- BENZYL-1H-PYRAZOLO[3,4-B]PYRIDINES AND USE THEREOF
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The present application relates to novel benzyl-1H-pyrazolo[3,4-b]pyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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Paragraph 03005-0307
(2016/06/13)
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- BENZYL-1H-PYRAZOLO[3,4-B]PYRIDINES AND USE THEREOF
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The present application relates to novel benzyl-1H-pyrazolo[3,4-b]pyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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Paragraph 0373-0377
(2016/11/02)
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- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
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Page/Page column 718
(2015/02/02)
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- Benzamides
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The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
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Paragraph 0103
(2014/05/07)
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- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
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Paragraph 1061
(2014/07/23)
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- [1,2,4]TRIAZOLOPYRIDINES AND THEIR USE AS PHOSPODIESTERASE INHIBITORS
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The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
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- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
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- OXO-HETEROCYCLICALLY SUBSTITUTED ALKYL CARBOXYLIC ACIDS AND USE THEREOF
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The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 18
(2012/02/06)
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- TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES
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The present invention relates to a compound according to formula I, wherein R1, R2 and A are as defined herein, which exhibit PDE4 inhibitory activity and may be used in the treatment of inflammatory diseases or autoimmune diseases,
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Page/Page column 47; 48
(2010/08/05)
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- Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
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The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model.
- Sun, Daqing,Wang, Zhulun,Cardozo, Mario,Choi, Rebekah,DeGraffenreid, Michael,Di, Yongmei,He, Xiao,Jaen, Juan C.,Labelle, Marc,Liu, Jinsong,Ma, Ji,Miao, Shichang,Sudom, Athena,Tang, Liang,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
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scheme or table
p. 1522 - 1527
(2009/12/07)
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- Substituted arylpyrazoles
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This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
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Page/Page column 80
(2008/06/13)
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- Latent inhibitors part 11. The synthesis of 5-spirocyclopropyl dihydroorotic acid
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Approaches to the synthesis of 5-spirocyclopropyldihydroorotic acid are described. Difficulties were encountered in the lack of reactivity of diethyl 2-oxobutandicarboxylate and its derivatives towards cyclopropanation. Potential intermediates were prepar
- Husbands, Stephen,Fraser, William,Suckling, Colin J.,Wood, Hamish C. S.
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p. 865 - 870
(2007/10/02)
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- Aldehydes from Nitriles. Formation of N-Alkylnitrilium Ions and Their Reduction to N-Alkylaldimines by Organosilicon Hydrides
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A two-step procedure for the partial reduction of nitriles to aldehydes under mild reaction conditions is presented.This approach involves the N-alkylation of nitriles in dichloromethane solution and reductive capture of the resulting nitrilium ions to N-alkylaldimines with an organosilicon hydride such as triethylsilane or tri-n-hexylsilane.Mild hydrolysis of the aldimines produces aldehydes in generally good-to-excellent yield.Use of both triethyloxonium tetrafluoroborate and isopropyl chloride-iron(III) chloride reagents to effect alkylation is reported.Selective reduction of the nitrile function in polyfunctional substrates is possible with this technique.Over reduction to amines does not occur.Close control of reducing agent and reaction temperatures is not required.Attempts to effect reduction of nirile-boron trifluoride complexes with triethylsilane were unsuccessful, even at elevated temperatures.
- Fry, James L.,Ott, Roger A.
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p. 602 - 607
(2007/10/02)
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