NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Dong, Gang
Chen, Ting
Abstract
Provided herein is a lipid nanoparticle (LNP) composition for the localized treatment of skin diseases and a method of treating skin diseases with the LNP composition.
C12N 15/88 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation using microencapsulation, e.g. using liposome vesicle
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
2.
A NON-HUMAN TRANSGENIC ANIMAL MODEL AND A METHOD OF PRODUCING THE SAME
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Wang, Qing
Xie, Yuting
Abstract
Disclosed herein are small-molecule modulators of spike protein, particularly modulators of betacoronavirus spike proteins, more particularly modulators of SARS-CoV-2 spike proteins. Also disclosed herein is the therapeutical use of the small molecular compounds for treating betacoronavirus infections.
C07D 217/06 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 401/00 - 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
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Yu
Hong, Yu
Si, Xiaofang
Liu, Wenjing
Mai, Xueying
Abstract
Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Cui, Bo
Yan, Bo
Abstract
A substituted cyclic compound as represented by formula (I) and having a selective inhibitory effect on MLKL, or a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, a pharmaceutical composition containing the compound and an application thereof in preparation of MLKL inhibitors.
C07D 239/12 - Nitrogen atoms not forming part of a nitro radical
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
C07D 413/02 - 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
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Sui, Jianhua
Du, Kaixin
Chen, Wei
Li, Yulu
Liu, Juan
Abstract
An isolated anti-CD47 antibody or fragment thereof has the ability of binding CD47 and competing with the binding of SIRPa to CD47, and comprises a heavy chain variable region comprising heavy chain complementarity determining regions HCDR1, HCDR2, and HCDR3; and a light chain variable region comprising light chain complementarity determining regions LCDR1, LCDR2, and LCDR3. A method for treating a disorder in which CD47 is overexpressed or upregulated in a subject, comprises using an isolated anti-CD47 antibody or fragment thereof having the ability of binding CD47 and competing with the binding of SIRPa to CD47. A bispecific antibody comprises a first antigen binding moiety that binds to human GPC3 (hGPC3); and a second antigen binding moiety that binds to human CD47 (hCD47).
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Qi, Xiangbing
Chen, Peihao
Wang, Jing
Wang, Yan
Sun, Yuze
Wu, Qingcui
Abstract
The present disclosure relates to a preparation method of TTX or its analogues, and also relates to compounds useful for preparation method for TTX or its analogues.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
National Institute of Biological Sciences, Beijing (China)
Inventor
Li, Wenhui
Qi, Yonghe
Chen, Jianhe
Sui, Jianhua
Liu, Juan
Mao, Fengfeng
Liu, Ximing
Abstract
A soluble ACF and a truncated form thereof, a fusion protein thereof and preparation methods therefor. A soluble ACEI and a truncated form thereof, as well as a use of the fusion protein in the preparation of a drug for an ACEI-related disease.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Chen, Ting
Xu, Zijian
Abstract
Provided is a drug target for vitiligo. The drug target is IFN-γ signaling. It also provides a method for establishing vitiligo animal model, or a vitiligo induction method in an animal, and the established vitiligo animal model. Further, provided is a method for screening candidate drugs for treating vitiligo using the said animal model.
A01K 67/027 - New or modified breeds of vertebrates
C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Lin, Rui
Yan, Ting
Luo, Minmin
Abstract
Provided is a recombinant adeno-associated virus (rAAV) vector comprising a nucleic acid molecule encoding a chimeric antigen receptor (CAR) which specifically binds to a central nervous system (CNS) tumor cell, preferably a solid CNS tumor cell. Further provided is a modified cell comprising a chimeric antigen receptor (CAR) which is obtained by transducing the cell with the rAAV vector, and a method for treating a CNS tumor using the rAAV vector or modified cell of the present disclosure.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
C07K 14/005 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from viruses
C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof
13.
