- Heterocyclic compound as well as pharmaceutical composition, preparation method, intermediate and application thereof
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The invention discloses a heterocyclic compound as well as a pharmaceutical composition, a preparation method, an intermediate and application thereof. The structure of the heterocyclic compound is shown as a formula I, and the heterocyclic compound has CDK7 inhibitory activity and can be used for treating diseases such as tumors.
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Paragraph 0437-0441
(2021/06/23)
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- INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
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Paragraph 00511
(2018/07/05)
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- BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
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The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
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Paragraph 00790
(2018/08/20)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0687; 0688
(2018/10/03)
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- SUBSTITUTED PYRIDINE AND PYRAZINE COMPOUNDS AS PDE4 INHIBITORS
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The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
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Paragraph 0353
(2014/09/30)
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- Synthesis of 5-bromo-6-methyl imidazopyrazine, 5-bromo and 5-chloro-6-methyl imidazopyridine using electron density surface maps to guide synthetic strategy
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Small heteroaromatic rings are valuable monomers in drug discovery that can enable rapid access to novel and desirable chemical space. Installation of a synthetic handle on a heteroaromatic core may be difficult if steric and electronic factors are not in alignment with the desired transformation. Described are practical routes for the construction of 5-bromo-6-methyl imidazopyrazine (1) as well as 5-bromo and 5-chloro-6-methyl imidazopyridines (2a and 2b), which were developed using electron density surface maps encoded with ionization potential to guide synthetic strategy.
- Harris, Anthony R.,Nason, Deane M.,Collantes, Elizabeth M.,Xu, Wenjian,Chi, Yushi,Wang, Zhihan,Zhang, Bingzhi,Zhang, Qingjian,Gray, David L.,Davoren, Jennifer E.
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experimental part
p. 9063 - 9066
(2011/12/03)
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- Heterocyclic compounds
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The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
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- N-heterocyclic sulfonamides having endothelin receptor activity
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The invention concerns pharmaceutically useful compounds of the formula I, in which R 1, R 2, R 3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.
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- Studies on Pyrazines. 6. A Facile Separation Method for a Mixture of the Isomeric 2-Amino-3,5, and 6-methylpyrazines
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This paper describes a facile separation method for a mixture of the isomeric aminomethylpyrazines by two-stage processes.Thus the mixture of aminomethylpyrazines was converted into that of the aminobromomethylpyrazines, which could be separated by chromatography on silica gel.Each of the bromopyrazines was hydrogenated to regenerate the original aminopyrazine as a pure form.
- Sato, Nobuhiro
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p. 143 - 147
(2007/10/02)
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