1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
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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: 7592461Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: GrantFiled: December 20, 2006Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang
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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: 20090227639Abstract: 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: ApplicationFiled: May 18, 2009Publication date: September 10, 2009Inventors: Jeffrey Lyle Gray, Kande K.D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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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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Patent number: 7585882Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: October 20, 2005Date of Patent: September 8, 2009Assignee: Memory Pharmaceuticals CorporationInventors: Allen Hopper, Robert Francis Dunn, Erik Mikal Kuester, Richard Dennis Conticello, Ruiping Liu, Ashok Tehim
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Patent number: 7585460Abstract: The invention relates to a method for inhibiting the biological acidification of water which is in contact with materials containing sulfur in reduced form or with elemental sulfur, susceptible to oxidation on the part of Thiobacilli, comprising putting said materials in contact with soluble inorganic salts at concentrations ranging from 0.4 normal to saturation.Type: GrantFiled: April 26, 2004Date of Patent: September 8, 2009Assignees: ENI S.p.A., Enitecnologie S.p.A.Inventors: Francesco Crescenzi, Antonella Crisari, Cesare Achille Piatti
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Patent number: 7576108Abstract: According to the present invention there is provided a compounds of formula (I): and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 16, 2003Date of Patent: August 18, 2009Assignee: Eli Lilly and CompanyInventors: Andreas Gerhard Weichert, David Gene Barrett, Stefan Heuser, Rainer Riedl, Mark Joseph Tebbe, Andrea Zaliani
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Patent number: 7557138Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: GrantFiled: October 4, 2004Date of Patent: July 7, 2009Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20090170845Abstract: Disclosed herein are methods and compositions for treating and/or prophylaxis of neuropathic pain in a subject. The methods comprise administering to the subject suffering from neuropathic pain, a therapeutically effective amount of a compound, according to Formula I: or a salt thereof, wherein A, R5 and R6 are defined herein.Type: ApplicationFiled: April 13, 2007Publication date: July 2, 2009Applicant: AEGERA THERAPEUTICS INC.Inventors: Jon Durkin, Kimberley Hewitt, Peter Winocour
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Patent number: 7553973Abstract: The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors. Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: March 21, 2006Date of Patent: June 30, 2009Assignee: Merck Frosst Canada Ltd.Inventors: 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: 20090131490Abstract: The present invention is directed to a method of treating a subject for a pulmonary disease by administering a therapeutically effective amount of a compound of the formula: wherein R1, R2 or R3 are each independently a C1 to C6 alkyl, a halogen, a sulfate, or a phosphate. The pulmonary disease in the subject can be hypoxic pulmonary vasoconstriction, pulmonary edema, pulmonary hypertension, asthma, chronic obstructive pulmonary disease, cystic fibrosis, interstitial fibrosis, high altitude residence, sleep apnea syndrome, atrial septal defects, and pulmonary diseases associated with other conditions. If this same compound is modified so that R1, R2 or R3 each independently is a C1 to C6 alkyl and the compound is not a carbonic acid inhibitor, it can be administered to a subject to block hypoxic pulmonary vasoconstriction and/or prevent high altitude pulmonary edema.Type: ApplicationFiled: December 10, 2007Publication date: May 21, 2009Applicant: UNIVERSITY OF WASHINGTONInventor: Erik R. SWENSON
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Publication number: 20090118286Abstract: Use of heterobicyclic acrylamides of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description, for controlling pests, novel heterobicyclic acrylamides and processes for preparing these compounds, and also compounds of the formula (IA) in which A2, R1, R2, R5 and R6 are as defined in the description.Type: ApplicationFiled: February 27, 2006Publication date: May 7, 2009Applicant: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Jurgen Scherkenbeck, Graham Holmwood, Jurgen Wieschemeyer, Peter Losel, Olga Malsam, Mark Wilhelm Drewes, Karl-Heinz Kuck, Ulrike Wachendorf-Neumann, Christian Arnold, Vincent Lee Salgado, Thomas Bretschneider
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Patent number: 7524863Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: June 21, 2006Date of Patent: April 28, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Publication number: 20090105306Abstract: The present invention relates compounds of formula (I) wherein A and R1 are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.Type: ApplicationFiled: October 7, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Jennifer Frost, Teodozyj Kolasa, Bo Liu, Steven P. Latshaw, Xueqing Wang
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Publication number: 20090105240Abstract: The present disclosure relates to methods for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure further relates to compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome and acute myelogenous leukemia. The present disclosure also relates to methods for identifying compounds that can be used for treating leukemia, pre-leukemic conditions, as well as myelodysplastic syndrome.Type: ApplicationFiled: October 17, 2007Publication date: April 23, 2009Inventors: Tomas Mustelin, Lutz Tautz, Nicholas David Peter Cosford, Eduard Sergienko
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Publication number: 20090099209Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treatiType: ApplicationFiled: December 12, 2008Publication date: April 16, 2009Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
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Publication number: 20090099233Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 10, 2008Publication date: April 16, 2009Inventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
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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: 20090082350Abstract: Disclosed are heterocylic or heteroaryl compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090060874Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 5, 2008Publication date: March 5, 2009Inventors: Yao-Ling QIU, Ce WANG, Lu YING, Yat Sun OR
