- INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
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Page/Page column 96
(2021/09/11)
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- Pyridazinol compound and derivatives, preparation method, weeding compositions and application thereof
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The invention belongs to the technical field of pesticides, and particularly relates to a pyridazinol compound and derivatives, a preparation method, weeding compositions and application thereof. Thepyridazinol compound is shown as a general formula I whi
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Paragraph 0214; 0217-0218
(2021/02/24)
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- PYRAZOLOTRIAZINES
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The present invention provides compounds of general formula (I), in which X, R1, R2 and R3 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.
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Page/Page column 447-448
(2021/06/22)
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- Amide compounds and uses thereof
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Provided herein are novel amide compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the definition of each symbol is as described in the description.
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Page/Page column 77
(2021/10/11)
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- RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
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Paragraph 00264
(2020/07/06)
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- Fused tricyclic compounds and application thereof in medicaments
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The invention relates to fused tricyclic compounds and an application thereof in medicaments, and in particular to an application of the fused tricyclic compounds in medicaments for treating and/or preventing hepatitis B. In particular, the invention rela
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Paragraph 0338-0342
(2020/03/17)
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- FUSED TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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The present invention relates to a fused tricyclic compound and application thereof in medicine, especially as a medicament for the treatment and/or prevention of hepatitis B. Specifically, the present invention relates to a compound having Formula (I) or
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Paragraph 00198
(2020/03/23)
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- INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 654
(2018/02/28)
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- 2,4-DISUBSTITUTED PHENYLENE-1,5-DIAMINE DERIVATIVES AND APPLICATIONS THEREOF, AND PHARMACEUTICAL COMPOSITIONS AND PHARMACEUTICALLY ACCEPTABLE COMPOSITIONS PREPARED THEREFROM
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The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.
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Paragraph 0324; 0325
(2017/01/31)
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- HETEROCYCLIC COMPOUND
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The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) (in the formula, the symbols are as defined in the description) or a salt thereof.
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Paragraph 0697; 0698
(2017/04/11)
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- Heterocyclic compound
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本發明提供一種具有CDK8/19抑制活性之雜環化合物。本發明提供一種如下式代表之化合物(其中各代號均如本文之定義)或其鹽。 The present invention provides a heterocyclic compound possessing CDK8/19 inhibitory activity. The present invention provides a compound represented by the formula wherein each symbol is as defined herein, or a salt thereof.
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Paragraph 0198
(2017/09/28)
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- HETEROCYCLIC COMPOUND
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A compound represented by the formula (I): wherein each symbol is as described in the SPECIFICATION, or a salt thereof has a PDE2A inhibitory action, and is useful as a prophylactic or therapeutic drug for schizophrenia, Alzheimer's disease and the like.
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Paragraph 1374; 1375
(2016/06/28)
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- HETEROARYL SYK INHIBITORS
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The invention relates to new substituted heteroarylsof formula (1) wherein A is selected from the group consisting of N and CH, D is selected from the group consisting of S and O, E is C, T is C, G is C, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
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Page/Page column 46; 47
(2015/11/10)
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- HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS
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Provided are certain histone deacetylase (HDAC) inhibitors of Formula (I), compositions thereof, and methods of their use.
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Paragraph 00218
(2014/10/15)
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- HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
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Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
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Paragraph 00256
(2014/10/15)
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- 5-AZAINDAZOLE COMPOUNDS AND METHODS OF USE
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5-Azaindazole compounds of Formula (I), including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 119; 120
(2014/01/17)
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- FUSED HETEROAROMATIC PYRROLIDINONES
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Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
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Page/Page column 74
(2011/07/06)
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- Pyridazinone compounds
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The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
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Page/Page column 84
(2010/08/08)
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- [1, 2, 4] TRIAZOLO [1, 5-A] PYRIDINES AS JAK INHIBITORS
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Novel [1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a Formula represented by the following: (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, joint disease, inflammation, and others.
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Page/Page column 91; 92
(2010/04/03)
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