Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/279)
-
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
-
Publication number: 20130338140Abstract: Compounds having the formula I wherein Z, Z1 Z2 Z, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.Type: ApplicationFiled: February 28, 2012Publication date: December 19, 2013Applicants: Genetech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Huifen Chen, Mark Joseph Chcarelli, Jason Demeese, Rustam Garrey, John J. Gaudino, Robert J. Kaus, Gabrielle R. Kolakowski, Allison L. Marlow, Peter J. Mohr, Li Ren, Jacob Schwartz, Christopher S. Siedem, Allen A. Thomas, Eli Wallace, Steven Mark Wenglowsky
-
Publication number: 20130338153Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: December 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130324516Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
-
Publication number: 20130317047Abstract: The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).Type: ApplicationFiled: November 9, 2012Publication date: November 28, 2013Applicant: Aventis Pharma Deutschland GmbHInventor: Aventis Pharma Deutschland GmbH
-
Patent number: 8586505Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: GrantFiled: July 15, 2010Date of Patent: November 19, 2013Assignee: SDS Biotech K. K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
-
Patent number: 8586747Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: GrantFiled: September 28, 2012Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
-
Publication number: 20130296338Abstract: A series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: September 2, 2011Publication date: November 7, 2013Applicant: UCB PHARMA S.A.Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Barry John Langham, Judi Charlotte Neuss, Joanna Rachel Quincey
-
Publication number: 20130296333Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: July 9, 2013Publication date: November 7, 2013Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Publication number: 20130289272Abstract: Methods for producing 1,5,7-triazabicyclo[4.4.0]dec-5-ene using a disubstituted carbodiimide, dipropylene triamine and optionally an ethereal solvent and/or an alcohol are disclosed. Use of 1,5,7-triazabicyclo[4.4.0]dec-5-ene produced by this method in an electrodepositable coating composition, and electrophoretic deposition of such coating onto a substrate to form a coated substrate, are also disclosed.Type: ApplicationFiled: April 25, 2012Publication date: October 31, 2013Applicant: PPG Industries Ohio, Inc.Inventors: Christopher Dacko, Richard F. Karabin, Craig Wilson, Steven R. Zawacky
-
Publication number: 20130289273Abstract: Methods for producing 1,5,7-triazabicyclo[4.4.0]dec-5-ene using a disubstituted carbodiimide, dipropylene triamine and optionally an ethereal solvent and/or an alcohol are disclosed. Use of 1,5,7-triazabicyclo[4.4.0]dec-5-ene produced by this method in an electrodepositable coating composition, and electrophoretic deposition of such coating onto a substrate to form a coated substrate, are also disclosed.Type: ApplicationFiled: February 28, 2013Publication date: October 31, 2013Applicant: PPG Industries Ohio, Inc.Inventors: Christopher A. Dacko, Richard F. Karabin, Craig A. Wilson, Steven R. Zawacky, Gregory J. McCollum
-
Patent number: 8569316Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R4, X1, X2, X3, X4, X5, Q, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.Type: GrantFiled: February 17, 2010Date of Patent: October 29, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Peter Ettmayer, Andreas Mantoulidis
-
Patent number: 8569295Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: Merck Patent GmbHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
-
Patent number: 8563560Abstract: Disclosed herein are bicyclic guanidine salts, useful as cure catalysts for electrodeposited coatings. The bicyclic guanidine salts are formed as the reaction product of reactants comprising (a) a compound having the general formula CXn, wherein X is N, O, or S and wherein n is 2 to 4; (b) an acid; (c) dipropylene triamine; and (d) water, and an associated method for forming a bicyclic guanidine salt from the same reaction ingredients.Type: GrantFiled: February 25, 2011Date of Patent: October 22, 2013Assignee: PPG Industries Ohio, Inc.Inventors: Charles R. Hickenboth, Christopher A. Dacko, Steven R. Zawacky, Gregory J. McCollum
-
Publication number: 20130274274Abstract: 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: March 15, 2013Publication date: October 17, 2013Inventors: Hong Woo Kim, Hee Kyu Lee, Ho-Juhn Song, Jaekyoo Lee, Jong Sung Koh, Youngsam Kim, Jung-Ho Kim, Se Won Kim, In Yong Lee
-
Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
-
Patent number: 8552205Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: November 20, 2008Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
-
Patent number: 8546405Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: December 22, 2009Date of Patent: October 1, 2013Assignee: Abbott LaboratoriesInventors: David A. DeGoey, Pamela L. Donner, Warren M. Kati, Charles W. Hutchins, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Preethi Krishnan, Neeta C. Mistry, Tami J. Pilot-Matias, Sachin V. Patel, Xiaoyan Li, Todd N. Soltwedel, Lissa T. Nelson
-
Publication number: 20130252967Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130252977Abstract: The present invention provides a pyrido[2,3-d]pyrimidine compound, or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in treating cancer.Type: ApplicationFiled: March 5, 2013Publication date: September 26, 2013Applicants: DECIPHERA PHARMACEUTICALS, LLC, ELI LILLY AND COMPANYInventors: Matthew Carl Allgeier, Daniel L. Flynn, Michael D. Kaufman, Phenil J. Patel, Craig D. Wolfangel
-
Publication number: 20130252966Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Patent number: 8541424Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: December 22, 2009Date of Patent: September 24, 2013Assignee: Abbott LaboratoriesInventors: David A. DeGoey, Pamela L. Donner, Warren M. Kati, Charles W. Hutchins, Mark A. Matulenko, Tammie K. Jinkerson, Ryan G. Keddy
-
Publication number: 20130245012Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Patent number: 8536187Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, for use in the treatment of hepatitis C.Type: GrantFiled: July 1, 2009Date of Patent: September 17, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael L. Mitchell, William J. Watkins, Jennifer R. Zhang