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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: 20090048228Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: December 9, 2005Publication date: February 19, 2009Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
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Publication number: 20090042953Abstract: 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: ApplicationFiled: April 7, 2008Publication date: February 12, 2009Applicant: AEGERA THERAPEUTICS, INC.Inventors: James B. JAQUITH, Gerald VILLENEUVE, Alain BOUDREAULT, Stephen J. MORRIS, Jon DURKIN, John W. GILLARD, Kimberley E. HEWITT, H. Nicholas MARSH
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Publication number: 20090030048Abstract: The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors. Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: June 27, 2008Publication date: January 29, 2009Inventors: Marc Blouin, Erich L. Grimm, Yves Gareau, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Richard Friesen
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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: 20080312256Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: ApplicationFiled: September 28, 2006Publication date: December 18, 2008Inventors: Gregory Raymond Bebernitz, Louise Kirman
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Publication number: 20080312163Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.Type: ApplicationFiled: June 13, 2007Publication date: December 18, 2008Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Publication number: 20080299176Abstract: A drug delivery device for placement in the eye includes a drug core comprising a hydrophobic pharmaceutically active agent, and a holder that holds the drug core. The holder is made of a material impermeable to passage of the active agent and includes an opening for passage of the pharmaceutically agent therethrough to eye tissue. The device includes polyurethane-siloxane-containing copolymers crosslinked with hydrophilic monomers.Type: ApplicationFiled: May 30, 2007Publication date: December 4, 2008Inventors: Yu-Chin Lai, Ruiwen Shi, O. William Lever, JR., Dominic V. Ruscio, Yan Huang
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Patent number: 7459473Abstract: 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: December 3, 1998Date of Patent: December 2, 2008Assignee: Glia Med, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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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: 20080280915Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: November 13, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Patent number: 7449486Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: GrantFiled: October 17, 2005Date of Patent: November 11, 2008Assignee: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
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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: 20080261931Abstract: A method of treating or preventing snoring, obstructive sleep apnea (OSA) and/or central sleep apnea (CSA) comprises administering a pharmacologically effective amount a salt of acetylhomotaurine (AcHT) such as calcium acamprosate (CA) to a patient. Also disclosed is the use of AcHT and CA for the manufacture of a medicament for treating or preventing snoring, OSA and/or CSA and of a diagnostic device, kit or composition; a protective patch comprising AcHT or CA; and a pharmaceutical composition comprising AcHT or CA and an agent capable of alleviating the effects of snoring OSA and/or CSA, in combined amounts effective in the treatment of snoring OSA and/or CSA, and a carrier.Type: ApplicationFiled: September 4, 2006Publication date: October 23, 2008Applicant: Cereu-Science ABInventors: Jan Hedner, Ludger Grote, Kaj Stenlof
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Publication number: 20080260643Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.Type: ApplicationFiled: March 27, 2008Publication date: October 23, 2008Applicant: OMEROS CORPORATIONInventors: John E. Bergmann, Neil S. Cutshall, Gregory A. Demopulos, Vincent A. Florio, George Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080253960Abstract: The present invention provides a non-naturally occurring lipoprotein nanoplatform (“LBNP”) comprising at least one cell surface receptor ligand; at least one lipoprotein; and at least one diagnostic agent and/or at least one therapeutic agent. In embodiments of the present invention, the cell surface receptor ligand is not a low-density lipoprotein receptor ligand and the cell surface receptor ligand is covalently bonded to the apoprotein. The present invention also provides pharmaceutical formulations comprising LBNPs and methods of making the LBNPs.Type: ApplicationFiled: April 1, 2005Publication date: October 16, 2008Applicant: The Trustees of the University of Pennsylvania Center for Technology TransferInventors: Gang Zheng, Jerry D. Glickson
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Publication number: 20080255123Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: October 12, 2007Publication date: October 16, 2008Applicant: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Publication number: 20080255145Abstract: 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: ApplicationFiled: March 19, 2008Publication date: October 16, 2008Applicant: Amgen Inc.Inventors: Holger Monenschein, James T. Rider, Guomin Yao, Qingping Zeng
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Patent number: 7435748Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: December 14, 2006Date of Patent: October 14, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison
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Publication number: 20080249093Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: ApplicationFiled: December 13, 2004Publication date: October 9, 2008Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
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Publication number: 20080249094Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R7, U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: ApplicationFiled: June 18, 2008Publication date: October 9, 2008Inventor: Yuhpyng L. Chen
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Publication number: 20080234273Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: June 3, 2006Publication date: September 25, 2008Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20080234233Abstract: A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is {circle around (1)} a fused polycyclic heteroaryl group wherein the ring which binds directly to —CONH— group in the formula (I) is a benzene ring, {circle around (2)} unsubstituted thiazol-2-yl group, or {circle around (3)} unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented byType: ApplicationFiled: May 20, 2008Publication date: September 25, 2008Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN INC.Inventors: Susumu MUTO, Akiko ITAI
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko