1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
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Publication number: 20100183658Abstract: The invention provides classes of novel compounds that accelerate peptide loading to DR in the absence of DM and related pharmaceutical compositions. The invention also provides conjugates of these compounds with peptides, antigens or other MHC-based therapeutics, including peptides that self-catalyze their loading onto MHC Class II molecules. Methods are provided for modulating an immune response in a subject. Also disclosed are methods of using the novel compounds, e.g., in combination with MHC-based therapeutics, for the treatment of autoimmune diseases and for the manufacture of medicaments. Methods of improving loading of viral peptides and tumor peptides for enhancing the CD4 T cell response following vaccination against viruses or tumors, and related vaccines, are also provided.Type: ApplicationFiled: March 28, 2008Publication date: July 22, 2010Applicants: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Kai W. Wucherpfennig, Melissa Joy Call, Xuechao Xing, Ross L. Stein, Gregory D. Cuny
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Publication number: 20100184746Abstract: An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.Type: ApplicationFiled: May 30, 2008Publication date: July 22, 2010Inventors: Eijirou Umemura, Kou Kumura, Satomi Masaki, Kazutaka Ueda, Yoshinari Wakiyama, Yasuo Sato, Mikio Yamamoto, Keiichi Ajito, Takashi Watanabe, Chizuko Kaji
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Publication number: 20100184794Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: October 17, 2007Publication date: July 22, 2010Inventors: Tsuneo Yasuma, Yasufumi Miyamoto
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Patent number: 7759370Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or S1P receptors.Type: GrantFiled: August 1, 2007Date of Patent: July 20, 2010Assignee: Praecis PharmaceuticalsInventors: Ghotas Evindar, Hongfeng Deng, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang
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Patent number: 7759371Abstract: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(?W)R6 or the like; R3 represents a hydrogen atom, —C(?WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.Type: GrantFiled: April 7, 2008Date of Patent: July 20, 2010Assignees: Kyowa Hakko Kinn Co., Ltd., FUJIFILM CorporationInventors: Chikara Murakata, Kazuhiko Kato, Yoshihisa Ohta, Ryuichiro Nakai, Yoshinori Yamashita, Takeshi Takahashi
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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: 20100168189Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.Type: ApplicationFiled: February 8, 2008Publication date: July 1, 2010Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo
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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: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100160371Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: November 17, 2009Publication date: June 24, 2010Inventors: Gerald RANGES, William Scott, Michael Bombara, Deborah Rauner, Aniko Redman, Roger Smith, Holger Paulsen, David Gunn, Jinshan Chen, Joel Renick
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Patent number: 7741349Abstract: 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: April 5, 2006Date of Patent: June 22, 2010Assignee: Aegera Therapeutics Inc.Inventors: James B. Jaquith, Gerald Villeneuve, Alain Boudreault, Stephen J. Morris, Jon Durkin, John W. Gillard, Kimberley Hewitt, H. Nicholas Marsh
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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: 7732468Abstract: Disclosed are 3-aryl-6-aryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles and related compounds thereof, represented by the Formula I: wherein Ar1, Ar2, and X are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: November 15, 2007Date of Patent: June 8, 2010Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, Nilantha Sudath Sirisoma, Han-Zhong Zhang
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Publication number: 20100137323Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, , L2,M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Applicant: Amgen Inc.Inventors: Sean P. Brown, Paul Dransfield, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang
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Publication number: 20100137380Abstract: Patients having exercise limiting conditions and those at risk of developing such conditions are exposed to a regimen of hypoxic conditions that simulate various altitude conditions. The exposure is of a temporary nature, being from a few hours to most of a day or night in any one day and repeated on a personally worked out regimen of from a series of consecutive days to a regular number of “on” and “off” days, to a random number of days. An alternate regimen is such exposure for a few minutes at a time followed by normoxic rest period of a few minutes, with the cycle repeated multiple times over the course of a treatment session. The conditioning treatment strengthens the cardiac tissue and skeletal muscle and the results extend beyond the treatment periods whereby the patient's condition is substantially improved.Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Inventor: Simon Maybaum
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Patent number: 7728017Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: GrantFiled: November 30, 2006Date of Patent: June 1, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
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Publication number: 20100125067Abstract: The present invention relates to new sulfonamide inhibitors of carbonic anhydrase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 19, 2009Publication date: May 20, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Patent number: 7718678Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. X is N or N+O?, and Y is N or N+O?, provided that at least X or Y is N. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD.Type: GrantFiled: June 27, 2006Date of Patent: May 18, 2010Assignee: Schering CorporationInventor: Purakkattle J. Biju
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Publication number: 20100119512Abstract: The present invention provides methods for the treatment and diagnosis of disorders associated with excessive vascular permeability and edema.Type: ApplicationFiled: January 25, 2008Publication date: May 13, 2010Applicant: Joslin Diabetes CenterInventors: Edward P. Feener, Lloyd P. Aiello
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Publication number: 20100120784Abstract: Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O)2—, —NR6—, —C(O)—, —C(CH3)(OH)— or —C(CH3)?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) 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, such as atherosclerosis, obesity, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosisType: ApplicationFiled: April 17, 2008Publication date: May 13, 2010Inventors: Nicolas Lachance, Chun Sing Li, Jean-Philppe Leclerc, Yeeman K. Ramtohul
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Patent number: 7714003Abstract: 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: May 7, 2007Date of Patent: May 11, 2010Assignee: Aegera Therapeutics Inc.Inventors: James B. Jaquith, Alain Boudreault, Stephen J. Morris, Jon Durkin, John W. Gillard, Kimberley E. Hewitt
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Publication number: 20100113486Abstract: 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: May 4, 2009Publication date: May 6, 2010Applicant: 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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Publication number: 20100099662Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: ApplicationFiled: January 9, 2008Publication date: April 22, 2010Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Patent number: 7700635Abstract: 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: May 7, 2007Date of Patent: April 20, 2010Assignee: Aegera Therapeutics Inc.Inventor: James B. Jaquith
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Patent number: 7700634Abstract: Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of the derivatives for the treatment of pain.Type: GrantFiled: February 28, 2005Date of Patent: April 20, 2010Assignee: N.V. OrganonInventors: Julia Adam-Worrall, Angus John Morrison, Grant Wishart, Takao Kiyoi, Duncan Robert McArthur
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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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Publication number: 20100087479Abstract: 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: September 10, 2009Publication date: April 8, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20100081644Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 22, 2009Publication date: April 1, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20100076014Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.Type: ApplicationFiled: October 31, 2007Publication date: March 25, 2010Inventors: James E. Sheppeck, John l. Gilmore, T.G. Murali Dhar, Hai-Yun Xiao
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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: 20100069349Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z 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: September 16, 2009Publication date: March 18, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20100056507Abstract: The present invention relates to new phenylic derivatives exhibiting a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. These derivatives are of particular interest in a method for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said new phenylic derivatives and to methods for the preparation and use thereof.Type: ApplicationFiled: October 26, 2007Publication date: March 4, 2010Applicant: IPSEN PHARMA S.A.S.Inventors: Lydie Poitout, Jeremiah Harnett, Dennis Bigg, Carole Sackur, Eric Ferrandis
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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: 20100041719Abstract: 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 of various disorders.Type: ApplicationFiled: October 3, 2007Publication date: February 18, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Kateri Ahrendt, Robert Kirk Delisle, Jeremy Hans, Joseph P. Lyssikatos, John E. Robinson, Eli M. Wallace, Qian Zhao
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Publication number: 20100041721Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same.Type: ApplicationFiled: August 14, 2009Publication date: February 18, 2010Applicant: Radius Health, Inc.Inventor: Chris P. Miller
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Publication number: 20100029625Abstract: A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].Type: ApplicationFiled: June 22, 2006Publication date: February 4, 2010Applicants: KYOWA HAKKO KIRIN CO., LTD., FUJIFILM CORPORATIONInventors: Ryuichiro Nakai, Emi Shimoike, Hideaki Kusaka, Chikara Murakata, Yoshinori Yamashita
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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: 20100009936Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 1, 2007Publication date: January 14, 2010Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang
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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: 20100004219Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to whType: ApplicationFiled: October 31, 2007Publication date: January 7, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko
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Publication number: 20090325961Abstract: 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: ApplicationFiled: August 18, 2009Publication date: December 31, 2009Inventors: Jingwu Duan, Bin Jiang
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Publication number: 20090326011Abstract: Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.Type: ApplicationFiled: June 13, 2006Publication date: December 31, 2009Inventors: Luca Arista, Francesca Cardullo, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
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Publication number: 20090325981Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: ApplicationFiled: February 11, 2005Publication date: December 31, 2009Applicant: IRM LLCInventors: Valentina Molteni, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
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Publication number: 20090312374Abstract: The present invention is in relation to the derivatives of 4,6-disubstituted 1,2,4-triazolo-1,3,4-thiadiazole and a process to synthesize the said derivatives. Also, the present invention was able to establish the activity of the instant derivatives against anti-cancerous activity specific to cervical and oral cancer.Type: ApplicationFiled: September 20, 2006Publication date: December 17, 2009Applicants: UNIVERSITY OF MYSORE, JAWAHARLAL NEHRU CENTRE FOR ADVANCED SCIENTIFIC RESEARCHInventors: Tapas Kumar Kundu, Kanchugarakoppal Subbegowda Rangappa, Badi Sri Sailaja, Radhika Ashish Varier, Nanjundaswamy Shivananju
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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: 7625932Abstract: The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.Type: GrantFiled: August 27, 2004Date of Patent: December 1, 2009Assignee: Eli Lilly and CompanyInventors: Pamela Ann Albaugh, Esteban Dominguez-Manzanares, Jian Eric Hong, William Joseph Hornback, Delu Jiang, Paul Leslie Ornstein, Michelle Lee Thompson, Eric George Tromiczak, Zhipei Wu, Hamideh Zarrinmayeh, Dennis Michael Zimmerman, Ana Maria Castano Mansanet, Larry Gene Huffman, William David Miller
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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: 20090253758Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.Type: ApplicationFiled: February 19, 2009Publication date: October 8, 2009Inventor: Chris P. Miller
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Publication number: 20090253699Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: October 13, 2005Publication date: October 8, 2009Applicant: PCT Therapeutics, Inc.Inventors: Neil G. Almstead, Guangming Chen, Gary M. Karp, Ellen Welch, Richard Wilde, Jeffrey A. Campbell