-
Publication number: 20130237538Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
-
Publication number: 20130231348Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 5, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130225813Abstract: The present invention relates generally intermediates for making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione.Type: ApplicationFiled: March 20, 2013Publication date: August 29, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: David Paul Provencal
-
Publication number: 20130225589Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
-
Patent number: 8518958Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: GrantFiled: October 16, 2007Date of Patent: August 27, 2013Assignee: Forma Therapeutics, Inc.Inventors: Krishna K. Murthi, Rebecca Casaubon, Arthur F. Kluge, Chase C. Smith, Joachim Vogt
-
Patent number: 8513265Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: GrantFiled: October 10, 2012Date of Patent: August 20, 2013Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Dean A. Wacker
-
Patent number: 8513262Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.Type: GrantFiled: January 22, 2010Date of Patent: August 20, 2013Assignee: GlaxoSmithKline LLCInventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
-
Publication number: 20130210819Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 22, 2011Publication date: August 15, 2013Applicant: MERCK PATENT GMBHInventor: Markus Klein
-
Publication number: 20130203756Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 24, 2011Publication date: August 8, 2013Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
-
Publication number: 20130203786Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: May 16, 2011Publication date: August 8, 2013Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
-
Publication number: 20130203787Abstract: The present invention relates to 1.5 hydrate of of 1-{(2S)-2-amino-4-[2,4-bis (trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl}-5,5-di-fluoropiperidin-2-one tartrate, a process for preparing the same, and a pharmaceutical composition for inhibiting DPP-IV, which comprises said compound as the active component.Type: ApplicationFiled: October 31, 2011Publication date: August 8, 2013Applicant: LG LIFE SCIENCES LTD.Inventors: Ki Sook Park, Jung Min Yun, Bong Chan Kim, Kyu Young Kim, Ji Hye Lee
-
Patent number: 8501749Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.Type: GrantFiled: January 26, 2010Date of Patent: August 6, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
-
Publication number: 20130197223Abstract: Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).Type: ApplicationFiled: September 22, 2011Publication date: August 1, 2013Applicant: NOVOMER, INC.Inventors: Jay J. Farmer, Gabriel E. Job
-
Patent number: 8497371Abstract: Novel and optimized classes of pipemidic acid derivative compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes of compounds exhibit exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.Type: GrantFiled: October 26, 2010Date of Patent: July 30, 2013Assignee: University of Memphis Research FoundationInventors: Abby Louise Parrill-Baker, Daniel Lee Baker, Adrienne Hoeglund
-
Patent number: 8492542Abstract: The present invention is directed to a method producing bicyclic guanidine comprising heating a cyclic thiourea to a temperature ranging from ?140° C. in a substantially non-hydrocarbon solvent to form the bicyclic guanidine.Type: GrantFiled: May 15, 2008Date of Patent: July 23, 2013Assignee: PPG Industries Ohio, Inc.Inventors: Britt A. Minch, Charles R. Hickenboth, Richard F. Karabin, Steven R. Zawacky, Thomas R. Hockswender, Gregory J. McCollum
-
Patent number: 8492392Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds of formula I, which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: May 24, 2010Date of Patent: July 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
-
Patent number: 8492393Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.Type: GrantFiled: September 13, 2012Date of Patent: July 23, 2013Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
-
Publication number: 20130184253Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 19, 2012Publication date: July 18, 2013Applicant: NOVARTIS AGInventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
-
Patent number: 8486954Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.Type: GrantFiled: September 13, 2012Date of Patent: July 16, 2013Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
-
Patent number: 8486952Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: July 28, 2010Date of Patent: July 16, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
-
Publication number: 20130178462Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: March 5, 2013Publication date: July 11, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
-
Publication number: 20130172372Abstract: The present application relates to novel fused 4-aminopyrimidines, 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 production of medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2011Publication date: July 4, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
-
Patent number: 8470837Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the presently described compounds.Type: GrantFiled: April 18, 2012Date of Patent: June 25, 2013Assignee: Takeda Pharmaceutical Company LimtedInventors: Qing Dong, Stephen W. Kaldor
-
Patent number: 8470836Abstract: Disclosed herein are novel compounds of Formula (1) as defined in the specification having excellent inhibitory activity against dipeptidyl peptidase-IV (DPP-IV), methods of preparing the same and pharmaceutical compositions comprising the same as an active agent.Type: GrantFiled: December 19, 2008Date of Patent: June 25, 2013Assignee: LG Life Sciences, Ltd.Inventors: Chang-Seok Lee, Hyeon Joo Yim, Kyoung-Hee Kim, Jaeick Lee, Sung-Hack Lee, Kyu Woong Lee, Hee Bong Lee, Wan Su Park, Changhee Min
-
Publication number: 20130158003Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: SUNOVION PHARMACEUTICALS INCInventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
-
Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN