1,3-diazine Ring Patents (Class 544/122)
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Patent number: 8114872Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.Type: GrantFiled: May 7, 2008Date of Patent: February 14, 2012Assignee: Eli Lilly and CompanyInventors: Joyce Z. Crich, Delu Jiang, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Melissa Kate Slater, Yan Wang, James Robert Henry, Hong Hu, Sachin Govindlal Maniar
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Publication number: 20120028952Abstract: 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 medicament having the above-mentioned properties.Type: ApplicationFiled: January 24, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
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Publication number: 20120028979Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: October 6, 2011Publication date: February 2, 2012Inventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
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Publication number: 20120028924Abstract: The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.Type: ApplicationFiled: August 2, 2011Publication date: February 2, 2012Applicant: ASTRAZENECA ABInventors: Brian AQUILA, Victor KAMHI, Bo PENG, Timothy PONTZ, Jamal Carlos SAEH, Kumar THAKUR, Bin YANG
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Publication number: 20120028958Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 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 medicament having the above-mentioned properties.Type: ApplicationFiled: January 24, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
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Patent number: 8106045Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R? represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: September 9, 2005Date of Patent: January 31, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Kazutoshi Watanabe, Fumiaki Uehara, Shinsuke Hiki, Toshiyuki Kohara, Kenji Fukunaga, Satoshi Yokoshima
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Patent number: 8093239Abstract: The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.Type: GrantFiled: May 28, 2008Date of Patent: January 10, 2012Assignee: GlaxoSmithKline LLCInventors: Kevin Kuntz, David Edward Uehling, Alex Gregory Waterson, Kyle Allen Emmitte, Kirk Stevens, John Brad Shotwell, Stephon Cornell Smith, Kristen E. Nailor, James M. Salovich, Brian John Wilson, Mui Cheung, Robert Anthony Mook, Erich W. Baum, Ganesh Moorthy
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Patent number: 8093246Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
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Patent number: 8093245Abstract: 4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Alexander Heim-Riether, Theodore C. Jessop, James E. Tarver, Jerry A. Taylor
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Patent number: 8088769Abstract: The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.Type: GrantFiled: December 31, 2004Date of Patent: January 3, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Martin Hendrix, Lars Bärfacker, Heike Heckroth, Dagmar Karthaus, Adrian Tersteegen
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Patent number: 8088766Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.Type: GrantFiled: September 12, 2008Date of Patent: January 3, 2012Assignee: Array BioPharma Inc.Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
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Publication number: 20110319392Abstract: 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: March 10, 2010Publication date: December 29, 2011Inventors: George Adjabeng, Erich Baum, Neil Bifulco, JR., Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Keith Hornberger, Kimberly Petrov, Tara Renae Reheault, Douglas McCord Sammond, Gregory M. Schaaf
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Publication number: 20110318393Abstract: Provided are substituted pyrazole compounds which are useful as protein kinase inhibitors, compositions comprising the compounds, and methods of use thereof. The protein kinase inhibitors are particularly for inhibition of Aurora A (Aurora-2) protein kinase and are useful in the treatment of diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.Type: ApplicationFiled: November 23, 2009Publication date: December 29, 2011Applicant: MIIKANA THERAPEUTICS, INC.Inventors: Gaetan Ladouceur, Gregory A. Agosto, Jamshed H. Shah, Lita Suwandi, Nnamdi Ofoegbu
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Publication number: 20110319615Abstract: Pyrimidinyl aryl hydrazones are effective at controlling insects.Type: ApplicationFiled: September 8, 2011Publication date: December 29, 2011Applicant: DOW AGROSCIENCES LLCInventors: Katherine A. Guenthenspberger, Timothy C. Johnson, Noormohamed M. Niyaz, Ricky Hunter, Annette V. Brown, Tony K. Trullinger
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Publication number: 20110318305Abstract: 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: ApplicationFiled: August 19, 2009Publication date: December 29, 2011Inventors: 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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Publication number: 20110312908Abstract: The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: November 28, 2008Publication date: December 22, 2011Applicants: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang, Amy Wojciechowski
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110306590Abstract: Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 9, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Kristin L. Andrews, Michael J. Frohn, Paul E. Harrington, Alexander J. Pickrell, Robert M. Rzasa
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Publication number: 20110306602Abstract: The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.Type: ApplicationFiled: April 24, 2008Publication date: December 15, 2011Inventors: Philipp Wabnitz, Heike Schauerte, Hans Allgeier, Lutz Zeitlmann, Anke Mueller, Martin Augustin, Michael A. Pleiss, Gabriele Stumm, Axel Choidas, Bert Klebl, Gerhard Mueller, Wilfried Schwab, Joelle Le, Jackie Macritchie, Don Simpson
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Publication number: 20110306589Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 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 therapeutics.Type: ApplicationFiled: June 2, 2011Publication date: December 15, 2011Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez Sarmiento
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Publication number: 20110306613Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: ASTRAZENECA ABInventors: Kevin Michael Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
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Publication number: 20110301161Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein R1-R7 are as defined herein. The invention 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 1, 2010Publication date: December 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Zhidong CHEN, Ming-Hong HAO, Weimin LIU, Ho-Yin LO, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Peter Allen NEMOTO, Hidenori TAKAHASHI, Heather TYE, Lifen WU
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Publication number: 20110301160Abstract: In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.Type: ApplicationFiled: December 3, 2010Publication date: December 8, 2011Applicant: ARQULE, INC.Inventors: Mark A. ASHWELL, Syed ALI, Jifeng LIU, Yanbin LIU, Peter LOHSE, Belew MEKONNEN, Robert SELLIAH, Manish TANDON, Woj WRONA, Valery ANTONENKO
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Publication number: 20110301141Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 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: June 1, 2011Publication date: December 8, 2011Applicant: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet Gunzner-Toste, Daniel Shore, Zachary Sweeney, Shumei Wang, Guiling Zhao
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Patent number: 8071768Abstract: The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: June 6, 2006Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Nand Baindur, Michael David Gaul, Kevin Douglas Kreutter, Christian Andrew Baumann, Alexander J. Kim, Guozhang Xu, Robert W. Tuman, Dana L. Johnson
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Publication number: 20110294749Abstract: 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: ApplicationFiled: June 28, 2011Publication date: December 1, 2011Applicant: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110294810Abstract: The present invention relates (pyridyl)-azinylamino derivatives of formula (I) wherein Q1 and p, Ra to Rc, X, Y, Z, 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 13, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, Pierre-Yves Coqueron, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Jean-Pierre Vors
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Patent number: 8067409Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: November 20, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
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Patent number: 8063035Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.Type: GrantFiled: May 7, 2008Date of Patent: November 22, 2011Assignee: Eli Lilly and CompanyInventors: Joyce Z. Crich, James Robert Henry, Hong Hu, Delu Jiang, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Melissa Kate Slater, Yan Wang
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Publication number: 20110281873Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.Type: ApplicationFiled: December 11, 2009Publication date: November 17, 2011Inventors: Phoebe Chiang, Shomir Ghosh
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Publication number: 20110281841Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.Type: ApplicationFiled: November 12, 2010Publication date: November 17, 2011Applicants: Oscotec, Inc., GenoscoInventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Kon, Hee Kyu Lee, Yougsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
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Publication number: 20110281872Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: ApplicationFiled: March 11, 2011Publication date: November 17, 2011Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
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Publication number: 20110281838Abstract: The present invention encompasses compounds of general Formula (1) wherein R1 to R4 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 medicament having the above-mentioned properties.Type: ApplicationFiled: July 28, 2009Publication date: November 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Tobias Wunberg, Ralph Brueckner, Dirk Kessler, Oliver Kraemer, Darryl McConnell, Siegfried Schneider, Lars van der Veen
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Patent number: 8058279Abstract: Pyrimidinyl aryl hydrazones are effective at controlling insects.Type: GrantFiled: September 26, 2008Date of Patent: November 15, 2011Assignee: Dow AgroSciences LLCInventors: Katherine A. Guenthenspberger, Timothy C. Johnson, Noormohamed M. Niyaz, Ricky Hunter, Annette V. Brown, Tony K. Trullinger
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Publication number: 20110275628Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: ApplicationFiled: November 24, 2009Publication date: November 10, 2011Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
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Publication number: 20110275611Abstract: 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.Type: ApplicationFiled: November 18, 2009Publication date: November 10, 2011Inventors: 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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Publication number: 20110275633Abstract: The present invention encompasses compounds of general formula (1) wherein R1-R3 and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 13, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Bodo Betzemeier, Heinz Stadtmueller
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Publication number: 20110269761Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: April 17, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Patent number: 8048881Abstract: The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 27, 2006Date of Patent: November 1, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Heinz Fretz, Kurt Hilpert, Olivier Houille, Francis Hubler, Emmanuel Meyer
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Publication number: 20110263565Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 28, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Thomas Karner, Ulrich Reiser
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Publication number: 20110263541Abstract: Described herein are compounds that are inhibitors of one or more protein kinases. Also described are pharmaceutical compositions and medicaments that include the compounds described herein. Also described herein are methods of using such protein kinase inhibitors, alone and in combination with other compounds, for conditions or diseases mediated or dependent upon protein kinases.Type: ApplicationFiled: April 27, 2011Publication date: October 27, 2011Applicant: SHANGHAI GENOMICS, INCInventors: Ying LUO, Fang SHU, Shudong WANG
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Publication number: 20110257154Abstract: 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: June 29, 2011Publication date: October 20, 2011Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Patent number: 8039465Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.Type: GrantFiled: January 28, 2010Date of Patent: October 18, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
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Publication number: 20110251174Abstract: 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: June 14, 2011Publication date: October 13, 2011Applicant: 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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Publication number: 20110245242Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R10 and L1, L2, E1, E2, E3, Y and Z have the meanings given in the description, and agrochemically active salts thereof, their use 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 heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hille, Kerstin Ilgö, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Arnd Voerste, Peter Dahmen, Rurth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano
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Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
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Publication number: 20110245249Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R12 and E1, E2, E3, L1, Y, Z and L2 have the meanings given in the description, and agrochemically active salts thereof, their use 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 heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 22, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Pierre Wasnaire, Jorg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Christoph Andreas Braun, Martin Kaussmann, Hiroyuki Hadano
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Publication number: 20110245205Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: October 6, 2011Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Patent number: 8030483Abstract: The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-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: GrantFiled: January 16, 2009Date of Patent: October 4, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, Rajinder Singh, Hui Li