The Additional Hetero Ring Is A Five-membered Nitrogen Hetero Ring Patents (Class 514/252.05)
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Publication number: 20130150344Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.Type: ApplicationFiled: August 3, 2011Publication date: June 13, 2013Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
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Publication number: 20130137675Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.Type: ApplicationFiled: August 9, 2011Publication date: May 30, 2013Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
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Publication number: 20130131062Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: May 23, 2013Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Patent number: 8445494Abstract: The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.Type: GrantFiled: June 4, 2009Date of Patent: May 21, 2013Assignees: Bristol-Myers Squibb Company, Albany Molecular Research, Inc.Inventors: Jun Qiu, Qi Gao, Shuang Liu, Matthew Isherwood
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Publication number: 20130116264Abstract: The present invention relates to hetaryl (thio)carboxamide compounds of formula I, to the tautomers and N-oxides thereof and to the salts thereof: wherein X, R1 and A are as defined in the description. The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one hetaryl (thio)carboxamide compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: July 18, 2011Publication date: May 9, 2013Applicant: BASF SEInventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Deborah L. Culbertson, Douglas D. Anspaugh
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Publication number: 20130116231Abstract: The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: July 7, 2011Publication date: May 9, 2013Inventors: Kevin Wilson, Michael Altman, Kathryn Lipford, Catherine White, Matthew Daniels
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Patent number: 8435981Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumors.Type: GrantFiled: July 12, 2007Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
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Patent number: 8435995Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: GrantFiled: July 6, 2012Date of Patent: May 7, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Jun Kunitomo
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Publication number: 20130109667Abstract: The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: June 28, 2011Publication date: May 2, 2013Applicants: Pfizer Limited, Icagen ,Inc.Inventors: Christopher John Markworth, Brian Edward Marron, David James Rawson, Robert Ian Storer, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130109696Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 1, 2011Publication date: May 2, 2013Applicant: Pfizer LimitedInventors: Benjamin Scott Greener, Brian Edward Marron, David Simon Millan, David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Publication number: 20130102462Abstract: The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III comprising the step of reacting a (hetero)aromatic halogen or sulfonate compound II wherein the variables are as defined in the claims and description, with a mixture of carbon monoxide and hydrogen in the presence of a transition metal complex catalyst. The invention also relates to specific compounds III, to compositions comprising them and to their use for combating invertebrate pests.Type: ApplicationFiled: June 22, 2011Publication date: April 25, 2013Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Christian Rein, Joachim Schmidt-Leithoff, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Juergen Langewald
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Publication number: 20130096128Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: September 28, 2012Publication date: April 18, 2013Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 8420623Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: GrantFiled: November 17, 2011Date of Patent: April 16, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
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Publication number: 20130085138Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: September 26, 2012Publication date: April 4, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130045914Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Applicant: Merck Sharp & Dohme CorpInventor: Merck Sharp & Dohme Corp.
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Publication number: 20130030002Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.Type: ApplicationFiled: April 15, 2011Publication date: January 31, 2013Applicant: E I DuPont De Nemours and CompanyInventors: Mary Ann Hanagan, Andris Juris Liepa, Eric Allen Marshall, Robert James Pasteris
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Publication number: 20130029999Abstract: Pyridazinyl compounds, compositions and related methods of use.Type: ApplicationFiled: October 1, 2012Publication date: January 31, 2013Applicant: NORTHWESTERN UNIVERSITYInventors: DANIEL MARTIN WATTERSON, LINDA J. VAN ELDIK, HEATHER BEHANNA, HANTAMALALA RALAY RANAIVO
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8362002Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: GrantFiled: March 15, 2011Date of Patent: January 29, 2013Assignee: Exelixis, Inc.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20130023539Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.Type: ApplicationFiled: June 18, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
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Publication number: 20130018055Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: January 17, 2012Publication date: January 17, 2013Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
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Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Patent number: 8354411Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: GrantFiled: February 4, 2010Date of Patent: January 15, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Jun Kunitomo
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Publication number: 20130012381Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents have the meanings as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: March 21, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20130012382Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents are as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20130012503Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: January 10, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Publication number: 20120329802Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: December 27, 2012Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger
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Publication number: 20120309752Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure.Type: ApplicationFiled: January 7, 2011Publication date: December 6, 2012Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
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Patent number: 8324211Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: GrantFiled: July 15, 2009Date of Patent: December 4, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth
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Patent number: 8324212Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: February 22, 2011Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Richard Pracitto
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Publication number: 20120283264Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: November 2, 2011Publication date: November 8, 2012Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
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Patent number: 8304414Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: April 25, 2008Date of Patent: November 6, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Françoise Pierard
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Publication number: 20120277243Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: April 24, 2012Publication date: November 1, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20120277204Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko TANIGUCHI, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20120277213Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: April 23, 2012Publication date: November 1, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8299253Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: December 22, 2006Date of Patent: October 30, 2012Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran
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Publication number: 20120270861Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: March 9, 2012Publication date: October 25, 2012Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, JUYI CHOI, KONRAD FEICHTINGER, SANGDON HAN, HONNAPPA JAYAKUMAR, THUY-AND TRAN, JINGDONG XU, NING ZOU
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Patent number: 8293744Abstract: The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: April 13, 2010Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore
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Publication number: 20120264735Abstract: The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: December 14, 2010Publication date: October 18, 2012Inventors: Jonathan Young, Barbara Czako, Michael Altman, David Guerin, Michelle Martinez, Alexey Rivkin, Kevin Wilson, Kathryn Lipford, Catherine White, Laura Surdi, Stephanie Chichetti, Matthew H. Daniels, Sean P. Ahearn, Danielle Falcone, Ekundayo Osimboni
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Patent number: 8278335Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: GrantFiled: April 9, 2009Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
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Patent number: 8278305Abstract: Pyridazinyl compounds, compositions and related methods of use.Type: GrantFiled: May 25, 2010Date of Patent: October 2, 2012Assignee: Northwestern UniversityInventors: Daniel Martin Watterson, Linda J. Van Eldik, Heather Behanna, Hantamalala Ralay Ranaivo
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Publication number: 20120225886Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 24, 2010Publication date: September 6, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gregori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
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Publication number: 20120225867Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 27, 2010Publication date: September 6, 2012Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Patent number: 8258134Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: March 9, 2009Date of Patent: September 4, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Publication number: 20120214789Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: May 2, 2012Publication date: August 23, 2012Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
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Publication number: 20120202819Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.Type: ApplicationFiled: September 27, 2010Publication date: August 9, 2012Applicant: Merck Sharp & Dohme CorporationInventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
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Patent number: 8231888Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: June 9, 2011Date of Patent: July 31, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120178761Abstract: The invention provides compounds of formula wherein R1, R2, R3, R4, R5, and R6 are as defined herein or a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: January 2, 2012Publication date: July 12, 2012Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian