10421-19-9Relevant academic research and scientific papers
A METHOD OF TREATING LIVER FIBROSIS
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, (2012/09/11)
The present invention relates to a method of treating hepatis C and/or liver fibroisis with 3-cycloalkylaminopyrrolidine derivatives of the present invention
Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist
Xue, Chu-Biao,Feng, Hao,Cao, Ganfeng,Huang, Taisheng,Glenn, Joseph,Anand, Rajan,Meloni, David,Zhang, Ke,Kong, Lingquan,Wang, Anlai,Zhang, Yingxin,Zheng, Changsheng,Xia, Michael,Chen, Lihua,Tanaka, Hiroyuki,Han, Qi,Robinson,Modi, Dilip,Storace, Lou,Shao, Lixin,Sharief, Vaqar,Li, Mei,Galya, Laurine G.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Emm, Tom,Yeleswaram, Swamy,Contel, Nancy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
, p. 450 - 454 (2011/08/22)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC 50 of 4.7 nM in antagonism of c
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
McMinn, Dustin L.,Rew, Yosup,Sudom, Athena,Caille, Seb,DeGraffenreid, Michael,He, Xiao,Hungate, Randall,Jiang, Ben,Jaen, Juan,Julian, Lisa D.,Kaizerman, Jacob,Novak, Perry,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Wang, Zhulun,Powers, Jay P.
scheme or table, p. 1446 - 1450 (2010/01/16)
Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 were optimized to account for liabilities relating to in vitro pharmacokinetics, cytotoxicity and protein-related shifts in potency. A representative compound showing favorable in vivo pharmacokinetics was found to be an efficacious inhibitor of 11β-HSD1 in a rat pharmacodynamic model (ED50 = 10 mg/kg).
PIPERAZINE COMPOUNDS USEFUL AS ANTAGONISTS OF C-C CHEMOKINES (CCR2B AND CCR5) FOR THE TREATMENT OF INFLAMMATORY DISEASES
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Page/Page column 90-91, (2010/11/27)
A compound of formula (I) P - W - C(=X) - L - Q (I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y11 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
3-Cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors
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Page/Page column 22, (2008/06/13)
The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 52, (2010/02/11)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
3-(4-Heteroarylcyclohexylamino)cyclopentanecarboxamides as modulators of chemokine receptors
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Page/Page column 20, (2010/02/14)
The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or act
Alpha 1a adrenergic receptor antagonists
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, (2008/06/13)
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
