Two Of The Ring Nitrogens Are Bonded Directly To Each Other Patents (Class 546/119)
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Publication number: 20130310418Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 23, 2013Publication date: November 21, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8586581Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: December 10, 2010Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche IncInventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20130303511Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Applicant: AbbVie Inc.Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
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Publication number: 20130303529Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: June 13, 2013Publication date: November 14, 2013Inventors: Brian K. ALBRECHT, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia W. Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang, Karina Romero, Katrina Woodin Copeland, Emily A. Peterson
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Publication number: 20130303770Abstract: The present invention relates to radiolabelled PDE10A ligands which are useful for imaging and quantifying the PDE10A enzyme using positron emission tomography (PET).Type: ApplicationFiled: November 10, 2011Publication date: November 14, 2013Applicant: H. Lundbeck A/SInventor: H. Lundbeck A/S
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Publication number: 20130296302Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: ApplicationFiled: May 3, 2013Publication date: November 7, 2013Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20130296307Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 8575145Abstract: Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.Type: GrantFiled: August 18, 2009Date of Patent: November 5, 2013Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Greschuk, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
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Patent number: 8569337Abstract: The present invention relates to compounds of tri-cyclic pyrazolopyridine useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions containing such compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: January 27, 2010Date of Patent: October 29, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Christopher John Davis, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
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Patent number: 8569281Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.Type: GrantFiled: September 21, 2011Date of Patent: October 29, 2013Assignees: Medical Research Council Technology, Genentech, Inc.Inventors: Bryan K. Chan, Huifen Chen, Anthony Estrada, Daniel Shore, Zachary Sweeney, Edward Giles McIver
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130280245Abstract: Disclosed are 3-aryl-6-aryl-[1,2,4]triazolo[4,3-?]pyridines thereof, represented by the Formula (I) wherein Ar1, Ar2, R1—R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation. Therefore, compounds of the invention may be used to treat clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: November 16, 2011Publication date: October 24, 2013Applicant: IMPACT Therapeutics, Inc.Inventors: Suixiong Cai, Ye Edward Tian, Haijun Dong, Lei Chen, Zenghui Yu, Feng Yin, Sheng Bi, Lijun Liu, Lizhen Wu
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Publication number: 20130281359Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: June 14, 2013Publication date: October 24, 2013Inventors: Samarendra N. MAITI, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8563730Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are 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: GrantFiled: May 15, 2009Date of Patent: October 22, 2013Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Patent number: 8563576Abstract: The present invention relates to compounds of tricyclic pyrazolopyridine useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: December 1, 2011Date of Patent: October 22, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Dean Boyall, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
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Publication number: 20130273037Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: ApplicationFiled: April 17, 2013Publication date: October 17, 2013Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
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Patent number: 8557809Abstract: Compounds of Formula (I): I in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.Type: GrantFiled: August 18, 2009Date of Patent: October 15, 2013Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Robert Kirk DeLisle, Julie Marie Greschuk, Erik James Hicken, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, John E. Robinson, Qian Zhao
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Patent number: 8557841Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: GrantFiled: June 11, 2012Date of Patent: October 15, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
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4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
Patent number: 8557848Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.Type: GrantFiled: December 17, 2007Date of Patent: October 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski -
Publication number: 20130267513Abstract: A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; -0-C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl and halogen, wherein said C1-6-alkyl, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independType: ApplicationFiled: May 16, 2011Publication date: October 10, 2013Inventors: Brayn Chan, Anthony Estrada, Zachary Sweeney, Edward Giles Mciver, Stephen Lewis
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Patent number: 8552045Abstract: This invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula 1. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: November 18, 2011Date of Patent: October 8, 2013Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgård
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Publication number: 20130261125Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Inventors: Gerald W. Shipps, JR., Xiaohua Huang, Yongqi Deng, Liang Zhu, Alan B. Cooper, Binyuan Sun, Abdelghani Achab, Sie-Mun Lo
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Publication number: 20130252941Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: F. Hoffmann-La Roche AGInventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
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Publication number: 20130252939Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 30, 2013Publication date: September 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Christopher John Davis, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
