- Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as selective adenosine A3 antagonists
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To investigate the potency of an adenosine A3 receptor (A 3AR) antagonist as an anti-asthmatic drug, a novel series of 4-phenyl-5-pyridyl-1,3-thiazole derivatives was synthesized and evaluated in human adenosine A1, A
- Miwatashi, Seiji,Arikawa, Yasuyoshi,Matsumoto, Tatsumi,Uga, Keiko,Kanzaki, Naoyuki,Imai, Yumi N.,Ohkawa, Shigenori
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experimental part
p. 1126 - 1137
(2009/09/25)
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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 42
(2008/06/13)
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- Triazolopyrimidine heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds a
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Page/Page column 12
(2010/11/25)
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- Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as p38 MAP kinase inhibitors
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A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-α (TNF-α) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-α). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg). Further elucidation of this class of compounds may provide novel anti-inflammatory agents, such as anti-rheumatoid arthritis drugs.
- Miwatashi, Seiji,Arikawa, Yasuyoshi,Naruo, Ken-Ichi,Igaki, Keiko,Watanabe, Yasumasa,Kimura, Hiroyuki,Kawamoto, Tomohiro,Ohkawa, Shigenori
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p. 410 - 418
(2007/10/03)
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- Adenosine A3 receptor antagonists
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A pharmaceutical composition for antagonizing adenosine at adenosine A3receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.
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- Process for making 5-substituted pyrazoles
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This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
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- Rate-equilibrium relationships for the deprotonation of 4-phenacylpyridines and 4-phenacylpyridinium cations
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Substituent effects upon the equilibria and kinetics of enolate ion formation from eight 4-(X-phenacyl)pyridines (5), eight 1-methyl-4-(X-phenacyl)pyridinium cations (6), five 1-benzyl-4-(X-phenacyl)pyridinium cations (7), and eight 1-(X-benzyl)-4-phenacy
- Stefanidis, Dimitrios,Bunting, John W.
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p. 3163 - 3168
(2007/10/02)
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