At Least Three Hetero Rings Containing Patents (Class 544/364)
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Patent number: 8859534Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.Type: GrantFiled: February 4, 2013Date of Patent: October 14, 2014Assignee: Acturum Life Science ABInventors: Johan Andersson, Helena Gyback, Anh Johansson, Christian Erik Linde, Jonas Malmstrom, Gunnar Nordvall, Tatjana Weigelt, Gitte Terp
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Patent number: 8859557Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: GrantFiled: August 21, 2012Date of Patent: October 14, 2014Assignee: Abbott GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Martin Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8859546Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: GrantFiled: January 20, 2012Date of Patent: October 14, 2014Assignee: AbbVie Inc.Inventors: Anil Vasudevan, Thomas D. Penning, Marina Pliushchev
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Publication number: 20140303164Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: February 28, 2014Publication date: October 9, 2014Inventors: Gediminas BRIZGYS, Eda CANALES, Chien-Hung CHOU, Michael GRAUPE, Yunfeng Eric HU, John O. LINK, Qi LIU, Yafan LU, Roland D. SAITO, Scott D. SCHROEDER, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140303138Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.Type: ApplicationFiled: December 3, 2013Publication date: October 9, 2014Inventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140303157Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: August 27, 2012Publication date: October 9, 2014Inventors: William J. Hoekstra, Robert J. Schotzinger
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Patent number: 8853207Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: GrantFiled: April 12, 2012Date of Patent: October 7, 2014Assignee: Development Center for BiotechnologyInventors: Chu-Bin Liao, Chao-Cheng Chiang, Huei-Ru Yang, Yuan-Chun Liao, Paonien Chen
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Publication number: 20140296513Abstract: The present disclosure relates to the use of a p75 receptor antagonist or its pharmaceutically acceptable salts for the preparation of a medicament for use in the treatment and/or prevention of overactive bladder.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Roberta AVALLONE, Marco BARONI, Tiziano CROCI
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Publication number: 20140296252Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Gary E. L. Brandt, Michael D. Kaufman, Hanumaiah Telikepalli, Timothy Malcolm Caldwell, Thiwanka Samarakoon
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20140288301Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Patent number: 8841306Abstract: The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H.Type: GrantFiled: November 18, 2009Date of Patent: September 23, 2014Assignee: Panacea Biotec Ltd.Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Sandeep Kanwar, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Patent number: 8841305Abstract: Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.Type: GrantFiled: October 9, 2009Date of Patent: September 23, 2014Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
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Publication number: 20140275110Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: April 11, 2014Publication date: September 18, 2014Inventors: Thorsten Oost, Astrid Netz, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140275041Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Sareum LimitedInventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
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Publication number: 20140275016Abstract: Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Thiwanka Samarakoon, Lakshminarayana Vogeti, Michael D. Kaufman, William C. Patt, YuMi Ahn
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Publication number: 20140275080Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Michael D. Kaufman, William C. Patt, Thiwanka Samarakoon, Lakshminarayana Vogeti, Karen M. Yates
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Publication number: 20140275033Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
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Patent number: 8835648Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: GrantFiled: June 9, 2010Date of Patent: September 16, 2014Assignee: Siena Biotech S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
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Patent number: 8835653Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: August 18, 2010Date of Patent: September 16, 2014Assignee: SanofiInventors: Markus Follmann, Volkmar Wehner, Jean-Michel Altenburger, Gilbert Lassalle, Jean-Pascal Herault
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Patent number: 8835436Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: GrantFiled: July 9, 2010Date of Patent: September 16, 2014Assignee: Green Cross CorporationInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong Yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho Kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Patent number: 8829001Abstract: The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.Type: GrantFiled: September 28, 2009Date of Patent: September 9, 2014Assignee: The Institute of Pharmacology and Toxicology Academy of Military Medical Science P.L.A. ChinaInventors: Jin Li, Rifang Yang, Rui Song, Hui Zhu, Ning Wu, Liuhong Yun, Ruibin Su, Rusheng Zhao
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Publication number: 20140249159Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: May 16, 2012Publication date: September 4, 2014Inventors: Noriyuki Kurose, Kayoko Hata, Yasuyoshi Iso, Naoko Yamaguchi, Bin Shao, Laykea Tafesse, Xiaoming Zhou, Jianming Yu
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Publication number: 20140249130Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.Type: ApplicationFiled: May 4, 2012Publication date: September 4, 2014Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
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Patent number: 8822447Abstract: The present invention is directed to substituted indazole compounds of formula (I) pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: GrantFiled: April 21, 2011Date of Patent: September 2, 2014Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Lawrence C. Kuo, Fengbin Song, Zhihua Sui
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Patent number: 8822472Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.Type: GrantFiled: March 23, 2011Date of Patent: September 2, 2014Assignee: Cornerstone Therapeutics, Inc.Inventors: Roger B. Clark, Daniel Elbaum
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Patent number: 8822476Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: March 3, 2010Date of Patent: September 2, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Patent number: 8822460Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: April 4, 2013Date of Patent: September 2, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael P. Winters, Nagy E. Fawzy, Fu-An Kang, Zhihua Sui
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Patent number: 8822464Abstract: 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, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: November 26, 2012Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Publication number: 20140243305Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: April 22, 2013Publication date: August 28, 2014Applicant: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J. Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20140243257Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Publication number: 20140243336Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
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Patent number: 8815839Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: GrantFiled: March 4, 2013Date of Patent: August 26, 2014Assignee: Janssen Pharmaceutica, NVInventors: Kristen Chevalier, Jose Clemente, Scott L Dax, Chris Flores, Li Liu, Mark J Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
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Patent number: 8815868Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases.Type: GrantFiled: December 28, 2007Date of Patent: August 26, 2014Assignee: Abbott GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8816079Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: GrantFiled: April 27, 2011Date of Patent: August 26, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20140235614Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.Type: ApplicationFiled: February 19, 2014Publication date: August 21, 2014Applicant: Eisai R&D Management Co., Ltd.Inventors: Setsuo Funasaka, Toshimi Okada, Keigo Tanaka, Satoshi Nagao, Isao Ohashi, Yoshinobu Yamane, Yusuke Nakatani, Yuki Karoji
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Publication number: 20140235609Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor.Type: ApplicationFiled: October 8, 2012Publication date: August 21, 2014Inventors: Tie-Lin Wang, Xuechun Zhang
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Publication number: 20140235641Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 21, 2014Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
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Publication number: 20140235859Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.Type: ApplicationFiled: April 29, 2014Publication date: August 21, 2014Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Rapolu RAJI REDDY, Dasari MURALIDHARA REDDY, Bandi VAMSI KRISHNA, Voggu RAMESH REDDY
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Publication number: 20140228351Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: March 14, 2014Publication date: August 14, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20140221334Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
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Publication number: 20140213580Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: June 18, 2012Publication date: July 31, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Patent number: 8791111Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in Claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: September 19, 2008Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20140206699Abstract: The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2— or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a steType: ApplicationFiled: August 17, 2012Publication date: July 24, 2014Applicant: REMYND NVInventors: Gerard Griffioen, Giuseppe Cecere, Matthias Nettekoven, Katrien Princen, Hasane Ratni, Mark Rogres-Evans, Walter Vifian
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Patent number: 8785449Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: September 18, 2012Date of Patent: July 22, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 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 in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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3-(BENZOIMIDAZOL-2-YL)-INDAZOLE INHIBITORS OF THE WNT SIGNALING PATHWAY AND THERAPEUTIC USES THEREOF
Publication number: 20140194441Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: January 8, 2014Publication date: July 10, 2014Applicant: Samumed, LLCInventors: Sunil Kumar KC, John Hood -
Publication number: 20140194440Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.Type: ApplicationFiled: September 27, 2013Publication date: July 10, 2014Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch