a synthesis method therefor and a use thereof. The thermally curable modified polymer has a monomer structure as shown in the following formula I. The thermally curable modified polymer can be widely applied to the fields of high-frequency communications, microelectronics industry, aerospace and the like as a low-dielectric-constant matrix resin or packaging material.
C08L 47/00 - Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, at least one having two or more carbon-to-carbon double bondsCompositions of derivatives of such polymers
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zuo, Zhiwei
Wen, Lu
Abstract
Disclose in the present invention is a method for preparing a chiral alcohol compound. The method comprises the following step: an achiral alcohol compound reacting in a solvent in the presence of a titanium catalyst, a ligand, and an alkali under illumination and anhydrous conditions to obtain the chiral alcohol compound. The method can successfully deracemize a series of achiral alcohols under photocatalysis to synthesize chiral alcohols by only one step of reaction only with the need for the addition of a titanium catalyst and a chiral ligand without the need for the addition of any additional oxidizing or reducing agent, and the reaction can well control the stereoselectivity of the reaction.
C07C 29/56 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by isomerisation
C07C 35/21 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a non-condensed ring
C07C 33/24 - Monohydroxylic alcohols containing only six-membered aromatic rings as cyclic part polycyclic without condensed ring systems
C07C 33/34 - Monohydroxylic alcohols containing six-membered aromatic rings and other rings
4.
CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Chinnaiyan, Arul M.
Wang, George X.
Chang, Yu
Tien, Jean
Ding, Ke
Yang, Jianzhang
Huang, Weixue
Wang, Zhen
Abstract
The present invention relates to a method for preparing a class of novel CDK12/13 covalent inhibitors or a pharmaceutical composition thereof, and use thereof. The class of novel CDK12/13 covalent inhibitors of the present invention have a structure shown in formula (I). Such compounds can serve as protein kinase inhibitors, can effectively and highly selectively inhibit the CDK12/13 protein kinase activity, and can inhibit the proliferation, migration, and invasion of various tumor cells.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Li, Zhanting
Yu, Shangbo
Feng, Ke
Cao, Jin
Zong, Yang
Lei, Zhuo
Guo, Peng
Tian, Jia
Qi, Qiaoyan
Abstract
Disclosed are a deuterated glycoluril tetramer compound having aryls incorporated at both ends, as shown in formula (1), and a pharmaceutical composition containing the compound. The deuterated compound can be used for antagonizing a clinically used non-depolarizing muscle relaxant. At the same dosage, the deuterated compound has significantly better antagonistic activity against rocuronium bromide and vecuronium bromide than sugammadex sodium, and has significantly better antagonistic activity against cisatracurium besylate and rocuronium bromide than a non-deuterated control molecule.
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
6.
CYCLIC 2-AMINOPYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ding, Ke
Ding, Jian
Chen, Hao
Geng, Meiyu
Lu, Xiaoyun
Xie, Hua
Wang, Zhen
Tong, Linjiang
Abstract
Provided are a cyclic 2-aminopyrimidine compound having a structure as shown in formula (I), or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof, and a use thereof. The compound can effectively inhibit the activity of EGFR protein kinase drug-resistant mutants (such as EGFRT790Mand EGFR19del/T790M/C797S), and can overcome the clinical drug resistance of patients suffering from tumors such as non-small cell lung cancer induced by existing third-generation selective EGFRT790M small molecule inhibitors Osimertinib(AZD9291), Olmutinib(HM6171), Rociletinib(CO-1686) and the like.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Yang, Shuailong
Zhao, Zhimin
Abstract
RIPK1 inhibitors for inhibiting necroptosis and their preparation methods. The RIPK1 inhibitors are as shown in general formula I, wherein, X1, X2, X3, X4, X5, Z1, Z2, Z3, L1, L2, L3, R, R1, ring D and n are as disclosed in the specification. Preparation methods of general formula I and the test results of inhibition of necroptosis and RIPK1 activity are also provided. The compounds in formula I can be used for used for treating and preventing inflammatory and degenerative diseases.
RIPK1 inhibitors for inhibiting necroptosis and their preparation methods. The RIPK1 inhibitors are as shown in general formula I, wherein, X1, X2, X3, X4, X5, Z1, Z2, Z3, L1, L2, L3, R, R1, ring D and n are as disclosed in the specification. Preparation methods of general formula I and the test results of inhibition of necroptosis and RIPK1 activity are also provided. The compounds in formula I can be used for used for treating and preventing inflammatory and degenerative diseases.
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Yuan, Junying
Li, Ying
Sun, Weimin
Tan, Li
Shan, Hengyue
Abstract
Provided are a series of compounds having the general formula as shown in formula (I), pharmaceutically acceptable salts, hydrates or solvates thereof, and a use of the compounds in combination with TRAIL in the treatment of tumors or inhibition of tumor cells. The pharmaceutical composition is used for resisting tumors, has the characteristics of good safety, strong tolerance, high sensitivity, etc., and is suitable for development of anti-tumor drugs.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
THE REGENTS OF THE UNIVERSITY OF MICHIGAN (USA)
LIVZON PHARMACEUTICAL GROUP INC. (China)
Inventor
Ding, Ke
Liu, Lianchao
Wang, Zhen
Chinnaiyan, Arul M.
Paroli, Abhijit
Abstract
The present invention provides an NSD protein degradation agent and a use thereof. Specifically, the present invention provides a compound having a structure as shown in formula (I) or a pharmaceutically acceptable salt thereof, or a stereoisomer or prodrug molecule thereof. The compound can degrade proteins such as NSD2, NSD1, NSD3, c-MYC, KLK3/PSA, AR, NKX3.1, and GSPT1 via target ubiquitination, and therefore can be used to treat indications related to abnormal expression of proteins such as NSD2, NSD1, NSD3, c-MYC, KLK3/PSA, AR, NKX3.1, and GSPT1.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
10.
CLASS OF PROGRAMMED CELL DEATH INHIBITORS, PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Yuan, Junying
Li, Ying
Qin, Ying
Abstract
The present invention provides a class of programmed cell death inhibitors, a preparation method therefor and a use thereof. Specifically, the present invention provides a compound, or a pharmaceutically acceptable salt, hydrate or solvate thereof, the compound being as shown in Formula I. The present invention also provides a method for preparing the compound and a pharmaceutical composition comprising the compound or a use thereof in treating or preventing diseases or conditions associated with programmed cell death and/or human receptor-interacting protein 1 kinase (RIPK1).
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Shengming
Xiao, Junzhe
Abstract
Disclosed are a preparation method for a 1,3-disubstituted allene compound at room temperature based on a metal carbene catalyst, comprising: reacting terminal alkynes, aldehydes and amines in an organic solvent under the action of a gold catalyst and a molecular sieve, and then synthesizing a 1,3-disubstituted allene compound at room temperature. The method of the present invention is simple to operate, raw materials and reagents are easily obtained, reaction conditions are mild, substrate universality is wide, functional group compatibility is good, yield is high (36-93%), the method is scalable (11 g), and practicability is strong. The 1,3-disubstituted allene compound obtained in the present invention may be used as an important intermediate to construct δ-caprolactone, trans-allyl alcohol, other allene-derived compounds and natural product molecules and the like.
C07C 2/86 - Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms by condensation between a hydrocarbon and a non-hydrocarbon
C07C 1/24 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from organic compounds containing only oxygen atoms as hetero atoms by elimination of water
C07C 1/26 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from organic compounds containing only halogen atoms as hetero atoms
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Yang, Shuailong
Abstract
The present disclosure relates to cyclic compounds as kinase inhibitors, a preparation method therefor and the use thereof. Specifically, provided in the present disclosure are compounds as shown in general formula I, in which ring A and ring B are as defined in the description and the claims. Also disclosed in the present disclosure are a preparation method for the compounds of general formula I and the effect of same in inhibiting the activities of a plurality of kinases, such as LRRK2 and tyrosine kinase. The compounds of general formula I of the present invention can be used for preparing drugs for treating kinase-related diseases, such as Parkinson's disease and carcinoma.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Dawei
Xu, Lanting
Li, Sailuo
Shao, Hua
Li, Xiang
Abstract
Provided in the present invention are a heterocyclic carboxylic acid hydrazide ligand and the use thereof in a copper-catalyzed aryl halide coupling reaction. Specifically, provided in the present invention is the use of a compound as shown in formula I below, wherein the definition of each group is as described in the description. The compound of formula I can be used as a ligand in the copper-catalyzed aryl halide coupling reaction, and is used for catalyzing a coupling reaction for forming aryl halides such as C-N, C-O, C-S and C-C bonds.
