The present invention relates to crystal forms A and B of a compound (HS378) of formula (I) and a preparation method therefor. The crystal forms A and B have a good physiochemical stability, a regular crystal habit, a good particle size uniformity, and a good fluidity; the preparation method for the crystal forms A and B is simple; moreover, a good impurity removal effect, easiness in filtration and a high yield are achieved, and samples with few impurities and a high purity can be obtained; and the purification problem of difficulties during impurity removal can be fully solved.
The present invention relates to crystal forms A and B of a compound (HS378) of formula (I) and a preparation method therefor. The crystal forms A and B have a good physiochemical stability, a regular crystal habit, a good particle size uniformity, and a good fluidity; the preparation method for the crystal forms A and B is simple; moreover, a good impurity removal effect, easiness in filtration and a high yield are achieved, and samples with few impurities and a high purity can be obtained; and the purification problem of difficulties during impurity removal can be fully solved.
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
2.
Method For Increasing Fermentation Yield Of PF1022A
The present disclosure provides a method for increasing a fermentation yield of PF1022A, the method comprises taking a Rosellinia sp. capable of producing PF1022A as a production strain and performing aerobic fermentation in a fermentation medium, the fermentation medium comprises an assimilable carbon source, an assimilable nitrogen source and an inorganic salt, wherein the assimilable carbon source contains solid malt extract. The technical solution provided by the present disclosure is simple and easy to implement, improves the production efficiency of PF1022A, greatly increases the output of PF1022A, reduces the production costs, and facilitates large-scale industrial production of PF1022A.
The present invention relates to a crystal form A of a compound of formula (I), and a preparation method therefor and the use thereof. The crystal form A has good properties in terms of physical and chemical stability, water solubility, bioavailability and processing adaptability.
The present invention relates to a crystal form A of a compound of formula (I), and a preparation method therefor and the use thereof. The crystal form A has good properties in terms of physical and chemical stability, water solubility, bioavailability and processing adaptability.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
4.
AROMATIC AMIDE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to an aromatic amide derivative, a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an aromatic amide derivative as shown in general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular a DHX9 inhibitor, wherein the definition of each substituent in general formula (I) is the same as defined in the description.
The present invention relates to the field of chemical pharmaceuticals, relates to a crystal form of (3R,11R)-6-fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentaazapentacyclo[13.5.2.18,11.04,9.018,22]tricosan-1(21),4,6,8,15(22),16,19-heptaen-14-one and a preparation method therefor and a use thereof, and specifically relates to a crystal form C of a compound of formula I and a preparation method therefor, solving the problems of small particle size, poor flowability, poor stability, hygroscopicity and the like of the compound of formula I.
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 31/529 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
The present invention relates to a sulfonamide derivative, a preparation method therefor, and a medical use of a pharmaceutical composition containing the derivative. Specifically, the present invention relates to a sulfonamide derivative represented by general formula (AAI), a preparation method therefor, and a pharmaceutically acceptable salt thereof, as well as a use thereof as a therapeutic agent, particularly as a CTPS1 inhibitor, the definitions of the substituents in the general formula (AAI) being the same as the definitions in the description.
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 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 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 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
The present invention provides crystalline forms of 6-[2-[1-(2-pyridylmethyl)-4-piperidyl]ethyl]spiro[[1,3]dioxolo[4,5-f]isoindole-7,1'-cyclopropane]-5-one phosphate (AD-35), and preparation methods therefor. The invention further provides a use of the crystalline forms of AD-35 in the preparation of a drug for treating Alzheimer's disease.
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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
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
8.
AZABICYCLO DERIVATIVE AND PREPARATION METHOD THEREFOR, AND USE
The present invention relates to an azabicyclo derivative and a preparation method therefor, and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an azabicyclo derivative represented by general formula (I), and a preparation method therefor and a pharmaceutically acceptable salt thereof, as well as a use of the azabicyclo derivative and the pharmaceutically acceptable salt as therapeutic agents, especially as WRN inhibitors, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
The present invention relates to a polysubstituted aryl derivative, a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to a polysubstituted aryl derivative as shown in general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular as a Kv1.3 potassium ion channel inhibitor, wherein the definition of each substituent in general formula (I) is the same as defined in the description.
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
A hybutimibe intermediate and a preparation method therefor, which relates to the improvement of a carboxylation process and a carboxyl reduction process, so that the total yield of intermediate (Z)-5-(4-fluorophenyl)-6-hydroxy-hex-4-enoic acid is increased by 75.3%, and the total yield of hybutimibe is also increased by 75.3%.
C07D 251/26 - 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 only hetero atoms directly attached to ring carbon atoms
C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
C07C 59/48 - Unsaturated compounds containing hydroxy or O-metal groups containing six-membered aromatic rings
C07C 67/31 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of functional groups containing oxygen only in singly bound form
C07C 69/732 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
11.
AROMATIC AMIDE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to an aromatic amide derivative, and a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an aromatic amide derivative as shown in general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular a KIF18A inhibitor, wherein the definition of each group in general formula (I) is the same as the definition in the description.
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 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 405/14 - 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
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
Provided are an aromatic amide derivative, a preparation method therefor, and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, provided are an aromatic amide derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use of the derivative and the salt as therapeutic agents, particularly KIF18A inhibitors, wherein the definition of each substituent in general formula (I) is the same as that in the description.
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
Disclosed in the present invention are an aromatic acetylene derivative, a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of the aromatic acetylene derivative or the pharmaceutical composition thereof in medicines. Specifically, disclosed in the present invention are an aromatic acetylene derivative as represented by general formula (A-I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, particularly an LPXC inhibitor, wherein the definition of each substituent in the general formula (A-I) is the same as that in the description.
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
C07D 411/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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 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
14.
AROMATIC AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
An aromatic amide derivative, a preparation method therefor, and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an aromatic amide derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use of the derivative and salt as a therapeutic agent, in particular a KIF18A inhibitor, wherein the definitions of substituents in general formula (I) are the same as those in the description.
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
15.
Quinazoline Derivative, Or Preparation Method Therefor And Use Thereof
The present invention relates to a substituted quinazoline derivative, a preparation method therefor, a pharmaceutical composition comprising the derivative, and use of the quinazoline derivative or a composition thereof in medicine. Specifically, the present invention relates to substituted quinazoline derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and use thereof as therapeutic agents, in particular as SOS1 inhibitors. The definition of each substituent in general formula (I) is the same as the definition in the description.
The present invention relates to a fused polycyclic Myc regulator and a preparation method therefor, a pharmaceutical composition containing the regulator, and a use of the regulator in medicine. Disclosed in the present invention are a fused polycyclic derivative represented by general formula (I), or a stereoisomer thereof, a tautomer thereof, a pharmaceutically acceptable salt thereof and a preparation method therefor, and a use thereof as a Myc regulator.
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 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
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
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/428 - Thiazoles condensed with carbocyclic rings
17.
AROMATIC AMIDE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to an aromatic amide derivative, a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an aromatic amide derivative as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular a KIF18A inhibitor, wherein the definition of each substituent in general formula (I) is the same as the definition in the description.
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 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 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
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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
A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide
The present invention relates to a mesylate or ethanesulfonate salt of the compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the salt, and an application of the salt.
The present invention relates to a mesylate or ethanesulfonate salt of the compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the salt, and an application of the salt.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to the field of chemical pharmacy, relates to a crystal form of a pyrimidine derivative and a preparation method therefor, and specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating a cancer disease.
The present invention relates to the field of chemical pharmacy, relates to a crystal form of a pyrimidine derivative and a preparation method therefor, and specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating a cancer disease.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
20.
AROMATIC ACETYLENE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to an aromatic acetylene derivative as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, particularly as an LPXC inhibitor, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
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 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 31/4439 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Provided are an aromatic amide derivative, a preparation method therefor, and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, provided are an aromatic amide derivative as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, particularly KIF18A inhibitors, wherein the definitions of the substituents in general formula (I) are the same as the definitions in the description.
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 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 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 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 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
An aromatic amide derivative, a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. Specifically, the present invention relates to an aromatic amide derivative as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, particularly as a KIF18A inhibitor, wherein the definition of each substituent in general formula (I) is the same as the definition in the description.
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 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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
Provided are an aromatic amide derivative, a preparation method therefor, and the pharmaceutical use of a pharmaceutical composition containing the derivative. Specifically, provided are an aromatic amide derivative as shown in general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular a KIF18A inhibitor.
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 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 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
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
Provided are engineering bacteria for producing acarbose, and a use thereof. The engineering bacteria for producing acarbose are obtained by inactivating a malL gene in actinoplanes producing acarbose; after fermentation, the fermentation unit of the obtained acarbose is increased by 24.7% compared with that of an original strain, the component content of an impurity A is reduced from 0.42% to about 0.06%, and the acarbose yield of the obtained strain is improved.
The present invention relates to an aromatic acetylene derivative, a preparation method therefor, and a medical use of a pharmaceutical composition containing the derivative. Specifically, the present invention relates to an aromatic acetylene derivative represented by a general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as a therapeutic agent, particularly an LPXC inhibitor; the definitions of the substituents in the general formula (I) are the same as in the description.
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
The present invention relates to an aromatic amide derivative, a preparation method therefor, and a use of a pharmaceutical composition comprising same in medicine. Specifically, the present invention relates to an aromatic amide derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as a therapeutic agent, especially, a KIF18A inhibitor, wherein the definitions of substituents in general formula (I) are the same as those in the description.
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 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 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 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
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
The present invention relates to an aromatic acetylene derivative, a preparation method therefor, and a medical use of a pharmaceutical composition containing said derivative. Specifically, the present invention relates to an aromatic acetylene derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, particularly LPXC inhibitors, the definitions of the substituents in the general formula (I) being the same as those in the description.
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 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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
The present invention relates to an aromatic acetylene derivative, a preparation method therefor, and pharmaceutical use of a pharmaceutical composition comprising the derivative. Specifically, the present invention relates to an aromatic acetylene derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and use thereof as a therapeutic agent, particularly as an LPXC inhibitor, wherein the definitions of the substituents in general formula (I) are the same as those in the specification.
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
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
A61K 31/422 - Oxazoles 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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Drugs for medical purposes; medicines for veterinary
purposes; biological preparations for veterinary purposes;
chemical preparations for veterinary purposes;
parasiticides; dietary supplements for animals; dietetic
foods adapted for medical purposes; preparations of trace
elements for human and animal use; animal washes
[insecticides].
30.
CRYSTAL FORM OF PIPERAZINE AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to the field of chemical pharmaceuticals, relates to a crystal form of a piperazine amide derivative, a preparation method therefor and a use thereof, specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof, and solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating diseases such as cancer.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
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 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 403/14 - 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
The present disclosure relates to a piperazine derivative, a preparation method therefor, and use thereof in medicine. Specifically, the present invention relates to a piperazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutically acceptable salt or prodrug thereof, and use thereof as a therapeutic agent, in particular, as an inhibitor of coagulation factor XIa (FXIa), wherein the definition of each substituent in general formula (I) is the same as that in the description.
The present disclosure relates to a piperazine derivative, a preparation method therefor, and use thereof in medicine. Specifically, the present invention relates to a piperazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutically acceptable salt or prodrug thereof, and use thereof as a therapeutic agent, in particular, as an inhibitor of coagulation factor XIa (FXIa), wherein the definition of each substituent in general formula (I) is the same as that in the description.
C07D 403/10 - 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 aromatic rings
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
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
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 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
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
33.
CRYSTAL FORMS OF HS378 AND PREPARATION METHOD THEREFOR
The present invention relates to crystal forms A and B of a compound (HS378) of formula (I) and a preparation method therefor. The crystal forms A and B have a good physiochemical stability, a regular crystal habit, a good particle size uniformity, and a good fluidity; the preparation method for the crystal forms A and B is simple; moreover, a good impurity removal effect, easiness in filtration and a high yield are achieved, and samples with few impurities and a high purity can be obtained; and the purification problem of difficulties during impurity removal can be fully solved.
The present invention provides a method for increasing a fermentation yield of PF1022A. By using a Rosellinia sp. strain that can produce PF1022A as a production strain, aerobic fermentation is carried out in a fermentation medium. The fermentation medium comprises an assimilable carbon source, an assimilable nitrogen source, and an inorganic salt, wherein the assimilable carbon source contains a solid malt extract. The technical solution provided by the present invention is simple and easy to implement, improves the production efficiency of PF1022A, increases the yield of PF1022A, and reduces the production cost, thus facilitating the large-scale industrial production preparation method of PF1022A.
C12P 17/14 - Nitrogen or oxygen as hetero atom and at least one other diverse hetero ring atom in the same ring
C12N 1/38 - Chemical stimulation of growth or activity by addition of chemical compounds which are not essential growth factorsStimulation of growth by removal of a chemical compound
The present invention relates to heteroaryl derivatives, preparation methods therefor, and applications thereof in medicine. Specifically, the present invention relates to a heteroaryl derivative represented by general formula (AI), a preparation method therefor, and a pharmaceutically acceptable salt, and use thereof as a therapeutic agent, in particular, as an SHP2 allosteric inhibitor, wherein the definition of substituents in general formula (AI) is the same as that in the description.
The present invention relates to heteroaryl derivatives, preparation methods therefor, and applications thereof in medicine. Specifically, the present invention relates to a heteroaryl derivative represented by general formula (AI), a preparation method therefor, and a pharmaceutically acceptable salt, and use thereof as a therapeutic agent, in particular, as an SHP2 allosteric inhibitor, wherein the definition of substituents in general formula (AI) is the same as that in the description.
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
The present invention relates to a substituted fused pyrimidine-based derivative, a method for preparing same, and pharmaceutical use of a pharmaceutical composition comprising the derivative. Specifically, the present invention relates to a substituted fused pyrimidine-based derivative represented by formula (I), a method for preparing same, a pharmaceutically acceptable salt thereof, and use thereof as a therapeutic agent, particularly an HPK1 inhibitor, wherein the substituents in formula (I) are defined in the specification.
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 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
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention relates to a crystal form A of a compound of formula (I), and a preparation method therefor and the use thereof. The crystal form A has good properties in terms of physical and chemical stability, water solubility, bioavailability and processing adaptability.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a tetracyclic derivative, a method for preparing same and the use thereof in medicine. In particular, the present invention relates to a tetracyclic derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, especially as a K-Ras GTPase inhibitor, with definitions of each substituent in general formula (I) being the same as of which are defined in the description.
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
The present invention relates to a heterocyclic derivative, a preparation method therefor, a pharmaceutical composition containing the derivative, and an application thereof in medicine. Specifically, the present invention relates to a heterocyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, as well as to the use of the above as therapeutic agents, especially as RAC1 inhibitors, wherein the definitions of each substituent in general formula (I) are the same as the definitions in the description.
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 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
The present invention relates to a substituted tricyclic derivative, a preparation method therefor, and pharmaceutical use of a pharmaceutical composition comprising same. Specifically, the present invention relates to a substituted tricyclic derivative represented by formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and use thereof as a therapeutic agent, particularly as an SOS1 inhibitor, wherein the definitions of substituents in formula (I) are the same as those in the specification.
The present invention relates to a pharmaceutically acceptable salt of (S)-2-(6-fluorobenzo[d]oxazol-2-yl)-6-methoxy-5-((5-methoxypyridin-2-yl))methoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, a preparation method therefor, a pharmaceutical composition comprising the pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular as an angiotensin II type-2 receptor antagonist.
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
42.
POSACONAZOLE IMPURITY REFERENCE SUBSTANCE AND PREPARATION METHOD THEREFOR
The present invention provides a posaconazole impurity reference substance and a preparation method therefor. Disclosed in the present invention are two new compounds: related substances A and B which are high in purity, can be used as reference substances to detect or monitor impurity residues and product quality of posaconazole active pharmaceutical ingredients to ensure the medication safety of posaconazole. Moreover, the preparation method of the present invention is simple and convenient, is easy to control and operate, and has good industrial prospects.
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
43.