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Patent number: 8541444Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R3, R3a, and R3b are defined herein.Type: GrantFiled: August 3, 2011Date of Patent: September 24, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Jun Li, Jeffrey A. Robl, James J. Li, Lawrence J. Kennedy, Haixia Wang, Jie Jack Li, Chenkou Wei, Michael Galella
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Publication number: 20130245002Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: September 13, 2012Publication date: September 19, 2013Applicant: NOVARTIS AGInventors: Chao CHEN, Haibing DENG, Haibing GUO, Feng HE, Lei JIANG, Fang LIANG, Yuan MI, Huixin WAN, Yao-Chang XU, Hongping YU, Ji Yue ZHANG
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Publication number: 20130245042Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: March 14, 2013Publication date: September 19, 2013Inventors: Ronald J. Mattson, Zhaoxing Meng
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Publication number: 20130237518Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: ApplicationFiled: October 24, 2011Publication date: September 12, 2013Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
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Publication number: 20130231354Abstract: Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: November 9, 2011Publication date: September 5, 2013Applicant: Bristol-Meyers Squibb CompanyInventors: Joel F. Austin, David B. Frennesson, Mark G. Saulnier
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Publication number: 20130230459Abstract: The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.Type: ApplicationFiled: November 8, 2011Publication date: September 5, 2013Applicant: Janssen Pharmaceuticals, Inc.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen, Michel Koole
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Publication number: 20130211090Abstract: The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) which serves as a synthesis intermediate for production of medicaments, especially for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Jens Ackerstaff
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Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
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Publication number: 20130209543Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.Type: ApplicationFiled: November 21, 2012Publication date: August 15, 2013Applicant: Intellikine LLCInventor: Intellikine LLC
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Patent number: 8507682Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.Type: GrantFiled: September 28, 2010Date of Patent: August 13, 2013Assignee: Allergan, Inc.Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Patent number: 8507469Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.Type: GrantFiled: March 20, 2008Date of Patent: August 13, 2013Assignee: Abbott GmbH & Co. KGInventors: Thomas Schultz, Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
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Publication number: 20130203786Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds 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: May 16, 2011Publication date: August 8, 2013Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
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Patent number: 8501936Abstract: This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.Type: GrantFiled: June 4, 2010Date of Patent: August 6, 2013Assignee: Cephalon, Inc.Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
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Publication number: 20130196985Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.Type: ApplicationFiled: June 3, 2011Publication date: August 1, 2013Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of SciencesInventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng
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Publication number: 20130197229Abstract: Disclosed are methods, reagents, and intermediates useful for making azaindazole derivatives, which may be used to modulate Glucokinase. The disclosed methods and materials are generally useful for making halo-esters and sulfonyl-substituted compounds.Type: ApplicationFiled: October 13, 2011Publication date: August 1, 2013Inventors: Christopher Matthews, Colin O'Bryan, David Paul Provencal
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Patent number: 8492392Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds of formula I, 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: GrantFiled: May 24, 2010Date of Patent: July 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
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Publication number: 20130184254Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: July 14, 2011Publication date: July 18, 2013Inventors: Upender Velaparthi, David B. Frennesson, Mark G. Saulnier, Joel F. Austin, Audris Huang, James Aaron Balog, Dolatrai M. Vyas
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Publication number: 20130184284Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
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Patent number: 8486967Abstract: The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: GrantFiled: February 9, 2011Date of Patent: July 16, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Patent number: 8487102Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, Ar, and n are as defined herein or to a pharmaceutically active acid addition salt. Compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.Type: GrantFiled: April 11, 2011Date of Patent: July 16, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Heinz Stadler
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Publication number: 20130178475Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: March 10, 2011Publication date: July 11, 2013Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Joel Moore, James Jia, Takashi Nakai, Charles Kim, Thomas Wai-Ho Lee, Jane Yang
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Patent number: 8481539Abstract: The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.Type: GrantFiled: December 4, 2008Date of Patent: July 9, 2013Assignee: Bayer Intellectual Property GmbHInventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulf Bömer
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Publication number: 20130172360Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.Type: ApplicationFiled: January 27, 2012Publication date: July 4, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
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Publication number: 20130172292Abstract: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on.Type: ApplicationFiled: August 3, 2011Publication date: July 4, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: Joseph Raker, Takahiko Taniguchi, Masato Yoshikawa, Tomoaki Hasui, Jun Kunitomo