C07B 43/04 - Formation or introduction of functional groups containing nitrogen of amino groups
C07B 41/04 - Formation or introduction of functional groups containing oxygen of ether, acetal or ketal groups
C07B 45/06 - Formation or introduction of functional groups containing sulfur of mercapto or sulfide groups
C07C 233/56 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
C07C 237/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07D 225/08 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered rings
C07D 317/58 - Radicals substituted by nitrogen atoms
C07D 211/76 - Oxygen atoms attached in position 2 or 6
C07D 295/033 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
C07D 217/22 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 213/65 - One oxygen atom attached in position 3 or 5
C07D 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
14.
COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Shen, Qilong
Xu, Songsong
Li, Xuemiao
Wu, Jiang
Wu, Xudong
Wu, Lianjia
Xu, Yanfen
Abstract
0123455 is selected from at least one of an alkyl group having 1-10 carbon atoms, a phenyl group, and a substituted phenyl group; and Q- is a sulfonate anion substituted with a fluorine-containing group. Further provided in the present application are a preparation method for the compound, a composition using the compound, a film material, a device and an electronic apparatus. The compound provided in the present application is a combined onium salt material formed by simultaneously matching a benzothiophene cation, which uses a sulfur atom as the center and is substituted with a fluorine-containing group, with sulfonate anions substituted with different fluorine-containing groups; the structure thereof is stable; the sensitivity and the acid production efficiency of the compound can be effectively improved; moreover, illumination energy is reduced, and productivity is improved.
C07D 333/54 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C07D 333/56 - Radicals substituted by oxygen atoms
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 317/70 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with ring systems containing two or more relevant rings
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
THE REGENTS OF THE UNIVERSITY OF MICHIGAN (USA)
LIVZON PHARMACEUTICAL GROUP INC. (China)
Inventor
Ding, Ke
Chinnaiyan, Arul M.
Li, Chungen
Wang, Zhen
Qiao, Yuanyuan
Abstract
A PIKfyve protein degradation agent and the use thereof. Specifically, provided is a compound having the structure as represented by formula (I) or a pharmaceutically acceptable salt thereof, or a stereoisomer or a prodrug molecule thereof. The compound can target and degrade the PIKfyve protein by means of the ubiquitin-proteasome pathway, and therefore the compound can be used for treating indications mediated by the abnormal expression of the PIKfyve protein.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Liu, Guosheng
Yang, Wencheng
Peng, Haihui
Chen, Pinhong
Abstract
The present invention relates to phosphine ligands and the use thereof in carbonylation of acetylene/ethylene to synthesize acrylate/propionate. The phosphine ligands of the present invention are represented by formula (I), formula (II), formula (III), formula (IV), formula (V), formula (VI), formula (VII), and formula (VIII). The phosphine ligands can be combined with a palladium catalyst to jointly catalyze the carbonylation reaction of acetylene/ethylene to synthesize acrylate/propionate. The method has the characteristics of high catalytic efficiency, high product yield, high selectivity, simple and convenient operation, etc.
C07C 69/24 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with monohydroxylic compounds
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
THE REGENTS OF THE UNIVERSITY OF MICHIGAN (USA)
LIVZON PHARMACEUTICAL GROUP INC. (China)
Inventor
Ding, Ke
Chinnaiyan, Arul M.
Yang, Jianzhang
Chang, Yu
Zhou, Licheng
Zhou, Kaijie
Wang, George Xiaoju
Wang, Zhen
Huang, Weixue
Zhou, Fengtao
Abstract
The present invention relates to an aryl substituent-containing degradation agent for cyclin-dependent kinase 12/13 (CDK12/13), a preparation method therefor, and a pharmaceutical composition and use thereof. The degradation agent for CDK12/13 of the present invention has a structure represented by formula (I). The compound can be used as a protein kinase degradation agent, and can effectively and highly selectively degrade a CDK12/13 protein and inhibit proliferation, migration, and invasion of various tumor cells.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
He, Zhuohao
Zhu, Junjie
Abstract
Disclosed in the present invention are a polycyclic compound as a tubulin stabilizer and a preparation method therefor. The polycyclic compound has the structure as shown in general formula (I), wherein Ar, W, Z, X, Y and heterocyclic ring A are as defined in the specification. Also disclosed in the present invention is a preparation method for the compound. The compound of general formula (I) of the present invention can be used for preparing a drug for the treatment and prevention of tumors and neurodegenerative diseases.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
LIVZON PHARMACEUTICAL GROUP INC. (China)
Inventor
Ding, Ke
Lei, Chong
Liu, Rong
Wang, Yongxing
Huang, Weixue
Lu, Xuzhi
Abstract
Provided in the present invention are a compound having a skeleton structure as represented by formula (I) or a pharmaceutically acceptable salt, an isotope derivative and a solvate thereof, or a stereoisomer, a geometric isomer and a tautomer thereof, or a prodrug molecule, a metabolite and a pharmaceutical composition thereof, and the use thereof. The compound involved in the present invention can efficiently inhibit the kinase activity of HPK1, has a relatively strong signal inhibition effect on a downstream pathway thereof, can be used for preparing an anti-tumor drug, and can also be used for preparing a drug for preventing and treating inflammatory diseases.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
SHANGHAI TENTH PEOPLE'S HOSPITAL (China)
Inventor
Tang, Wenjun
Peng, Ai
Peng, Henian
Zhao, Dake
Abstract
Disclosed are a non-bipyridyl salt herbicide, a preparation method therefor, and a use thereof. Specifically, the present invention provides a diene diamine compound having the structure of formula (I) or a tricyclic diene piperazine structure represented by formula (II). The non-bipyridyl salt compound can be converted into paraquat or diquat under light and air conditions, has equivalent herbicidal properties to paraquat or diquat, and the toxicity thereof is not significant. Therefore, the non-bipyridyl salt compound of the present invention can be used as an herbicide as a non-toxic substitute for paraquat or diquat.
C07D 213/22 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing two or more pyridine rings directly linked together, e.g. bipyridyl
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Weichen
Yang, Shuailong
Abstract
Disclosed in the present invention are cyclic compounds used as multi-target kinase inhibitors and a preparation method therefor. The multi-target kinase inhibitors of the present invention are represented by general formula I, wherein R1, R2, R3, R3a, L1, L2, L3, ring A and ring B are shown in the description and claims. Further disclosed in the present invention are a preparation method for general formula I, and an activity inhibition test result thereof for inhibiting a plurality of kinases. The compounds of general formula I can be used for preparing drugs for treating neurodegenerative diseases, such as cancers and Parkinson's disease.
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ding, Ke
Zhang, Xin
Xu, Fang
Ren, Xiaomei
Lu, Xiaoyun
Ma, Dawei
Huang, Weixue
Abstract
The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.
The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
23.
Polymer Impurity Removal Method Based on Steam Distillation
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Zhou, Jiaolong
Zhao, Zehao
Tang, Yong
Sun, Xiuli
Zhu, Jie
Abstract
The present invention provides a method for depth removal of a volatile organic compound (VOC) in polymer resins and products thereof by means of a steam distillation method and apparatus thereof and significantly reducing the odor of the polymer resins and products thereof. The method provided in the present invention can further remove residual inorganic ash in the polymer resins. In the method, saturated steam at a certain temperature continuously keeps in contact with materials for a certain period of time, the VOC and an inorganic small molecule (ash) adsorbed on the surface of a polymer and wrapped inside the polymer are promoted to be enriched in a gas phase or a liquid phase and discharged, so as to reduce the VOC and ash in polymer materials, and the odor of the polymer resins or materials is decreased to a better level.
