- SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS
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The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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- CHEMOKING RECEPTOR ANTAGONISTS
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Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 139
(2013/03/26)
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- SPIROPIPERIDINES FOR USE AS TRYPTASE INHIBITORS
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The present invention is directed to a compound of Formula (I): (I) or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.
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Page/Page column 143
(2009/06/27)
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- Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives
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We have explored a series of spirocyclic piperidine amide derivatives (5) as tryptase inhibitors. Thus, 4 (JNJ-27390467) was identified as a potent, selective tryptase inhibitor with oral efficacy in two animal models of airway inflammation (sheep and guinea pig asthma models). An X-ray co-crystal structure of 4 · tryptase revealed a hydrophobic pocket in the enzyme's active site, which is induced by the phenylethynyl group and is comprised of amino acid residues from two different monomers of the tetrameric protein.
- Costanzo, Michael J.,Yabut, Stephen C.,Zhang, Han-Cheng,White, Kimberley B.,de Garavilla, Lawrence,Wang, Yuanping,Minor, Lisa K.,Tounge, Brett A.,Barnakov, Alexander N.,Lewandowski, Frank,Milligan, Cynthia,Spurlino, John C.,Abraham, William M.,Boswell-Smith, Victoria,Page, Clive P.,Maryanoff, Bruce E.
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p. 2114 - 2121
(2008/12/21)
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- Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
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Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R1 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.
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Page/Page column 25
(2008/06/13)
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- The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists
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Bipiperidine amide 1 has been identified as a CC chemokine receptor 3 (CCR3) antagonist. Optimization of its structure-activity relationship has resulted in the identification of cis (R,R)-4-[(3,4-dichlorophenyl)methyl]-3- hydroxymethyl-1′(6-quinolinylcar
- Ting, Pauline C.,Lee, Joe F.,Wu, Jie,Umland, Shelby P.,Aslanian, Robert,Cao, Jianhua,Dong, Youhao,Garlisi, Charles G.,Gilbert, Eric J.,Huang, Ying,Jakway, James,Kelly, Joseph,Liu, Zhidan,McCombie, Stuart,Shah, Himanshu,Tian, Fang,Wan, Yuntao,Shih, Neng-Yang
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p. 1375 - 1378
(2007/10/03)
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- Piperdine derivatives useful as CCR3 antagonists
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The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment
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Page/Page column 11
(2008/06/13)
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- Spiro-substituted azacycles as neurokinin antagonists
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Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
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- SPIRO-SUBSTITUTED AZACYCLES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to spiro-substituted azacycles of the Formula 1: STR1 (wherein R 1, l, m, Q, W, X, Y, and Z are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
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- Spiro piperidines and homologs which promote release of growth hormone
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There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
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