- 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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- Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: Discovery of novel, highly potent inhibitors of Factor Xa
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Ortho-substituted biphenyl moieties are widely used in drug design. We herein report a successful use of the perpendicular conformation of the alpha-substituted phenylcyclopropyl groups to mimic the aplanar, biologically active conformation of the ortho-substituted biphenyl moieties to achieve structural diversity. This is exemplified by the design and synthesis of a series of highly potent pyrazole bicyclic-based Factor Xa (FXa) inhibitors bearing alpha-substituted phenylcyclopropyl P4 moieties. The designed perpendicular conformation was confirmed by the X-ray structure of FXa-bound compound 2r. The potential structural basis for the high FXa potency in the phenylcyclopropyl P4 analogs and their improved FXa inhibitory activities compared with the biphenyl P4 counterparts are discussed.
- Qiao, Jennifer X.,Cheney, Daniel L.,Alexander, Richard S.,Smallwood, Angela M.,King, Sarah R.,He, Kan,Rendina, Alan R.,Luettgen, Joseph M.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
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scheme or table
p. 4118 - 4123
(2009/05/30)
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- COMPOUNDS USEFUL AS PHOSPHOTYROSINE MIMICS
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New uses are disclosed for compositions containing compounds of formula (I) wherein A, B, C, G, Q and R are defined herein. The compositions inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing li
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- HYDROXAMID ACID DERIVATIVES AS HISTONE DEACETYLASE (HDAC) INHIBITORS
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A compound having the following formula (I): wherein R?1? is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R?2? is hydroxyamino, R?3? is hydrogen or a suitable substituent, L?1? is -(CH?2#191)?n#191- (wherein n is an integer of 0 to 6) optionally substituted with one or more suitable substituent(s), wherein one or more methylene(s) may be replaced with suitable heteroatom(s), and L?2? is lower alkenylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
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- HDAC inhibitor
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A compound having the following formula (I): wherein R1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R2 is hydroxyamino, R3 is hydrogen or a suitable substituent, L1 is —(CH2)n— (wherein n is an integer of 0 to 6) optionally substituted with one or more suitable substituent(s), wherein one or more methylene(s) may be replaced with suitable heteroatom(s), and L2 is lower alkenylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
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- 1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS
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The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Compounds useful as phosphotyrosine mimics
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Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of
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- Substituted-aryl cyclopropanecarbonitriles and derivatives thereof as herbicide antidotes
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Substituted-aryl cyclopropanecarbonitriles and derivative compounds are antidotes for thiocarbamate, triazine-type and acetamide herbicides. These antidote compounds are especially effective in safening thiocarbamate herbicides used to control grassy weed
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