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIVERSITY SCHOOL OF MEDICINE (China)
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Li, Peiying
Li, Yan
Zou, Chengyu
Yu, Weifeng
Chen, Chen
Abstract
Provided in the present invention is the use of a macrophage migration inhibitory factor (MIF), RIPK1, an MIF inhibitor and an RIPK1 inhibitor in perioperative ischemic brain injuries. The present invention discloses the key functions of MIF secreted by macrophages in promoting a perioperative inflammatory response and activating RIPK1-mediated apoptosis and necroptosis of brain microvascular endothelial cells, which provides a new potential therapeutic target for perioperative ischemic brain injuries, and provides a new method for synergistically relieving and/or preventing perioperative ischemic brain injuries using the MIF inhibitor and the RIPK1 inhibitor.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Zhang, Jian
Cao, Jinrui
Abstract
The present invention relates to a novel oleanamide derivative for activating a KEAP/NRF2/ARE signaling pathway. The compound of the present invention is represented by general formula (I), wherein L, R3, R4, Z, and n are set forth in the description specification and the claims. Also disclosed are a method for preparing the compound represented by general formula I and an activity test result thereof for activating the KEAP/NRF2/ARE signaling pathway. The compound represented by general formula (I) of the present invention can be used for treating and preventing multiple sclerosis (MS), Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), Friedreich's ataxia (FRDA), spinal muscular atrophy (SMA), neuromyelitis optica (NMO), spinocerebellar ataxia (SCA), and other neurodegenerative diseases, and can also be used for treating cerebral apoplexy, autoimmune diseases, diabetes, kidney diseases, and other chronic diseases.
C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
26.
CHEMICAL-ENZYME COUPLING METHOD FOR SYNTHESIZING ERGOTHIONEINE
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Lin, Liang
Lv, Long
Jiang, Yan
Wu, Yaming
Song, Shucheng
Sun, Lili
Ding, Xiaoran
Abstract
Provided is a chemical-enzyme coupling method for synthesizing ergothioneine. The method comprises the steps of chemically synthesizing histidine betaine, and synthesizing ergothioneine from the histidine betaine by using Schizosaccharomyces pombe ergothioneine synthetases SPEGT1-tr M10 and SPEGT2 M3 after directed evolution.
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Tan, Li
Li, Ying
Qin, Ying
Qi, Chunting
Xiang, Huaijiang
Abstract
The present invention provides a programmed cell necrosis inhibitor, a preparation method therefor, and a use thereof. Specifically, the present invention provides a compound, or a pharmaceutically acceptable salt, hydrate, or solvent thereof, wherein the compound is as represented by formula I. The present invention further provides a preparation method for the compound and a pharmaceutical composition containing same, or a use of the compound in treatment or prevention of diseases or disorders related to programmed cell necrosis and/or human receptor interacting protein kinase 1 (RIPK1).
The present invention provides a programmed cell necrosis inhibitor, a preparation method therefor, and a use thereof. Specifically, the present invention provides a compound, or a pharmaceutically acceptable salt, hydrate, or solvent thereof, wherein the compound is as represented by formula I. The present invention further provides a preparation method for the compound and a pharmaceutical composition containing same, or a use of the compound in treatment or prevention of diseases or disorders related to programmed cell necrosis and/or human receptor interacting protein kinase 1 (RIPK1).
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY , CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhao, Yanchuan
Meng, Huan
Chen, Yixuan
Xu, Zhenchuang
Abstract
The present invention provides a recyclable hypervalent iodine reagent having a high reactivity. Specifically, the invention provides a hypervalent iodine reagent capable of realizing high-selectivity coupling, and a method for preparing the reagent. The method of the present invention is mild in terms of conditions, simple to operate, wide in terms of substrate range and low in terms of cost, has high selectivity and reactivity in subsequent application reactions, uses recoverable raw materials, and is suitable for large-scale production.
C07D 261/10 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
29.
BENZO[C]CINNOLINE SKELETON DIIMIDE LIGAND AND PREPARATION METHOD THEREFOR
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Xiaoming
Yang, Yang
Chen, Hongda
Qi, Xiaolong
Abstract
Disclosed in the present invention are a benzo[c]cinnoline skeleton diimide ligand and a preparation method therefor. The ligand has the structure represented by general formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 are as described in the description. The preparation method of the present invention is simple, the benzo[c]cinnoline skeleton diimine ligand can be prepared, the ligand can be used as a catalyst for catalytic reaction, and the ligand has economic practicability and industrial application prospects.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Liu, Jun O.
Datan, Emmanuel
Pomper, Martin Gilbert
Minn, Il
Xu, Peng
Yu, Biao
Abstract
A major hurdle in the treatment of cancer is chemoresistance induced under hypoxia that is characteristic of tumor microenvironment. Triptolide, a potent inhibitor of eukaryotic transcription, possesses potent antitumor activity. However, its clinical potential has been limited by toxicity and water solubility. To address those limitations of triptolide, the present disclosure designed and synthesized glucose-triptolide conjugates (glutriptolides) and demonstrated their antitumor activity in vitro and in vivo. The glutriptolides disclosed herein possess improved stability in human serum, greater selectivity towards cancer over normal cells and increased potency against cancer cells. Importantly, the glutriptolides are more potent against cancer cells under hypoxic conditions in contrast to existing cytotoxic drugs. These glutriptolides also exhibit sustained antitumor activity, prolonging survival in a prostate cancer metastasis animal model. Together, these findings suggest a new strategy to overcome chemoresistance through conjugation of cytotoxic agents to glucose.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Hong, Miao
Sun, Yangyang
Xia, Yongliang
Yuan, Pengjun
Abstract
Disclosed in the present invention is a method for preparing a sulphur-containing polymer based on isomerisation-driven irreversible ring-opening polymerisation. The method comprises: in an organic solvent and in the presence of a main catalyst, implementing a polymerisation reaction of one or more polymerisable monomers, wherein the main catalyst is an anionic main catalyst or a cationic main catalyst; the anionic main catalyst is a phosphazene base, guanidine organic base, amidine organic base, N-heterocyclic carbene organic base, N-heterocyclic olefin organic base, carboxylate, or thiocarboxylate; and the cationic main catalyst is a zwitterionic pair catalyst, a neutral Lewis acid type catalyst, or a proton acid (ester) type catalyst; and the polymerisable monomer is a five-membered ring skeleton compound as shown in formula I. The present method provides convenience for the industrial production of environmentally-friendly sulphur-containing polymer materials. The synthesised sulphur-containing polymer has the advantages of high molecular weight, a wide range of adjustable physical properties, and excellent degradability, and can be used for plastic, rubber, elastomer, and fibre products.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Wenjun
Xu, Siyao
Abstract
Provided is a metal complex as represented by formula I. The metal complex may be used as a catalyst for asymmetric catalytic hydrogenation, is capable of efficiently catalyzing and synthesizing a series of chiral p-aryl amides having high optical purity, and is especially capable of asymmetrically catalyzing and hydrogenating a tetra-substituted enamide compound, chiral amides having high optical purity are synthesized, and the carrying amount of ligand may reach 100,000.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Shengming
Xiao, Junzhe
Abstract
Disclosed are a preparation method for a 1,3-disubstituted allene compound at room temperature based on a metal carbene catalyst, comprising: reacting terminal alkynes, aldehydes and amines in an organic solvent under the action of a gold catalyst and a molecular sieve, and then synthesizing a 1,3-disubstituted allene compound at room temperature. The method of the present invention is simple to operate, raw materials and reagents are easily obtained, reaction conditions are mild, substrate universality is wide, functional group compatibility is good, yield is high (36-93%), the method is scalable (11g), and practicability is strong. The 1,3-disubstituted allene compound obtained in the present invention may be used as an important intermediate to construct δ-caprolactone, trans-allyl alcohol, other allene-derived compounds and natural product molecules and the like.
C07B 37/00 - Reactions without formation or introduction of functional groups containing hetero atoms, involving either the formation of a carbon-to-carbon bond between two carbon atoms not directly linked already or the disconnection of two directly linked carbon atoms
C07C 2/86 - Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms by condensation between a hydrocarbon and a non-hydrocarbon
C07C 15/44 - Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic part substituted by unsaturated hydrocarbon radicals monocyclic the hydrocarbon substituent containing a carbon-to-carbon double bond
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Yang, Shuailong
Zhao, Zhimin
Abstract
Disclosed are a RIPK1 inhibitor that inhibits programmed cell necrosis and a preparation method therefor. The disclosed RIK1 inhibitor is represented by general formula I, where X1, X2, X3, X4, X5, Z1, Z2, Z3, L1, L2, L3, R, R1, ring D and n are shown in the description and claims. Further disclosed are a method for preparing general formula I and an activity test result of inhibition of programmed cell necrosis and RIPK1. The compound of general formula I of the present invention can be used to prepare drugs for treating and preventing inflammation and degenerative diseases.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhang, Xingang
Min, Qiaoqiao
Feng, Xiaotian
Gao, Xing
Ren, Jinxiu
Abstract
Provided are a 3, 3-difluoroallylic onium salt as represented by formula (C), and a preparation method of the substance. Cheap industrial raw materials are used to prepare the important fluorine-containing reagent, which can be used as an α,α-gem-difluoroallylation reagent. The present invention provides a more universal and cheap new method for α,α-gem-difluoroallylation, and is high in efficiency and good in application prospects.
C07C 17/263 - Preparation of halogenated hydrocarbons by reactions involving an increase in the number of carbon atoms in the skeleton by condensation reactions
C07C 22/08 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings containing fluorine
C07C 25/24 - Halogenated aromatic hydrocarbons with unsaturated side chains
C07C 69/65 - Halogen-containing esters of unsaturated acids
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07C 69/92 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/50 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
C07C 319/20 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
C07C 323/09 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and halogen atoms, or nitro or nitroso groups bound to the same carbon skeleton having sulfur atoms of thio groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Chen, Yelin
Su, Tonghui
Lu, Yi
Fu, Chaoying
Geng, Yang
Abstract
An application of GluN2A and an NMDA receptor containing GluN2A as targets in screening antidepressant drugs, which may achieve rapid and low-cost screening of antidepressant drugs. Specifically, provided is a use of GluN2A, a binding fragment thereof or an NMDA receptor containing GluN2A in screening antidepressant drugs or in the preparation of a reagent for screening antidepressant drugs. Also provided are a method and apparatus for screening antidepressant drugs, and a kit.
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
37.
METHOD FOR SYNTHESIZING MOLECULAR GLASS, AND USE THEREOF AS HIGH-FREQUENCY LOW-DIELECTRIC-CONSTANT MATERIAL
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Qiang
Huang, Gang
Sun, Jing
Abstract
The present invention provides a method for synthesizing molecular glass, and the use thereof as a high-frequency low-dielectric-constant material. Specifically, the present invention provides a molecular glass monomer, which has a molecular structure as shown in formula (I) below. The molecular glass monomer has excellent processability and can form an infusible and insoluble resin after a high-temperature treatment; and such molecular glass only displays a glass transition but no melting point when heated, which is similar to an amorphous state. In the present invention, the resin obtained after the molecular glass is cured has high heat resistance and low water absorption, especially shows an excellent dielectric constant and dielectric loss at a high frequency, and can be widely used as a low-dielectric-constant matrix resin or packaging material in fields including high-frequency communication, the microelectronic industry, aerospace, etc.
C07D 251/22 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
C08F 112/34 - Monomers containing two or more unsaturated aliphatic radicals
38.
METHOD FOR CAPTURING MODIFIED NUCLEIC ACID AND APPLICATION THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Liu, Nan
Niu, Kongyan
Abstract
A method for capturing a modified nucleic acid and an application thereof are involved. Specifically provided are a method for capturing an NAD cap-modified RNA or enriching an NAD cap-modified RNA in a sample. The method comprises making a compound as represented by formula (I) be in contact with a sample to be tested, wherein the contact is performed under the presence of adenosine diphosphate ribosyl cyclase, said sample contains the NAD cap-modified RNA, and in X-L-B (I), X represents a nucleophilic group, L represents a linking group, B represents biotin or desthiobiotin, and X is connected to B by means of L.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
LIVZON PHARMACEUTICAL GROUP CO., LTD (China)
Inventor
Ding, Ke
Ma, Dawei
Zhang, Zhang
He, Sheng
Song, Zhiqiang
He, Rui
Bai, Yu
Huang, Jing
Huang, Weixue
Zhou, Fengtao
Wang, Yongxing
Abstract
The present invention provides a protein kinase degradant and use thereof. Specifically, the present invention provides a compound having a structure represented by formula (I) or a pharmaceutically acceptable salt thereof, or a stereoisomer or prodrug molecule thereof. The compound can perform ubiquitination and degradation on AXL, FLT3, AURORA-A, AURORA-B, B-RAF, A-RAF, MET, LCK, MEK2, and other proteins in a targeted mode, and thus can be used for the treatment of indications related to abnormal expression of proteins such as AXL, FLT3, AURORA-A, AURORA-B, B-RAF, A-RAF, MET, LCK, and MEK2.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhu, Jidong
Chen, Yelin
Geng, Yang
Cao, Hengyi
Li, Shiyun
Li, Ziwen
Wang, Qiuyan
Su, Tonghui
Fu, Chaoying
Abstract
22 are as described herein. The present invention also provides a pharmaceutical composition comprising these compounds, and use of these compounds in the preparation of a drug for treating or preventing NMDA receptor-mediated diseases.
C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Cao, Jinrui
Abstract
Disclosed in the present invention are an RIPK1 inhibitor for inhibiting programmed cell death and a preparation method therefor. The RIPK1 inhibitor of the present invention is as represented by general formula I, wherein X, Y, Z, L, R1, R2, R3, R4, a ring A, a ring B, and n are as shown in the description and claims. Further disclosed in the present invention are a preparation method of general formula I and an activity test result of general formula I for inhibiting programmed cell death and RIPK1. The compound of general formula I of the present invention can be used for preparing a drug for the treatment and prevention of inflammatory and degenerative diseases.
C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Wenyuan
Wang, Zhaoyin
Zhang, Lin
Abstract
22) group or modified with a hydroxylamine group, and a drug molecule B having a maleimide group or modified with a maleimide group according to any sequence so as to obtain the antibody-drug conjugate. The method provided in the present invention can efficiently prepare the antibody-drug conjugate with reduced drug resistance and improved efficacy by means of a one-pot method.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
43.
Class of phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Shengming
Liu, Qi
Xu, Haibo
Abstract
The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ding, Ke
Zhang, Xin
Xu, Fang
Ren, Xiaomei
Lu, Xiaoyun
Ma, Dawei
Huang, Weixue
Abstract
Provided are a pyridopyrimidine-based compound having the structure as represented by formula (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof, and an application thereof. The compound can efficiently and highly selectively degrade an AKT3 protein in cells and have no effect on AKT1/2, such that the proliferation of tumor cells mediated by high expression of an AKT3 protein can be significantly inhibited, and thus the compound can be used in the preparation of a drug for treating cancers related to abnormal expression of an AKT3 protein and other related diseases.
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
46.
HETEROARYL-FUSED BICYCLIC COMPOUND AS RIP1-KINASE INHIBITORS AND USES THEREOF
C07D 498/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
47.
