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: 20090270389Abstract: 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: ApplicationFiled: April 29, 2009Publication date: October 29, 2009Inventors: 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
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Publication number: 20090270430Abstract: 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: October 9, 2006Publication date: October 29, 2009Applicant: Exelixix, 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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Patent number: 7601713Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: GrantFiled: December 15, 2006Date of Patent: October 13, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20090253696Abstract: This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C.Type: ApplicationFiled: June 20, 2007Publication date: October 8, 2009Inventors: Piet Andre' Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong, Jennifer Zhang
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Publication number: 20090247518Abstract: 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-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: March 26, 2009Publication date: October 1, 2009Inventors: Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
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Publication number: 20090232828Abstract: The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s).Type: ApplicationFiled: July 3, 2007Publication date: September 17, 2009Applicant: EXELIXIS, INC.Inventor: Wentao Zhang
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Publication number: 20090233923Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.Type: ApplicationFiled: March 31, 2009Publication date: September 17, 2009Applicant: Sanofi-aventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
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Publication number: 20090221600Abstract: Provided are novel pyrido-pyrimidine derivatives, having the structure of Formula (I): which can be used as anti-inflammatory agents. Also provided are pharmaceutical compositions comprising one or more pyrido-pyrimidine derivatives, as well as methods of treating autoimmune diseases, inflammation or associated pathologies, including for example, sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, comprising administering such compounds or pharmaceutical compositions comprising them.Type: ApplicationFiled: September 28, 2006Publication date: September 3, 2009Inventors: Ashwani Kumar Verma, Yogesh Bhaskarrao Waman, Venkata P. Palle, Atul Kondaskar, Abhijit Ray, Malini Bajpai, Geeta Sharma
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Patent number: 7582643Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.Type: GrantFiled: February 18, 2008Date of Patent: September 1, 2009Assignee: Pfizer IncInventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, Jr., Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
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Patent number: 7572801Abstract: The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.Type: GrantFiled: May 11, 2007Date of Patent: August 11, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos Panousis, Jens-Uwe Peters, Fabienne Ricklin, Stephan Roever
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Publication number: 20090186910Abstract: Methods are disclosed for determining whether organ toxicity, particularly cardiotoxicity, will occur in a patient selected for treatment with various kinase inhibitors, such as tyrosine kinase inhibitors, more particularly erbB inhibitors such as Herceptin. In addition, methods are disclosed for determining whether a potential drug is likely to produce a cardiotoxic effect. The methods involve analyzing lipid levels or the expression fatty acid oxidation enzymes, pAMP activated protein kinase, glucose uptake, to determine whether a fatty acid oxidation disorder is present. The identification of a fatty acid oxidation disorder can be used as a predictor of toxicity, especially cardiac toxicity, and as an indication that organ function should be carefully monitored if a drug such as a tyrosine kinase inhibitor is administered. Methods are also disclosed for protecting organs from metabolic stress and for the treatment of cells, such as adipocytes, to reduce their lipid content.Type: ApplicationFiled: February 27, 2007Publication date: July 23, 2009Applicant: Targeted Molecular Diagnostics, LLCInventor: Sarah S. Bacus
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Publication number: 20090181965Abstract: 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: ApplicationFiled: January 5, 2009Publication date: July 16, 2009Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
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Publication number: 20090176811Abstract: Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical preparations containing these compounds the use thereof for the production of pharmaceutical preparations and related method of treating or inhibiting certain disorders or conditions, including pain.Type: ApplicationFiled: March 11, 2009Publication date: July 9, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBORSCH, Bernd SUNDERMANN, Corinna SUNDERMANN, Michael HAURAND, Hagen-Heinrich HENNIES, Edward BIJSTERVELD
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Publication number: 20090156597Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.Type: ApplicationFiled: June 4, 2008Publication date: June 18, 2009Inventors: James F. Callahan, Jeffrey C. Boehm, Anthony William James Cooper, Stefano Livia, Paul Bamborough, Neysa Nevins, Zehong Wan, Beth A. Norton, Xichen Lin
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Patent number: 7547695Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X? have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumors.Type: GrantFiled: October 14, 2004Date of Patent: June 16, 2009Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
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Patent number: 7544682Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.Type: GrantFiled: January 8, 2007Date of Patent: June 9, 2009Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
