Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
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Patent number: 8697685Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and 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: GrantFiled: November 18, 2009Date of Patent: April 15, 2014Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Charles William Blackledge, Jr., Gerald Patrick Brady, Jr., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
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Patent number: 8697694Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: April 15, 2014Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Jeremy Clark, Hollis S. Kezar, III, Vinay M. Girijavallabhan, Yuhua Huang, Regina Huelgas, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, Anita T. Fowler, Feng Geng, John A. Secrist, III, Neng-Yang Shih, Vishal Verma, Francisco Velazquez, Srikanth Venkatraman
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Patent number: 8685972Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: July 31, 2009Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
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Patent number: 8680269Abstract: The present invention concerns novel heteroaryl-N-aryl thiosemicarbazones and their use in pest control, as insecticides and aca?cides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: GrantFiled: August 5, 2010Date of Patent: March 25, 2014Assignee: Dow AgroSciences, LLC.Inventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
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Patent number: 8664236Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: GrantFiled: October 12, 2011Date of Patent: March 4, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Publication number: 20140045845Abstract: The invention provides novel pyrimidine derivatives of formula (I), methods of preparing such compounds, pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer; wherein R1-R11, Z, and Y are as defined in the specification.Type: ApplicationFiled: March 23, 2012Publication date: February 13, 2014Applicant: CHEMILIA ABInventors: Marita Högberg, Emma Dahlstedt, Olof Smitt, Tommy Johansson
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Patent number: 8642611Abstract: The invention relates to alkynylpyrimidines according to the general formula (I): in which A, R1, R2, R3, R4, R5, and R6 are as defined in the claims, and salts, N-oxides, metabolites, solvates, tautomers and prodrugs thereof, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 and VEGFR2 signalling.Type: GrantFiled: June 19, 2008Date of Patent: February 4, 2014Assignee: Bayer Intellectual Property GmbHInventors: Ingo Hartung, Ulrich Bothe, Georg Kettschau, Ulrich Luecking, Anne Mengel, Martin Krueger, Karl Thierauch, Philip Lienau, Ulf Boemer
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Publication number: 20140031350Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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Publication number: 20140018344Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.Type: ApplicationFiled: July 8, 2013Publication date: January 16, 2014Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Patent number: 8618103Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 9, 2010Date of Patent: December 31, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
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Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20130345180Abstract: 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 15, 2013Publication date: December 26, 2013Applicant: NOVARTIS AGInventor: Novartis AG
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130331374Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 4, 2013Publication date: December 12, 2013Inventor: Rigel Pharmaceuticals, Inc.
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Publication number: 20130331377Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.Type: ApplicationFiled: February 24, 2012Publication date: December 12, 2013Applicant: YUHAN CORPORATIONInventors: Hyun-Joo Lee, Dong-Hoon Kim, Tae-Kyun Kim, Young-Ae Yoon, Jae-Young Sim, Myung-Hun Cha, Eun-Jung Jung, Kyoung-Kyu Ahn, Tai-Au Lee
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Patent number: 8604032Abstract: Provided herein are compounds of formula (I), pharmaceutical compositions comprising the compounds, and methods of use thereof The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity.Type: GrantFiled: May 20, 2011Date of Patent: December 10, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Publication number: 20130320262Abstract: The present invention relates to a compound of a formula (I), (II) or (III), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I), (II) or (III). The invention furthermore relates to a process for the preparation of a compound of the formula (I), (II) or (III) and to a formulation comprising one or more compounds of the formula (I), (II) or (III).Type: ApplicationFiled: January 18, 2012Publication date: December 5, 2013Applicant: MERCK PATENT GMBHInventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
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Publication number: 20130324524Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: August 7, 2013Publication date: December 5, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 8598157Abstract: 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.Type: GrantFiled: January 24, 2012Date of Patent: December 3, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Tobias Wunberg, Oliver Kraemer, Lars van der Veer
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Publication number: 20130306959Abstract: An aromatic heterocyclic derivative represented by the following formula (1)-1 or (1)-2: wherein in the formula (1)-1 or (1)-2, A is a substituted or unsubstituted nitrogen-containing heterocyclic group including 2 to 30 ring carbon atoms; B is a substituted or unsubstituted aromatic hydrocarbon group including 6 to 30 ring carbon atoms or a substituted or unsubstituted aromatic heterocyclic group including 2 to 30 ring carbon atoms; n is an integer of 2 or more; and Czs are independently an aromatic heterocyclic group including a predetermined structure.Type: ApplicationFiled: December 19, 2011Publication date: November 21, 2013Inventors: Kiyoshi Ikeda, Mitsunori Ito
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Publication number: 20130310361Abstract: The invention provides novel pyrimidine derivatives 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-1R) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: July 23, 2013Publication date: November 21, 2013Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Publication number: 20130310364Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: July 16, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20130303559Abstract: The present application relates to novel fused, heteroatom-bridged pyrazole and imidazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: July 15, 2013Publication date: November 14, 2013Inventors: Alexander STRAUB, Frank SÜßMEIER, Frank WUNDER, Johannes-Peter STASCH, Volkhart Min-Jian LI, Joachim MITTENDORF
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Patent number: 8580960Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.Type: GrantFiled: July 12, 2011Date of Patent: November 12, 2013Assignee: Roche Palo Alto LLCInventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
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Patent number: 8575338Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: GrantFiled: April 8, 2009Date of Patent: November 5, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasuyuki Tsuzuki, Miki Hirai
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Patent number: 8569323Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: GrantFiled: January 13, 2012Date of Patent: October 29, 2013Assignee: Intellikine, LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20130281429Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 26, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
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Patent number: 8563569Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: October 27, 2011Date of Patent: October 22, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Rajinder Singh
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Patent number: 8563566Abstract: This invention provided compounds of formula I where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula I; a pharmaceutically acceptable salt of a compound of formula I; a pharmaceutically acceptable ester of a compound of formula I. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt or ester or solvate thereof.Type: GrantFiled: July 28, 2008Date of Patent: October 22, 2013Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Martha De la Rosa
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Publication number: 20130274242Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).Type: ApplicationFiled: January 18, 2013Publication date: October 17, 2013Inventors: Jang-Sik Choi, Hae-Jun Hwang, Eunho Lee, Jaekyoo Lee, Ho-Juhn Song, Se Won Kim, Jung-Ho Kim, Jong Sung Koh, Sunhwa Chang, Tae-im Lee, Yung-geun Choi, Ik-hwan Han, Jaesang Lee
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Publication number: 20130267548Abstract: The present application relates to novel substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for preparing Medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 3, 2011Publication date: October 10, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat
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Publication number: 20130267705Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: July 20, 2011Publication date: October 10, 2013Applicant: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Patent number: 8552186Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: GrantFiled: March 6, 2012Date of Patent: October 8, 2013Assignee: Cephalon, Inc.Inventors: Gulzar Ahmed, Henry J. Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce D. Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph Lisko, Rong-qiang Liu, Eugen F. Mesaros, Karen L. Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
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Publication number: 20130252941Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: F. Hoffmann-La Roche AGInventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
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Publication number: 20130245262Abstract: The present invention provides a commercially viable process for preparing pazopanib and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate. The present invention also provides a process for the purification of pazopanib hydrochloride.Type: ApplicationFiled: November 11, 2011Publication date: September 19, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
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Patent number: 8530491Abstract: The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.Type: GrantFiled: October 8, 2008Date of Patent: September 10, 2013Assignee: Medicines for Malaria Venture (MMV)Inventors: Yongyuth Yuthavong, Tirayut Vilaivan, Sumalee Kamchonwongpaisan, Bongkoch Tarnchompoo, Chawanee Thongpanchang, Penchit Chitnumsub, Jirundon Yuvaniyama, David Matthews, William Charman, Susan Charman, Livia Vivas, Sanjay Babu Katiyar
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Patent number: 8530655Abstract: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substitutType: GrantFiled: July 6, 2011Date of Patent: September 10, 2013Assignee: Janssen Pharmaceutica NVInventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries, Frank Xavier Jozef Herwig Arts
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Patent number: 8530656Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: September 22, 2011Date of Patent: September 10, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Yan Chen, Rajinder Singh
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Publication number: 20130231519Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 12, 2011Publication date: September 5, 2013Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Patent number: 8524724Abstract: The invention relates to alkynylpyrimidines according to the general formula (I): in which A, R1, R2, R3, R4, R5, and R6 are as defined in the claims, and salts, N-oxides, metabolites, solvates, tautomers and prodrugs thereof, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 and VEGFR2 signalling.Type: GrantFiled: June 19, 2008Date of Patent: September 3, 2013Assignee: Bayer Intellectual Property GmbHInventors: Ingo Hartung, Ulrich Bothe, Georg Kettschau, Ulrich Luecking, Anne Mengel, Martin Krueger, Karl Thierauch, Philip Lienau, Ulf Boemer
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Publication number: 20130225620Abstract: Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: August 24, 2012Publication date: August 29, 2013Applicant: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
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Publication number: 20130210810Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 18, 2012Publication date: August 15, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: Rigel Pharmaceuticals, Inc.
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Patent number: 8492397Abstract: The present invention relates to a compound of Formula (I): wherein R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H, hydroxy, C1-2 alkyl, or OCH3; and R10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: March 12, 2010Date of Patent: July 23, 2013Assignees: Vertex Pharmaceuticals Incorporated, MSD K.K.Inventors: Hayley Binch, Masaya Hashimoto, Toshiharu Iwama, Nobuhiko Kawanishi, Michael Mortimore, Mitsuru Ohkubo, Tomoko Sunami
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Publication number: 20130178486Abstract: Compounds having the formula I wherein A, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: December 21, 2012Publication date: July 11, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
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Publication number: 20130165431Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: October 23, 2012Publication date: June 27, 2013Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20130165464Abstract: This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: MILLENNIUM PHARMACEUTICALS, INC.
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Publication number: 20130158006Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130156700Abstract: A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the compound includes at least one C11 or F18 label thereon; allowing the compound to penetrate into the tissue of the subject; and collecting a PET image of the CNS or brain tissue of the subjectType: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130150349Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rigel Pharmaceuticals, Inc.