The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/280)
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Publication number: 20130102621Abstract: The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic ? cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and the compound represented by the following formula (1): wherein one of A and B represents a nitrogen atom and the other represents a nitrogen atom or CR10, X represents an oxygen atom, a sulfur atom or —(CH2)n-N(R12)—, Y represents an oxygen atom, a sulfur atom or —N(R13)—, and R1 to R9 each represent a hydrogen atom or another substituent, or a salt thereof, or a solvate of the compound or the salt.Type: ApplicationFiled: June 24, 2011Publication date: April 25, 2013Applicant: KOWA CO., LTD.Inventors: Toshiharu Morimoto, Tomoaki Koshizawa, Gen Watanabe, Tadaaki Ohgiya, Nao Yamasaki, Noriyuki Inoue
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Patent number: 8426428Abstract: Provided herein are electrophilically enhanced kinase inhibitors of Formula I. Also provided herein are methods of making and utilizing the same.Type: GrantFiled: December 5, 2008Date of Patent: April 23, 2013Assignee: Principia Biopharma, Inc.Inventor: Richard Miller
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Publication number: 20130096141Abstract: Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.Type: ApplicationFiled: June 14, 2011Publication date: April 18, 2013Inventors: Bernard R. Neustadt, Hong Liu
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Publication number: 20130096144Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Incyte CorporationInventor: Incyte Corporation
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Patent number: 8420657Abstract: The invention relates to compounds of formula I and salts thereof wherein the substituens are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.Type: GrantFiled: February 5, 2009Date of Patent: April 16, 2013Assignee: Novartis AGInventors: Christoph Gaul, Marc Gerspacher, Philipp Holzer, Carole Pissot Soldermann
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Patent number: 8420629Abstract: The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.Type: GrantFiled: December 9, 2011Date of Patent: April 16, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard
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Patent number: 8415355Abstract: The present invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and pharmaceutical compositions thereof. The present invention also relates to use of the compounds of formula (I) in modulating the activity of protein kinases and in the treatment of disease, particularly a disease, disorder or syndrome associated with CDK 4 inhibition.Type: GrantFiled: August 21, 2009Date of Patent: April 9, 2013Assignees: Novartis AG, Astex Therapeutics Ltd.Inventors: Christopher Thomas Brain, Moo Je Sung, Bharat Lagu
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Patent number: 8415362Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines of Formula I: that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: June 12, 2008Date of Patent: April 9, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Stacey Shepard, Thomas P. Maduskuie, Haisheng Wang, Nikoo Falahatpisheh, Maria Rafalski, Argyrios G. Arvanitis, Louis Storace, Ravi Kumar Jalluri
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Patent number: 8410265Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: GrantFiled: January 14, 2010Date of Patent: April 2, 2013Assignee: Incyte CorporationInventors: Jiacheng Zhou, Pingli Liu, Qiyan Lin, Brian W. Metcalf, David Meloni, Yongchun Pan, Michael Xia, Mei Li, Tai-Yuen Yue, James D. Rodgers, Haisheng Wang
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Patent number: 8410089Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.Type: GrantFiled: February 17, 2010Date of Patent: April 2, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130079324Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Hengmiao Cheng, Theodore Otto Johnson, JR., John Charles Kath, Kevin Kun-Chin Liu, Elizabeth Ann Lunney, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken, Scott Channing Sutton
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Patent number: 8404683Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Publication number: 20130072492Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2011Publication date: March 21, 2013Inventors: Subharekha Raghavan, John E. Stelmach, Cameron J. Smith, Hong Li, Alan Whitehead, Sherman T. Waddell, Yi-Heng Chen, Shouwu Miao, Olga A. Ornoski, Joie Garfunkle, Xibin Liao, Jiang Chang, Xiaoqing Han, Jian Guo, Jonathan A. Groeper, Linda L. Brockunier, Keith Rosauer, Emma R. Parmee
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Publication number: 20130060026Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: September 6, 2012Publication date: March 7, 2013Applicant: INCYTE CORPORATIONInventors: Jiacheng Zhou, Yongzhong Wu, Pingli Liu, Ganfeng Cao
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Publication number: 20130053407Abstract: Pyrrolopyrimidones compounds of the formula (I), salts thereof, and pharmaceutical compositions containing them are disclosed herein, as well as methods for their use in medicine, for instance as activators of AMPK.Type: ApplicationFiled: May 3, 2011Publication date: February 28, 2013Applicant: GlaxoSmithKline LLCInventors: Olivier Mirguet, Anne Marie Jeanne Bouillot
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Patent number: 8383636Abstract: The present invention relates to compounds of the general formula (I) which are inhibitors of 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.Type: GrantFiled: September 7, 2007Date of Patent: February 26, 2013Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Keith Clinch, Gary Brian Evans, Richard Frohlich, Richard Hubert Furneaux, Peter Michael Kelly, Jennifer Mary Mason, Vern L. Schramm, Peter Charles Tyler, Shivall Ashwah Ashwin Gulab
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Publication number: 20130045963Abstract: The present invention provides cyclohexyl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: INCYTE CORPORATIONInventors: James D. Rodgers, Argyrios G. Arvanitis
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Patent number: 8377946Abstract: Disclosed herein are compounds of Formula (II) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: June 21, 2012Date of Patent: February 19, 2013Assignee: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury
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Publication number: 20130040949Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: December 29, 2010Publication date: February 14, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
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Publication number: 20130040973Abstract: Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicants: INCYTE CORPORATION, NOVARTIS PHARMA AGInventors: Alessandro M. Vannucchi, Costanza Bogani, Niccolo Bartalucci
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Patent number: 8372852Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: May 11, 2012Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Patent number: 8372854Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.Type: GrantFiled: December 10, 2010Date of Patent: February 12, 2013Assignee: Pfizer Inc.Inventors: Jin Xie, Michele Ann Promo, Eric Jon Jacobsen, Horng-Chih Huang, Todd M. Maddux
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Publication number: 20130035342Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently 0, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.Type: ApplicationFiled: December 16, 2010Publication date: February 7, 2013Applicant: NEUROPORE THERAPIES, INC.Inventors: Eliezer Masliah, Edward M. Rockenstein, Wolfgang Wrasidlo, Igor Flint Tsigelny
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Publication number: 20130035325Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.Type: ApplicationFiled: November 16, 2010Publication date: February 7, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
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Publication number: 20130029993Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: January 27, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Heinz Stadtmueller
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130029944Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: June 20, 2012Publication date: January 31, 2013Applicant: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
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Patent number: 8362245Abstract: Provided are processes for preparing intermediates of pemetrexed.Type: GrantFiled: June 30, 2011Date of Patent: January 29, 2013Assignee: Sicor Inc.Inventors: Nicola Diulgheroff, Moran Pirkes, Alessandro Pontiroli, Marco Zrinski Villa
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Publication number: 20130018034Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: June 19, 2012Publication date: January 17, 2013Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, David M. Burns, Jincong Zhuo
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8354532Abstract: This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: May 11, 2012Date of Patent: January 15, 2013Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Yung-hyo Koh, Stephanie Shaw, Hong Woo Kim, Zhi Hong
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Patent number: 8349848Abstract: The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: November 6, 2008Date of Patent: January 8, 2013Assignee: Dogwoof Pharmaceuticals, Inc.Inventors: Guoquan Wang, Robert D. Thompson
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Publication number: 20120329819Abstract: The present invention relates to a new polymorphic or crystalline form of Pemetrexed Disodium, processes for its preparation and its use, in particular for the preparation of medicaments.Type: ApplicationFiled: November 24, 2010Publication date: December 27, 2012Applicants: UNIVERSITY OF ZURICH, AZAD PHARMACEUTICAL INGREDIENTS AGInventors: Uwe Jens Albrecht, Hannes Helmboldt, Vsevold Valerievich Nikolaev
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Publication number: 20120330013Abstract: The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cyclopentenone with isopropylidene, regioselective cleavage of isopropylidene moiety, and synthesis of cyclic sulfate.Type: ApplicationFiled: March 20, 2012Publication date: December 27, 2012Applicant: Ewha University - Industry Collaboration FoundationInventors: Lak Shin JEONG, Hyuk Woo Lee
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Publication number: 20120322782Abstract: The present invention relates to veterinary compositions in a form of an orally deliverable tablet, and more particularly to a controlled-release composition that provides sufficiently long duration to permit once daily administration.Type: ApplicationFiled: February 15, 2011Publication date: December 20, 2012Inventors: Sunil Thomas Kumar Narishetty, Jeffrey Ellis Price, Sreenath Repakula
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Publication number: 20120316186Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. 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.Type: ApplicationFiled: February 23, 2012Publication date: December 13, 2012Inventors: Mark Ledeboer, David Messersmith, Francois Maltais, Huai Gao, Tiansheng Wang, Jingrong Cao, John Duffy, Gabriel Martinez-Botella, Cornelia Forster, Marion Wannamaker, Francesco Salituro, Albert Pierce, Luc Farmer, Valerie Marone
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Publication number: 20120316185Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: ApplicationFiled: January 31, 2011Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Publication number: 20120316166Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: January 10, 2011Publication date: December 13, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
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Patent number: 8329725Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: May 22, 2009Date of Patent: December 11, 2012Assignee: SanofiInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
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Publication number: 20120309776Abstract: The present invention provides pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: January 24, 2011Publication date: December 6, 2012Inventors: Ashley Fenwick, Timothy Allen Johnson, Graham M. Kyne
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Patent number: 8324382Abstract: Three new crystalline forms of pemetrexed diacid, preparation methods and uses thereof are disclosed. These preparation processes are simple and have better practicality.Type: GrantFiled: September 21, 2009Date of Patent: December 4, 2012Assignee: Chongqing Pharmaceutical Research Institute Co., Ltd.Inventors: Jie Luo, Meng Lin, Zhengyong Zhu, Junlai Luo, Wenrun Ye, Yongmei Qin, Jie Deng
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Patent number: 8324225Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.Type: GrantFiled: May 24, 2007Date of Patent: December 4, 2012Assignees: Novartis AG, Astex Therapeutics LimitedInventors: Christopher Thomas Brain, Moo Je Sung, Gebhard Thoma
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Publication number: 20120302567Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.Type: ApplicationFiled: January 28, 2011Publication date: November 29, 2012Applicants: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, HANMI PHARM. CO. LTD.Inventors: Seung Hyun Jung, Young Hee Jung, Wha Il Choi, Jung Beom Son, Eun Ju Jeon, In Ho Yang, Tae Hun Song, Mi Kyoung Lee, Myoung Sil Ko, Young Gil Ahn, Maeng Sup Kim, Young Jin Ham, Tae Bo Sim, Hwan Geun Choi, Jung Mi Han, Dong-sik Park, Hwan Kim
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Publication number: 20120295926Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: ApplicationFiled: July 26, 2012Publication date: November 22, 2012Inventors: Aleem Gangjee, Larry H. Matherly
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Publication number: 20120295925Abstract: This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier.Type: ApplicationFiled: September 1, 2010Publication date: November 22, 2012Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Roger D. Tung, Craig E. Masse
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Patent number: 8314234Abstract: The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.Type: GrantFiled: September 20, 2007Date of Patent: November 20, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Peter J. Connolly, Stuart Emanuel, Ronghui Lin, Yanhua Lu, Steven A. Middleton
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Patent number: 8314112Abstract: Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: January 9, 2009Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
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Publication number: 20120289501Abstract: The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.Type: ApplicationFiled: November 23, 2010Publication date: November 15, 2012Applicant: NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Andreas Floersheimer, Pascal Furet, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Andrea Vaupel
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Patent number: 8309716Abstract: This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.Type: GrantFiled: June 20, 2012Date of Patent: November 13, 2012Assignee: Pfizer Inc.Inventors: Sally Gut Ruggeri, Joel M Hawkins, Teresa M Makowski, Jennifer L Rutherford, Frank J Urban