INHIBITORS FOR PROGRAMMED CELL NECROSIS AND PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Qin, Ying
Abstract
Provided in the present invention are inhibitors for programmed cell necrosis, a preparation method therefor and a use thereof. Specifically, provided in the present invention are a compound represented by formula I and a composition comprising same. The described compound may be used to prepare a pharmaceutical composition for the prevention and/or treatment of diseases involving cell death and/or inflammation.
Provided in the present invention are inhibitors for programmed cell necrosis, a preparation method therefor and a use thereof. Specifically, provided in the present invention are a compound represented by formula I and a composition comprising same. The described compound may be used to prepare a pharmaceutical composition for the prevention and/or treatment of diseases involving cell death and/or inflammation.
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
48.
PHARMACEUTICAL COMPOSITION FOR TREATMENT OF NEURODEGENERATIVE DISEASES OR DISEASES CAUSED BY ABNORMALITY OF RNA BINDING PROTEIN AND APPLICATIONS THEREOF
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Fang, Yanshan
Duan, Yongjia
Abstract
Disclosed are a pharmaceutical composition for treatment of neurodegenerative diseases or diseases caused by abnormality of RNA binding protein and applications thereof, in particular the application in the treatment of ALS. The pharmaceutical composition can significantly enhance the dynamic performance of stress particles containing RNA binding proteins such as hnRNP A1 and TDP-43 proteins; influences the interaction between the RNA binding proteins and other poly ADP ribosylation modified proteins or other PAR binding proteins; influences the subcellular localization and stress response of RNA binding proteins; influences the liquid-liquid phase separation and aggregation tendency of RNA binding proteins; influences the co-phase separation between RNA binding proteins; influences the interaction of RNA binding proteins in cells; and has a significant inhibitory effect on neurotoxicity caused by RNA binding proteins.
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhu, Benhu
Su, Wei
Tan, Kai
Tang, Yong
Zhou, Jiaolong
Li, Junfang
Sun, Xiuli
Peng, Aiqing
Abstract
Provided is ultra-high-molecular-weight polyethylene particles. The particle size of the particles is less than that of a conventional commercially available ultra-high-molecular-weight polyethylene, and the density of the particles is small. In particular, provided is microparticles having properties as shown below: (a) the viscosity average molecular weight being in the range of 1.5 to 8 million; (b) the fraction by weight through a 100-mesh screen being at least 85% or more, with the median particle size (d50) being 80 μm ≤ d50 ≤ 110 μm; (c) the powder bulk density being 0.20 to 0.30 g/cm3; and (d) the number of branches per 100,000 backbone carbon atoms being less than 1. The ultra-high-molecular-weight polyethylene particles provided by the present invention are suitable for producing microporous filter materials.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Li, Ying
Qin, Ying
Qi, Chunting
Xiang, Huaijiang
Abstract
The present invention provides a programmed cell necrosis inhibitor, a preparation method therefor, and a use thereof. Specifically, the present invention provides a compound, or a pharmaceutically acceptable salt, hydrate, or solvent thereof, wherein the compound is as represented by formula I. The present invention further provides a preparation method for the compound and a pharmaceutical composition containing same, or a use of the compound in treatment or prevention of diseases or disorders related to programmed cell necrosis and/or human receptor interacting protein kinase 1 (RIPK1).
C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Qiang
Liu, Fengping
Sun, Jing
Abstract
The present invention relates to a siloxane having a low dielectric constant and low dielectric loss at high frequencies, and a preparation method therefor and a use thereof. Specifically disclosed is a siloxane monomer. A resin obtained by curing the monomer has a low dielectric constant and low dielectric loss at high frequencies, high heat resistance, good processability and a low water absorption rate, and is particularly suited for use in preparing high-frequency circuit boards.
C07F 7/08 - Compounds having one or more C—Si linkages
C08F 130/08 - Homopolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and containing phosphorus, selenium, tellurium or a metal containing a metal containing silicon
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Cao, Chunyang
Ji, Yonghua
Liu, Xinlian
Tao, Jie
Zhang, Shuzhang
Wang, Chunxi
Abstract
Anti-epileptic toxin Martentoxin (MarTX), derivatives thereof, and uses thereof are described. Specifically, the use of Martentoxin or an active fragment thereof or a pharmaceutically acceptable salt thereof in preparing a preparation or composition for treating and/or preventing epilepsy is described. It has been confirmed for the first time that the Martentoxin can effectively treat and/or prevent epileptic symptoms.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhu, Benhu
Su, Wei
Zhou, Jiaolong
Tang, Yong
Tan, Kai
Li, Junfang
Peng, Aiqing
Sun, Xiuli
Abstract
Provided in the present invention are extra-high to ultra-high molecular weight polyethylene particles and a catalyst for preparing same. Specifically, provided in the present invention is particles having the following characteristics: (a) a viscosity-average molecular weight ranging from 50 to 10 millions; (b) at least 95% of the particles in weight ratio passing through a 150 micron mesh sieve, in which the median particle diameter (d50) is 40 μm ≤ d50 ≤ 80 μm; (c) the branched chain content of backbone carbon atoms being less than 1/100,000C; and (d) primary crystallinity > 70%, and secondary crystallinity > 55%. Also provided in the present invention are a special catalyst for preparing such high molecular weight polyethylene particles and a preparation method therefor, and an extra-high to ultra-high molecular weight polyethylene prepared by using said catalyst.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Li, Ying
Zhou, Shaoqing
Zhuang, Guanglei
Abstract
12123455 and n are as defined in the description. The compound of the present invention has a high inhibitory activity and high specificity for PKM2 and is well suited for the preparation of a drug inhibiting tumors by inhibiting a PKM2 pathway.
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Wenjun
Xu, Guangqing
Zhou, Mingkang
Abstract
Disclosed in the present invention are a diboron glycol ester, a preparation method therefor, an intermediate thereof, and an application thereof. The diboron glycol ester can be used for inducing a reduction coupling reaction in which imine is used as a substrate, and the substrate can be obtained by reacting aldehyde with ammonia, is very easy to obtain, and has a quite low cost; a product can be separated from a reaction system only by an acid-base operation, without needing column chromatography purification, so that the post-treatment mode is convenient and fast, and the operation is easy; and the obtained product has a high yield and no protective group operation is needed. The diboron glycol ester has chirality, the stereoselectivity of the reduction coupling reaction is generally excellent, and 99% ee of chiral diamine can be obtained only by simple recrystallization. The diboron glycol ester can be obtained by reacting diol and diboron glycol ester; and the diol is convenient to prepare and easy to amplify, and can be recycled from reaction liquid by means of a simple acid-base operation, the recovery rate is up to 95%, and preparation costs are further saved.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Liu, Jun O.
Datan, Emmanuel
Pomper, Martin Gilbert
Minn, Il
Xu, Peng
Yu, Biao
Abstract
in vitroin vivoin vivo. The glutriptolides disclosed herein possess improved stability in human serum, greater selectivity towards cancer over normal cells and increased potency against cancer cells. Importantly, the glutriptolides are more potent against cancer cells under hypoxic conditions in contrast to existing cytotoxic drugs. These glutriptolides also exhibit sustained antitumor activity, prolonging survival in a prostate cancer metastasis animal model. Together, these findings suggest a new strategy to overcome chemoresistance through conjugation of cytotoxic agents to glucose.
A61K 47/51 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
57.
COMPOUND FOR REGULATING GENE EDITING EFFICIENCY AND APPLICATION THEREOF
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
SHANGHAITECH UNIVERSITY (China)
Inventor
Liu, Jia
Dong, Jiajia
Abstract
A compound for improving the gene editing specificity and application thereof. Specifically disclosed is a compound represented by formula I or a use of a pharmaceutically acceptable salt thereof. The compound and the pharmaceutically acceptable salt thereof are used for preparing an inhibitor, a composition, or a formulation for inhibiting gene editing and/or improving the gene editing specificity. The structure of the formula I is as stated in the description. The compound can significantly improve the accuracy of CRISPR gene editing, thereby providing a simple and high-efficient policy for accurate gene editing.
C12N 15/90 - Stable introduction of foreign DNA into chromosome
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
TIANJIN INSTITUTE OF INDUSTRIAL BIOTECHNOLOGY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Qiang
Chen, Xingrong
Wang, Qinhong
Sun, Jing
Gu, Qun
Hou, Jiaren
Gao, Junfei
Fang, Linxuan
Abstract
Synthesis and use of a protocatechuic acid-based epoxy resin. Specifically, a protocatechuic acid epoxidized monomer has a structure as shown in the following formula (I). The monomer can be cured to form a protocatechuic acid epoxy resin, thereby being used for preparing aerospace special materials.
C08G 59/32 - Epoxy compounds containing three or more epoxy groups
C07D 301/28 - Condensation of epihalohydrins or halohydrins with compounds containing active hydrogen atoms by reaction with hydroxyl radicals
C07D 301/30 - Condensation of epihalohydrins or halohydrins with compounds containing active hydrogen atoms by reaction with carboxyl radicals
C07D 303/30 - Ethers of oxirane-containing polyhydroxy compounds in which all hydroxyl radicals are etherified with oxirane-containing hydroxy compounds
59.
CLASS OF CDK INHIBITOR BASED ON ORGANIC ARSINE, PREPARATION METHOD AND APPLICATION THEREOF
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Li, Ying
Zhou, Shaoqing
Zhuang, Guanglei
Abstract
Provided is a class of CDK inhibitor based on organic arsine, a preparation method, and an application thereof. Specifically, provided is a compound represented by formula I, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a hydrate, or a solvate thereof. Also provided is a preparation method and an application thereof. Each group in the formula is as defined in the specification.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhou, Jiaolong
Zhao, Zehao
Tang, Yong
Sun, Xiuli
Zhu, Jie
Abstract
The present invention provides a method for depth removal of a volatile organic compound (VOC) in polymer resins and products thereof by means of a steam distillation method and apparatus thereof and significantly reducing the odor of the polymer resins and products thereof. The method provided in the present invention can further remove residual inorganic ash in the polymer resins. In the method, saturated steam at a certain temperature continuously keeps in contact with materials for a certain period of time, the VOC and an inorganic small molecule (ash) adsorbed on the surface of a polymer and wrapped inside the polymer are promoted to be enriched in a gas phase or a liquid phase and discharged, so as to reduce the VOC and ash in polymer materials, and the odor of the polymer resins or materials is decreased to a better level.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Chai, Yongshuai
Abstract
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 215/14 - Radicals substituted by oxygen atoms
C07D 401/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing alicyclic rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
62.
PHENYLTHIOPHENE SULFONAMIDE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Renxiao
Hong, Ran
Fan, Wenjie
Tian, Jie
Li, Yan
Zhou, Mi
Li, Qing
Kong, Wenna
Li, Yangfeng
Li, Jie
Abstract
Disclosed herein are phenylthiophene sulfonamide compounds, pharmaceutical compositions, a preparation method therefor and use thereof. The compounds of the present invention are capable of effectively and selectively inhibiting Bcl-xL, Bcl-2 or Mcl-1, particularly Mcl-1, in the critical protein Bcl-2 family during apoptosis at the molecular level. At the same time, they have obvious killing effect and high selectivity against cancer cells, especially human cervical cancer cell HeLa, human acute lymphocytic leukemia cell line RS4; 11 or human promyelocytic leukemia cell line HL-60, have the potential to be prepared as a new anti-tumor medicament, and have a good market prospect.
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
C07C 43/29 - Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing halogen
C07C 43/295 - Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing hydroxy or O-metal groups
C07C 217/90 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a six-membered aromatic ring, e.g. amino-diphenylethers
C07C 205/38 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a six-membered aromatic ring, e.g. nitrodiphenyl ethers
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Dong, Jiajia
Sharpless, Karl Barry
Meng, Genyi
Guo, Taijie
Ma, Tiancheng
Abstract
The present invention provides a high throughput method for constructing and screening a compound library and a reaction device. Specifically, the method of the present invention comprises: (a) providing a reactor comprising n independent and addressable reaction chambers; (b) performing m independent synthesis reactions in said n reaction chambers, thereby constructing a compound library; and (c) performing activity tests in reaction chambers in which synthesis reactions are performed. In the present invention, the preparation and screening processes of a compound can be completed in the same reaction system. As the reactions of the present invention almost quantitatively generate products, the products can be directly used in enzymatic or even cytological activity test experiments without separation.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Shengming
Liu, Qi
Xu, Haibo
Abstract
Disclosed are a phosphine nitrogen ligand having multiple chiral centers, a synthesis method therefor and use thereof. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials by means of a simple five-step reaction, and the finally obtained diastereomeric product can be separated only by means of simple column chromatography or recrystallization. The synthesized chiral phosphine nitrogen ligand of the present invention can be used for catalyzing an asymmetric three-component coupling reaction of a terminal alkyne, an aldehyde and an amine, thereby realizing the efficient preparation of a chiral propargylamine compound having high optical activity.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Qiang
Wang, Yuanqiang
Sun, Jing
Abstract
The present invention provides a colorless polyimide of which a chemical structural formula is as shown in formula (II), and a preparation method and application of the polyimide.
C08G 65/40 - Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from hydroxy compounds or their metallic derivatives derived from phenols from phenols and other compounds
C08L 79/08 - PolyimidesPolyester-imidesPolyamide-imidesPolyamide acids or similar polyimide precursors
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tan, Li
Qin, Ying
Abstract
Provided in the present invention are inhibitors for programmed cell necrosis, a preparation method therefor and a use thereof. Specifically, provided in the present invention are a compound represented by formula I and a composition comprising same. The described compound may be used to prepare a pharmaceutical composition for the prevention and/or treatment of diseases involving cell death and/or inflammation.
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/104 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
67.
Chiral 1,3-diarylimidazolium salt carbene precursor, synthesis method therefor, metal salt compound and application thereof
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Shi, Shiliang
Cai, Yuan
Yang, Xintuo
Li, Feng
Abstract
Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations.
C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
C07D 239/06 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Gongli
Dong, Lei
Hou, Xianfeng
Pan, Haixue
Abstract
The present invention relates to an LL-D49194α1 analog, a preparation method therefor and an application thereof. Specifically, provided by the present invention is a deglycosylated and demethylated LL-D49194α1 analog. The obtained LL-D49194α1 analog has a better antitumor activity than LL-D49194α1.
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Wenjun
Yang, He
Abstract
The present invention discloses a phosphine ligand and a preparation method thereof, and an application in catalytic synthesis of ortho-tetra-substituted biaromatics. The phosphine ligand of the present invention has a structure of formula I. The phosphine ligand or its racemate of the present invention can be used as a metal ligand to obtain ortho-tetra-substituted biaryl compounds having various functional groups with high yield or high optical purity.
C07F 9/6571 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
C07F 15/00 - Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic Table
PHARMACEUTICAL COMPOSITION FOR TREATMENT OF NEURODEGENERATIVE DISEASES OR DISEASES CAUSED BY ABNORMALITY OF RNA BINDING PROTEIN AND APPLICATIONS THEREOF
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Fang, Yanshan
Duan, Yongjia
Abstract
Disclosed are a pharmaceutical composition for treatment of neurodegenerative diseases or diseases caused by abnormality of RNA binding protein and applications thereof, in particular the application in the treatment of ALS. The pharmaceutical composition can significantly enhance the dynamic performance of stress particles containing RNA binding proteins such as hnRNP A1 and TDP-43 proteins; influences the interaction between the RNA binding proteins and other poly ADP ribosylation modified proteins or other PAR binding proteins; influences the subcellular localization and stress response of RNA binding proteins; influences the liquid-liquid phase separation and aggregation tendency of RNA binding proteins; influences the co-phase separation between RNA binding proteins; influences the interaction of RNA binding proteins in cells; and has a significant inhibitory effect on neurotoxicity caused by RNA binding proteins.
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Dong, Jiajia
Jiang, Ying
Shen, Yucheng
Wang, Tianyu
Abstract
Provided are a phenol salt and application thereof as a catalyst in a hexavalent sulfur-fluoride exchange reaction, said phenol salt comprising cations and anions. The phenol salt is easy to synthesize and can be used as a catalyst for a hexavalent sulfur-fluoride exchange (SuFEx) reaction, and has good operability and high catalytic activity; it can be used under conditions of relatively low catalyst dosage and no solvent for the mild preparation of large volumes of polysulfate or polysulfonate compound; the prepared polymer has the advantages of high molecular weight and simple post-processing.
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Wenjun
Xu, Siyao
Abstract
Disclosed are an oxycodone compound, and an intermediate and a preparation method therefor. Specifically disclosed is a preparation method for a compound represented by formula A9, comprising the following steps: under a protective gas, and under the action of a palladium catalyst and a phosphine ligand, dearomatization and cyclization as shown below is performed on a compound represented by formula A8b in an organic solvent to obtain the compound represented by formula A9. The phosphine ligand is a phosphine ligand represented by formula L1 or a phosphine ligand represented by formula L2. (I)
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
C07D 217/20 - Aralkyl radicals with oxygen atoms directly attached to the aromatic ring of said aralkyl radical, e.g. papaverine
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Cao, Chunyang
Ji, Yonghua
Liu, Xinlian
Tao, Jie
Zhang, Shuzhang
Wang, Chunxi
Abstract
The present invention provides uses for the anti-epileptic toxin Martentoxin and derivatives thereof. Specifically, the present invention provides the use of Martentoxin (or MarTX toxin) or an active fragment thereof or a pharmaceutically acceptable salt thereof in preparing a preparation or composition for treating and/or preventing epilepsy.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Cao, Chunyang
Liu, Xinlian
Tao, Jie
Ji, Yonghua
Lan, Wenxian
Abstract
Provided is a method for preparing a recombinant Martentoxin (MarTX toxin for short), the method comprising: connecting a Martentoxin gene and a maltose binding protein with a vector pETDuent-1 to obtain a recombinant expression vector pETDuent-1-MarTX; converting the recombinant expression vector into E.coli Origami B (DE3), and by means of screening, obtaining a strain with a high-efficiency expression level; and by means of inducible expression and affinity chromatography purification, obtaining a recombinant MarTX toxin with a biological activity, which can significantly inhibit a large-conductance, calcium ion- and voltage-activated potassium ion (BK) channel current. Further provided is the use of the MarTX toxin in drug screening of a (α+β4) BK channel current inhibitor.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Jing
Guo, Min
Fang, Pengfei
Yu, Biao
Abstract
Provided is the use of an aromatic ring drug in inhibiting a key transcription factor of malignant melanoma. In particular, provided is the use of a compound as represented by formula A, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition or preparation. The pharmaceutical composition or preparation is used for: (a) inhibiting a key transcriptional regulatory factor of malignant melanoma, namely MITF (Microphthalmia-associated Transcription Factor); (b) treating MITF-related diseases such as melanoma, pancreatic cancer, skin hypersensitivity and asthma; and (c) regulating physiological activities in which MITF is involved, such as skin whitening. In the formula, each group is as defined in the description.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Tang, Wenjun
Xu, Siyao
Abstract
Provided is a metal complex as represented by formula I. The metal complex may be used as a catalyst for asymmetric catalytic hydrogenation, is capable of efficiently catalyzing and synthesizing a series of chiral β-aryl amides having high optical purity, and is especially capable of asymmetrically catalyzing and hydrogenating a tetra-substituted enamide compound, chiral amides having high optical purity are synthesized, and the carrying amount of ligand may reach 100,000.
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 233/06 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
77.
Wolfberry glycopeptide composition and methods for preparing and using the same
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Lu, Long
Jiang, Yan
Shen, Juan
Ding, Zhigang
Xiang, Yuhua
Chen, Guiqing
Tian, Gengyuan
Abstract
Wolfberry glycopeptide composition and methods for preparing and using the same, the part with a molecular weight distribution of 1000 Da to 10000 Da of the wolfberry glycopeptide accounts for 50-85% on the HPLC differential refractive index map; and the protein content is 20-35% weight percentage, neutral polysaccharide content is 20-35% weight percentage. Optionally, the uronic acid content is 5-20% weight percentage. The preparation method of the present invention removes part of insoluble impurities by a heating flocculation method, instead of the conventional organic solvent extraction process, and without using any organic solvents in the whole process.
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Dawei
Ji, Yuhua
He, Weiming
Fang, Chao
Zhao, Jinlong
Wang, Kailiang
Xia, Shanghua
Li, Zheng
Li, Ying
Abstract
Provided by the present application are a cell necrosis inhibitor, a preparation method therefor and a use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). The inhibitor has a structure as shown in the following formula I. The compound and a composition comprising same may be used to prevent and/or treat diseases involving cell death and/or inflammation. (I)
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 11/00 - Drugs for disorders of the respiratory system
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
SHANGHAI TECHNOLOGY UNIVERSITY (China)
Inventor
Liu, Jia
Dong, Jiajia
Abstract
A compound for improving the gene editing specificity and application thereof. Specifically disclosed is a compound represented by formula I or a use of a pharmaceutically acceptable salt thereof. The compound and the pharmaceutically acceptable salt thereof are used for preparing an inhibitor, a composition, or a formulation for inhibiting gene editing and/or improving the gene editing specificity. The structure of the formula I is as stated in the description. The compound can significantly improve the accuracy of CRISPR gene editing, thereby providing a simple and high-efficient policy for accurate gene editing.
C12N 15/90 - Stable introduction of foreign DNA into chromosome
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Zhu, Jidong
Cao, Hengyi
Mi, Ting
Abstract
The present invention provides an amide pyrazole compound used as a FGFR irreversible inhibitor, a preparation method therefor and uses thereof. The present invention specifically provides a compound of formula (I), a stereoisomer, a racermate, or a pharmaceutically acceptable salt thereof. Said compound of formula (I) has FGFR inhibiting activity, and can be used for treating cancers induced by FGFR activity or expression.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Chai, Yongshuai
Abstract
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Dawei
He, Weiming
Zhang, Zhigao
Abstract
The present invention provides a preparation method for a natural product Trabectedin. Specifically, the present invention provides a preparation method for Et-743. In the method, tyrosine is used as an initial substrate, and after 26 steps of reaction, the Et-743 is synthesized. Raw materials and agents used in the synthetic route can all easily be obtained, reaction conditions are relatively mild, and preparation in large scale can be implemented.
C07D 515/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings
85.
FLUOROSULFONYL-CONTAINING COMPOUND, INTERMEDIATE THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSITITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Dong, Jiajia
Yang, Qian
Guo, Taijie
Zhan, Xiongjie
Meng, Genyi
Abstract
Disclosed in the present invention are a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, is simple to prepare, is convenient to use, and is in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and is the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.
C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 235/08 - Radicals containing only hydrogen and carbon atoms
C07C 309/06 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing halogen atoms, or nitro or nitroso groups bound to the carbon skeleton
C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
C07C 305/26 - Halogenosulfates, i.e. monoesters of halogenosulfuric acids
C07C 317/22 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
C07D 291/08 - Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07C 323/20 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton with singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
86.
Indoleamine-2,3-dioxygenase inhibitor and preparation method therefor
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Zhu, Jidong
Abstract
Disclosed are a compound represented by general formula I and a preparation method therefor. The compound can be used as indoleamine-2,3-dioxygenase inhibitor to prepare medicines for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Shi, Shiliang
Cai, Yuan
Yang, Xintuo
Li, Feng
Abstract
Provided are a chiral 1,3-diarylimidazolium salt carbene precursor (S), a synthesis method therefor, a metal salt compound, and an application thereof. The chiral 1,3-diarylimidazolium salt carbene precursor catalyzes a reaction between a non-activated terminal olefin and diborate by means of forming a complex with copper so as to obtain a chiral martensitic boride in a highly regioselective and highly enantioselective manner. Thus, the problem wherein a non-activated terminal olefin has difficulty in directly forming chiral martensitic borate by means of a hydroboration reaction is successfully solved, which is of great significance for the expansion of the variety of chiral alkyl boride; the chiral azacarbene precursor may potentially be applied in various metal-catalyzed asymmetric reactions.
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
C07D 239/06 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07C 251/04 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 211/53 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring having the nitrogen atom of at least one of the amino groups further bound to a hydrocarbon radical substituted by amino groups
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Hu, Xinbo
Guo, Wei
Abstract
Disclosed are a salt of indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. In particular, disclosed are a salt of a compound of formula I and a variety of amorphous substances and polymorphs thereof, wherein the definitions of each group are as described in the description. The salt has a stable structure, good light stability, thermostability, nonhygroscopic and pharmacokinetic properties, and good solubility, significantly improved purity and bioavailability, and is particularly suitable for the development and production of an IDO enzyme inhibitor with high quality.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADMENY OF SCIENCES (China)
HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
Inventor
Cao, Xin
Yu, Biao
Wang, Ning
Chen, Junwei
Abstract
Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.
C07C 69/84 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07C 233/54 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
A61P 35/04 - Antineoplastic agents specific for metastasis
C07C 229/56 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho- position
C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
90.
Glucose conjugates of triptolide, analogs and uses thereof
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Liu, Jun
He, Qingli
Pomper, Martin G.
Minn, Il
Yu, Biao
Wang, Qiaoling
Abstract
Provided are compounds generated by conjugation of triptolide with glucose to form glucose-triptolide conjugates, provides compounds with effective anti-proliferative activity and improved tolerability as compared to naturally occurring triptolide compounds.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Yuan, Junying
Zhou, Yijun
Qian, Shan
Ma, Dawei
Abstract
A compound having the following structure (I):
or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 233/78 - Radicals substituted by oxygen atoms
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
92.
USE OF AROMATIC RING DRUG IN INHIBITING KEY TRANSCRIPTION FACTOR OF MALIGNANT MELANOMA
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Jing
Guo, Min
Fang, Pengfei
Yu, Biao
Abstract
Provided is the use of an aromatic ring drug in inhibiting a key transcription factor of malignant melanoma. In particular, provided is the use of a compound as represented by formula A, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition or preparation. The pharmaceutical composition or preparation is used for: (a) inhibiting a key transcriptional regulatory factor of malignant melanoma, namely MITF (Microphthalmia-associated Transcription Factor); (b) treating MITF-related diseases such as melanoma, pancreatic cancer, skin hypersensitivity and asthma; and (c) regulating physiological activities in which MITF is involved, such as skin whitening. In the formula, each group is as defined in the description.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Huzhou Center of Bio-Synthetic Innovation, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences (China)
Inventor
Liu, Wen
Wang, Min
Xu, Dongxiao
Zhao, Qunfei
Zhang, Qinglin
Abstract
Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
C07H 15/14 - Acyclic radicals, not substituted by cyclic structures attached to a sulfur, selenium or tellurium atom of a saccharide radical
C07H 1/00 - Processes for the preparation of sugar derivatives
C07H 5/10 - Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to sulfur, selenium, or tellurium to sulfur
C07H 13/10 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to heterocyclic rings
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
94.
HIGHLY-EFFICIENT IDO/TDO DUAL INHIBITOR IN NITROGEN-CONTAINING HETEROCYCLIC HELICAL STRUCTURE
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Zhu, Jidong
Hu, Xinbo
Abstract
The present invention relates to a highly-efficient IDO/TDO dual inhibitor in a nitrogen-containing heterocyclic helical structure, and in particular, to a compound represented by formula (I) or pharmaceutically acceptable salts thereof, stereoisomers thereof, or tautomers thereof, or a prodrug thereof. The compound represented by formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor and tryptophan-2,3-dioxygenase for preparing drugs for preventing and/or treating indoleamine-2,3-dioxygenase and tryptophan-2,3-dioxygenase mediated diseases.
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
SHANGAHI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Ma, Dawei
Zhou, Wei
Fan, Mengyang
Wu, Haibo
Yin, Junli
Jiang, Xi
Zhai, Yuntong
Niu, Songtao
Abstract
Provided are a heterocyclic carboxylic acid amide ligand and applications thereof in a copper catalyzed coupling reaction. Specifically, provided are uses of a compound represented by formula (I), definitions of radical groups being described in the specifications. The compound represented by formula (I) can be used as the ligand in the copper catalyzed coupling reaction of the aryl halogeno substitute, and is used or catalyzing the coupling reaction for forming the aryl halogeno substitute having C-N, C-O, C-S and other bonds.
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Yang
Liu, Mingming
Zhou, Pengfei
Feng, Kechang
Ding, Kuiling
Wang, Xiaoming
Abstract
The present invention relates to the field of synthetic medicinal chemistry and provides a novel diaryl-β-lactam compound having significant anti-tumor activity, and a pharmaceutical use thereof. The present invention also comprises a use of the compound, pharmaceutical salt, and pharmaceutical composition thereof for preparing a pharmaceutical for the prevention or treatment of tumor-associated disease. The diaryl-β-lactam compound of the present invention has the following general formula: (I).
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 205/085 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a nitrogen atom directly attached in position 3
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
Inventor
Cao, Xin
Yu, Biao
Wang, Ning
Chen, Junwei
Abstract
Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07C 69/84 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
SHANGAHI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Zhu, Jidong
Hu, Xinbo
Abstract
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The structure of the inhibitor of the present invention is shown in general formula (I), wherein the definitions of X, R1, R2, R3, R4, R7, R8, R9, n and m are as shown in the description and the claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound in general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for the preparation of a drug for preventing and/or treating diseases mediated by indoleamine-2,3-dioxygenase.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
99.
SULFAMIC ACID ESTER AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGAHI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
Inventor
Wang, Zhaoyin
Guo, Wei
Zhu, Jidong
Abstract
Provided in the present invention are a sulfamic acid ester as an indoleamine-2,3-dioxygenase inhibitor, a preparation method therefor and a use thereof. The structure of the inhibitor in the present invention is shown in general structure I, wherein the definitions of X, R1, R2, R3, R4, R5 and n are shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound in general formula I of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for the preparation of a drug for preventing and/or treating diseases mediated by indoleamine-2,3-dioxygenase.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CHONGQING SOUND LIGHT ELECTRIC ZHILIAN ELECTRONICS CO., LTD. (China)
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES (China)
EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY (China)
SHANGHAI MUSEUM (China)
Inventor
Jiang, Biao
Zhang, Chen
Tao, Liming
Zhou, Xinguang
Wu, Laiming
Abstract
Disclosed is a method of fumigation for the prevention and treatment of pests and mildew on cultural relics. The method comprises the following operation processes: placing a fumigant and cultural relics into a fumigation chamber, fumigating the cultural relics at 25-45°C for 1-36 hours, followed by extracting air under a reduced pressure for 1-3 hours, opening the fumigation chamber, and removing the cultural relics. The fumigant is a compound of the chemical structure shown by general formula I or general formula II. The invention not only realizes the safe and effective prevention and treatment of common pests and mildew damage to cultural relics, but also has the advantages of minimal environmental pollution and environmental protection. In particular, the invention can realize the one-time treatment of cultural relics of various materials and with a variety of mildew, bacteria and pests on the cultural relics under the same fumigation environment; and after the fumigation treatment of the invention, the cultural relics can be placed in a museum environment of a historical relics collection for at least half a year and will no longer regenerate mildew, bacteria and pests. In addition, the method of the invention also has advantages such as simple operation, a low cost, and a wide range of applicable materials and mildew, bacteria and pests.
patents