ANALYSIS METHOD FOR DETECTING CHIRAL ISOMER IMPURITIES IN METHOPRENE
22 as a mobile phase, and detecting impurities by using a supercritical chromatographic instrument (WatersACQUITYUPC2). The method is simple to operate, short in detection time, and good in separation effect, and using CO2 as a main mobile phase has the advantages of being rich, cheap, pollution-free, environmentally-friendly, etc.
Provided in the present invention is the use of rosuvastatin calcium in the preparation of a drug for preventing and treating cholestasis and liver fibrosis. By means of research, it is found that rosuvastatin calcium can significantly improve the condition of cholestasis in the liver and the corresponding biochemical indicators of liver fibrosis in rats, and has the potential to prevent and treat cholestasis and liver fibrosis caused by same.
A61K 31/00 - Medicinal preparations containing organic active ingredients
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
An ultra-high performance liquid chromatography–mass spectrometry method for detecting a genotoxic impurity 14-bromo-4'-epi-daunorubicin, comprising the following steps: respectively testing a test solution and a reference solution by using ultra-high performance liquid chromatography–mass spectrometry, recording a generated chromatogram, calculating a peak area according to an external standard method, and measuring the content of 14-bromo-4'-epi-daunorubicin in a drug. According to the detection method, sample derivatization pretreatment is not required, the time required for detection is shortened, and the method has the advantages of high detection speed, high sensitivity and accurate analysis result.
The present invention provides a preparation method for 1,4-butanedisulfonic acid (II). According to the method, disodium 1,4-butanedisulfonate (I) and a hydrogen chloride solution are mixed for reaction, filtration and concentration are performed after the reaction is finished to obtain 1,4-butanedisulfonic acid (II), and water is added to prepare an aqueous solution of 1,4-butanedisulfonic acid (II). The method is simple and convenient to operate. The obtained product does not need to be refined, and the purity and the yield are high. The amount of solvent used is small, the cost is low, and the method is environmentally friendly.
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
C07C 303/02 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
A method for measuring amino acid impurities in a special solvent for butanedisulfonic acid adenosine methionine for injection. The measurement method comprises: preparing a standard solution and a sensitivity solution of each amino acid impurity (DL-aminocaprolactam, phenylalanine, leucine, and threonine); preparing a sample to be measured: diluting a special solvent for butanedisulfonic acid adenosine methionine for injection with diluents into a solution having a certain concentration to form said sample, the diluents being methanol and purified water at a volume ratio of 60 : 40; preparing a mobile phase into a mobile phase A (5:95) and a mobile phase B (50:50) by using a buffer salt (the pH of 10mM ammonium formate being adjusted to 3.0 with formate acid) and acetonitrile according to a certain ratio; and carrying out sample measurement by using a high-performance liquid chromatography-mass spectrometer, so that the content of each amino acid impurity in the solvent special for the butanedisulfonic acid adenosine methionine for injection can be measured by the method.
Provided in the present invention is a method for preparing amorphous anidulafungin. The preparation method comprises: dissolving a crude product of anidulafungin in an organic solvent containing a certain proportion of water; and adding an anti-solvent in a dropwise manner to precipitate anidulafungin, and performing separation to obtain pure amorphous anidulafungin. The method provided in the present invention has a good refining effect and a high crystallization yield, the obtained solid is large in terms of particle size, easy to filter, and good in stability, the operation is simple and convenient, and the method is suitable for industrial production.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
C07K 1/30 - ExtractionSeparationPurification by precipitation
The present invention provides a method for preparing 1,4-butanedisulfonic acid sodium salt. The method comprises: mixing 1,4-dihalogenated butane (I), sodium sulfite, water and a catalyst, and undergoing a reaction to obtain 1,4-butanedisulfonic acid sodium salt (II). According to the present invention, by using a catalyst and controlling an amount of sodium sulfite, the reaction of 1,4-dihalogenated butane and sodium sulfite is easier to carry out, the reaction temperature, the reaction time and the solvent usage amount are obviously reduced, a side reaction is reduced, a side product amount is reduced, the consumption of sodium sulfite is more sufficient, the residue of a sulfate (containing sulfite) is less, a product does not need to be recrystallized, the yield is high, the present invention is suitable for industrial production, an organic solvent does not need to be used, and the present invention is environment-friendly.
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
C07C 303/02 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
The present invention relates to an apixaban tablet and a preparation process therefor. A hydrophilic polymer material is introduced into a prescription as a water-soluble carrier. Apixaban and the hydrophilic polymer material are mixed and then subjected to hot melt granulation to form a solid dispersion. The problem that apixaban tablets have poor in-vitro solubility is effectively solved without adding an surfactant. The hot melt granulation process is simple, has good reproducibility, and can be easily industrialized.
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
A gas chromatography-mass spectrometry combined analysis method for genotoxic impurity 1,3-dichloro-2-propanol, the method comprising the following steps: (1) carrying out pretreatment on a sample to prepare a sample solution, wherein perfluoropropionic acid is used as a derivatization reagent; and (2) measuring the sample solution using a gas chromatography-mass spectrometry combined instrument so as to determine the content of the impurity 1,3-dichloro-2-propanol in the sample. A gas chromatography-mass spectrometry analysis method for genotoxic impurity 1,3-dichloro-2-propanol. The method comprises: (1) carrying out pretreatment on a sample to prepare a sample solution, wherein perfluoropropionic acid is used as a derivatization reagent; and (2) detecting the sample solution using a gas chromatography-mass spectrometer to determine the content of the impurity 1,3-dichloro-2-propanol in the sample.
