- NOVEL CYCLIC AMINOBENZOIC ACID DERIVATIVE
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The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or - (CH2)n- (n represents 0,1 or 2) ; X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and -COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
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Page/Page column 54-55
(2010/11/27)
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- ORGANIC COMPOUNDS
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Compounds of the formula (I) are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
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Page/Page column 108
(2008/06/13)
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- Synthesis of potent and highly selective inhibitors of human tryptase
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The serine protease tryptase has been implicated in allergic and inflammatory diseases and associated with asthma. The synthesis and SAR of a series of N1-activated-4-carboxy azetidinones are described, resulting in identification of BMS-363131 (2) as a potent inhibitor of human tryptase (IC503000-fold) for tryptase versus related serine proteases including trypsin.
- Slusarchyk, William A.,Bolton, Scott A.,Hartl, Karen S.,Huang, Ming-Hsing,Jacobs, Glenn,Meng, Wei,Ogletree, Martin L.,Pi, Zulan,Schumacher, William A.,Seiler, Steven M.,Sutton, James C.,Treuner, Uwe,Zahler, Robert,Zhao, Guohua,Bisacchi, Gregory S.
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p. 3235 - 3238
(2007/10/03)
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- Beta lactam compounds and their use as inhibitors of tryptase
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Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.
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Page column 211
(2010/11/29)
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- (E) and (Z)-3-styrylpiperidines as sigma ligands
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A class of (E) and Q-3-styrylpiperidine derivatives was prepared as racemates and evaluated for affinity at σ binding sites labeled with [3H]-(±-SKF-10,047. Some of these compounds exhibited high affinity and selectivity for σ verus D1 and D2 binding sites.
- Mantegani, Sergio,Brambilla, Enzo,Cremonesi, Paolo,Caccia, Carla,Fornaretto, Maria Gioia,Carfagna, Nicola,Colombo, Monica,McArthur, Robert A.,Varasi, Mario
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p. 1525 - 1530
(2007/10/03)
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