The Other Cyclo In The Bicyclo Ring System Is A Pyridine Ring (including Hydrogenated) (e.g., Pyrido[2,3-d]pyrimidine, Etc.) Patents (Class 514/264.1)
-
Publication number: 20120316149Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Inventors: Ramulu PODDUTOORI, Can WANG, Xianglin ZHAO
-
Publication number: 20120316184Abstract: Compounds of formula (I) wherein G1 represents together with the two ring atoms of the pyrimidine ring to which it is attached, a 5- to 6-membered aromatic heterocyclic ring system which contains one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the other substituents are as defined in claim 1, are suitable for use as micro-biocides.Type: ApplicationFiled: February 18, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Martin Pouliot, David Guillaume Claude Francois Lefranc, Laura Quaranta, Clemens Lamberth, Nityakalyani Srinivas
-
Publication number: 20120316136Abstract: The present patent application relates to treatment of a respiratory disorder using TRPA1 antagonists. Particularly, the present patent application relates to treatment of a respiratory disorder using a TRPA1 antagonist, wherein the TRPA1 antagonist is administered by inhalation route to a subject in need thereof.Type: ApplicationFiled: June 13, 2012Publication date: December 13, 2012Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Neelima KHAIRATKAR-JOSHI, Abhay KULKARNI, Indranil MUKHOPADHYAY, Vidya Ganapati KATTIGE, Vikram Mansingh BHOSALE, Dinesh Pradeep WALE, Abraham THOMAS, Sukeerthi KUMAR, Sachin Sundarlal CHAUDHARI
-
Patent number: 8329712Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: July 6, 2011Date of Patent: December 11, 2012Assignee: Roche Palo Alto LLCInventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
-
Patent number: 8329070Abstract: The present invention provides apparatus and processes for producing liposomes. By providing a buffer solution in a first reservoir, and a lipid solution in a second reservoir, continuously diluting the lipid solution with the buffer solution in a mixing chamber produces a liposome. The lipid solution preferably comprises an organic solvent, such as a lower alkanol.Type: GrantFiled: December 10, 2010Date of Patent: December 11, 2012Assignee: Protiva Biotherapeutics, Inc.Inventors: Ian MacLachlan, Lloyd Jeffs, Lorne R. Palmer, Cory Giesbrecht, Noelle Giesbrecht, legal representative
-
Patent number: 8318751Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.Type: GrantFiled: April 17, 2008Date of Patent: November 27, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Craig D. Boyle, Samuel Chackalamannil, Claire M. Lankin, Unmesh G. Shah, Bernard R. Neustadt, Hong Liu, Andrew W. Stamford
-
Publication number: 20120283278Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.Type: ApplicationFiled: September 23, 2010Publication date: November 8, 2012Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
-
Publication number: 20120282255Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.Type: ApplicationFiled: April 6, 2012Publication date: November 8, 2012Inventor: Greg Plucinski
-
Publication number: 20120283279Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a mTOR inhibitor, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or mTOR is beneficial, e.g. cancer.Type: ApplicationFiled: November 17, 2010Publication date: November 8, 2012Inventors: Tona Gilmer, Rakesh Kumar, Sylvie Laquerre
-
Publication number: 20120277240Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof 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-IV 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: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
-
Publication number: 20120269831Abstract: Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.Type: ApplicationFiled: December 17, 2010Publication date: October 25, 2012Applicant: TEMPLE UNIVERSITY- OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: E. Premkumar Reddy, M.V. Ramana Reddy
-
Publication number: 20120264770Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 11, 2011Publication date: October 18, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Erick Co, John D. Lawson, Jeffrey A. Stafford
-
Patent number: 8288408Abstract: The invention relates to a method of inhibiting abnormal cell growth or treating a hyperproliferative disorder in a mammal comprising administering to said mammal a therapeutically effective amount of an imidazopyridine of formula I with anti-hyperproliferative activity.Type: GrantFiled: March 7, 2011Date of Patent: October 16, 2012Assignee: Genentech, Inc.Inventors: Stephen Price, Robert Heald, Wendy Lee, Mark E. Zak, Joanne Frances Mary Hewitt
-
Publication number: 20120258170Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.Type: ApplicationFiled: March 19, 2012Publication date: October 11, 2012Applicant: Nutracryst Therapeutics Private LimitedInventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
-
Publication number: 20120245187Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.Type: ApplicationFiled: June 5, 2012Publication date: September 27, 2012Applicant: NOVARTIS AGInventors: Gerald David ARTMANN, III, Jason Matthew ELLIOTT, Nan JI, Donglei LIU, Fupeng MA, Nello MAINOLFI, Erik MEREDITH, Karl MIRANDA, James J. POWERS, Chang RAO
-
Publication number: 20120238587Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3? OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.Type: ApplicationFiled: March 19, 2012Publication date: September 20, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Gilnam Lee, Chul Soo Lim, Han Won Cho, Jeongbeob Seo, Albert Charles Gyorkos, Suk Young Cho, Eun Kyung Choi, Choung Soo Kim, Jung Jin Hwang
-
Patent number: 8268840Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.Type: GrantFiled: April 29, 2009Date of Patent: September 18, 2012Assignee: Roche Palo Alto LLCInventors: Frederick Brookfield, Florence Eustache, Michael Patrick Dillon, David Michael Goldstein, Leyi Gong, Xiaochun Han, Joan Heather Hogg, Jaehyeon Park, Deborah Carol Reuter, Eric Brian Sjogren
-
Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
-
Publication number: 20120208829Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: August 22, 2011Publication date: August 16, 2012Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
-
Publication number: 20120208819Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.Type: ApplicationFiled: October 5, 2010Publication date: August 16, 2012Inventors: Joseph Arndt, Timothy Chan, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Daniel Scott, Lihong Sun, Jermaine Thomas, Kurt van Vloten, Deping Wang, Lei Zhang, Daniel Erlanson
-
Patent number: 8242124Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: June 24, 2009Date of Patent: August 14, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, Nicholas A. Meanwell, David J. Carini, Wenying Li
-
Patent number: 8242125Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.Type: GrantFiled: December 7, 2009Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
-
Publication number: 20120202790Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: November 4, 2011Publication date: August 9, 2012Inventors: John M. Fevig, Dean A. Wacker
-
Publication number: 20120196879Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.Type: ApplicationFiled: October 15, 2010Publication date: August 2, 2012Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
-
Patent number: 8232283Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: GrantFiled: May 12, 2011Date of Patent: July 31, 2012Assignee: Forma Therapeutics, Inc.Inventors: Andreas Schoop, Alexander Backes, Joachim Vogt, Lars Neumann, Jan Eickhoff, Stefan Hannus, Kerrin Hansen, Peter Amon, Igor Ivanov, Matthias Borgmann, Chase Smith, Arthur F. Kluge, Krishan Murthi, Rebecca Casaubon
-
Patent number: 8232282Abstract: The present invention relates to a bicyclic pyrimidine compound of the following formula (I) or a salt thereof. wherein R1 is lower alkyl, cyclic lower alkyl. etc.; R2 is H, lower alkyl, lower alkenyl, etc.; R3 is H, lower alkyl, lower alkenyl, etc.; X is O, S or —N(R4)—; R4 is H or lower alkyl; or R2 and R4 may combine each other to form cyclic amino; Y is amido, keto, sulfonyl, etc.; R5 is H or lower alkyl; Z is O or S; m and n are 1 or 2. Said compound (I) or a salt thereof have MGAT inhibitory activity, and are useful as an agent for treatment or prophylaxis of adiposity, metabolic syndromes, hyperlipidemia, hyper neutral lipemia, hyper VLDL-mia, hyper fatty acidemia, diabetes mellitus, arteriosclerosis.Type: GrantFiled: September 28, 2007Date of Patent: July 31, 2012Assignees: Dainippon Sumitomo Pharma Co., Ltd., Sumitomo Chemical Company, LimitedInventors: Keiji Nakamura, Hiroyuki Nakagawa, Yoko Kan
-
Publication number: 20120190654Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2010Publication date: July 26, 2012Applicant: MERCK PATENT GMBHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
-
Publication number: 20120184542Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.Type: ApplicationFiled: January 12, 2012Publication date: July 19, 2012Inventors: Kevin Anderson, Yi Chen, Zhi Chen, Kin-Chun Luk, Pamela Loreen Rossman, Hongmao Sun, Peter Michael Wovkulich
-
Publication number: 20120183613Abstract: Disclosed are novel pharmaceutical compositions containing N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.Type: ApplicationFiled: December 20, 2011Publication date: July 19, 2012Inventors: Douglas J. DeMARINI, Francisco Henriquez, Ngocdiep T. LE, Lihong Wang
-
Publication number: 20120184526Abstract: Provided herein are a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.Type: ApplicationFiled: July 30, 2010Publication date: July 19, 2012Inventors: Jianwei Che, Qiang Ding, Xiaohui He, Hong Liu, Yahua Liu, Pierre-Yves Michellys, Barun Okram, Xu Wu, Kunyong Yang, Xuefeng Zhu
-
Patent number: 8222263Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: GrantFiled: March 14, 2008Date of Patent: July 17, 2012Assignee: Exelixis Patent Company LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
-
Publication number: 20120178681Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
-
Patent number: 8211900Abstract: Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: wherein A and D are independently —CHR7— or —NR7—; E and G are independently ?CR7— or ?N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein RType: GrantFiled: April 24, 2007Date of Patent: July 3, 2012Assignee: Chroma Therapeutics Ltd.Inventor: Alan Hornsby Davidson
-
Publication number: 20120165313Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Applicant: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Kevin Hon Luen Lau, Coung Ly, Joseph P. Lyssikatos, Daniel Ortwine, Zhonghua Pei, Xianrui Zhao
