- HALOALLYLAMINE COMPOUNDS AND APPLICATION THEREOF
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The present invention relates to the technical field of pharmaceuticals. Specifically, the present invention relates to a halo-allylamine compound, or a pharmaceutically acceptable salt, an ester, a stereoisomer or a tautomer thereof, and a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, and use in preventing and/or treating a disease related to or mediated by the SSAO/VAP-1 protein,wherein R1, R2, R3, R4, R5, R6, L1 and Cy1 are defined in the specification.
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Paragraph 0514-0516
(2021/10/15)
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- HETEROCYCLICALLY SUBSTITUTED TRIFLUOROMETHYLPYRIMIDINONES AND THEIR USE
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The present application relates to novel heterocyclically substituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.
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Paragraph 0201
(2017/02/24)
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- Benzhydrol-pyrazole derivatives having kinase inhibitory activity and uses thereof
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The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventi
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Page/Page column 47
(2016/08/17)
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- HETEROCYCLIC SUBSTITUTED TRIFLUOROMETHYL PYRIMIDINONES AND THEIR USE
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The present application relates to novel heterocyclically substituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.
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Paragraph 0436
(2016/10/04)
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- Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup
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Our investigation of the structure-activity and structure-liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can impact in
- Devasthale, Pratik,Wang, Wei,Hernandez, Andres S.,Moore, Fang,Renduchintala, Kishore,Sridhar, Radhakrishnan,Pelleymounter, Mary Ann,Longhi, Daniel,Huang, Ning,Flynn, Neil,Azzara, Anthony V.,Rohrbach, Kenneth,Devenny, James,Rooney, Suzanne,Thomas, Michael,Glick, Susan,Godonis, Helen,Harvey, Susan,Cullen, Mary Jane,Zhang, Hongwei,Caporuscio, Christian,Stetsko, Paul,Grubb, Mary,Huang, Christine,Zhang, Lisa,Freeden, Chris,Li, Yi-Xin,Murphy, Brian J.,Robl, Jeffrey A.,Washburn, William N.
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p. 2793 - 2799
(2015/06/08)
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- BENZHYDROL-PYRAZOLE DERIVATIVES HAVING KINASE INHIBITORY ACTIVITY AND USES THEREOF
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The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventi
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Page/Page column 49
(2013/07/25)
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- SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS
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An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described.
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Page/Page column 19
(2011/06/10)
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- AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) including all pharmaceutically acceptable salts and stereoisomers thereof: wherein A is a mo
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Page/Page column 131-132
(2010/05/13)
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