C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
C07C 69/63 - Halogen-containing esters of saturated acids
52.
PYRIDOPYRIMIDONE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to a substituted pyridopyrimidone derivative, and a preparation method therefor and the use of a pharmaceutical composition containing same in medicines. Specifically, the present invention relates to a substituted pyridopyrimidone derivative as represented by general formula (I), and a preparation method therefor and a pharmaceutically acceptable salt thereof, and the use of same as a therapeutic agent, especially as an SOS1 inhibitor, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
The present invention relates to a pyridolactam derivative, a preparation method therefor, and a medical use of a pharmaceutical composition comprising the derivative. Specifically, the present invention relates to a substituted pyridolactam derivative represented by general formula (I), a preparation method therefor and a pharmaceutical salt thereof, and a use thereof as a therapeutic agent, in particular as an HPK1 inhibitor, wherein the definition of each substituent in general formula (I) is the same as the definition in the description.
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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
The present invention relates to a substituted quinazoline derivative, a preparation method therefor, a pharmaceutical composition comprising the derivative, and a use of a quinazoline derivative or a composition thereof in medicine. Specifically, the present invention relates to a substituted quinazoline derivative represented by general formula (I), a preparation method therefor, a pharmaceutical salt thereof, and a use thereof as therapeutic agents, in particular as an SOS1 inhibitor. The definition of each substituent in general formula (I) is the same as the definition in the description.
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
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a heterocyclic derivative, a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a heterocyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, as well as the use thereof as a therapeutic agent, especially as a KRas G12D inhibitor; the definitions of each substituent in general formula (I) are the same as the definitions thereof in the description.
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
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for human purposes; drugs for medical purposes;
chemico-pharmaceutical preparations; chinese preparations
for medical purposes; camphor for medical purposes; crude
drugs; radiopharmaceutical products; dietetic foods adapted
for medical purposes; medicines for veterinary purposes;
solvents for bacteriological cultures; vermin destroying
preparations.
57.
METHOD FOR SYNTHESIZING FAVIPIRAVIR INTERMEDIATE 6-BROMO-3-HYDROXYPYRAZINE-2-FORMAMIDE
A method for synthesizing a favipiravir intermediate 6-bromo-3-hydroxypyrazine-2-formamide (II). The method comprises oxidizing bromide ions into high-activity bromine by using 3-hydroxypyrazine-2-formamide (I) as a raw material, hydrobromic acid as a bromine source and hydrogen peroxide as an oxidizing agent, and carrying out a bromination reaction. In the reaction, the utilization rate of bromine atoms is higher, and when the generated high-activity elemental bromine participates in the reaction, the produced by-product hydrogen bromide can be further quickly oxidized to generate elemental bromine to participate in the bromination reaction. The present invention avoids the use of bromine, is environmentally friendly, and has a low production cost. The obtained product has a relatively high purity and yield and is easy for industrial production.
Disclosed in the present invention are an aromatic acetylene derivative, a preparation method therefor, a pharmaceutical composition containing the derivative, and the use of the aromatic acetylene derivative or the pharmaceutical composition thereof in medicines. Specifically, disclosed in the present invention are an aromatic acetylene derivative as represented by general formula (A-I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, particularly an LPXC inhibitor, wherein the definition of each substituent in the general formula (A-I) is the same as that in the description.
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 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 31/4439 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to an aromatic acetylene derivative, a preparation method therefor, and a medical use of a pharmaceutical composition containing the derivative. Specifically, the present invention relates to an aromatic acetylene derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as a therapeutic agent, especially an LPXC inhibitor, the definition of each substituent in general formula (I) being the same as the definition thereof in the description.
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to a pyrimidocyclic derivative, a preparation method therefor, and a medical application of a pharmaceutical composition containing the derivative. Specifically, the present invention relates to a substituted pyrimidocyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, especially SOS1 inhibitors. The definition of each substituent in general formula (I) is the same as the definition thereof in the description.
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 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
Provided in the present invention is a method for synthesizing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethyl-phenyl)pyrazole disulfide (III), which belongs to the field of pharmaceutical synthesis. The method comprises: (1) allowing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)pyrazole (I) to react with ammonium thiocyanate and hydrogen peroxide to obtain a thiocyanate intermediate (II); and (2) carrying out a condensation reaction on the thiocyanide intermediate (II) prepared in step (1) to obtain the 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethyl-phenyl)pyrazole disulfide (III). In the present invention, the method avoids the use of bromine, is environmentally friendly, and has low production costs, the obtained product has a high purity and yield, and industrial production thereof is easy.
The present invention relates to a trideuteromethyl-substituted pyrazino pyrazino quinolinone derivative, and a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a trideuteriomethyl-substituted pyrazino pyrazino quinolinone derivative as represented by general formula (I), and a preparation method therefor and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, especially as a KRAS GTPase inhibitor, wherein the definition of each substituent in general formula (I) is the same as the definition in the description.
The present invention relates to the field of chemical pharmacy, relates to a crystal form of a pyrimidine derivative and a preparation method therefor, and specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating a cancer disease.
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
A method for analyzing and detecting trace aflatoxin in a water-soluble fermented medicament. The method comprises: (1) extracting an aqueous solution of a sample with dichloromethane, blow-drying same with nitrogen, and then dissolving same with a 30% aqueous solution (V/V) of methanol to obtain a test solution; and (2) performing detection by means of ultra-high performance liquid chromatography-mass spectrometry. The problems of a matrix interfering with the determination of a target peak and residual samples in an instrument causing the contamination of the instrument are solved by means of extraction. Aflatoxin and a sample can be fully and effectively separated within 7 min, the linearly dependent coefficient r of aflatoxin in respective linear ranges is more than 0.99, the lowest limit of quantification is 3 ng/L, the lowest limit of detection is 1 ng/L, and the average spiked recovery rate is 80%-120%. The detection method has the characteristics of high speed, high efficiency, high sensitivity, no matrix interference in sample detection, good durability, etc., and can be suitable for quantitative and qualitative detection of aflatoxin in a water-soluble medicament.
The present invention provides a hybutimibe intermediate and a preparation method therefor. The method comprises the steps of: reacting an easily available raw material of p-fluorobenzoyl butyrate with cheap sulfonylhydrazine to obtain sulfonylhydrazone valerate, then reacting sulfonylhydrazone valerate with carbon dioxide under an alkaline condition to obtain a compound of formula VI with a Z configuration, followed by subjecting the compound of formula VI to acylation, reduction and hydrolysis to obtain the hybutimibe intermediate of (Z)-5-(4-fluorophenyl)-6-hydroxy-hex-4-enoic acid. The preparation method involves readily available and cheap raw materials, has mild reaction conditions, simple and safe operation, a good stereoselectivity, a high yield and low costs, and is suitable for industrial mass production.
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
66.
SALT OF SELECTIVE FGFR4 INHIBITOR, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
The present invention relates to a mesylate or ethanesulfonate salt of a compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the salt, and an application of the salt.
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
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a bicyclic heteroaryl derivative and a preparation method therefor and a use thereof in medicine. Specifically, the present invention relates to a bicyclic heteroaryl derivative represented by formula (AI) and a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, especially SHP2 allosteric inhibitors, wherein substituents in formula (AI) have the same definitions as those in the description.
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention relates to a heterocyclic derivative and a preparation method therefor and an application thereof in medicine. Specifically, the present invention relates to a heterocyclic derivative represented by general formula (I) and a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, especially as KRas G12D inhibitors, wherein the definition of substituents in the general formula (I) is the same as the definition in the description.
The present invention relates to a substituted aromatic condensed ring derivative, a preparation method therefor and an application of a pharmaceutical composition comprising the derivative in medicine. Specifically, the present invention relates to a substituted aromatic condensed ring derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use thereof as therapeutic agents, especially as a HPK1 inhibitor, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present invention relates to a heterocyclic derivative, and a preparation method therefor and an application thereof in medicine. In particular, the present invention relates to a heterocyclic derivative represented by general formula (I), a preparation method therefor and the use thereof as a therapeutic agent, especially as a KRas G12D inhibitor, with definitions of each substituent in general formula (I) being the same as those defined in the description.
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 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
A61K 31/435 - 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
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention relates to a heterocyclic derivative, and a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a heterocyclic derivative as represented by general formula (A-I) or (A-II), and a preparation method therefor, and the use thereof as a therapeutic agent, particularly as a KRas G12D inhibitor, wherein the definition of each substituent in general formula (A-I) or (A-II) is the same as the definition in the description.
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
The present invention relates to a tetracyclic derivative, and a preparation method therefor and the medical use thereof. Specifically, the present invention relates to a tetracyclic derivative, as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use of the tetracyclic derivative and the pharmaceutically acceptable salt as therapeutic agents, especially as KRas G12D inhibitors. The definition of each substituent in general formula (I) are the same as that in the description.
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
The invention relates to a key intermediate of formula (I) and formula (II) of a KRAS inhibitor and a preparation method therefor. By means of the present invention, by changing the initial raw materials, optimizing the reaction conditions, changing the post-treatment methods, etc., the purity and yield of key intermediates is significantly improved and the cost is reduced, and the method is conducive to industrial scaled-up production.
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
74.
TRICYCLIC DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to a tricyclic derivative, and a preparation method therefor and an application thereof in medicines. Specifically, the present invention relates to a tricyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutical salt thereof, and use of the tricyclic derivative and the pharmaceutical salt as a therapeutic agent, especially as a KRas G12D inhibitor, wherein the definitions of substituents in general formula (I) are the same as definitions in the description.
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present invention relates to a substituted pyridopyrimidine derivative, a preparation method therefor, and the use of a pharmaceutical composition containing the derivative in medicine. In particular, the present invention relates to a substituted pyridopyrimidine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and the use of same as therapeutic agents, in particular as SOS1 inhibitors, wherein the definition of each substituent in the general formula (I) is the same as the definition in the description.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Analgesics; Cardiovascular pharmaceuticals; Pharmaceutical agents affecting metabolism; Pharmaceutical preparations for the prevention and treatment of ocular disorders or diseases, for the treatment of bacteria-based diseases, and for the treatment of diabetes, and anti - infective preparations, antiviral preparations, antibiotics, antifungal preparations and vaccines; Pharmaceutical preparations for the treatment of musculo-skeletal disorders; Pharmaceutical preparations, namely, a blood clotting aid and delivery system for use in human and veterinary medicine; Placebo pills and mixes for the psychological benefit of cleansing one's karma; Therapeutic agents for weight control and appetite suppression; Tumor suppressing agents; Urinary tract disinfectants
77.
