1,2,5-thiadiazoles (including Hydrogenated) Patents (Class 514/362)
-
Patent number: 7396838Abstract: A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1: wherein R1, R2, R3, R4, and n are as defined herein.Type: GrantFiled: June 6, 2005Date of Patent: July 8, 2008Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
-
Publication number: 20080161366Abstract: The present invention is directed to aminoalkyl-substituted aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: July 3, 2008Applicant: WyethInventors: Casey Cameron McComas, Stephen Todd Cohn, Matthew Lantz Crawley, Andrew Fensome, Joel Adam Goldberg, Douglas John Jenkins, Callain Younghee Kim, Paige Erin Mahaney, Charles William Mann, Michael Anthony Marella, David John O'Neill, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski, An Thien Vu, Richard Page Woodworth, Puwen Zhang
-
Publication number: 20080153832Abstract: Disclosed herein is a pharmaceutical composition comprising a relaxant and a pan-alpha-2 receptor agonist. The composition is effective for treating gastrointestinal motility disorders, and methods of treating such disorders using the composition and compounds comprising it are also disclosed.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Inventors: Gregory F. Brooks, Daniel W. Gil
-
Publication number: 20080153829Abstract: Disclosed herein is a pharmaceutical composition comprising a 5-HT4 serotonin receptor agonist and a pan-alpha-2 receptor agonist. The composition is effective for treating gastrointestinal motility disorders, and methods of treating such disorders using the composition and compounds comprising it are also disclosed.Type: ApplicationFiled: December 10, 2007Publication date: June 26, 2008Inventors: Gregory F. Brooks, Daniel W. Gil
-
Publication number: 20080146624Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 18, 2007Publication date: June 19, 2008Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Eddy Wai Tsun Yue
-
Patent number: 7388006Abstract: The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.Type: GrantFiled: March 11, 2003Date of Patent: June 17, 2008Assignee: Bayer Schering Pharma AGInventors: Norbert Schmees, Manfred Lehmann, Ulrike Fuhrmann, Peter Muhn, Christa Hegele-Hartung, Michael Klotzbuecher
-
Publication number: 20080139576Abstract: Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels.Type: ApplicationFiled: September 24, 2007Publication date: June 12, 2008Inventors: Gary Mark Coppola, John William Davies, Charles Francis Jewell, Yu-Chin Li, James Richard Wareing, Donald Mark Sperbeck, Travis Matthew Stams, Sidney Wolf Topiol, Isidoros Vlattas
-
Publication number: 20080119476Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: July 1, 2005Publication date: May 22, 2008Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
-
Publication number: 20080113990Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: October 12, 2006Publication date: May 15, 2008Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
-
Patent number: 7368479Abstract: The invention relates to ?-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar1, and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1, and R2 stand independently of each other for hydrogen, optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R3 designates hydrogen, C3-C5alkenyl, C3-C5alkynyl or optionally substituted C1,-C5alkyl; R4 is optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R7, and R8 are independently of each other hydrogen or optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally suType: GrantFiled: June 18, 2003Date of Patent: May 6, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Eberle, Daniel Stierli, Urs Müller
-
Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
-
Patent number: 7354941Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.0): wherein R5 and R6 are taken together to form a moiety of partial Formulas (1.1.1) through (1.1.5): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 30, 2001Date of Patent: April 8, 2008Assignee: Pfizer Products Inc.Inventors: Anthony Marfat, Robert James Chambers
-
Publication number: 20080081815Abstract: A novel heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: September 29, 2006Publication date: April 3, 2008Applicant: GREEN CROSS CorporationInventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Youn Kang, Hee Jeong Seo, Kwang-Seop Song, Sung-Han Lee, Kwang-Woo Ahn
-
Publication number: 20080064688Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: January 20, 2006Publication date: March 13, 2008Inventors: Daniel L. Flynn, Peter A. Petillo
-
Patent number: 7338968Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.Type: GrantFiled: December 16, 2004Date of Patent: March 4, 2008Assignee: Schering CorporationInventors: Purakkattle J. Biju, Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Younong Yu, Junying Zheng, Jianhua Chao, Cynthia J. Aki
-
Patent number: 7335653Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: GrantFiled: April 23, 2007Date of Patent: February 26, 2008Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
-
Publication number: 20080039431Abstract: A method of improving the growth of a plant is provided by reducing the incidence of one or more insect-vectored viral infections. The method comprises the step of applying a primary treatment composition in-furrow during planting of a seed or seedling or during transplanting of the plant, wherein the primary treatment composition comprises an effective amount of a fungicide such as prothioconazole.Type: ApplicationFiled: August 1, 2007Publication date: February 14, 2008Inventors: Charles L. Cleary, Richard D. Rudolph, John E. Curtis, George H. Musson
-
Publication number: 20080004325Abstract: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1b (PTP1b).Type: ApplicationFiled: June 29, 2007Publication date: January 3, 2008Applicant: WyethInventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Eva Binnun, David V. Erbe, Eddine Saiah
-
Patent number: 7307078Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: September 20, 2006Date of Patent: December 11, 2007Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
-
Publication number: 20070281978Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.Type: ApplicationFiled: June 1, 2007Publication date: December 6, 2007Applicant: NIIGATA UNIVERSITYInventors: Tsutomu Nakada, Vincent J. Huber
-
Publication number: 20070281979Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in the application and which can be used in the form of pharmaceutical compositions.Type: ApplicationFiled: May 30, 2007Publication date: December 6, 2007Inventors: Marcel Gubler, Wolfgang Haap, Paul Hebeisen, Eric A. Kitas, Bernd Kuhn, Rudolf E. Minder, Brigitte Schott, Hans P. Wessel
-
Patent number: 7291635Abstract: Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels.Type: GrantFiled: April 2, 2003Date of Patent: November 6, 2007Assignee: Novartis AGInventors: Gary Mark Coppola, John William Davies, Charles Francis Jewell, Jr., Yu-Chin Li, James Richard Wareing, Donald Mark Sperbeck, Travis Mathew Stams, Sidney Wolf Topiol, Isidoros Vlattas
-
Patent number: 7288567Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 26, 2001Date of Patent: October 30, 2007Assignee: Methylgene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
-
Publication number: 20070249561Abstract: Disclosed are methods and compositions useful for treatment of neuropathic pain. In particular, the present invention provides methods of activating gamma-subtype peroxisome proliferator-activated receptors (PPAR?) to inhibit, relieve, or treat neuropathic pain.Type: ApplicationFiled: April 25, 2007Publication date: October 25, 2007Inventor: Bradley K. Taylor
-
Patent number: 7282512Abstract: Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.Type: GrantFiled: January 15, 2003Date of Patent: October 16, 2007Assignee: SmithKline Beecham CorporationInventors: John George Catalano, David Norman Deaton, Aaron Bayne Miller, Francis Xavier Tavares
-
Patent number: 7282513Abstract: Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein. The compounds are inhibitors of the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: March 2, 2006Date of Patent: October 16, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Laura Catherine Cooper, Timothy Harrison, Linda Elizabeth Keown, Andrew Madin, Mark Peter Ridgill
-
Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
-
Publication number: 20070155799Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.Type: ApplicationFiled: December 18, 2006Publication date: July 5, 2007Inventors: Tomasz W. Glinka, Dale Edward Shuster, Chander Shekher Celly, Robert D. Simmons, Jason Zhang
-
Patent number: 7230019Abstract: This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.Type: GrantFiled: December 16, 2002Date of Patent: June 12, 2007Assignee: Aegera Therapeutics, Inc.Inventors: James B. Jaquith, Gerald Villeneuve, Alain Boudreault, Stephen Morris, Jon Durkin, John W. Gillard, Kimberly Hewitt, H. Nicholas Marsh
-
Patent number: 7186743Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.Type: GrantFiled: April 25, 2005Date of Patent: March 6, 2007Assignee: Pharmacia CorporationInventors: Arija A. Bergmanis, Michael Clare, Joyce Z. Crich, Lifeng Geng, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Donna M. Iula, Francis J. Koszyk, Shuyuan Liao, Scott B. Mohler, Maria Nguyen, Richard A. Partis, Michael A. Stealey, Michael B. Tollefson, Richard M. Weier, Xiangdong Xu, Dominique Bonafoux, Theresa R. Fletcher, Bruce C Hamper, Patrick J. Lennon, Subo Liao, Suzanne Metz, David S. Oburn, Thomas J. Owen, Angela M. Scates, Michael L. Vazquez, Serge G. Wolfson
-
Patent number: 7183299Abstract: The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero ring-substituted oxime derivative. A tetrazoyloxime derivative represented by the general formula (1): X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a cyano group, a methanesulfonyl group, a nitro group, a trifluoromethyl group, or an aryl group; A represents a 1-alkyltetrazoyl-5-yl group or a 5-alkyltetrazoyl-1-yl group; and Het represents a pyridyl group having a substituent or a thiazoyl group having a substituent, and a plant disease controlling agent containing the same as an active ingredient are disclosed.Type: GrantFiled: August 16, 2002Date of Patent: February 27, 2007Assignee: Nippon Soda Co., Ltd.Inventors: Takeo Kobori, Hitoshi Kondo, Hiroyuki Tsuboi, Kumiko Akiba, Akihiro Koiso, Tsuneyuki Otaguro, Hidetoshi Nakayama, Hiroyuki Hamano, Akira Ohno, Toru Asada
-
Patent number: 7169797Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.Type: GrantFiled: February 4, 2004Date of Patent: January 30, 2007Assignee: Abbott LaboratoriesInventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
-
Patent number: 7160909Abstract: A novel class of tricyclic compounds of the following formula (I) is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.Type: GrantFiled: July 29, 2002Date of Patent: January 9, 2007Assignee: Eli Lilly and CompanyInventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Daniel Jon Sall, Jason Scott Sawyer
-
Patent number: 7157478Abstract: Compounds of formula I: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's diseaseType: GrantFiled: April 24, 2003Date of Patent: January 2, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Laura Catherine Cooper
-
Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
-
Patent number: 7125869Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: June 10, 2005Date of Patent: October 24, 2006Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
-
Patent number: 7125887Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: October 9, 2001Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: Jeffrey J. Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Yuan Cheng, legal representative, Christopher A. Willoughby, deceased
-
Patent number: 7115624Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.Type: GrantFiled: September 11, 2000Date of Patent: October 3, 2006Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Thomas Kruse Hansen, Lars Fogh Iversen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
-
Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
-
Patent number: 7078403Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.Type: GrantFiled: June 16, 2000Date of Patent: July 18, 2006Assignee: Biota Scientific Management Pty Ltd.Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
-
Patent number: 7078418Abstract: Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of one another are selected from the group consisting of —H, —CH3, —C2H5, —CN, —COOH, —COOCH3, —COOC2H5, —CONH2, or —C6H5 group, and n is the whole number 2, provided that R1 and R2 are not both —H and provided that R1 is not —H if R2 is —CH3 and R1 is not —CH3 if R2 is —H The compounds of general formula (I) show antitumor activity.Type: GrantFiled: September 22, 2000Date of Patent: July 18, 2006Inventors: Ivars Kalvins, Viktor Adrianov, Irina Shestakova, Iveta Kanepe, Ilona Domracheva
-
Patent number: 7078424Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: June 24, 2003Date of Patent: July 18, 2006Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
-
Patent number: 7071180Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: June 22, 2004Date of Patent: July 4, 2006Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
-
Patent number: 7041688Abstract: Compounds of formula (I) are disclosed.Type: GrantFiled: April 24, 2003Date of Patent: May 9, 2006Assignee: Merck Sharp & Dohme Lt.d.Inventors: Alister Campbell, Mark Peter Ridgill
-
Patent number: 7041689Abstract: Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein.Type: GrantFiled: April 24, 2003Date of Patent: May 9, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian James Collins, Laura Catherine Cooper, Timothy Harrison, Linda Elizabeth Keown, Andrew Madin, Mark Peter Ridgill
-
Patent number: 7030119Abstract: The invention features a method for treating chronic pain using a compound of formula (I).Type: GrantFiled: July 5, 2000Date of Patent: April 18, 2006Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Alistair Dixon, Kevin Lee, Robert Pinnock
-
Patent number: 6974829Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: GrantFiled: May 7, 2003Date of Patent: December 13, 2005Assignee: Elan Pharmaceuticals, Inc.Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
-
Patent number: 6927215Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 2 to 10, n represents 0, 1 or 2. y represents unsubstituted or substituted methylene and p represents 1, 2 or 3, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 29, 2001Date of Patent: August 9, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Peter Lösel, Andreas Turberg, Olaf Hansen, Achim Harder
-
Patent number: 6911457Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.Type: GrantFiled: April 11, 2003Date of Patent: June 28, 2005Assignee: Carbomer, Inc.Inventor: Manssur Yalpani
-
Patent number: RE39130Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: June 6, 1994Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori