Nitrogen Attached Directly To The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/138)
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Publication number: 20110201609Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.Type: ApplicationFiled: June 30, 2009Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20110144066Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.Type: ApplicationFiled: April 14, 2009Publication date: June 16, 2011Applicants: The Board of Regents of the University of Texas System, Arizona Board of Regents on Behalf of the University of ArizonaInventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Vijay Gokhale, Garth Powis, Shuxing Zhang
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Publication number: 20110130396Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: July 1, 2009Publication date: June 2, 2011Inventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
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Patent number: 7919514Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: March 19, 2008Date of Patent: April 5, 2011Assignee: Amgen Inc.Inventors: Holger Monenschein, James Thomas Rider, Guomin Yao, Qingping Zeng
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Patent number: 7910612Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: March 22, 2011Assignee: Sanofi-AventisInventors: Stefanie Keil, Karl Schoenafinger, Hans Matter, Matthias Urmann, Maike Glien, Wolfgang Wendler, Hans-Ludwig Schaefer, Eugen Falk
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Patent number: 7858647Abstract: The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: December 28, 2010Assignee: Sanofi-AventisInventors: Stefanie Keil, Hans Matter, Karl Schoenafinger, Matthias Urmann, Maike Glien, Wolfgang Wendler, Hans-Ludwig Schaefer, Eugen Falk
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Publication number: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 7772257Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: September 24, 2009Date of Patent: August 10, 2010Assignee: Sanofi-AventisInventors: Karl Schoenafinger, Stefanie Keil, Matthias Urmann, Hans Matter, Maike Glien, Wolfgang Wendler
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Patent number: 7754745Abstract: Azacyclopentane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: GrantFiled: June 8, 2007Date of Patent: July 13, 2010Assignee: Merck Frosst Canada Ltd.Inventors: Chun Sing Li, Yeeman K. Ramtohul
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Publication number: 20100168190Abstract: The present invention relates to novel heterocyclic compounds, including oxadiazole compounds, pharmaceutical compositions and their use in the inhibition of reverse transcriptase and the treatment of HIV (1 and 2) infections, AIDS and ARC and other viral infections.Type: ApplicationFiled: July 2, 2008Publication date: July 1, 2010Applicant: YALE UNIVERSITYInventor: William L. Jorgensen
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Publication number: 20100152254Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.Type: ApplicationFiled: February 19, 2008Publication date: June 17, 2010Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Meir Bialer, Boris Yagen, Neta Pessah
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Patent number: 7700636Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: March 19, 2008Date of Patent: April 20, 2010Assignee: Amgen Inc.Inventors: Holger Monenschein, George Erich Wohlhieter, Qingping Zeng
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Patent number: 7683181Abstract: The present invention comprises cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their functional derivatives as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various R1-R9 substituents are defined herein. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: March 23, 2010Assignee: Sanofi-aventisInventors: Karl Schoenafinger, Stefanie Keil, Matthias Urmann, Hans Matter, Maike Glien, Wolfgang Wendler
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Publication number: 20100041720Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein Y, X1, X2, X3, R1, and R2 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Steven P. Latshaw, Bo Liu, Meena V. Patel, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20100022603Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: September 24, 2009Publication date: January 28, 2010Applicant: SANOFI-AVENTISInventors: Karl SCHOENAFINGER, Stefanie KEIL, Matthias URMANN, Hans MATTER, Maike GLIEN, Wolfgang WENDLER
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Publication number: 20100004298Abstract: Provided are 5-membered heterocycle-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: ApplicationFiled: September 11, 2009Publication date: January 7, 2010Inventors: Qing Dong, Fabrice Pierre, Jianqiang Wang
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Publication number: 20090298836Abstract: The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: ApplicationFiled: July 15, 2008Publication date: December 3, 2009Applicant: Amgen Inc.Inventors: Qingping Zeng, Chester Chenguang Yuan, Guomin Yao, Xianghong Wang, Seifu Tadesse, Andreas Reichelt, Qingyian Liu, Matthew R. Lee, Xin Huang, Fang-Tsao Hong, Nianhe Han, Christopher H. Fotsch, Celia Dominguez, Matthew P. Bourbeau, John G. Allen
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Patent number: 7612104Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: November 3, 2009Assignee: Sanofi-AventisInventors: Karl Schoenafinger, Stefanie Keil, Matthias Urmann, Hans Matter, Maike Glien, Wolfgang Wendler
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Publication number: 20090247500Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: ApplicationFiled: March 11, 2009Publication date: October 1, 2009Applicant: Abbott LaboratoriesInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rosemarie Tietje, Sridhar Peddi, William A. Carroll
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Patent number: 7589212Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising one or more human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: GrantFiled: June 26, 2007Date of Patent: September 15, 2009Assignee: Procter & Gamble CompanyInventors: Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Publication number: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Publication number: 20090227638Abstract: The instant invention provides compounds of Formula (Ia) which are leukotriene biosynthesis inhibitors, wherein X is O or S, Y is O, S, —NR6—CHR7— or —NR8—C(O)— and A is selected from 5-membered aromatic heterocyclic ring, 6-membered aromatic heterocyclic ring, naphthelenic or heterobicyclic aromatic ring system, phenyl and benzyl. A is optionally mono- or disubstituted. Compounds of Formula (Ia) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: March 21, 2006Publication date: September 10, 2009Inventors: Marc Blouin, Erich L. Grimm, Yves Gareau, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Richard Friesen
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Publication number: 20090136473Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: May 28, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao, Timothy Hagen
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Publication number: 20090118164Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: ApplicationFiled: February 22, 2008Publication date: May 7, 2009Inventors: William M. Pierce, JR., K. Grant Taylor, Leonard C. Waite
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Publication number: 20090093527Abstract: Azacyclopentane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: June 8, 2007Publication date: April 9, 2009Inventors: Chun Sing Li, Yeeman K. Ramtobul
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Publication number: 20090062286Abstract: The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.Type: ApplicationFiled: May 5, 2008Publication date: March 5, 2009Inventors: Kenneth William Foreman, Frances E. Park, Lee Arnold
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Publication number: 20090054494Abstract: The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: April 4, 2008Publication date: February 26, 2009Applicant: SANOFI-AVENTISInventors: Stefanie KEIL, Hans MATTER, Karl SCHOENAFINGER, Mathias URMANN, Maike GLIEN, Wolfgang WENDLER, Hans-Ludwig SCHAEFER, Eugen FALK
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Publication number: 20090012131Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: April 4, 2008Publication date: January 8, 2009Applicant: SANOFI-AVENTISInventors: Stefanie KEIL, Karl SCHOENAFINGER, Hans MATTER, Matthias URMANN, Maike GLIEN, Wolfgang WENDLER, Hans-Ludwig SCHAEFER, Eugen FALK
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Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
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Publication number: 20080280959Abstract: The present invention comprises cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their functional derivatives as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various R1-R9 substituents are defined herein. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: April 4, 2008Publication date: November 13, 2008Applicant: SANOFI-AVENTISInventors: Karl SCHOENAFINGER, Stefanie KEIL, Matthias URMANN, Hans MATTER, Maike GLIEN, Wolfgang WENDLER
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Publication number: 20080261996Abstract: The present invention relates to substituted propiolic acid amides, methods for the production thereof, medicaments containing these compounds and the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: October 23, 2008Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
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Publication number: 20080200371Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.Type: ApplicationFiled: March 28, 2008Publication date: August 21, 2008Inventors: Zacharia S. CHERUVALLATH, Colin J. Loweth, Ruth F. Nutt, Darryl Rideout, Joseph E. Semple, Jing Wang, Feiyue Wu, Shankari Mylvaganam, Hengyi Zhu, Jianzhong Sun
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Publication number: 20080146625Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: ApplicationFiled: December 6, 2007Publication date: June 19, 2008Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
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Patent number: 7354944Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: October 18, 2005Date of Patent: April 8, 2008Assignee: Amgen Inc.Inventors: Qingping Zeng, Guomin Yao, George Erich Wohlhieter, Vellarkad N. Viswanadhan, Andrew Tasker, James Thomas Rider, Holger Monenschein, Celia Dominguez, Matthew Paul Bourbeau
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Patent number: 7338966Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: June 9, 2005Date of Patent: March 4, 2008Assignee: SmithKline Beecham CorporationInventors: Karen Elizabeth Lackey, Edgar Raymond Wood, III