SPECIFIC HOST FACTOR OF HEPATITIS B VIRUS INFECTION, AND USE THEREOF
National Institute of Biological Sciences, Beijing (China)
Inventor
Li, Cong
Wang, Yixue
Li, Wenhui
Abstract
Provided is a host factor specific for hepatitis B virus (HBV) infection. The specific host factor CREBH can remarkably enhance HBV infection. The specific host factor can, on the one hand, enhance entry of HBV, and on the other hand, enhance transcription of HBV to some extent. In the CREBH regulatory pathway there is a specific host factor SCARF2. During HBV infection, an N-terminus EGF-like domain of SCARF2 plays a crucial role in the infection and entry of HBV. The two correlated specific host factors provide a new target for inhibiting HBV infection.
National Institute of Biological Sciences, Beijing (China)
Inventor
Sui, Jianhua
Liu, Ximing
Tang, Nan
Wu, Huijuan
Abstract
Provided are anti-AREG antibodies or immunoreactive fragments thereof for the treatment, diagnosis or prophylaxis of fibrotic diseases, including but not limited to renal fibrosis, hepatic fibrosis, pulmonary fibrosis, in particular, IPF. Polynucleotides or nucleic acid molecules encoding the antibodies, expression vectors, host cells and methods for making the antibodies are also provided. The anti-AREG antibodies specifically bind to AREG and block the function of AREG, through binding residues that locate in the EGF like domain.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Jiang, Hui
Liu, Shanshan
Liu, Qinghua
Abstract
A method for modulating Gro3P (glycerol-3-phosphate) biosynthesis, and uses thereof, e.g. therapeutic uses thereof in treating mitochondrial complex I diseases or cancers.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
TSINGHUA UNIVERSITY (China)
Inventor
Wang, Xiaodong
Huang, Niu
Qi, Xiangbing
Wang, Hongwei
Chen, Jie
Li, Dianrong
Sun, Yuxing
Wang, Yuanxun
Liu, Nan
Wu, Qingcui
Huang, Yinpin
Abstract
Provided herein are polycyclic compounds, compositions, and methods for modulating the PDE3A activity or regulating the interaction of PDE3A/SLFN12. The compounds modulate the PDE3A activity or regulate the interaction of PDE3A/SLFN12, and are useful as antitumor agents.
It relates to methods of treating prostatitis comprising administering to a male in need thereof a necroptosis inhibitor, including inhibitors of RIP1, RIP3 or MLKL. It also relates to pharmaceutical composition comprising a necroptosis inhibitor and a second different drug for treating prostatitis.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
18.
ANIMAL MODEL OF IDIOPATHIC PULMONARY FIBROSIS, ITS CONSTRUCTION METHOD AND USE
National Institute of Biological Sciences, Beijing (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
The present invention relates to a method for constructing an animal model of pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), the constructed animal model using the said method, and a method for screening the candidate drugs for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
National Institute of Biological Sciences, Beijing (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
Provided is a drug target for idiopathic pulmonary fibrosis, and the use thereof. The drug target is AREG signaling in AT2 cells of the lung. The drug target can be used to screen drugs for treating and/or preventing pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF) of animals and human beings.
National Institute of Biological Sciences, Beijing (China)
Inventor
Tang, Nan
Wu, Huijuan
Li, Jiao
Abstract
The invention relates to prosthesis for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), and a method for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Qi, Xiangbing
Han, Ting
Chen, Peihao
Lv, Lu
Li, Yamei
Cao, Longzhi
Wu, Qingcui
Li, Jiao
Abstract
Provided is a new kind of molecular glues for triggering polyubiquitination and degradation of CCNK (cyclin K). Specifically, a new kind of molecular glues for creating a modified CDK12 protein so as to bind DDB1 of DDB1-CUL4-RBX1. The molecular glues convert CDK12 into a substrate-specific receptor to trigger the polyubiquitination and subsequent degradation of CDK12's partner protein CCNK.
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 417/02 - 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
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 283/02 - Heterocyclic compounds containing rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms, according to more than one of groups having the hetero atoms in positions 1 and 3
C07D 247/02 - Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups having the nitrogen atoms in positions 1 and 3
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Erquan
Qi, Xiangbing
Ju, Dapeng
Wang, Zhiqiang
Wu, Qingcui
Zhao, Haijiao
Mei, Long
Abstract
The present invention provides a kind of nucleoside analogue compounds, and a composition comprising the compound and pentostatin, their use for modulating circadian rhythm, preferably, for shifting circadian phase, and methods for modulating circadian rhythm, preferably, for shifting circadian phase via the compound or the composition.
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Chen, Ting
Xie, Yuhua
Abstract
Provided is mechanical change sensed by mechanosensitive ion channel Piezo1 mediates niche atrophy caused hair follicle stem cell loss through apoptosis. The decreased niche size causes hair cycle dependent ectopic hair follicle stem cell apoptosis, which can be completely rescued by re-expanding the three-dimensional niche space alone. In vivo pharmacological compound screen and intravital Ca2+ imaging indicate stem cells rely on mechanosensitive calcium channels to sense niche size decrease. Guided by transcriptome screen, epithelial specific disruption of mouse Piezo1 and compound activation experiments show that Piezo1 is necessary and sufficient to mediate niche size regulated hair follicle stem cell survival. Stretch activated Piezo1 confers sensitivity to catagen specific death signal TNFα on otherwise resistant stem cells. Pathological niche atrophy caused stem cell loss in the pure hair and nail ectodermal dysplasia disease model is rescued by loss of epithelial Piezo1.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Chen, Ting
Xu, Zijian
Abstract
Provided is a drug target for vitiligo. The drug target is IFN-γ signaling. It also provides a method for establishing vitiligo animal model, or a vitiligo induction method in an animal, and the established vitiligo animal model. Further, provided is a method for screening candidate drugs for treating vitiligo using the said animal model.
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Huang, Shaoqiang
Jiang, Xian
Li, Li
Zhang, Zhaolan
Han, Jianguang
Abstract
The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 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
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 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic 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
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 37/00 - Drugs for immunological or allergic disorders
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/28 - 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
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Sui, Jianhua
Liu, Ximing
Tang, Nan
Wu, Huijuan
Abstract
Provided are anti-AREG antibodies or immunoreactive fragments thereof for the treatment, diagnosis or prophylaxis of fibrotic diseases, including but not limited to renal fibrosis, hepatic fibrosis, pulmonary fibrosis, in particular, IPF. Polynucleotides or nucleic acid molecules encoding the antibodies, expression vectors, host cells and methods for making the antibodies are also provided. The anti-AREG antibodies specifically bind to AREG and block the function of AREG, through binding residues that locate in the EGF like domain.
C07K 14/485 - Epidermal growth factor [EGF], i.e. urogastrone
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Sui, Jianhua
Liu, Ximing
Tang, Nan
Wu, Huijuan
Abstract
Provided are anti-AREG antibodies or immunoreactive fragments thereof for the treatment, diagnosis or prophylaxis of fibrotic diseases, including but not limited to renal fibrosis, hepatic fibrosis, pulmonary fibrosis, in particular, IPF. Polynucleotides or nucleic acid molecules encoding the antibodies, expression vectors, host cells and methods for making the antibodies are also provided. The anti-AREG antibodies specifically bind to AREG and block the function of AREG, through binding residues that locate in the EGF like domain.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
C07K 14/485 - Epidermal growth factor [EGF], i.e. urogastrone
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Li, Wenhui
Qi, Yonghe
Chen, Jianhe
Sui, Jianhua
Liu, Juan
Mao, Fengfeng
Liu, Ximing
Abstract
Soluble ACE2 and a truncated form thereof, a fusion protein thereof and preparation methods therefor. Soluble ACE2 and a truncated form thereof, as well as a use of the fusion protein in the preparation of a medicine for ACE2-related diseases.
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C12N 15/00 - Mutation or genetic engineeringDNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purificationUse of hosts therefor
C12N 15/62 - DNA sequences coding for fusion proteins
30.
SOLUBLE ACE2 AND FUSION PROTEIN, AND APPLICATIONS THEREOF
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Li, Wenhui
Qi, Yonghe
Chen, Jianhe
Sui, Jianhua
Liu, Juan
Mao, Fengfeng
Liu, Ximing
Abstract
Soluble ACE2 and a truncated form thereof, a fusion protein thereof and preparation methods therefor. Soluble ACE2 and a truncated form thereof, as well as a use of the fusion protein in the preparation of a medicine for ACE2-related diseases.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C12N 15/62 - DNA sequences coding for fusion proteins
C12N 15/00 - Mutation or genetic engineeringDNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purificationUse of hosts therefor
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 9/00 - Drugs for disorders of the cardiovascular system
31.
SPECIFIC HOST FACTOR FOR HEPATITIS B VIRUS INFECTION AND USE THEREOF
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Li, Cong
Wang, Yixue
Li, Wenhui
Abstract
The present invention relates to a specific host factor for hepatitis B virus infection, and finds that the specific host factor CREBH can remarkably enhance hepatitis B virus infection. On the one hand, the specific host factor can promote the invasion of a hepatitis B virus and on the other hand, the specific host factor can also enhance the transcription of the hepatitis B virus to a certain extent. The specific host factor is found and identified, thereby expanding the scientific community's understanding of the invasion process of the hepatitis B virus, and finding a new target for inhibiting hepatitis B virus infection.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
32.
SPECIFIC HOST FACTOR OF HEPATITIS B VIRUS INFECTION, AND USE THEREOF
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Li, Cong
Wang, Yixue
Li, Wenhui
Abstract
The present invention provides a specific host factor of hepatitis B virus infection. The specific host factor CREBH can remarkably enhance hepatitis B virus infection, can promote the invasion of a hepatitis B virus, and also has certain enhancement for the transcription of the hepatitis B virus. During the hepatitis B virus infection, the EGF-like structure field of the amino end of a specific host factor SCARF2 in a CREBH regulation and control pathway plays a crucial role in the infection and invasion of the hepatitis B virus. By means of two kinds of specific host factors having correlation, a new target is found for inhibiting the hepatitis B virus infection.
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 401/04 - 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 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - 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
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
PEKING UNIVERSITY (China)
Inventor
Shao, Feng
Liu, Zhibo
Wang, Qinyang
Wang, Yupeng
Abstract
Pyroptosis-induced immunotherapy is effected by activating a pore-forming, pyrpotogenic molecule, wherein the activating induces tumor cell pryoptosis and causes tumor regression by T-cell mediated anti-tumor immunity.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Ren, Yan
Abstract
It relates to methods of treating prostatitis comprising administering to a male in need thereof a necroptosis inhibitor, including inhibitors of RIP1, RIP3 or MLKL. It also relates to pharmaceutical composition comprising a necroptosis inhibitor and a second different drug for treating prostatitis.
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Li, Wenhui
Ruan, Hanying
Liu, Yang
Mao, Fengfeng
Li, Ying
Zhou, Zhongmin
Abstract
The invention provides cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection(s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.
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 307/18 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 407/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Li, Jiao
Abstract
Prosthesis for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), and a method for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
Provided are a method for constructing an animal model of pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), the constructed animal model using the said method, and a method for screening the candidate drugs for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Li, Jiao
Abstract
Prosthesis for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), and a method for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
Provided is a drug target for idiopathic pulmonary fibrosis, and the use thereof. The drug target is AREG signaling in AT2 cells of the lung. The drug target can be used to screen drugs for treating and/or preventing pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF) of animals and human beings.
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
Provided are a method for constructing an animal model of pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF), the constructed animal model using the said method, and a method for screening the candidate drugs for treating pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF).
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Tang, Nan
Wu, Huijuan
Abstract
Provided is a drug target for idiopathic pulmonary fibrosis, and the use thereof. The drug target is AREG signaling in AT2 cells of the lung. The drug target can be used to screen drugs for treating and/or preventing pulmonary fibrosis, in particular, idiopathic pulmonary fibrosis (IPF) of animals and human beings.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Mao, Fengfeng
Zhou, Zhongmin
Li, Wenhui
Abstract
The present invention relates to a heme oxygenase-1 inducer. The inducer is a compound as represented by general formula I or a salt thereof. The novel heme oxygenase-1 inducer provided in the present invention can highly-efficiently induce the expression of heme oxygenase-1, is high in safety and small in side effect, and has wide application value in the field of prevention and treatment of inflammation-related diseases.
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Mao, Fengfeng
Zhou, Zhongmin
Liu, Yang
Zhao, Hanqing
Sui, Jianhua
Li, Wenhui
Abstract
The invention provides use of NTCP inhibitors in preventing and/or treating hepatocarcinogenesis. The hepatocarcinogenesis may induced by HBV and/or HDV infection (s), fatty liver disease or chemical (s). The hepatocarcinogenesis may happen in males. In some cases, the NTCP inhibitor down-regulates or inhibits the expression of NTCP. In other cases, the NTCP inhibitor regulates the function of NTCP, preferably, inhibits the function of NTCP or makes the NTCP dysfunction. Preferably, the NTCP inhibitor is cyclosporine A or comprising at least one compound with the structure of formula I or its pharmaceutically acceptable salts.
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Su, Yaning
Ruan, Hanying
Ren, Yan
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/38 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 231/02 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 231/04 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 231/08 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
C07D 233/38 - One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 261/02 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
C07D 263/22 - Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
C07D 203/18 - Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with acylated ring nitrogen atoms by carboxylic acids, or by sulfur or nitrogen analogues thereof
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/333 - Radicals substituted by oxygen or sulfur atoms
C07D 211/16 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
C07D 211/82 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
G01C 19/5747 - Structural details or topology the devices having two sensing masses in anti-phase motion each sensing mass being connected to a driving mass, e.g. driving frames
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 255/34 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 251/16 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 211/82 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 235/08 - Radicals containing only hydrogen and carbon atoms
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 277/24 - Radicals substituted by oxygen atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 307/46 - Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
C07C 255/43 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms the carbon skeleton being further substituted by singly-bound oxygen atoms
47.
MONO HALOGEN OR METHYL-SUBSTITUTED 5-HT2B ANTAGONISTS WITH INCREASED ACTIVITY
C07C 211/28 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by unsaturated carbon chains
C07C 211/29 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
C07C 211/31 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by at least three rings
C07C 211/32 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by at least three rings containing dibenzocycloheptane or dibenzocycloheptene ring systems or condensed derivatives thereof
C07D 313/10 - Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
C07D 337/10 - Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
National Institute of Biological Sciences, Beijing (China)
Inventor
Wang, Xiaodong
Li, Dianrong
Meng, Lingjun
Zhang, Zhiyuan
Abstract
The invention provides methods of treating male reproductive senescence comprising administering to a male in need thereof a necroptosis inhibitor, including inhibitors of RIP1, RIP3 or MLKL. The invention also provides pharmaceutical compositions comprising a necroptosis inhibitor and a second different drug for treating male senescence.
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/396 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
C07D 213/73 - Unsubstituted amino or imino radicals
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61P 37/00 - Drugs for immunological or allergic disorders
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Ying, Zhengxin
Pan, Chenjie
Wang, Xiaodong
Abstract
Methods of inhibiting or treating demyelination (or treating demyelinating disease) comprise administering to a person in need thereof an MLKL inhibitor.
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Shao, Feng
Zhou, Ping
She, Yang
He, Huabin
Li, Peng
Ding, Jingjin
Gao, Wenqing
Abstract
Pharmaceutical compositions comprise a 1-ADP-heptose conjugate and may include an immunogen or an immune checkpoint inhibitor, and are used to promote an immune response.
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Li, Wenhui
Ruan, Hanying
Liu, Yang
Mao, Fengfeng
Li, Ying
Zhou, Zhongmin
Abstract
Provided are cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection (s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.
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
53.
USE OF ISHCR FOR EXM AND SOLVENT-BASED TISSUE CLEARING
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Lin, Rui
Luo, Minmin
Abstract
The invention provides an antibody-based bioanalytical method, specifically a hybridization Chain Reaction-based Method for Amplifying Immunosignals named immunosignal HCR (isHCR), which combines antibody-antigen interactions with hybridization Chain Reaction (HCR) technology for amplifying immunosignals. The invention also provides a kit for performing the above isHCR.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Lin, Rui
Luo, Minmin
Abstract
The invention provides a method for optimizing isHCR for multiplexed labeling, which combines binder-biomolecule interactions with hybridization Chain Reaction (HCR).
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
The invention provides use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, to treat or inhibit macular degeneration or age-related macular degeneration, and related compostions.
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/535 - 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
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Huang, Shaoqiang
Jiang, Xian
Li, Li
Zhang, Zhaolan
Han, Jianguang
Abstract
The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 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
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 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic 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
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 37/00 - Drugs for immunological or allergic disorders
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/28 - 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
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
He, Wanzhong
Jin, Xiumei
Abstract
Metal nanoparticles are directly synthesized on polymers comprising a plurality of thiol groups to form compositions useful as electron microscopy tags.
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Su, Yaning
Ruan, Hanying
Ren, Yan
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 231/04 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 231/08 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
C07D 233/38 - One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 261/02 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
C07D 263/22 - Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
C07D 203/18 - Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with acylated ring nitrogen atoms by carboxylic acids, or by sulfur or nitrogen analogues thereof
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/333 - Radicals substituted by oxygen or sulfur atoms
C07D 211/16 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
C07D 211/82 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 231/02 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/38 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Zhi, Gang
Chai, Jijie
Peng, Shiming
Hou, Nannan
Abstract
Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Wang, Xiaodong
Li, Dianrong
Meng, Lingjun
Zhang, Zhiyuan
Abstract
The invention provides methods of treating male reproductive senescence comprising administering to a male in need thereof a necroptosis inhibitor, including inhibitors of RIP1, RIP3 or MLKL. The invention also provides pharmaceutical compositions comprising a necroptosis inhibitor and a second different drug for treating male senescence.
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Lei, Xiaoguang
Su, Yaning
He, Sudan
Ruan, Hanying
Sun, Liming
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
C07C 275/24 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
C07C 311/14 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
C07D 277/28 - Radicals substituted by nitrogen atoms
C07D 211/28 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
C07D 213/64 - One oxygen atom attached in position 2 or 6
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 233/13 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 233/59 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Huang, Shaoqiang
Yan, Bo
Liu, Lei
Wang, Huayi
Yao, Zhenglin
Han, Jianguang
Huang, Zhi
Cao, Weiye
Abstract
Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
C07D 473/12 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1, 3, and 7, e.g. caffeine
C07D 473/08 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
C07D 473/10 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 3 and 7, e.g. theobromine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61P 25/00 - Drugs for disorders of the nervous system
65.
ADENOSINE ANALOG AND ITS USE IN REGULATING THE CIRCADIAN CLOCK
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Erquan
Qi, Xiangbing
Ju, Dapeng
Zhao, Haijiao
Mei, Long
Wang, Zhiqiang
Wu, Qingcui
Abstract
Provided are a kind of nucleoside analogue compounds, and compositions comprising these compounds and pentostatin, their use for modulating circadian rhythm, preferably, for shifting circadian phase, and methods for modulating circadian rhythm, preferably, for shifting circadian phase via these compounds or the compositions.
C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61P 25/00 - Drugs for disorders of the nervous system
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Qi, Xiangbing
Lou, Mingliang
Wu, Enlong
Chen, Peihao
Wu, Qingcui
Abstract
Provided are compounds that are inhibitors of pyruvate dehydrogenase kinase (PDK), and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 255/34 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 251/16 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 211/82 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 235/08 - Radicals containing only hydrogen and carbon atoms
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 277/24 - Radicals substituted by oxygen atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 307/46 - Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
C07C 255/43 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms the carbon skeleton being further substituted by singly-bound oxygen atoms
68.
ENTACAPONE-RELATED COMPOUNDS TO TREAT MACULAR DEGENERATION
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
Use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, in treating or inhibiting macular degeneration or age-related macular degeneration. And the pharmaceutical composition or formulation comprising entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
Use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, in treating or inhibiting macular degeneration or age-related macular degeneration. And the pharmaceutical composition or formulation comprising entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
Use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, in treating injury or promoting wound healing or tissue regeneration. And the pharmaceutical composition or formulation comprising entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, and a second different medicament for treating injury or promoting wound healing or tissue regeneration.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Huang, Shaoqiang
Jiang, Xian
Li, Li
Zhang, Zhaolan
Han, Jianguang
Abstract
ABSTRACT The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition. R2 R4 /1%N I ,Q1 R N S 1 I 0 0 0 N I Rs 11 CA 3030581 2020-03-04
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 37/00 - Drugs for immunological or allergic disorders
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Huang, Shaoqiang
Jiang, Xian
Li, Li
Zhang, Zhaolan
Han, Jianguang
Abstract
The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Zhou, Yu
Lin, Xingyu
Abstract
2B antagonist of formula I:
2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
C07D 251/72 - Heterocyclic compounds containing 1,3,5-triazine rings condensed with carbocyclic rings or ring systems
C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Su, Yaning
Ruan, Hanying
Ren, Yan
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 231/02 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/38 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
National Institute of Biological Sciences, Beijing (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Lei, Xiaoguang
Su, Yaning
He, Sudan
Ruan, Hanying
Sun, Liming
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Qi, Xiangbing
Wang, Yanli
Sun, Yuze
Abstract
Compounds that inhibit kinase Lck or Btk, pharmaceutically acceptable salts, hydrides, stereoisomers and pharmaceutical compositions thereof are disclosed.
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Zhou, Yu
Lin, Xingyu
Abstract
2B antagonist of formula I:
2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
C07D 251/72 - Heterocyclic compounds containing 1,3,5-triazine rings condensed with carbocyclic rings or ring systems
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 255/51 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings containing at least two cyano groups bound to the carbon skeleton
C07C 255/53 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and hydroxy groups bound to the carbon skeleton
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Peng, Shiming
Abstract
The invention provides compounds of Formula l that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity and/or inhibiting weight gain or promoting weight loss, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition are also provided. (see formula I)
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/535 - 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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Su, Yaning
Ruan, Hanying
Ren, Yan
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Lei, Xiaoguang
Su, Yaning
He, Sudan
Ruan, Hanying
Sun, Liming
Abstract
The invention provides amides of Formula I that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition. (see formula I)
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 275/06 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton
C07C 311/03 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07D 213/06 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Su, Yaning
Ruan, Hanying
Ren, Yan
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
A61P 43/00 - Drugs for specific purposes, not provided for in groups
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Wang, Xiaodong
Lei, Xiaoguang
Su, Yaning
He, Sudan
Ruan, Hanying
Sun, Liming
Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 235/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 275/06 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton
C07C 311/03 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07D 213/06 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Zhang, Zhiyuan
Huang, Shaoqiang
Zhang, Zhaolan
Su, Yaning
Ren, Yan
Abstract
Provided are compounds of SGLT-2 inhibitors, pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
C07D 307/10 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 307/30 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Lei, Xiaoguang
He, Sudan
Li, Chao
Dong, Ting
Abstract
The invention provides novel compounds and compositions for inhibiting IKKα/β, including treating disorders associated with IKKα/β activity, including cancer, autoimmune and inflammatory disorders, with a compound of structure shown above.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Zhou, Yu
Lin, Xingyu
Abstract
The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
C07D 251/22 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 5/00 - Drugs for disorders of the endocrine system
A61P 9/00 - Drugs for disorders of the cardiovascular system
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Xi, Rongwen
Liu, Xicheng
Abstract
IL-6 or STAT3 signaling is attenuated and associated disorders are treated with a hREG3A protein or an expression vector encoding said hREG3A protein, and optionally with a second, different drug for the disorder.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Zhou, Yu
Lin, Xingyu
Abstract
The invention provides novel compounds and compositions comprising a 5-HT2B antagonist of formula I and related methods for treating a person having a disorder characterized by undesirable 5-HT2B receptor signaling, such as migraine, irritable bowel syndrome (IBS), pulmonary arterial hypertension (PAH), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (GI) tract disorders.
C07D 251/22 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 5/00 - Drugs for disorders of the endocrine system
A61P 9/00 - Drugs for disorders of the cardiovascular system
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Zhi, Gang
Chai, Jijie
Peng, Shiming
Hou, Nannan
Abstract
Weight gain is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2- enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-weight gain medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-weight gain medicament.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
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
90.
ENTACAPONE FOR PREVENTION AND TREATMENT OF OBESITY AND RELATED METABOLIC DISEASES
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Huang, Niu
Zhi, Gang
Chai, Jijie
Peng, Shiming
Hou, Nannan
Abstract
Weight gain is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2- enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-weight gain medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-weight gain medicament.
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
National Institute of Biological Sciences, Beijing (China)
Inventor
Huang, Niu
Zhi, Gang
Chai, Jijie
Peng, Shiming
Hou, Nannan
Abstract
Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Li, Wenhui
Yan, Huan
Zhong, Guocai
Xu, Guangwei
He, Wenhui
Sui, Jianhua
Jing, Zhiyi
Huang, Yi
Abstract
The present invention relates to compositions and methods of treating or preventing HBV and/or HDV infection or a disease associated with said infection in a mammal through modulation of the production and/or function of the NTCP protein and polynucleotide, or its interaction with the viruses. Also provided are cell lines and non- human transgenic or humanized animals expressing an exogenous SLC10A1 gene that are susceptible to HBV and/or HDV infection, and use thereof for screening for drug candidate against infection or an associated disease.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
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
93.
USE OF XANTHOMONAS CAMPESTRIS EFFECTOR PROTEIN AS URIDINE MONOPHOSPHATE TRANSFERASE
The invention provides a use of the effector protein AvrAC derived from Xanthomonas campestris as a uridine monophosphate (UMP) transferase. AvrAC protein has UMP transferase activity and enables accomplishing UMP modification of itself and the substrate thereof, with serine and/or threonine as the modified site. Meanwhile, AvrAC protein can also UMP modify the substrate BIK1 and/or RIPK protein and inhibit the kinase activity of the substrate effectively.
The present invention discloses the use of substances targeting GC-C signaling pathway in the diagnosis and treatment for midbrain dopamine neurons diseases. One of the uses disclosed by the present invention is the method for constructing the animal model of attention deficit hyperactivity disorder using GC-C gene as the target. The method comprises the following steps: the GC-C gene of target mammal is knocked out, and the GC-C gene knockout animal obtained is the animal model of attention deficit hyperactivity disorder. The animal model of attention deficit hyperactivity disorder can be used to screen products for preventing and/or treating diseases related with midbrain dopamine system.
NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING (China)
Inventor
Shao, Feng
Li, Hongtao
Xu, Hao
Zhou, Yan
Abstract
A method for inactivating mitogen activated protein kinase, which comprises introducing recombinant eukaryote expression vector of genes encoding OspF protein and/or SpvC protein and/or HopAI1 protein into target eukaryote cell, disabling mitogen activated protein kinase of the eukaryote cell.
patents
