C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
  • GLUCOKINASE ACTIVATORS
    Publication number: 20110275665
    Abstract: Compounds are provided for use with hexokinases that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: July 18, 2011
    Publication date: November 10, 2011
    Applicant: TAKEDA SAN DIEGO, INC.
    Inventors: Sheldon X. Cao, Jun Feng, Stephen L. Gwaltney, David J. Hosfield, Robert J. Skene, Jeffrey A. Stafford, Mingnam Tang
  • Trisubstituted thiazole compounds, preparations methods, pharmaceutical compositions and medicals uses thereof
    Patent number: 8053581
    Abstract: The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.
    Type: Grant
    Filed: August 15, 2006
    Date of Patent: November 8, 2011
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.C. China
    Inventors: Song Li, Changbin Guo, Xiancheng Jiang, Junhai Xiao, Zhong Wu
  • Thiazole derivatives which inhibit stearoyl-CoA desaturase enzymes
    Patent number: 8049016
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: November 1, 2011
    Assignees: Novartis AG, Xenon Pharmaceuticals Inc
    Inventors: Sultan Chowdhury, Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Qi Jia, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
  • New Compounds
    Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Method for reducing side effects of CBreceptor agonist therapy using a combination of a selective CBreceptor agonist and a selective CBreceptor antagonist
    Patent number: 8044071
    Abstract: The present application describes a method of treating pain with a combination of a CB2 cannabinoid receptor agonist and rimonabast.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: October 25, 2011
    Assignee: Abbott Laboratories
    Inventor: William A. Carroll
  • Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics
    Publication number: 20110257211
    Abstract: Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 20, 2011
    Applicants: ADVANCED CANCER THERAPEUTICS, LLC, UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
  • PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
    Publication number: 20110251176
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: April 6, 2011
    Publication date: October 13, 2011
    Inventor: Xiaojing Wang
  • Glucokinase activator
    Patent number: 8034819
    Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: October 11, 2011
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
  • RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE
    Publication number: 20110245304
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Application
    Filed: April 25, 2011
    Publication date: October 6, 2011
    Inventors: Yun YEN, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L. Perkins Harki, Leila Su
  • ORGANIC COMPOUNDS
    Publication number: 20110245239
    Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.
    Type: Application
    Filed: December 17, 2009
    Publication date: October 6, 2011
    Inventors: Steve Nanchen, Noëlle Gauvry, Thomas Goebel
  • PHARMACEUTICAL COMPOSITIONS FOR POORLY SOLUBLE DRUGS
    Publication number: 20110245305
    Abstract: The invention relates to solid dispersions of poorly soluble compounds formed by co-precipitation and hot melt extrusion, resulting in improved stability and bioavailability. The invention also relates to hot melt extrusion processes used to prepare such solid dispersions.
    Type: Application
    Filed: June 8, 2011
    Publication date: October 6, 2011
    Inventors: Ashish Chatterji, Zedong Dong, Harpreet K. Sandhu, Navnit Hargovindas Shah
  • BENZAMIDE GLUCOKINASE ACTIVATORS
    Publication number: 20110230529
    Abstract: The present invention relates to N-heteroaryl-benzamides of the formula (I), pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful as glucokinase activators.
    Type: Application
    Filed: December 6, 2010
    Publication date: September 22, 2011
    Applicant: TransTech Pharma, Inc.
    Inventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedso
  • Modulators Of HEC1 Activity And Methods Therefor
    Publication number: 20110230486
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.
    Type: Application
    Filed: March 15, 2011
    Publication date: September 22, 2011
    Inventors: Johnson Lau, Jiann-Jyh Huang
  • COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS
    Publication number: 20110230477
    Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
    Type: Application
    Filed: December 7, 2009
    Publication date: September 22, 2011
    Applicant: Euroscreen S.A.
    Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
  • Pyrrolidine derivatives
    Patent number: 8022096
    Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: September 20, 2011
    Assignee: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
  • PLATELET ADP RECEPTOR INHIBITORS
    Publication number: 20110212983
    Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 18, 2009
    Publication date: September 1, 2011
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
  • Small Molecule Choline Kinase Inhibitors, Screening Assays, and Methods for Safe and Effective Treatment of Neoplastic Disorders
    Publication number: 20110212994
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Application
    Filed: June 28, 2010
    Publication date: September 1, 2011
    Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
  • N-(2-THIAZOLYL)-AMIDE DERIVATIVES FOR THE TREATMENT OF OBESITY, DIABETES AND CARDIOVASCULAR DISEASES
    Publication number: 20110213000
    Abstract: The invention relates to the use of a compound of formula (I): its pharmaceutically acceptable salts, prodrugs and/or solvates, in the preparation of a medicinal product for the treatment of a disease presenting altered adiponectin levels or in which it is necessary to alter the adiponectin protein levels.
    Type: Application
    Filed: August 1, 2008
    Publication date: September 1, 2011
    Applicant: ZELTIA, S.A.
    Inventors: Ana Martínez Gil, Mercedes Alonso Cascón, Gema Santamaría Núñez, Marta Martínez Díez, Javier López Ogalla
  • Substituted indazoles as glucokinase activators
    Patent number: 8008332
    Abstract: Compounds are provided for use with hexokinases that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: August 30, 2011
    Assignee: Takeda San Diego, Inc.
    Inventors: Sheldon X. Cao, Jun Feng, Stephen L. Gwaltney, David J. Hosfield, Robert J. Skene, Jeffrey A. Stafford, Mingnam Tang
  • FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES
    Publication number: 20110201613
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Application
    Filed: July 3, 2009
    Publication date: August 18, 2011
    Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • 5-phenyl-thiazol-2-yl-urea derivatives and use as PI3 kinase inhibitors
    Patent number: 7998990
    Abstract: The present invention concerns a compound of formula Ia wherein: Ra* is hydrogen or C1-C4-alkyl; Rb* is —(C1-C4-alkylene)-Y—C1-C4-haloalkyl or —(C1-C4-alkylene)-Y—C1-C4-hydroxyalkyl; Y represents —CONH— or a five membered heteroaryl group.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: August 16, 2011
    Assignee: Novartis AG
    Inventors: Emma Budd, Judy Fox Hayler, Ian Bruce, Darren Mark Legrand, Brian Cox
  • Modulators of cystic fibrosis transmembrane conductance regulator
    Patent number: 7999113
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: August 16, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sarah Hadida-Ruah, Frederick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • METHODS TO TREAT NEURODEGENERATIVE CONDITIONS OR DISEASES BY TARGETING COMPONENTS OF A PTEN SIGNALING PATHWAY
    Publication number: 20110189308
    Abstract: The disclosure provides that components of a PTEN cell signaling pathway may be utilized as therapeutic targets for treating, preventing, slowing the progression of or delaying the onset of a neurodegenerative disease or disorder. Such components that may be targeted include, phosphatase and tensin homologue (PTEN), glycogen synthase kinase 3 beta (GSK3?), and AKT. The subject matter disclosed herein relates to the therapeutic use of inhibitors of PTEN, inhibitors of GSK3?, or activators of AKT to treat a neurodegenerative disease or disorder in a subject. Compounds are disclosed which may be used in the methods provided.
    Type: Application
    Filed: March 17, 2009
    Publication date: August 4, 2011
    Inventors: Asa Abeliovich, Keiichi Inoue
  • Benzoimidazole Derivatives and Glycogen Synthase Kinase-3 Beta Inhibitors Containing the Same
    Publication number: 20110190351
    Abstract: Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.
    Type: Application
    Filed: July 30, 2009
    Publication date: August 4, 2011
    Applicant: Oncotherapy Science, Inc.
    Inventors: Mitsuaki Ohtani, Yo Matsuo, Yingfu Li, Joel R. Walker, David M. Jenkins, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada
  • Modulators of ATP-Binding Cassette transporters
    Patent number: 7973169
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: July 5, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
  • Aminothiazoles as FBPase inhibitors for diabetes
    Patent number: 7973051
    Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: July 5, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Eric A. Kitas, Rudolf E. Minder, Peter Mohr, Hans Peter Wessel
  • CYCLOPENTYLACRYLAMIDE DERIVATIVE
    Publication number: 20110160211
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Application
    Filed: April 27, 2009
    Publication date: June 30, 2011
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Modulators of glucocorticoid receptor, AP-1, and/or NF-?B activity and use thereof
    Patent number: 7968577
    Abstract: 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 inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
  • Ribonucleotide reductase inhibitors and methods of use
    Patent number: 7956076
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: June 7, 2011
    Assignee: City of Hope
    Inventors: Yun Yen, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L Perkins Harki, Leila Su
  • PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF
    Publication number: 20110130397
    Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.
    Type: Application
    Filed: September 21, 2007
    Publication date: June 2, 2011
    Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
  • SPIROINDOLINONE PYRROLIDINES
    Publication number: 20110130398
    Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: November 4, 2010
    Publication date: June 2, 2011
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Bradford James Graves, Nan Jiang, Jing Zhang, Zhuming Zhang
  • HETEROAROMATIC GLUCOKINASE ACTIVATORS
    Publication number: 20110130402
    Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.
    Type: Application
    Filed: February 8, 2011
    Publication date: June 2, 2011
    Applicant: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Marit Kristiansen
  • 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY DISEASES
    Publication number: 20110124624
    Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Application
    Filed: February 3, 2011
    Publication date: May 26, 2011
    Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine LeBlanc, Darren Mark Le Grand, Clive McCarthy
  • 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY DISEASES
    Publication number: 20110124693
    Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Application
    Filed: February 3, 2011
    Publication date: May 26, 2011
    Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine Leblanc, Darren Mark Le Grand, Clive McCarthy
  • BENZIMIDAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20110124637
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: July 2, 2009
    Publication date: May 26, 2011
    Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • HETEROCYCLIC COMPOUND
    Publication number: 20110118236
    Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.
    Type: Application
    Filed: March 25, 2009
    Publication date: May 19, 2011
    Inventors: Michiyo Mochizuki, Shotaro Miura
  • COMPOSITIONS AND METHODS RELATING TO HEAT SHOCK TRANSCRIPTION FACTOR ACTIVATING COMPOUNDS AND TARGETS THEREOF
    Publication number: 20110112073
    Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 12, 2011
    Applicant: DUKE UNIVERSITY
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • OXAZOLINE DERIVATIVES
    Publication number: 20110112080
    Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 12, 2011
    Inventors: Guido Galley, Roger Norcross, Alessandra Polara
  • Compounds which modulate the CB2 receptor
    Patent number: 7928123
    Abstract: 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: Grant
    Filed: September 13, 2007
    Date of Patent: April 19, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Thiazole Derivatives and Use Thereof
    Publication number: 20110086843
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: November 23, 2010
    Publication date: April 14, 2011
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
    Publication number: 20110086855
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Applicant: Abbott Laboratories
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
  • N-HETEROARYL INDOLE CARBOXAMIDES AND ANALOGUES THEREOF, FOR USE AS GLUCOKINASE ACTIVATORS IN THE TREATMENT OF DIABETES
    Publication number: 20110082144
    Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.
    Type: Application
    Filed: September 30, 2010
    Publication date: April 7, 2011
    Applicant: TransTech Pharma, Inc.
    Inventors: Jesper F. Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
  • NOVEL 17 BETA LUPANE DERIVATIVES
    Publication number: 20110077251
    Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
  • Urea Glucokinase Activators
    Publication number: 20110077234
    Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
    Type: Application
    Filed: December 7, 2010
    Publication date: March 31, 2011
    Applicant: Novo Nordisk A/S
    Inventors: Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
  • INHIBITORS OF IAP
    Publication number: 20110077265
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.
    Type: Application
    Filed: April 29, 2008
    Publication date: March 31, 2011
    Applicant: Genentech, Inc.
    Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
  • Thiazole Derivatives and Use Thereof
    Publication number: 20110071113
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: November 23, 2010
    Publication date: March 24, 2011
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jérôme Dorbais, Thomas Rueckle
  • NEW CHEMICAL COMPOUNDS
    Publication number: 20110059938
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
  • MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20110053958
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: March 17, 2009
    Publication date: March 3, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • ANTI-CYTOKINE HETEROCYCLIC COMPOUNDS
    Publication number: 20110053955
    Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.
    Type: Application
    Filed: February 7, 2008
    Publication date: March 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
  • Aryl carbonyl derivatives as therapeutic agents
    Patent number: 7897628
    Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: March 1, 2011
    Assignee: Novo Nordisk A/S
    Inventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen