1,3-diazine Ring Patents (Class 544/122)
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Publication number: 20110237578Abstract: Compounds are provided according to formula (I), where A, B, W, X?, L, R1, R3, R4b, 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: September 14, 2009Publication date: September 29, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Publication number: 20110237586Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, JR.
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Publication number: 20110230478Abstract: Use of 4-alkyl-substituted diaminopyrimidines of the formula (I) as fungicide in which R1 to R13 and X1 and X2 have the meanings given in the description, and agrochemically active salts thereof, and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing diaminopyrimidines of the formulae (Ia), (Ib) and (Ic).Type: ApplicationFiled: August 26, 2009Publication date: September 22, 2011Applicant: Bayer ScienceCrop AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Urike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano, Marcel Calleja
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Publication number: 20110230484Abstract: This invention relates to novel pyrazolyl-pyrimidine derivatives and their use as potassium channel modulating agents. In another aspect the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: August 26, 2009Publication date: September 22, 2011Applicant: NEUROSEARCH A/SInventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Patent number: 8022061Abstract: Compounds having formula I: where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.Type: GrantFiled: October 9, 2007Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Yasuyuki Ogawa, Ryo Okuyama, Satoshi Shibuya, Narihiro Toda, Zhaodan Cao, Zice Fu, Xiaolin Hao, Yong-Jae Kim, Leping Li, Sarah E. Lively, Mike Lizarzaburu, Hui Tian, Ming Yu
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Publication number: 20110218187Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Werner BREITENSTEIN, Pascal FURET, Sandra JACOB, Paul William MANLEY
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Publication number: 20110218198Abstract: Compounds of the formula I in which X, R1, R2, R3, R4 and R6 have the meanings indicated in Claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: June 4, 2009Publication date: September 8, 2011Applicant: MERCK PATENT GESELLSCHAFTInventors: Margarita Wucherer-Plietker, David Bruce, Dirk Finsinger, Ulrich Graedler, Dieter Dorsch, Christina Esdar
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Publication number: 20110218188Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8012959Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: GrantFiled: September 22, 2008Date of Patent: September 6, 2011Assignee: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masashiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110212077Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: August 24, 2010Publication date: September 1, 2011Applicant: TargeGen, Inc.Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
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Patent number: 8003643Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: November 18, 2009Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20110201606Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising themType: ApplicationFiled: April 27, 2011Publication date: August 18, 2011Applicant: Novartis AGInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Publication number: 20110201599Abstract: A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: July 2, 2009Publication date: August 18, 2011Applicant: EXELIXIS, INC.Inventors: Suleyman Bahceci, Bryan Chan, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Maurizio Franzini, Vasu Jammalamadaka, Joon Won Jeong, Lisa Renee Jones, Ryan Michael Kelley, Moon Hwan Kim, James W. Leahy, Morrison B. Mac, Robin Tammie Noguchi, Pallavi Rao, Brian Hugh Ridgway, Wei Xu, Yong Wang
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Publication number: 20110201605Abstract: 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: ApplicationFiled: February 9, 2011Publication date: August 18, 2011Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20110201602Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: ApplicationFiled: November 22, 2010Publication date: August 18, 2011Applicant: Amgen Inc.Inventors: Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Stuart C. CHAFFEE, Paul TEMPEST, Phillip R. OLIVIERI, Rebecca E. JOHNSON, Brian K. ALBRECHT, Vinod F. PATEL, Victor J. CEE, Joseph L. KIM, Steven BELLON, Xiaotian ZHU, Yuan CHENG, Ning XI, Karina ROMERO, Hanh Nho NGUYEN, Holly L. DEAK
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110190259Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: March 15, 2011Publication date: August 4, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20110190280Abstract: The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: August 27, 2008Publication date: August 4, 2011Inventors: George Adjabeng, Neil Bifulco, Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Philip Anthony Harris, Keith Hornberger, Kimberly Petrov, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, David Edward Uehling, Alex Gregory Waterson
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Patent number: 7989446Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: GrantFiled: September 22, 2010Date of Patent: August 2, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Publication number: 20110183957Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 4, 2009Publication date: July 28, 2011Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20110183979Abstract: The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: January 13, 2011Publication date: July 28, 2011Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Eric Vieira
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Publication number: 20110183975Abstract: The present invention relates to a compound of formula I: wherein: R1 is C1-6 alkyl, C3-8 cycloalkyl, aryl, heterocyclyl, or —COR1x, where the C1-6 alkyl, C3-8 cycloalkyl, aryl, and heterocyclyl may be substituted; and R1x is C3-8 cycloalkyl, aryl, or heterocyclyl, any of which may be substituted; R2, R3, R4, R5, R6, and R7 are each independently hydrogen, halogen, C1-6 alkyl, or aryl, where the C1-6 alkyl or aryl may be substituted; R8 is hydrogen, C1-6 alkyl, aryl, or heterocyclyl, any of which may be substituted; or a pharmaceutically acceptable salt or ester thereof.Type: ApplicationFiled: September 28, 2009Publication date: July 28, 2011Inventors: Yasuhiro Goto, Takeshi Sagara, Weiming Fan, Thomas F. N. Hacell, Matthew G. Jenks, Michael J. Malaska, Joseph A. Moore, III, Gilles Ouvry, Bharathi Pandi, Michael R. Peel, Kimberty M. Steward
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Publication number: 20110172231Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.Type: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Inventors: Rolf BAENTELI, Gerhard Zenke, Nigel Graham Cooke, Rudolf Duthaler, Gebhard Thoma, Anette Von Matt, Toshiyuki Honda, Naoko Matsuura, Kazuhiko Nonomura, Osamu Ohmori, Ichiro Umemura, Klaus Hinterding, Christos Papageorgiou
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Publication number: 20110172215Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: May 4, 2009Publication date: July 14, 2011Inventors: George Adjabeng, Jeffrey Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
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Publication number: 20110166120Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
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Publication number: 20110166137Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: July 7, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
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Publication number: 20110166117Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 30, 2010Publication date: July 7, 2011Inventors: Roger Bonnert, Stephen Brough, Andrew Davies, Timothy Luker, Thomas McInally, Ian Millichip, Garry Pairaudeau, Anil Patel, Rukhsana Rasul, Stephen Thom
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Publication number: 20110159019Abstract: Provided is a compound which is useful as an active ingredient for a pharmaceutical having a PKC? inhibition activity, particularly a pharmaceutical composition for inhibiting acute rejection occurring in transplantation. The present inventors have conducted extensive studies on a compound having a PKC? inhibition activity, and as a result, they have found that a compound having a structure such as aralkyl and the like on an amino group at the 2-position and also having a structure such as an adamantylalkyl group and the like on an amino group at the 4-position of 2,4-diaminopyrimidine, or a salt thereof has an excellent PKC? inhibition activity, thereby completing the present invention. The 2,4-diaminopyrimidine compound of the present invention can be used as a PKC? inhibitor or an inhibitor of acute rejection occurring in transplantation.Type: ApplicationFiled: August 31, 2009Publication date: June 30, 2011Inventors: Akira Tanaka, Koichiro Mukoyoshi, Shigeki Kunikawa, Yuji Takasuna, Jun Maeda, Noboru Chida, Shinya Nagashima
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Publication number: 20110152245Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Katrin Groebke Zbinden, Roger Norcross, Philippe Pflieger
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Publication number: 20110152518Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.Type: ApplicationFiled: November 22, 2010Publication date: June 23, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Li, Ankush Argade, Rajinder Singh, Sambaiah Thota, David Carroll, Kin Tso, Vanessa Taylor, John McLaughlin, Vadim Markovtsov
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Publication number: 20110152235Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Patent number: 7964592Abstract: Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: March 12, 2004Date of Patent: June 21, 2011Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Publication number: 20110136764Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.Type: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Applicant: OSI Pharmaceuticals, Inc.Inventors: Rama Devi APPARI, Xin CHEN, Ramesh Chllukuri, Andrew P. CREW, Hanqing DONG, Caterina FERRARO, Kenneth FOREMAN, Ramesh C. GUPTA, An-Hu LI, Dan SHERMAN, Kathryn M. STOLZ, Brian VOLK, Robert ZAHLER
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Publication number: 20110136666Abstract: The present invention relates to substituted pyrimidine derivatives as well as N-oxides and agriculturally acceptable salts thereof, and their use to control undesired plant growth, in particular in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredient (such as, for example, an herbicide, fungicide, insecticide and/or plant growth regulator) and/or a safener.Type: ApplicationFiled: April 30, 2009Publication date: June 9, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: William Guy Whittingham, Caroline Louise Winn, John Williams, Harry Glithro
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Patent number: 7956053Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: GrantFiled: June 22, 2009Date of Patent: June 7, 2011Assignee: Novartis AGInventors: Werner Breitenstein, Pascal Furet, Sandra Jacob, Paul W Manley
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Publication number: 20110130401Abstract: Compounds of general formula (1) wherein A, B, R1 to R5, Rx m, n and p are defined as described in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and the use thereof [as] medicaments.Type: ApplicationFiled: May 21, 2010Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Daniel Kuhn, Heinz Stadtmueller
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Publication number: 20110124632Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: October 18, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Nwe Y. Ba-maung, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Megumi Kawai, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang
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Publication number: 20110112063Abstract: The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: June 24, 2009Publication date: May 12, 2011Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Publication number: 20110112096Abstract: The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: June 24, 2009Publication date: May 12, 2011Applicant: ITM LLCInventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Songchun Jiang, Kunyong Yang
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Publication number: 20110105472Abstract: Use of diaminopyrimidines of the formula (I) in which R1 to R11a,b,c and X1, X2 have the meanings given in the description, and also agrochemically active salts thereof as crop protection agents. Diaminopyrimidines of the formulae (Ia), (Ib) and (Ic) in which R8a, R8b, R8c, and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11a,b,c and X1, X2 have the meanings given in the description, and also agrochemically active salts thereof and their use for controlling animal pests and/or phytopathogenic harmful fungi.Type: ApplicationFiled: March 16, 2009Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Olive Gaertzen, Stefan Hillebrand, Amos Mattes, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Peter Schreier, Ulrich Görgens, Heinz Kehne, Christian Paulitz, Hiroyuki Hadano, Oliver Guth, Angela Becker, Olga Malsam
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Publication number: 20110105486Abstract: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.Type: ApplicationFiled: December 6, 2010Publication date: May 5, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Publication number: 20110098296Abstract: The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: ApplicationFiled: December 4, 2008Publication date: April 28, 2011Inventors: George Adjabeng, Neil Bifulco, Ronda G. Davis-Ward, Scott Howard Dickerson, Keith Hornberger, Kimberly Petrov, Tara Renae Rheault, Daivd Edward Uehling, Alex Gregory Waterson
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Publication number: 20110098280Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 4, 2011Publication date: April 28, 2011Applicants: Novartis AG, IRM LLCInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura, Ruo Steensma, Greg Chopiuk, Jiqing Jiang, Yongqin Wan, Qiang Ding, Qiong Zhang, Nathanael Schiander Gray, Donald Karanewsky
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Publication number: 20110098301Abstract: Pyrimidine derivatives of formula pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are disclosed and claimed.Type: ApplicationFiled: March 9, 2006Publication date: April 28, 2011Applicant: BAYER HEALTHCARE LLCInventors: Julie A. Dixon, Dhanapalan Nagarathnam, Lei Zhang, Chunguang Wang, Lin Yi, Yuanwei Chen, Jianqing Chen, Brian R. Bear, Michael Brands, Alexander Hillisch, Donald Bierer, Ming Wang, Wenlang Fu
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Publication number: 20110098288Abstract: The invention relates to compounds of formula (I) wherein R1 to R9 and R4a have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: March 10, 2009Publication date: April 28, 2011Inventors: Jeremy Major, Richard John Harrison, Nigel Ramsden, David Middlemiss, Ulrich Kruse, Gerard Drewes
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Patent number: 7932246Abstract: Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N? or —C?; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.Type: GrantFiled: May 15, 2006Date of Patent: April 26, 2011Assignee: Chroma Therapeutics Ltd.Inventors: David Festus Charles Moffat, Sanjay Ratilal Patel, Francesca Ann Mazzei, Andrew James Belfield, Sandra Van Meurs
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Publication number: 20110092490Abstract: A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two heteroatoms or Ar is a 6-membered aromatic ring, wherein heteroatoms are selected from S, O, N, Se; Z is NH, NHCO, NHSO2, N-alkyl, CH2NH, CH2N-alkyl, CH2, CH2CH2, CH?CH, CH2CONH, SO2, or SO; Y is N CR3; R1, R2, R5, R6, R7, R8 and R9 are each independently H, or a substituent; R3, when present, is selected from alkyl and a substituent, with the proviso that when Y is CR3, Ar is a 5-membered heterocycle comprising one or two N heteroatoms and Z is NH, then R3 is selected from C3+ alkyl and a substituent; R4 is selected from H, alkyl and R13 as hereinbefore defined, with the proviso that when R3 is absent, R4 is selected from alkyl and a substituent; processes for the preparation thereof, intermediates and precursors therefore and the use thereof as a medicament, and therapeutic compType: ApplicationFiled: March 26, 2009Publication date: April 21, 2011Applicant: THE UNIVERSITY OF NOTTINGHAMInventors: Shudong Wang, Shenhua Shi, Andrey Zaytsev, Peter Martin Fischer
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Publication number: 20110092481Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.Type: ApplicationFiled: April 21, 2009Publication date: April 21, 2011Inventors: Christopher John Love, Joseph Elisabeth Leenaerts, Ludwig Paul Cooymans, Donald Alec Labsack, Bryan James Branstetter, Jason Christopher Rech, Elizabeth Ann Gleason, Jennifer Diane Venable, Danielle Wiener, Deborah Margaret Smith, James Guy Breitenbucher
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Publication number: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. 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, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Publication number: 20110082140Abstract: Compounds of the formula (I), in which R1, R2, R3 and R4 have the meanings indicated in claim (1), are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: May 23, 2008Publication date: April 7, 2011Applicant: Merck Patent GmbHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Lars Thore Burgdorf, Christian Sirrenberg, Christina Esdar, Thomas J.J. Mueller, Eugen Merkul