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Publication number: 20090137550Abstract: This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N?-substituted-N?-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: March 24, 2006Publication date: May 28, 2009Inventors: Jeffrey C. Boehm, John J. Taggart
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Publication number: 20090131430Abstract: The present invention relates to novel azabicyclo derivatives as anti-inflammatory agents. The compounds provided herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis. Also provided herein are pharmacological compositions containing compounds provided herein and associated methods of treating sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, and other inflammatory and/or autoimmune disorders, using the compounds.Type: ApplicationFiled: November 23, 2005Publication date: May 21, 2009Inventors: Venkata P. Palle, Rakesh Kumar Singh, Sanjay Malhotra, Yogesh Bhaskarrao Waman, Ashwani Verma, Abhijit Ray, Geeta Sharma
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Publication number: 20090131460Abstract: The present invention relates to the use of pyrido[2,3-d]pyrimidines 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 pyrido-[2,3-d]pyrimidines compounds 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: ApplicationFiled: May 12, 2006Publication date: May 21, 2009Applicant: 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: 20090130097Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds.Type: ApplicationFiled: June 19, 2008Publication date: May 21, 2009Applicant: ArQule, Inc.Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
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Publication number: 20090124596Abstract: 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: January 10, 2008Publication date: May 14, 2009Inventors: Roger Victor Bonnert, Frank Burkamp, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Premji Meghani, Austen Pimm, Hitesh Jayantilal Sanganee
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Patent number: 7531545Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.Type: GrantFiled: October 25, 2006Date of Patent: May 12, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ellen E. Baxter, Christopher John Creighton, Yifang Huang, Chi Luo, Michael H. Parker, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Eric D. Strobel, Brett A. Tounge
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Publication number: 20090118310Abstract: Methods for preventing or treating Ras-induced cancer in a patient by (a) detecting v-Ha-Ras-transformed cells in a patient and (b) administering to the patient a therapeutically effective amount of a chemotherapeutic composition comprising an effective amount of an inhibitor for activated Cdc42-associated kinase (ACK) kinase.Type: ApplicationFiled: August 9, 2006Publication date: May 7, 2009Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Alam Nur-E-Kamal, Ailing Zhang, William J. Welsh, Susan M. Keenan, Xin I. Wang
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Publication number: 20090118311Abstract: 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: ApplicationFiled: April 24, 2007Publication date: May 7, 2009Inventor: Alan Hornsby Davidson
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Patent number: 7524852Abstract: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(?O)—, —SO2—, —OC(?O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided.Type: GrantFiled: June 6, 2003Date of Patent: April 28, 2009Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Tsutomu Matsumura, Hiroshi Ishida, Yosuke Yamaura, Seiji Aratake, Etsuo Ohshima, Koji Yanagawa, Motoki Miyama, Koji Suzuki, Ari Kawabe, Satoshi Nakanishi, Katsuya Kobayashi, Takashi Sato, Ichiro Miki, Kimihisa Ueno, Shinya Fujii, Miho Iwase
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Publication number: 20090105233Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: August 31, 2007Publication date: April 23, 2009Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
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Patent number: 7504406Abstract: The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same.Type: GrantFiled: December 13, 2007Date of Patent: March 17, 2009Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Claude Muneaux, Pierre Perreaut
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Publication number: 20090062316Abstract: The present application describes deuterium-enriched pelitrexol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 25, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090062274Abstract: 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: October 9, 2006Publication date: March 5, 2009Applicant: Exelixis, IncInventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Longcheng Wang, Bryan K.S. Yeung
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Publication number: 20090062276Abstract: The present invention comprises pyridopyrimidinediamine compounds of the general formula I: The compounds of the present invention are potent inhibitors of PTP1B. Accordingly, the invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.Type: ApplicationFiled: October 28, 2008Publication date: March 5, 2009Inventors: Steven Joseph Berthel, Adrian Wai-Hing Cheung, Kyungjin Kim, Shiming Li, Kshitij Chhabilbhai Thakkar, Weiya Yun
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Publication number: 20090048277Abstract: The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.Type: ApplicationFiled: July 2, 2008Publication date: February 19, 2009Applicant: SANOFI-AVENTISInventors: Pierre PERREAUT, Samir JEGHAM, Bernard BOURRIE, Pierre CASELLAS, Jean-Robert LABROSSE, Florence DURAND
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Publication number: 20090036472Abstract: The present invention relates to novel azabicyclo derivatives of Formula (I) as anti-inflammatory agents which are useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis.Type: ApplicationFiled: February 1, 2006Publication date: February 5, 2009Inventors: Venkata P. Palle, Ashwani Verma, Rakesh Kumar Singh, Yogesh Bhaskarrao Waman, Arti Walia, Abhijit Ray, Geeta Sharma