Macrolide derivatives, preparation method and application thereof
Provided are a macrolide derivative represented by formula (I), a preparation method thereof, and an application of the macrolide derivative as an inhibitor of one or more protein kinases of TRK, ALK and ROS1,
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
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]
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Medicines for human purposes for the treatment of tumor, gout, osteoarthritis, muscular dystrophy, anemia, cartilage injuries, fractures, rheumatism, autoimmune diseases, immunologic deficiency syndromes, ophthalmology diseases, cardiovascular diseases, immune diseases, metabolic diseases, blood diseases, diabetes, endocrine system diseases, reproductive system diseases, respiratory system diseases, central and peripheral nervous system diseases, genetic diseases, and for anti-virus; drugs for medical purposes for the treatment of tumor, gout, osteoarthritis, muscular dystrophy, anemia, cartilage injuries, fractures, rheumatism, autoimmune diseases, immunologic deficiency syndromes, ophthalmology diseases, cardiovascular diseases, immune diseases, metabolic diseases, blood diseases, diabetes, endocrine system diseases, reproductive system diseases, respiratory system diseases, central and peripheral nervous system diseases, genetic diseases, and for anti-virus; chemico-pharmaceutical preparations for the treatment of tumor, gout, osteoarthritis, muscular dystrophy, anemia, cartilage injuries, fractures, rheumatism, autoimmune diseases, immunologic deficiency syndromes, ophthalmology diseases, cardiovascular diseases, immune diseases, metabolic diseases, blood diseases, diabetes, endocrine system diseases, reproductive system diseases, respiratory system diseases, central and peripheral nervous system diseases, genetic diseases, and for anti-virus; chinese preparations for medical purposes for the treatment of tumor, gout, osteoarthritis, muscular dystrophy, anemia, cartilage injuries, fractures, rheumatism, autoimmune diseases, immunologic deficiency syndromes, ophthalmology diseases, cardiovascular diseases, immune diseases, metabolic diseases, blood diseases, diabetes, endocrine system diseases, reproductive system diseases, respiratory system diseases, central and peripheral nervous system diseases, genetic diseases, and for anti-virus; camphor for medical purposes; drug delivery agents in the form of powders that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; radiopharmaceuticals; dietetic preparations consisting of vitamins, minerals and trace elements; medicines for veterinary purposes for the prevention and treatment of parasites, swine dysentery, bacterial enteritis, pneumonia, vitamin deficiencies; bouillons for bacteriological cultures; vermin destroying preparations.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines for human purposes, namely, pharmaceutical preparations for suppressing tumors, medicines for the treatment of hematopathy, cardiovascular pharmaceuticals, anti-infectives, stimulatory medications for use in weight reduction programs, analgesics; pharmaceutical preparations and substances for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; chemical preparations for pharmaceutical or medical purposes, namely, for the treatment of cancer; medicines made of chinese traditional medicinal herbs; camphor for medical purposes; vermin destroying preparations; diagnostic radiopharmaceutical preparations; dietetic foods adapted for medical purposes; medicines for veterinary purposes, namely, anti-infective products for veterinary use, anthelmintics; bacteriological culture mediums
80.
DETERMINATION METHOD FOR RELATED SUBSTANCES IN FAVIPIRAVIR
The present invention relates to the field of analytical chemistry, and provides a method for detecting related substances of favipiravir, comprising: using a phosphate solution (mobile phase A)-acetonitrile (mobile phase B) as a mobile phase and a sodium carbonate solution as a diluent; taking an appropriate amount of favipiravir and an appropriate amount of a favipiravir-containing tablet, adding the diluent to prepare a sample solution containing 0.5 mg/mL of favipiravir, and taking the favipiravir and adding the diluent to dilute same into a reference solution of 2.5 μg/mL; and quantitatively determining the content of related substances in the favipiravir and a preparation by using a principal component plus correction factor method. According to the method for detecting related substances of favipiravir, the impurities and degradation products of the favipiravir can be quickly and accurately detected. The method is easy to operate, good in accuracy and high in sensitivity, and can better control the product quality.
A gas-phase detection method for dicyclohexylamine in favipiravir that has a short analysis time, high sensitivity and good reproducibility. A 30% sodium hydroxide solution that has a mass percentage concentration unit of g/g is used, heated and set aside, so that the interference of a matrix on a detection substance dicyclohexylamine may be eliminated with good linearity and quantitative accuracy. Adding the 30% sodium hydroxide solution may eliminate the reaction and adsorption of phenolic hydroxyl groups on the detection substance. Once a sample is treated by adding alkali and set aside, the sample is injected. The results are accurate and reproducible.
Crystal forms A, B, C, D, E, F, G and H of a compound represented by formula I and a preparation method therefor, as well as medical uses for the various crystal forms and advantages thereof in various aspects.
Crystal forms A, B, C, D, E, F, G and H of a compound represented by formula I and a preparation method therefor, as well as medical uses for the various crystal forms and advantages thereof in various aspects.
The invention relates to novel crystal forms A, B and C of midostaurin, a preparation method therefor and the use thereof. The crystal forms have excellent properties in terms of physical and chemical stability and processing adaptability; and the crystallization process is simple and convenient to operate, and industrial production can be realized.
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 31/553 - 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
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 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
The present invention relates to a piperazine derivative, a preparation method therefor and the use thereof in medicine. Specifically, the present invention relates to a piperazine derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof or a prodrug thereof, and the uses of same as a therapeutic agent, particularly as a blood coagulation factor XIa (FXIa) inhibitor, wherein the definition of each substituent in general formula (I) is the same as that in the description.
C07D 403/10 - 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 aromatic rings
A61K 31/4425 - Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
The present invention relates to an amide phosphine oxide derivative, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to an amide phosphine oxide derivative represented by general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof, and a use thereof as a therapeutic agent, especially as an inhibitor of coagulation factor XIa (FXIa). The definition of each substituent in general formula (I) is the same as the definition in the description.
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
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 401/14 - 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 31/551 - 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
A61P 9/00 - Drugs for disorders of the cardiovascular system
87.
CYCLOSERINE CRYSTAL FORM AND PREPARATION METHOD THEREFOR
The present invention elates to crystal forms I and II of cycloserine and a preparation method therefor. The crystal forms I and II have a uniform particle size distribution and a larger particle size, the crystal structure is similar to a single crystal, a length-width ratio is less than 3:1, the mobility is good, and the property in the aspect of machining adaptability is excellent, and thus the problem of uneven sample mixing in the preparation process is solved.
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
The present invention relates to a tetracyclic derivative, a method for preparing same and the use thereof in medicine. In particular, the present invention relates to a tetracyclic derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, especially as a K-Ras GTPase inhibitor, with definitions of each substituent in general formula (I) being the same as of which are defined in the description.
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
The present invention relates to a heterocyclic derivative and a preparation method therefor and use thereof in medicine. Specifically, the present invention relates to a heterocyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and use thereof as therapeutic agents, especially as K-Ras GTPase inhibitors, wherein the definition of substituents in the general formula (I) is the same as the definition in the description.
The present invention relates to a pyridine or pyrimidine derivative, a preparation method therefor, and a medical use thereof. Specifically, the present invention relates to a pyridine or pyrimidine derivative as shown in general formula (I), a preparation method therefor, and a pharmaceutical salt thereof, and use of same as a therapeutic agent, especially the use of an SHP2 allosteric inhibitor. The definition of each substituent group in general formula (I) is the same as the definition in the description.
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 401/14 - 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 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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
The present invention relates to a pharmaceutically acceptable salt of (S)-2-(6-fluorobenzo[d]oxazol-2-yl)-6-methoxy-5-((5-methoxypyridin-2-yl))methoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, a preparation method therefor, a pharmaceutical composition comprising the pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular as an angiotensin II type-2 receptor antagonist.
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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61P 25/04 - Centrally acting analgesics, e.g. opioids
92.
Indazole amine derivative, preparation method therefor and medical use thereof
Indazole derivatives represented by formula (I) or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof are provided. A preparation method of indazole derivatives represented by formula (I) and a method of use of the indazole derivatives as therapeutic agents is also provided. The indazole derivatives of formula (I) are especially useful as interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors
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 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
93.
Tetrahydroisoquinoline derivative, preparation method therefor and use thereof
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 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 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
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
94.
PYRAZOLO[1,5-A]PYRAZINE DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to a pyrazolo[1,5-a]pyrazine derivative and a preparation method therefor and a use thereof in medicines. In particular, the present invention relates to a pyrazolo[1,5-a]pyrazine derivative shown in general formula (I), a preparation method therefor, a pharmaceutically acceptable salt thereof and a use thereof as a therapeutic agent, particularly as a JAKS family kinase inhibitor. The definition of each substituent group in the general formula (I) is the same as that in the description.
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The present invention relates to a pyridine or pyrimidine derivative, and a preparation method therefor and pharmaceutical use thereof. Specifically, the present invention relates to a pyridine or pyrimidine derivative represented by general formula (I), a preparation method therefor, a pharmaceutical salt thereof, and the use thereof as therapeutic agents, particularly as an SHP2 allosteric inhibitor, wherein the definitions of substituents in general formula (I) are the same as those in the description.
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 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 413/04 - 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
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/537 - 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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular 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
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
96.
Pyrimidine derivative, method for preparing same and use thereof in medicine
The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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
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 403/04 - 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
97.
HETEROARYL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present invention relates to a heteroaryl derivative, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a heteroaryl derivative as represented by general formula (AI), a preparation method therefor, and a pharmaceutically acceptable salt, and use thereof as a therapeutic agent, in particular, as an SHP2 allosteric inhibitor, wherein the definition of substituents in general formula (AI) is the same as that in the description.
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 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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
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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A method for enzymatic preparation of fludarabine phosphate, comprising reaction of fludarabine with a high-energy phosphate compound under the action of deoxyribonucleic acid kinase. According to said method, acetate kinase and acetyl phosphate free acid or acetyl phosphate are also added. The technical problems present in the existing processes are successfully addressed by employing the enzymatic process to prepare the fludarabine phosphate. The usage of the high-energy phosphate compound is reduced by means of adding acetate kinase to recycle and regenerate a small amount of the high-energy phosphate compound, thereby reducing the generation of by-products having similar structures to the fludarabine phosphate, enhancing the operation convenience of purification steps in the industrial production of the fludarabine phosphate. The process is environment friendly, the reaction conditions are moderate, the cost is low, and the yield and the purity of the product obtained are high.
C12P 19/32 - Nucleotides having a condensed ring system containing a six-membered ring having two nitrogen atoms in the same-ring, e.g. purine nucleotides, nicotineamide-adenine dinucleotide
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
An HS-25 tablet, an HS-25 solid dispersion composition, a preparation method therefor and usage thereof. The HS-25 tablet is made by using HS-25 and excipients for wet granulation, drying, granulating and tablet pressing.
The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof as a therapeutic agent, particularly as a selective rearranged during transfection (RET) kinase inhibitor. The definition of each substituent in formula (I) is the same as the definition in the description.
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
