- PIPERIDINE COMPOUNDS AS PCSK9 INHIBITORS
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One aspect of the invention relates to a series of new PCSK9 inhibitor compounds comprising piperidine ring structures, including compounds of formula (I) and/or pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating PCSK9 receptor related diseases comprising administration of one or more compounds of formula (I) or a pharmaceutically acceptable salt thereof.
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- BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
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Paragraph 0368; 0460
(2015/06/25)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds of formula I, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in th
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Page/Page column 49
(2012/08/28)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection of following Fomula (I). Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 105
(2012/12/13)
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- Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: Pyrrole regioisomers and propionic acid replacement
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S-Nitrosoglutathione reductase (GSNOR) is a member of the alcohol dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, cardiovascular, and gastrointestinal systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently undergoing clinical development. We describe here the synthesis and structure-activity relationships (SAR) of novel pyrrole based analogues of N6022 focusing on scaffold modification and propionic acid replacement. We identified equally potent and novel GSNOR inhibitors having pyrrole regioisomers as scaffolds using a structure based approach.
- Sun, Xicheng,Qiu, Jian,Strong, Sarah A.,Green, Louis S.,Wasley, Jan W.F.,Colagiovanni, Dorothy B.,Mutka, Sarah C.,Blonder, Joan P.,Stout, Adam M.,Richards, Jane P.,Chun, Lawrence,Rosenthal, Gary J.
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supporting information; experimental part
p. 3671 - 3675
(2011/08/06)
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- Discovery of biphenylketones as dual modulators of inflammation and bone loss
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Biphenylketones were identified as novel inhibitors of NFκB activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 μM), showed oral activity, and was able to compl
- Greig, Iain R.,Coste, Emmanuel,Ralston, Stuart H.,Van'T Hof, Rob J.
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supporting information; experimental part
p. 5548 - 5551
(2010/12/29)
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- Organic compounds
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There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
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Page/Page column 76
(2010/03/02)
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- SUBSTITUTED HYDANTOINS
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The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
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Page/Page column 17
(2009/07/17)
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- MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 93-94
(2008/12/07)
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- Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors
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Aryldihydropyridazinones and aryldimethylpyrazolones with 2-benzyl vinylogous amide substituents have been identified as potent PDE3B subtype selective inhibitors. Dihydropyridazinone 8a (PDE3B IC50=0.19 nM, 3A IC50=1.3 nM) was selec
- Edmondson, Scott D.,Mastracchio, Anthony,He, Jiafang,Chung, Christine C.,Forrest, Michael J.,Hofsess, Scott,MacIntyre, Euan,Metzger, Joseph,O'Connor, Naphtali,Patel, Kajal,Tong, Xinchun,Tota, Michael R.,Van Der Ploeg, Lex H. T.,Varnerin, Jeff P.,Fisher, Michael H.,Wyvratt, Matthew J.,Weber, Ann E.,Parmee, Emma R.
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p. 3983 - 3987
(2007/10/03)
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