-
Patent number: 8207176Abstract: The present invention is directed to novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds, compositions, and use in therapy as CSBP/RK/p38 kinase inhibitors of Formulas (V) and (Va) wherein inter alia, G5 and G6 are nitrogen and CH, provided that only one of G5 or G6 is nitrogen and the other is CH; R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb, N(R10?)C(Z)N(R10?)(CR10R20)vRb, or N(R10?)OC(Z)(CR10R20)vRb; R1? is independently selected at each occurrence from halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v?NRdRd?, (CR10R20)v?C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v?OR13; Rb is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or heterocyclylC1-10 alkyl moiety, which moieties, excluding hydrogen, may all be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)Type: GrantFiled: March 24, 2006Date of Patent: June 26, 2012Assignee: Glaxo Group LimitedInventors: James F. Callahan, Jeffrey C. Boehm, Anthony William James Cooper, Stefano Livia, Paul Bamborough, Neysa Nevins, Zehong Wan, Beth A. Norton, Xichen Lin
-
Publication number: 20120142638Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be modulated by action on the renin-angiotensin system (RAS), appetency disorders or substance abuse disorders.Type: ApplicationFiled: February 13, 2012Publication date: June 7, 2012Inventor: Randy Lee Webb
-
Patent number: 8188101Abstract: Dihydropyridopyrimidine compounds of formula (Ia) and therapeutically acceptable salts thereof, wherein R1, R2 and Z are as defined in the specification; processes for making them and methods for using them in the treatment of A?-related pathologies.Type: GrantFiled: November 6, 2009Date of Patent: May 29, 2012Assignee: AstraZeneca ABInventors: Rickard Forsblom, Kim Paulsen, Didier Rotticci, Ellen Santangelo, Magnus Waldman
-
Publication number: 20120108597Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.Type: ApplicationFiled: January 26, 2010Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
-
Patent number: 8163763Abstract: Disclosed are compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: GrantFiled: July 31, 2009Date of Patent: April 24, 2012Assignee: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F. T. Koehler, Kevin Hon Luen Lau, Cuong Ly, Joseph P. Lyssikatos, Daniel Ortwine, Zhonghua Pei, Xianrui Zhao
-
Publication number: 20120095028Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: March 4, 2010Publication date: April 19, 2012Inventors: Michael Paul DeNinno, Kentaro Futatsugi, Bruce Allen Lefker, Vincent Mascitti, Kim Francis McClure, Michael John Munchhof
-
Publication number: 20120087928Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.Type: ApplicationFiled: October 28, 2011Publication date: April 12, 2012Inventor: Kameran Lashkari
-
Publication number: 20120077801Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: August 3, 2011Publication date: March 29, 2012Inventors: Roger Victor Bonnert, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Austen Pimm, Hitesh Jayantilal Sanganee, Frank Burkamp, Premji Meghani
-
Publication number: 20120077800Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.Type: ApplicationFiled: August 23, 2011Publication date: March 29, 2012Applicant: Alkermes, Inc.Inventors: Daniel Deaver, Mark Todtenkopf
-
Publication number: 20120065183Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: July 1, 2011Publication date: March 15, 2012Applicant: NOVARTIS AGInventors: Nigel Graham COOKE, Paulo FERNANDES GOMES DOS SANTOS, Nadege GRAVELEAU, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Alexander Baxter SMITH, Nicolas SOLDERMANN, Frank STOWASSER, Ross STRANG, Nicola TUFILLI, Anette VON MATT, Romain WOLF, Frédéric ZECRI
-
Publication number: 20120065211Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: May 24, 2010Publication date: March 15, 2012Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
-
Patent number: 8133898Abstract: The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the formula:—wherein the variables are as defined herein.Type: GrantFiled: March 11, 2008Date of Patent: March 13, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Stephen L. Gwaltney, Zhiyuan Zhang, Betty Lam
-
Publication number: 20120059002Abstract: Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: April 21, 2010Publication date: March 8, 2012Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
-
Publication number: 20120059019Abstract: 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: ApplicationFiled: March 9, 2011Publication date: March 8, 2012Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
-
Publication number: 20120028958Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 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 24, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
-
Patent number: 8106081Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising as active ingredients (i) an AT1-receptor antagonist or a pharmaceutically acceptable salt thereof; (ii) (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof or (b) an insulin sensitizer or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.Type: GrantFiled: February 15, 2010Date of Patent: January 31, 2012Assignee: Novartis AGInventors: Malcolm Allison, Marjorie R Gatlin