- SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY
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Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R1-R7, X, X', Y, Y', Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.
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Paragraph 00121
(2020/02/23)
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- HEPATITIS B CAPSID ASSEMBLY MODULATORS
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Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
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Paragraph 0416; 0417
(2019/12/30)
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- SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition of thrombin and/or kallikrein.
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- SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl) piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
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Described herein is the initial optimization of (+/-) N-benzyl-4- heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamide (1), a hit discovered in a high throughput screen run against the NS5B polymerase enzyme of the hepatitis C virus. This effort resulted in the identification of (S)-N-sec-butyl-6-((R)-3- (4-(trifluoromethoxy)benzylcarbamoyl)-4-(4-(trifluoromethoxy)phenylsulfonyl) piperazin-1-yl)pyridazine-3-carboxamide (2), that displayed potent replicon activities against HCV genotypes 1b and 1a (EC50 1b/1a = 7/89 nM).
- Gentles, Robert G.,Ding, Min,Zheng, Xiaofan,Chupak, Louis,Poss, Michael A.,Beno, Brett R.,Pelosi, Lenore,Liu, Mengping,Lemm, Julie,Wang, Ying-Kai,Roberts, Susan,Gao, Min,Kadow, John
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scheme or table
p. 3142 - 3147
(2011/06/24)
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- OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE
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Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
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Page/Page column 117-118
(2010/12/31)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 47
(2010/07/04)
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- DIKETO AZOLOPIPERIDINES AND AZOLOPIPERAZINES AS ANTI-HIV AGENTS
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Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful the treatment of HIV and AIDS.
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Page/Page column 109; 112
(2010/01/30)
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- Substituted β-alanine derivatives as cell adhesion inhibitors
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β-Alanine derivatives of Formula I are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
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- Efflux pump inhibitors
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Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.
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