Carbocyclic Ring Containing Patents (Class 546/194)
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Publication number: 20120149676Abstract: 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. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120149705Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is a group selected from A1 and A2 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicant: BASF SEInventors: Thomas SCHMIDT, Michael PUHL, Joachim DICKHAUT, Henricus Maria Martinus BASTIAANS, Michael RACK, Deborah L. CULBERTSON, Douglas D. Anspaugh, Franz-Josef BRAUN, Toni BUCCI, Henry Van Tuyl COTTER, David G. KUHN, Hassan OLOUMI-SADEGHI
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Publication number: 20120149683Abstract: The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: September 15, 2010Publication date: June 14, 2012Inventors: Jason M. Cox, Tesfaye Biftu, Hong Dong Chu, Danqing Feng, Ann E. Weber
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Publication number: 20120149674Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: February 23, 2012Publication date: June 14, 2012Applicant: Merck Sharpe & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Patent number: 8198304Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20120142733Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: November 30, 2011Publication date: June 7, 2012Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
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Publication number: 20120142688Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.Type: ApplicationFiled: May 24, 2010Publication date: June 7, 2012Applicant: CENTRAL SOUTH UNIVERSITYInventors: Gaoyun Hu, Lijian Tao, Jun Chen
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Publication number: 20120142687Abstract: The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Inventors: Akira KUGIMIYA, Yuki Tachibana
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Patent number: 8193362Abstract: A compound of formula (I): wherein R1 is pyrid-4-yl optionally substituted by one to four substituents independently selected from halogen, C1-3 alkyl or C1-3 haloalkyl; R2 is hydrogen, halogen, C1-4 haloalkyl or C1-4 haloalkoxy; R3 is trifluoromethyl, difluoromethyl or difluoromethoxy and R4 is hydrogen, fluoro or chloro, or R3 is fluoro, chloro or bromo and R4 is fluoro, chloro or trifluoromethyl; and R5 is hydrogen or halogen; or salts or N-oxides thereof. Furthermore, the present invention relates to intermediates used to prepare compounds of formula (I), to methods of using them to combat and control insect, acarine, mollusc and nematode pests and to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them.Type: GrantFiled: May 13, 2009Date of Patent: June 5, 2012Assignee: Syngenta Crop Protection LLCInventors: Jerome Yves Cassayre, Camilla Corsi, Thomas Pitterna, Peter Maienfisch
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Patent number: 8188280Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.Type: GrantFiled: February 4, 2009Date of Patent: May 29, 2012Assignee: MSD K.K.Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
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Publication number: 20120129859Abstract: 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.Type: ApplicationFiled: May 24, 2010Publication date: May 24, 2012Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120122926Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20120122850Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Patent number: 8178668Abstract: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: GrantFiled: February 4, 2009Date of Patent: May 15, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Arno G. Steinig, Mark J. Mulvihill, Jing Wang, Douglas S. Werner, Qinghua Weng, Heather Coate, Xin Chen
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Patent number: 8178531Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: GrantFiled: February 23, 2011Date of Patent: May 15, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Publication number: 20120115861Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R7 and Y have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours and for the treatment of inflammatory diseases.Type: ApplicationFiled: June 17, 2010Publication date: May 10, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Michel Calderini, Margarita Wucherer-Plietker, Ulrich Graedler, Christina Esdar
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Publication number: 20120115909Abstract: The presently described subject matter relates to new derivatives of tazarotene that also exhibit retinoid activity, pharmaceutical compositions comprising the derivatives, method of treating skin disorders with the pharmaceutical compositions, and process of making the derivatives.Type: ApplicationFiled: July 16, 2010Publication date: May 10, 2012Inventors: Xue Ge, Hansen Wong, Wendy Huang Chern, Hans Hofland, Michael J. Bishop, Xin Frank Cai, Alan Colborn
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Publication number: 20120115866Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: January 12, 2012Publication date: May 10, 2012Applicant: TYROGENEX, INC.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20120115827Abstract: The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.Type: ApplicationFiled: June 7, 2011Publication date: May 10, 2012Applicant: Japan Tobacco Inc.Inventors: Yoshihisa Koga, Shinji Yata, Takashi Watanabe, Takuya Matsuo, Masahiro Sakata, Wataru Kondo
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Publication number: 20120116075Abstract: An acrylamide derivative represented by formula (I), pharmaceutically acceptable salts and solvates thereof, as well as a medicament containing said acrylamide derivative or its pharmaceutically acceptable salts as the active ingredient, which can be used to treat disorders associated with tyrosine kinase especially Bcr-Abl, including proliferative disorders such as cancers, and inflammation and the like are provided.Type: ApplicationFiled: April 27, 2010Publication date: May 10, 2012Applicants: BEIJING JIASHILIANBO PHARM SCI & TECH CO. LTD, BEIJING SHIQIAO BIOPHARM CO. LTDInventor: Shuping Sun
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Publication number: 20120108572Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: August 26, 2009Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
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Publication number: 20120108567Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 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: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl McCONNELL, Maria IMPAGNATIELLO, Dirk KESSLER, Oliver KRAEMER, Siegfried SCHNEIDER, Lars VAN DER VEEN, Ulrike WEYER-CZERNILOFSKY, Tobias WUNBERG
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Publication number: 20120108611Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: December 29, 2011Publication date: May 3, 2012Inventors: Jean-Michel Altenburger, Valérie Fossey, Gilbert Lassalie, Frédéric Petit, Jean Claude Vernieres, Philip Janiak
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Publication number: 20120108529Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
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Publication number: 20120108566Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: May 3, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Yonghong Song, Qing Xu, Jack W. Rose, Zhaozhong J. Jia, Brian Kane, Wolin Huang, Anjali Pandey, Mukund Mehrotra
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Publication number: 20120108618Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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: ApplicationFiled: April 22, 2010Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl Mcconnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
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Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
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Publication number: 20120101079Abstract: 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: ApplicationFiled: October 19, 2011Publication date: April 26, 2012Applicant: Grunenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120101064Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: ApplicationFiled: April 30, 2010Publication date: April 26, 2012Applicants: Astex Therapeutics Limited, Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
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Publication number: 20120095047Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Applicant: UNIVERSITY OF CONNECTICUTInventors: Alexandros Makriyannis, Rajesh Thotapally, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Publication number: 20120094980Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
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Publication number: 20120094999Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 5, 2010Publication date: April 19, 2012Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
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Publication number: 20120094981Abstract: This invention is directed to compounds of the formula (I) and salts therefore that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds of this invention, pharmaceutical compositions and kits comprising the compounds of this invention, uses of the compounds of this invention to make medicaments, and treatments comprising the administration of the compounds of this invention to animals in need of the treatments.Type: ApplicationFiled: June 16, 2010Publication date: April 19, 2012Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
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Publication number: 20120094830Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: ApplicationFiled: December 14, 2011Publication date: April 19, 2012Applicant: BAYER CROPSCIENCE AGInventors: Bernd ALIG, Rüdiger FISCHER, Christian FUNKE, Ernst Rudolf F. GESING, Achim HENSE, Olga MALSAM, Mark Wilhelm DREWES, Ulrich GÖRGENS, Tetsuya MURATA, Katsuaki WADA, Christian ARNOLD, Erich SANWALD
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Publication number: 20120094996Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
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Publication number: 20120094986Abstract: The invention relates to nicotinamide derivatives which can be used as anticancer drugs.Type: ApplicationFiled: March 22, 2010Publication date: April 19, 2012Applicant: SANOFI-AVENTISInventors: Jérôme Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Publication number: 20120095010Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
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Patent number: 8153805Abstract: The invention is concerned with novel biaryl derivatives of formula (I), wherein m, R1, R2, R3, X1, X2 and X3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: GrantFiled: September 26, 2008Date of Patent: April 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Patent number: 8153644Abstract: 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 diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 1, 2008Date of Patent: April 10, 2012Assignee: Madrigal Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Aopstle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Patent number: 8153804Abstract: Aryl pyridines, compositions comprising them, and methods of their use for the treatment, prevention and management of a variety of diseases and disorders are disclosed.Type: GrantFiled: July 31, 2006Date of Patent: April 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, James E. Tarver, Jr., Qinghong Fu, Michael Victor Voronkov, Doan Hackley, Michael E. Mertzman, Marianne Carlsen
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Patent number: 8153647Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: GrantFiled: December 15, 2008Date of Patent: April 10, 2012Assignee: Sanofi-AventisInventors: Jozsef Zsolt Bocskei, Gary McCort, Hans Matter, Henning Steinhagen, Bérangère Thiers
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Patent number: 8153658Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: GrantFiled: November 14, 2007Date of Patent: April 10, 2012Assignee: Astellas Pharma, Inc.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120083602Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: September 28, 2011Publication date: April 5, 2012Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20120082702Abstract: Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 10, 2010Publication date: April 5, 2012Inventors: George V. DeLucca, Qing Shi, Chunjian Liu, Jingwu Duan, Andrew J. Tebben
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Patent number: 8148400Abstract: The invention provides compounds of formula II: and pharmaceutically acceptable salts thereof. The formula II thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.Type: GrantFiled: December 19, 2007Date of Patent: April 3, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Anne Marinier, Claude A. Quesnelle, Marco Dodier, Stephan Roy, Patrice Gill, Mark D. Wittman, David R. Langley
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Publication number: 20120077812Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: JING FANG, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy