Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Bicyclo Ring System Patents (Class 514/264.11)
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Publication number: 20120046270Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R4, X1, X2, X3, X4, X5, Q, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.Type: ApplicationFiled: February 17, 2010Publication date: February 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Ettmayer, Andreas Mantoulidis, Steffen Steurer
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Publication number: 20120035181Abstract: A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.Type: ApplicationFiled: April 26, 2010Publication date: February 9, 2012Applicant: NIPPON SUISAN KAISHA, LTD.Inventors: Fumi Kawano, Noritaka Hirazawa
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Patent number: 8101622Abstract: The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.Type: GrantFiled: September 29, 2009Date of Patent: January 24, 2012Assignee: Exelixis, Inc.Inventors: Tae-Gon Baik, Sunghoon Ma, Chris A. Buhr, John M. Nuss
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Publication number: 20110319409Abstract: The present invention is directed to 7-aza-quinazoline compounds of general structural formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10).Type: ApplicationFiled: June 23, 2010Publication date: December 29, 2011Inventors: Christopher D. Cox, Izzat T. Raheem, Broc A. Flores, David B. Whitman
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Patent number: 8076345Abstract: Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: GrantFiled: March 31, 2008Date of Patent: December 13, 2011Assignee: Evotec AGInventors: Zhi-Liang Wei, Donogh John Roger O'Mahony, Matthew Duncton, John Kincaid, Michael G. Kelly, Zhan Wang
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Patent number: 8071766Abstract: 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: GrantFiled: January 30, 2009Date of Patent: December 6, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Young K. Chen, Erick Co, Prasuna Guntupalli, John D. Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
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Publication number: 20110287069Abstract: A solid oral dosage pharmaceutical formulation of (R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one or its salt; and a surfactant or an acid.Type: ApplicationFiled: January 28, 2010Publication date: November 24, 2011Inventors: Daya Verma, Yue (Helen) Teng, Rajinder Singh, Dan Thompson
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Publication number: 20110281867Abstract: Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.Type: ApplicationFiled: December 16, 2010Publication date: November 17, 2011Inventors: Daniel KALMAN, William Gerard Bornmann, Patrick Michael Reeves, Alyson Irene Swimm
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Patent number: 8058282Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: August 19, 2010Date of Patent: November 15, 2011Assignee: GlaxoSmithKline LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
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Patent number: 8058283Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: January 29, 2007Date of Patent: November 15, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Honold, Jane Paul, Carl Roeschlaub, Wolfgang Schaefer, Stefan Scheiblich, Thomas Von Hirschheydt, Alan Whittle
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Publication number: 20110269758Abstract: Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.Type: ApplicationFiled: June 29, 2009Publication date: November 3, 2011Applicant: MERCK PATENT GMBHInventors: Yufang Xiao, Bayard R. Huck, Amanda E. Sutton, Xiaoling Chen, Srinivasa R. Karra, Andreas Goutopoulos
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Publication number: 20110269739Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.Type: ApplicationFiled: October 29, 2010Publication date: November 3, 2011Applicants: Oscotec, Inc., GenoscoInventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
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Publication number: 20110263561Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: May 13, 2009Publication date: October 27, 2011Applicant: Merck Patent GmbHInventors: Timo Heinrich, Mireille Krier, Thorsten Knoechel, Alfred Jonczyk, Frank Zenke, Holger Enderle
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Patent number: 8044062Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: GrantFiled: October 9, 2006Date of Patent: October 25, 2011Assignee: Exelixis, Inc.Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K. S. Yeung
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Publication number: 20110257207Abstract: 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: ApplicationFiled: May 12, 2011Publication date: October 20, 2011Applicants: Agennix USA Inc, Agennix AGInventors: Alexander BACKES, Joachim VOGT, Peter AMON, Igor IVANOV, Stefan HANNUS, Matthias BORGMANN, Kerrin HANSEN, Rebecca CASAUBON, Chase SMITH, Krishna MURTHI, Arthur KLUGE, Andreas SCHOOP, Lars NEUMANN, Jan EICKHOFF
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Patent number: 8030318Abstract: Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.Type: GrantFiled: March 27, 2006Date of Patent: October 4, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson, Sarvajit Chakravarty, Barry Patrick Hart
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Patent number: 8030317Abstract: Compounds of the following formula are provided for use with MEK: 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: December 18, 2007Date of Patent: October 4, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Stephen W. Kaldor
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Publication number: 20110237608Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: June 2, 2011Publication date: September 29, 2011Applicant: Exelixis, Inc.Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K.S. Yeung
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Publication number: 20110237583Abstract: The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: November 3, 2009Publication date: September 29, 2011Inventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle, Ingo Kober, Dirk Wienke, Mireille Krier
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Publication number: 20110230468Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.Type: ApplicationFiled: June 1, 2011Publication date: September 22, 2011Inventors: Joseph Barbosa, William J. Pitts, Junqing Guo
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Publication number: 20110230499Abstract: The use of a Hsp90 inhibitor for the treatment of cancer of the bladder, the colon, the liver, the lung, the breast, the vagina, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the peritoneal cavity, the thyroid, the bone, the brain, the central nervous system and/or the blood and/or for the treatment of myelodysplastic syndrome, systemic mastocytosis, von Hippel-Lindau syndrome, multicentric Castleman disease and/or psioriasis.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Michael Rugaard Jensen, Cornelia Quadt
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Publication number: 20110230444Abstract: A pharmaceutical combination comprising an Hsp90 inhibitor and an mTOR inhibitor, and methods of using the combination to treat or prevent proliferative disorders.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Michael Rugaard Jensen
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Patent number: 8022077Abstract: The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of formula (I) as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds of formula (I) per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.Type: GrantFiled: May 12, 2006Date of Patent: September 20, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110212937Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: July 28, 2010Publication date: September 1, 2011Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Patent number: 8008310Abstract: Derivatives of pyrido[2,3-d]pyrimidine are provided having formula (I) with Ar1, Ar2 and R1 as defined herein, which are useful for treating cell proliferative conditions, and to the preparation thereof, and to the therapeutic application of the same.Type: GrantFiled: January 30, 2009Date of Patent: August 30, 2011Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Claude Muneaux, Pierre Perreaut
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Publication number: 20110207741Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.Type: ApplicationFiled: February 22, 2011Publication date: August 25, 2011Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Samuel Dudley
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Publication number: 20110207717Abstract: Certain 2-aminopyrimidine compounds are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Gregor J. MacDonald, Brock T. Shireman, Vi T. Tran
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Publication number: 20110201594Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: October 16, 2008Publication date: August 18, 2011Inventors: Krisna Murthi, Rebecca Casaubon, Arthur F. Kluge, Chase Smith, Joachim Vogt
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Publication number: 20110172254Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.Type: ApplicationFiled: September 17, 2009Publication date: July 14, 2011Applicant: ENDOCYTE, INC.Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Philip Stewart Low
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Publication number: 20110160210Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Applicant: ALCON, INC.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
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Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Publication number: 20110152277Abstract: Substituted bicyclic heteroaryls 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, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: February 28, 2011Publication date: June 23, 2011Inventors: Yi Chen, Timothy D. Cushing, Xiaolin Hao, Xiao He, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20110136838Abstract: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: August 12, 2009Publication date: June 9, 2011Inventors: Francis Louis Atkinson, Jeffrey Michael Axten, Maria Cichy-Knight, Michael Lee Moore, Vipulkumar Kantibhai Patel, Xinrong Tian, Christopher Roland Wellaway, Allison K. Dunn
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Publication number: 20110123493Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, for use in the treatment of hepatitis C.Type: ApplicationFiled: July 1, 2009Publication date: May 26, 2011Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael L. Mitchell, William J. Watkins, Jennifer R. Zhang
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Patent number: 7923450Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.Type: GrantFiled: January 5, 2009Date of Patent: April 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
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Publication number: 20110077256Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.Type: ApplicationFiled: April 28, 2010Publication date: March 31, 2011Inventors: Oivin M. Guicherit, Lee Rubin
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Patent number: 7910595Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: December 20, 2006Date of Patent: March 22, 2011Assignee: Abbott LaboratoriesInventors: David A. Betebenner, David A. DeGoey, Clarence J. Maring, Allan C. Krueger, Nobuhiko Iwasaki, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Dachun Liu, Keith F. McDaniel, Darold L. Madigan, Christopher E. Motter, John K. Pratt, Jason P. Shanley, Michael D. Tufano, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu, David J. Grampovnik
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Publication number: 20110065714Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Kim Hirst
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Publication number: 20110053873Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) 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: January 30, 2009Publication date: March 3, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Young K. Chen, Eric Wang Co, Prasuna Guntupalli, John David Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
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Publication number: 20110046145Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: March 11, 2009Publication date: February 24, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Publication number: 20110034458Abstract: The present invention is related to pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: October 18, 2010Publication date: February 10, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Thomas RUECKLE, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Patent number: 7879866Abstract: The present invention provides a method of treating diseases or disorders benefiting from inactivating or down regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capsaicin receptor. The present invention also provides a method of treating obesity and obesity-related diseases and disorders in a mammal by inhibiting the activity of the capasaicin receptor.Type: GrantFiled: July 18, 2005Date of Patent: February 1, 2011Assignee: Dorte Xenia GramInventors: Dorte Xenia Gram, Anker Jon Hansen
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Publication number: 20110009432Abstract: Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: March 31, 2008Publication date: January 13, 2011Inventors: Zhi-Liang Wei, John Kincaid, Michael G. Kelly, Donogh John Roger O'Mahony, Carl Kaub
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Patent number: 7868018Abstract: The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2?2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.Type: GrantFiled: August 9, 2006Date of Patent: January 11, 2011Assignee: IRM LLCInventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
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Publication number: 20110003790Abstract: The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Qiang Ding, Yahua Liu, Xu Wu, Qihui Jin, Jianwei Che, S. Frank Yan
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Publication number: 20100317676Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: March 1, 2010Publication date: December 16, 2010Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
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Patent number: 7851468Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: GrantFiled: May 14, 2007Date of Patent: December 14, 2010Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
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Publication number: 20100311759Abstract: An antiparasitic agent for fish containing an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.Type: ApplicationFiled: October 29, 2008Publication date: December 9, 2010Applicant: NIPPON SUISAN KAISHA, LTD.Inventors: Fumi Kawano, Noritaka Hirazawa
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Patent number: 7846927Abstract: Compounds of the formula (I), in which R1, R3 and X have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: October 12, 2005Date of Patent: December 7, 2010Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Alfred Jonczyk, Wilfried Rautenberg