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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
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Patent number: 7226931Abstract: Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.Type: GrantFiled: July 21, 2005Date of Patent: June 5, 2007Assignee: Cumbre Pharmaceuticals Inc.Inventors: Charles Z. Ding, Zhenkun Ma, Jing Li, Susan Harran, Yong He, Keith P. Minor, In Ho Kim, Jamie C. Longgood, Yafei Jin, Keith D. Combrink
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Patent number: 7183277Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: March 31, 2003Date of Patent: February 27, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
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Patent number: 7122565Abstract: The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R?3, in which X2 is a binding group and R?3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.Type: GrantFiled: October 1, 2001Date of Patent: October 17, 2006Assignee: Warner-Lambert LLCInventors: Fabrice Vergne, Pierre Ducrot, Charles Andrianjara, Patrick Bernardelli, Edwige Lorth Ois
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Patent number: 7074532Abstract: Improved organophotoreceptors comprise: (a) a charge transport compound having the formula where n is an integer from 0 to 1; X is an (N,N-disubstituted)arylamine group; Ar is an aryl group or a heterocyclic group; A is a first linking group with the formula —(CH2)p— which can be branched or linear, where p is an integer from 3 to 20 inclusive and where one or more methylene groups can be optionally replaced by O, S, a carbonyl group, urethane, urea, an ester group, a —NR16 group, a CHR17 group, or a CR18R19 group where R16, R17, R18 and R19 are, independently, H, hydroxyl, thiol, an amine group, an alkyl group, an alkaryl group, an aryl group, or part of a ring; and B is a second linking group having the formula -Q-Z-Q?-, where Q and Q? are, independently, O, S, or NR1, where R1 is an H, an alkyl group, an alkaryl group or an aryl group, and Z comprises a heterocyclic group; (b) a charge generating compound; and (c) an electrically conductive substrate over which said charge transport compound aType: GrantFiled: September 16, 2003Date of Patent: July 11, 2006Assignee: Samsung Electronics, Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Maryte Daskeviciene, Vygintas Jankauskas, Janina Gavutiene
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Patent number: 7071217Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III
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Patent number: 7041670Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: GrantFiled: April 8, 2003Date of Patent: May 9, 2006Assignee: Schering-Plough Animal Health CorporationInventors: Constantine G. Boojamra, Lee S. Chong, Scott J. Hecker, Tomasz W. Glinka, Dale E. Shuster
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Patent number: 6835725Abstract: Optical data carrier comprising a preferably transparent substrate which may, if desired, have previously been coated with one or more reflection layers and to whose surface a light-writeable information layer, if desired one or more reflection layers and if desired a protective layer or a further substrate or a covering layer have been applied, which can be written on or read by means of blue, red or infrared light, preferably laser light, where the information layer comprises a light-absorbent compound and, if desired, a binder, characterized in that at least one cyanine dye is used as light-absorbent compound.Type: GrantFiled: March 20, 2002Date of Patent: December 28, 2004Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Friedrich-Karl Bruder, Wilfried Haese, Rainer Hagen, Karin Hassenrück, Serguei Kostromine, Peter Landenberger, Rafael Oser, Thomas Sommermann, Josef-Walter Stawitz, Thomas Bieringer
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Publication number: 20040171651Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: February 19, 2004Publication date: September 2, 2004Inventors: Robert Eugene Hormann, Orestes Chortyk, Dat Phat Le
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Publication number: 20040127526Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1Type: ApplicationFiled: December 10, 2003Publication date: July 1, 2004Applicant: WyethInventors: Robert J. Steffan, Amedeo A. Failli
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Publication number: 20040116414Abstract: 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 &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-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: ApplicationFiled: May 7, 2003Publication date: June 17, 2004Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
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Patent number: 6716841Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: GrantFiled: July 26, 2002Date of Patent: April 6, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Irina C. Jacobson, Mimi L. Quan
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Patent number: 6713498Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:Type: GrantFiled: May 30, 2002Date of Patent: March 30, 2004Assignee: Alteon IncorporatedInventor: Martin Gall
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Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Patent number: 6686363Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: November 27, 2002Date of Patent: February 3, 2004Assignee: Kyorin Pharmaceutical Co., Ltd.Inventor: Yasumichi Fukuda