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Publication number: 20090030002Abstract: 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) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: March 24, 2008Publication date: January 29, 2009Inventors: 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: 20090028855Abstract: The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering all effective amount of a compound of formula I to the person or animal.Type: ApplicationFiled: July 14, 2008Publication date: January 29, 2009Applicant: University of South FloridaInventors: Jin Q. Cheng, Mei Sun, Said M. Sebti
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Publication number: 20080300246Abstract: The invention provides 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 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: ApplicationFiled: August 9, 2006Publication date: December 4, 2008Applicant: IRM LLCInventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
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Patent number: 7456168Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).Type: GrantFiled: April 11, 2007Date of Patent: November 25, 2008Assignee: Warner-Lambert CompanyInventors: Mark Barvian, Richard John Booth, John Quin, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Laurence Toogood, Scott Norman Vanderwel, Hairong Zhou
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Publication number: 20080275037Abstract: 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: ApplicationFiled: March 31, 2008Publication date: November 6, 2008Inventors: Zhi-Liang Wei, Donogh John Roger O'Mahony, Matthew Duncton, John Kincaid, Michael G. Kelly, Zhan Wang
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Publication number: 20080269227Abstract: The present invention is related to fused 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: September 2, 2005Publication date: October 30, 2008Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Thomas Rueckle, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Publication number: 20080255162Abstract: The present invention provides pyrimidines of Formula I: wherein R2, R4, R5, R6, R8 and J have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: April 22, 2005Publication date: October 16, 2008Inventors: Michelle Marie Bruendl, Rocco Dean Gogliotti, Annise Paige Goodman, Gregory Adam Reichard
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Publication number: 20080255163Abstract: This invention provides cells and methods for stimulating proliferation and migration of endogenous and exogenous mammalian stem cells in vivo and in vitro. The invention provides reagents and methods for efficiently proliferating mammalian stem cells in an animal in need thereof and producing stem cells that can be re-introduced into an animal in need thereof to alleviate neurological and corporal disorders.Type: ApplicationFiled: March 21, 2008Publication date: October 16, 2008Applicant: The Board of Trustees of the University of IllinoisInventors: Kiminobu Sugaya, Tingyu Qu
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Patent number: 7423042Abstract: This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N?-substituted-N?-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.Type: GrantFiled: March 24, 2006Date of Patent: September 9, 2008Assignee: Glaxo Group LimitedInventors: Jeffrey C. Boehm, John J. Taggart
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Publication number: 20080207652Abstract: The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: wherein: Z=O or S; n=1-3; R3?—CO2R8, —C(O)SR8, —C(O)NHR8, —C(S)OR8, —C(S)SR8, —C(S)NHR8, —C(NH)SR8 or —C(NH)NHR8, wherein R8 is —H or alkyl; R4?—H, —CH2R5 or —CH2CH2R5, wherein R5 independently has one of the meanings of R3; B?—NR2—, —CH2NR2—, —CH2CH2NR2—, —CH2CHR7— or —CH2O—, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C1-3 alkyl or alkoxy group; wherein R1?—NH2 or —OH, and C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.Type: ApplicationFiled: April 7, 2008Publication date: August 28, 2008Inventor: Dan Stoicescu
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Publication number: 20080207647Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 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: ApplicationFiled: July 24, 2006Publication date: August 28, 2008Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
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Publication number: 20080207651Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.Type: ApplicationFiled: February 18, 2008Publication date: August 28, 2008Inventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
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Publication number: 20080200481Abstract: Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.Type: ApplicationFiled: April 16, 2008Publication date: August 21, 2008Inventors: David A. Cheresh, Robert Paul, Brian Eliceiri
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Publication number: 20080182863Abstract: Certain appropriately 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: ApplicationFiled: March 27, 2006Publication date: July 31, 2008Inventors: 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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Publication number: 20080132528Abstract: Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of p38 MAP kinase-mediated diseases, and methods of using the compounds for treatment of Raf kinase-mediated diseases.Type: ApplicationFiled: November 8, 2007Publication date: June 5, 2008Inventors: Tobias Gabriel, Joel McIntosh, Kin-Chun Thomas Luk
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Patent number: 7361662Abstract: A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as kinase modulators.Type: GrantFiled: November 4, 2003Date of Patent: April 22, 2008Assignee: Les Laboratoires ServierInventors: Sylvain Rault, Jean-Charles Lancelot, Marina Kopp, Daniel-Henri Caignard, Bruno Pfeiffer, Pierre Renard
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Patent number: 7348331Abstract: Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in treating p38 mediated disorders in a patient.Type: GrantFiled: November 12, 2004Date of Patent: March 25, 2008Assignee: Roche Palo Alto LLCInventor: David Michael Goldstein