- BIARYLAMIDE INHIBITORS OF LEUKOTRIENE PRODUCTION
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 95
(2012/06/30)
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- 3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
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Page/Page column 30
(2009/08/16)
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- Synthesis and anticancer activities of some thiazole derivatives
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In this study, 2-substituted 4-[3/4-(4-arylthiazole-2-yl)aminophenyl] thiazole derivatives and 2-[4-[2-substituted 4-methylthiazole-5-yl]thiazole-2- yl]amino-5-arylidenethiazoline-4-one derivatives have been synthesized. The cytotoxic and/or growth inhibitory effects of the 16 selected compounds were evaluated in vitro against approximately 66 human tumor cell lines derived from nine neoplastic diseases. Some of the compounds were found to act as anticancer agents.
- Kayagil, Ismail,Demirayak, Seref
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scheme or table
p. 2197 - 2207
(2010/04/24)
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- 1, 3, 4-BENZOTRIAZEPIN-2-ONE SALTS AND THEIR USE AS CCK RECEPTOR LIGANDS
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This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+-O-; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is -(CR11R12)m-X-(CR13R14)p-R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR15=CR16-, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H ; C1 to C6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.
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- Fructose 1,6-bisphosphatase inhibitors
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The present invention relates to certain quinazoline compounds which have utility in the treatment of diabetes mellitus, hypercholesterolemia, hyperlipidemia, diabetic complications and cancer. The invention also relates to pharmaceutical compositions and
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- Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: Synthesis, in vitro characterization, and x-ray crystallography
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The synthesis and in vitro structure-activity relationships (SAR) of a novel series of anilinoquinazolines as allosteric inhibitors of fructose-1,6-bisphosphatase (F16Bpase) are reported. The compounds have a different SAR as inhibitors of F16Bpase than a
- Wright, Stephen W.,Carlo, Anthony A.,Carty, Maynard D.,Danley, Dennis E.,Hageman, David L.,Karam, George A.,Levy, Carolyn B.,Mansour, Mahmoud N.,Mathiowetz, Alan M.,McClure, Lester D.,Nestor, Nestor B.,McPherson, R. Kirk,Pandit, Jayvardhan,Pustilnik, Leslie R.,Schulte, Gayle K.,Soeller, Walter C.,Treadway, Judith L.,Wan, Ing-Kae,Bauer, Paul H.
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p. 3865 - 3877
(2007/10/03)
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- SUBSTITUTED HETEROCYCLYL-PHENYLFORMAMIDINES AND SALTS THEREOF
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Compounds of the formula STR1 wherein R is hydrogen or methyl;R 1 is straight or branched alkyl of 1 to 6 carbon atoms, hydroxy(alkyl of 1 to 6 carbon atoms), mono-or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 cabon atoms) thio(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R 2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andX is pyrazol-3-yl, 1,2,4-triazol-3-yl, pyridin-2-yl, pyridin-3-yl, thiazol-4-yl, 2-methyl-thiazol-4-yl or 2-methylamino-thiazol-4-yl;tautomers thereof, and non-toxic, pharmacologiically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.
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