Thiadiazoles (including Hydrogenated) Patents (Class 546/268.7)
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Publication number: 20120321563Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.Type: ApplicationFiled: May 9, 2012Publication date: December 20, 2012Inventors: Kevin Groves, Bagna Bao
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Publication number: 20120316188Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 14, 2011Publication date: December 13, 2012Inventor: Christelle Boléa
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Publication number: 20120309795Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: August 20, 2012Publication date: December 6, 2012Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, JR.
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Patent number: 8324133Abstract: The present invention relates to 2-pyridyl-methylene-carboxamide derivatives of formula (I) in which the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:Type: GrantFiled: May 11, 2006Date of Patent: December 4, 2012Assignee: Bayer Cropscience AGInventors: Stéphanie Gary, Brian Hill, Joseph Perez, Rachel Rama, Gilbert Spica, Jean-Pierre Vors
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Patent number: 8288554Abstract: The invention relates to pyridin-3-yl derivatives of Formula (I) wherein R1, R2, R3, R4, R5; R6 and A are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: GrantFiled: September 6, 2007Date of Patent: October 16, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Patent number: 8273772Abstract: The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: GrantFiled: November 17, 2009Date of Patent: September 25, 2012Assignee: Bristol-Myers Squibb CompanyInventors: James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y. S. Lam
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120225879Abstract: The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.Type: ApplicationFiled: October 4, 2010Publication date: September 6, 2012Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFACAS ( CSIC)Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Valle Palomo Ruiz, Daniel Perez Fernandez, Concepción Perez Martín, Ana María Perez Castillo, María Isabel Loza Garcia, María Isabe Cadavid Torres, José Brea Floriani
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Patent number: 8252936Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: GrantFiled: April 25, 2007Date of Patent: August 28, 2012Assignee: Syngenta Crop Protection LLCInventors: Pierre Jung, Patricia Durieux, William Lutz, Peter Maienfisch, Thomas Pitterna, Peter Renold, Werner Zambach
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Publication number: 20120214812Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: ApplicationFiled: March 7, 2012Publication date: August 23, 2012Applicant: IRM LLCInventors: VALENTINA MOLTENI, XIAOLIN LI, JULIET NABAKKA, DAVID ARCHER ELLIS, BETH ANACLERIO, ENRIQUE SAEZ, JOHN WITAK
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Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8236825Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: GrantFiled: April 25, 2011Date of Patent: August 7, 2012Assignee: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
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Publication number: 20120196862Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Wael SAEB, Carine CHEVRIER
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Publication number: 20120183537Abstract: According to the invention there is provided a compound of formula (I) wherein: A represents C(?N—W-D) or S; B represents S or C(—NH—W-D); when: A represents C(?N—W-D) and B represents S then the bond between B and the NH atom is a single bond; or A represents S and B represents C(—NH—W-D) then the bond between B and the NH atom is a double bond; X represents -Q-[CRxRy]n—; W represents —[CRxRy]m— or —C(O)—[CRxRy]p—; Q represents a bond, —N(Ra)—, —S—, or —O—; A1 to A5 respectively represent C(R1), C(R2), C(R3), C(R4) and C(R5), or, alternatively, up to two of A1 to A5 may independently represent N; D represents phenyl, pyridyl or pyrimidinyl optionally substituted by one or more R6 groups, which compounds are useful in the treatment of cancer.Type: ApplicationFiled: July 8, 2010Publication date: July 19, 2012Inventors: Jacob Westman, Allan Hallett, Jan Vagberg
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Patent number: 8212045Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: GrantFiled: September 15, 2008Date of Patent: July 3, 2012Assignee: Array BioPharma, Inc.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner, Eli M. Wallace
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120149679Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: February 20, 2012Publication date: June 14, 2012Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20120142710Abstract: The invention relates to ketolide compound of Formula-I and the pharmaceutically acceptable salts thereof having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compound of invention.Type: ApplicationFiled: May 26, 2010Publication date: June 7, 2012Inventors: Bharat Kalidas Trivedi, Mahesh Vithalbhai Patel
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Publication number: 20120121727Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
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Publication number: 20120122907Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 14, 2010Publication date: May 17, 2012Inventor: Christelle Boléa
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Publication number: 20120115811Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.Type: ApplicationFiled: February 12, 2010Publication date: May 10, 2012Applicant: Amgen Inc.Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, Xian Yun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
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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: 20120094993Abstract: 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: ApplicationFiled: October 7, 2011Publication date: April 19, 2012Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
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Publication number: 20120077847Abstract: The present invention is directed to ?-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: ApplicationFiled: September 26, 2011Publication date: March 29, 2012Inventors: Michael N. Greco, Margery A. Connelly, Shyamali Ghosh, Dennis J. Hlasta, Edward C. Lawson, Eric Strobel, Michele A. Weidner-Wells, Hong Ye
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Publication number: 20120064121Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Shoujun Chen
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Publication number: 20120053146Abstract: Molecules according to Formula One: and their uses are disclosed herein.Type: ApplicationFiled: August 29, 2011Publication date: March 1, 2012Inventors: Marshall H. Parker, Maurice C.H. Yap, Joseph D. Eckelbarger, Ann M. Buysse, Jonathan M. Babcock, Ricky Hunter, Yelena Adelfinskaya, Jack G. Samaritoni, Negar Garizi, Tony K. Trullinger
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Publication number: 20120046273Abstract: Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.Type: ApplicationFiled: March 5, 2010Publication date: February 23, 2012Applicant: MITHRIDION, INC.Inventors: Trevor M. Twose, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Melinda L. Verdone
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Patent number: 8119666Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.Type: GrantFiled: December 6, 2006Date of Patent: February 21, 2012Assignee: Novartis AGInventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
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Publication number: 20120040999Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: April 26, 2010Publication date: February 16, 2012Inventors: Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
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Publication number: 20120040984Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.Type: ApplicationFiled: January 27, 2010Publication date: February 16, 2012Applicant: SANOFIInventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Patent number: 8088802Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: GrantFiled: October 21, 2009Date of Patent: January 3, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Atsushi Naganawa, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
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Patent number: 8076486Abstract: The invention provides novel heteroaryl-substituted arylaminopyridine derivative MEK inhibitors of Formula (Ia) Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: April 18, 2007Date of Patent: December 13, 2011Assignee: Merck Serono S.A.Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Xiaoling Chen, Srinivasa Karra, Henry Yu
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Publication number: 20110294829Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: December 8, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20110288089Abstract: A compound of Formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: January 13, 2010Publication date: November 24, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
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Publication number: 20110281870Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 24, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Publication number: 20110263612Abstract: 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: ApplicationFiled: April 12, 2011Publication date: October 27, 2011Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110224263Abstract: The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: June 9, 2010Publication date: September 15, 2011Applicant: SANOFI-AVENTISInventors: Karl SCHOENAFINGER, Stefanie KEIL, Matthias URMANN, Hans MATTER, Maike GLIEN, Wolfgang WENDLER, Ulrike Wendler
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Publication number: 20110212949Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 4, 2009Publication date: September 1, 2011Inventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Füßlein, Achim Hense, Joachim Kluth, Hans-Georg Schwarz, Adeline Köhler, Olga Malsam, Arnd Voerste, Angela Becker
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Publication number: 20110206783Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 21, 2009Publication date: August 25, 2011Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw
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Publication number: 20110201651Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R. Laird, John Robinson, Shelley Allen
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Publication number: 20110200557Abstract: The present disclosure relates to 2-amidothiadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.Type: ApplicationFiled: October 13, 2009Publication date: August 18, 2011Inventors: Pedro Manuel Grima Poveda, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Manuel Lopez Martinez
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Patent number: 7994174Abstract: The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 17, 2008Date of Patent: August 9, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Tara Hampton
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Publication number: 20110190289Abstract: There is provided compounds of formula (I), wherein Z, M, R1, X, R2, R3 and B 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 kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, and particularly in the treatment of cancer.Type: ApplicationFiled: September 29, 2008Publication date: August 4, 2011Applicant: Centro Nacional De Investigaciones Oncologicas (CNIO)Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Ana Belen Garcia Garcia
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Publication number: 20110183981Abstract: 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: ApplicationFiled: March 30, 2011Publication date: July 28, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake