Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/349)
  • Publication number: 20120101079
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: October 19, 2011
    Publication date: April 26, 2012
    Applicant: Grunenthal GmbH
    Inventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Publication number: 20120094993
    Abstract: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: October 7, 2011
    Publication date: April 19, 2012
    Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
  • Publication number: 20120071482
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: August 24, 2011
    Publication date: March 22, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20120058985
    Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
    Type: Application
    Filed: April 29, 2011
    Publication date: March 8, 2012
    Applicant: DECIPHERA PHARMACEUTICALS, LLC
    Inventors: DANIEL L. FLYNN, MICHAEL D. KAUFMAN
  • Patent number: 8129416
    Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: March 6, 2012
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Laurence Clary, Corinne Millois Barbuis
  • Publication number: 20120053213
    Abstract: The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.
    Type: Application
    Filed: September 28, 2009
    Publication date: March 1, 2012
    Applicant: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA
    Inventors: Lan Xie, Xingtao Tian, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
  • Publication number: 20120034272
    Abstract: The present invention relates to a pharmaceutical dosage form comprising an active ingredient combination of nifedipine or nisoldipine and at least one angiotensin II antagonist and/or at least one diuretic, characterized in that nifedipine or nisoldipine is released in the body in a controlled (modified) manner and the angiotensin II antagonist and/or the diuretic is released rapidly (immediate release (IR)), and also to processes for their preparation, to their use as medicaments and to their use for the prophylaxis, secondary prophylaxis or treatment of disorders.
    Type: Application
    Filed: November 19, 2009
    Publication date: February 9, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexander Kuhl, Erich Brendel, Frank Bröcker, Adrian Funke, Andreas Ohm, Dennis Kvesic, Thomas Volkmer
  • Patent number: 8093272
    Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: January 10, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann
  • Publication number: 20110288092
    Abstract: Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R1, R2, R7, R8, R9 and W are as defined in the specification.
    Type: Application
    Filed: November 22, 2010
    Publication date: November 24, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Patent number: 8063039
    Abstract: A method for treating pain, migraine, inflammation, gastrointestinal tract disorders, disorders of the genito-urinary tract, ophthalmic diseases or obesity in a subject, the method including administering to the subject an effective amount of a compound of a general formula, specific examples of which include 3-(4-Butyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(4-trifluorobutyloxy)-benzylamino]-pyrrolidin-2-one, 3-(4-Pentyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(5-trifluoropentyloxy)-benzylamino]-pyrrolidin-2-one, and 3-(4-Phenylethyl-benzylamino)-pyrrolidin-2-one.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: November 22, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • Patent number: 8058272
    Abstract: The present disclosure relates to XIAP inhibitor compound of the formula I:
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: November 15, 2011
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
  • Publication number: 20110275599
    Abstract: The invention describes the use of a methylated vegetable oil having less than 10 percent by weight of saturated fatty acid methyl esters and less than 10 percent by weight of fatty acid methyl esters of carbon chain length less than C10 as a low-cloud point coformulant in pesticidal compositions.
    Type: Application
    Filed: May 3, 2011
    Publication date: November 10, 2011
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Christopher J. Voglewede, Karen M. Swayze, Holger Tank
  • 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
  • Publication number: 20110263612
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: April 12, 2011
    Publication date: October 27, 2011
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8044211
    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z—X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.
    Type: Grant
    Filed: May 1, 2007
    Date of Patent: October 25, 2011
    Assignee: Chroma Therapeutics Ltd.
    Inventors: David Charles Festus Moffat, Stephane Pintat, Stephen Davies
  • Patent number: 8044059
    Abstract: The use of an N,N-dimethyl alkylamide or an N-alkanoyl morpholine provides a stable emulsifiable concentrate composition that hinders de-esterification and transesterification of mixtures of a carboxylic acid herbicide and an ester of a different carboxylic acid herbicide. The N,N-dimethyl alkylamide or N-alkanoyl morpholine additionally stabilizes emulsifiable concentrates containing a triazolopyrimidine herbicide having at least one methoxy group on the triazolopyrimidine ring.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: October 25, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Derek J. Hopkins, Robert Matthew Buttimor
  • Patent number: 8039632
    Abstract: This invention relates to novel 2-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: November 12, 2007
    Date of Patent: October 18, 2011
    Assignee: Neurosearch A/S
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Palle Christophersen
  • Publication number: 20110251220
    Abstract: The present invention relates to pharmaceutical compositions comprising gamma secretase modulators as well as to the use of gamma secretase modulators for treating renal disorders, cancer, neurodegenerative disorders as well as related disorders.
    Type: Application
    Filed: June 2, 2009
    Publication date: October 13, 2011
    Inventors: Özlem Acikgöz, Jessica Ahmed, Bernd Dörken, Cornelius Frömmel, Andrean Goede, Franziska Jundt, Rudolf Kunze, Robert Preissner
  • Patent number: 8034949
    Abstract: The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: October 11, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasunori Moritani, Shigeru Furukubu, Yasunori Tsuboi, Chieko Okagaki, Akira Oku, Naomitsu Hirano
  • Publication number: 20110230483
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: March 14, 2011
    Publication date: September 22, 2011
    Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20110218199
    Abstract: Compounds of formula I are disclosed. These compounds are useful in the control or prevention of cancer.
    Type: Application
    Filed: August 20, 2008
    Publication date: September 8, 2011
    Inventors: Guy Georges, Klaus Kaluza, Matthias Koerner, Ulrike Reiff, Stefan Scheiblich, Wolfgang Von Der Saal, Stefan Weigand
  • Publication number: 20110218219
    Abstract: The present invention relates to substituted sulphonamido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 28, 2009
    Publication date: September 8, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ingo Hartung, Marion Hitchcock, Florian Puhler, Gerhard Siemeister, Roland Neuhaus
  • Publication number: 20110195979
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.
    Type: Application
    Filed: February 7, 2011
    Publication date: August 11, 2011
    Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
  • Publication number: 20110190285
    Abstract: The present invention provides methods of treating a botulinum toxin related condition in a subject. In certain embodiments, the methods involve administering a compound of the following formulas: (I), (II), (III), (IV), (V).
    Type: Application
    Filed: August 26, 2009
    Publication date: August 4, 2011
    Applicant: ABSOLUTE SCIENCE, INC.
    Inventors: Alan Jacobson, Scott Moe
  • Patent number: 7989441
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: August 2, 2011
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
  • Publication number: 20110183981
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 28, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110178136
    Abstract: Disclosed are amino acid and phosphate prodrugs of compounds of the Formula V wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: March 31, 2011
    Publication date: July 21, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110178120
    Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.
    Type: Application
    Filed: June 4, 2009
    Publication date: July 21, 2011
    Applicant: AMBRILIA BIOPHARMA, INC.
    Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
  • Publication number: 20110166161
    Abstract: This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 7, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Takeshi Terasawa, Shinji Shigenaga, Shinji Itoh, Jun Maeda, Hideyuki Watanabe, Satoshi Kubo, Noe Iahii
  • 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
  • Publication number: 20110159005
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 30, 2011
    Applicant: Abbott Laboratories
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Patent number: 7968592
    Abstract: 3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases.
    Type: Grant
    Filed: November 16, 2004
    Date of Patent: June 28, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • Publication number: 20110152323
    Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.
    Type: Application
    Filed: June 9, 2009
    Publication date: June 23, 2011
    Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Jianqi Li, Juan Feng, Wangping Cai
  • Publication number: 20110150873
    Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 23, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventor: David John Grainger
  • Publication number: 20110144160
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 16, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns
  • Publication number: 20110144164
    Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 16, 2011
    Applicant: H. LUNDBECK A/S
    Inventors: Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
  • Patent number: 7960415
    Abstract: The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: June 14, 2011
    Assignee: Vertex Pharmaceutical Incoporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Michael Mortimore, John Studley
  • Publication number: 20110112152
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: January 19, 2011
    Publication date: May 12, 2011
    Inventors: Shunqi Yan, Jean-Michel Vemier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20110092506
    Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 21, 2011
    Inventors: Yoshinori NAKAMURA, Norimitsu Hayashi, Takanori Higasahijima, Hitoshi Kubota, Kozo Oka
  • Publication number: 20110086761
    Abstract: The present invention relates to fungicidal compositions and their use for controlling oomycete pathogen induced disease or diseases in one or more plants.
    Type: Application
    Filed: October 13, 2010
    Publication date: April 14, 2011
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Norman R. Pearson, Lei Liu, Robert J. Ehr, John M. Atkinson
  • Publication number: 20110081426
    Abstract: The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 7, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Publication number: 20110071197
    Abstract: There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
    Type: Application
    Filed: April 16, 2009
    Publication date: March 24, 2011
    Inventors: Peter Nilsson, Martins Katkevics, Benjamin Pelcman
  • Publication number: 20110071164
    Abstract: This invention relates to the use of ERG channel openers for the treatment of cardiac arrhythmias, and to the use of specific compounds for such treatment. In a separate aspect the invention provides novel compounds useful as ERG channel openers.
    Type: Application
    Filed: November 9, 2010
    Publication date: March 24, 2011
    Inventors: Søren Peter OLESEN, Morten Grunnet, Palle Christophersen, Dorte STRØBÆK, Joachim Demnitz, Rie S. Hansen
  • 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
  • Patent number: 7897624
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 1, 2011
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20110046088
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: February 20, 2008
    Publication date: February 24, 2011
    Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMTIED
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20110046092
    Abstract: A method of preparing neural precursor cells by exposing pluripotent stem cells or neural stem cells to a differentiation agent. The agent is a pyridine analog, which in preferred embodiments is a phenylethynyl-substituted or phenylazo-substituted pyridine. In other embodiments, a method of enhancing neural precursor cell survival is provided in which the survival is enhanced by exposure to the pyridine analog. In further embodiments, a method of preparing neuronal cells is provided in which pluripotent or neural stem cells exposed to the pyridine analog are then incubated without the pyridine analog, resulting in differentiation into neurons, astrocytes and oligodendrocytes. These methods may be used in toxicological screens, e.g., to evaluate the neurotoxicity of a test compound.
    Type: Application
    Filed: December 11, 2008
    Publication date: February 24, 2011
    Applicant: Research Development Foundation
    Inventors: David M. Suter, Olivier Preynat-Seauve, Karl-Heinz Krause
  • Publication number: 20110034520
    Abstract: Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.
    Type: Application
    Filed: February 27, 2009
    Publication date: February 10, 2011
    Inventors: David Festus Charles Moffat, Stephen John Davies, Stephane Pintat
  • Patent number: 7868026
    Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: January 11, 2011
    Assignee: Pfizer Inc.
    Inventors: Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
  • Publication number: 20110003792
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialky
    Type: Application
    Filed: September 7, 2010
    Publication date: January 6, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J. Grainger, David John Fox