- BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
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- HETEROARYL COMPOUNDS AS NECROSIS INHIBITORS, COMPOSITION AND METHOD USING THE SAME
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The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to necrosis. Formula (I) i
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Paragraph 00107; 00112-00113
(2020/07/25)
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- ANTI-BACTERIAL COMPOUNDS
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A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.
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Page/Page column 93-94
(2017/06/28)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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Paragraph 001239
(2016/12/22)
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- SUBSTITUTED 2,4,5,6-TETRAHYDROPYRROLO[3,4-C] PYRAZOLE AND 4,5,6,7-TETRAHYDRO-2H-PYRAZOLO [4,3-C] PYRIDINE COMPOUNDS AS GLYT1 INHIBITORS
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The invention provides a chemical entity of Formula (I), wherein R1, R2, R3, R4, R5 and X 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; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.
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Page/Page column 63
(2015/11/16)
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- 4-Azaindole Derivatives
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4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
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Paragraph 0427-0429
(2015/04/15)
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- 4-AZAINDOLE DERIVATIVES
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4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
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Page/Page column 49; 50
(2015/04/22)
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- Discovery of bacterial NAD+-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series
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Optimization of clearance of adenosine inhibitors of bacterial NAD +-dependent DNA ligase is discussed. To reduce Cytochrome P-450-mediated metabolic clearance, many strategies were explored; however, most modifications resulted in compounds wi
- Stokes, Suzanne S.,Gowravaram, Madhusudhan,Huynh, Hoan,Lu, Min,Mullen, George B.,Chen, Brendan,Albert, Robert,O'Shea, Thomas J.,Rooney, Michael T.,Hu, Haiqing,Newman, Joseph V.,Mills, Scott D.
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scheme or table
p. 85 - 89
(2012/03/10)
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- 4 - [CYCLOALKYLOXY (HETERO) ARYLAMINO] THIENO [2, 3 - D] PYRIMIDINES HAVING MNKL/ MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyrimidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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- CYCLOALKYL CONTAINING THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
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The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
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- PYRIDOOXAZEPINE DERIVATIVE AND USE THEREOF
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The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formula wherein A is -OR1 or -S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.
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Page/Page column 41
(2010/08/09)
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