- PERIPHERAL ALKYL AND ALKENYL CHAINS EXTENDED BENZENE DERIVATIVES AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX) / histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.
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- A novel benzoyl amide compounds
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The invention relates to the field of medicinal chemistry, in particular to a novel benzamides compound or a salt acceptable in parmacy of the novel benzamides compound, a preparation method of the novel benzamides compound, a pharmaceutical composition containing the novel benzamides compound and an application of the pharmaceutical composition in preparation of antineoplastic drugs.
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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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- PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
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The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR,
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- Discovery of INCB9471, a potent, selective, and orally bioavailable CCR5 antagonist with potent anti-HIV-1 activity
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To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinit
- Xue, Chu-Biao,Chen, Lihua,Cao, Ganfeng,Zhang, Ke,Wang, Anlai,Meloni, David,Glenn, Joseph,Anand, Rajan,Xia, Michael,Kong, Ling,Huang, Taisheng,Feng, Hao,Zheng, Changsheng,Li, Mei,Galya, Laurine,Zhou, Jiacheng,Shin, Niu,Baribaud, Fredric,Solomon, Kim,Scherle, Peggy,Zhao, Bitao,Diamond, Sharon,Emm, Tom,Keller, Douglas,Contel, Nancy,Yeleswaram, Swamy,Vaddi, Kris,Hollis, Gregory,Newton, Robert,Friedman, Steven,Metcalf, Brian
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p. 483 - 487
(2011/03/20)
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- Conformationally constrained 3-(4-hydroxy-phenyl)-substituted-propanoic acids useful for treating metabolic disorders
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The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
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Page/Page column 48; 69
(2008/06/13)
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- 3-(4-PIPERIDINE-1YLMETHYL-PHENYL)-PROPION ACID-PHENYLAMIDE-DERIVATIVES AND RELATED COMPOUNDS USED IN THE FORM OF MCH ANTAGONISTS (MELANINE CONCENTRATING HORMONE) FOR TREATING EATING DISORDERS
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The invention relates to amid compounds of general formula (I), wherein groups and residuals A, B, b, W, X, Y, Z, R1, R2 and R3 have significances given in a claim 1. In addition, said invention relates to drugs containing at least one type of inventive amid. Because of the antagonist activity of an MCH-receptor, the inventive drugs are suitable for treating metabolic disturbances and/or eating disorders, in particular adiposity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 137-138
(2008/06/13)
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- Piperazinylpiperidine derivatives as chemokine receptor antagonists
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The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR
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Page/Page column 19
(2008/06/13)
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- Quinolone-based IMPDH inhibitors: Introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues
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The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone-based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1.
- Dhar, T. G. Murali,Watterson, Scott H.,Chen, Ping,Shen, Zhongqi,Gu, Henry H.,Norris, Derek,Carlsen, Marianne,Haslow, Kristin D.,Pitts, William J.,Guo, Junqing,Chorba, John,Fleener, Catherine A.,Rouleau, Katherine A.,Townsend, Robert,Hollenbaugh, Diane,Iwanowicz, Edwin J.
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p. 547 - 551
(2007/10/03)
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- Angiotensin II receptor antagonists
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The present invention relates to novel heterocyclic derivatives of the formulaAr--W--Hetwherein Ar, W and Het are as defined below, and related compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as regulators of the action of angiotensin II in mammals. The compounds of this invention are useful in the treatment and prevention of hypertension, glaucoma, renal disease, congestive heart failure, cognitive dysfunction, and other conditions in which the action of angiotensin II is implicated. This invention also relates to pharmaceutical compositions containing these compounds and to methods of inhibiting angiotensin II in mammals by administration of such compounds.
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