Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
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Publication number: 20140315903Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventors: HASSAN JULIEN IMOGAI, JOSE MARIA CID-NUNEZ, JOSE IGNACIO ANDRES-GIL, ANDRES AVELINO TRABANCO-SUAREZ, JULEN OYARZABAL SANTAMARINA, FRANK MATTHIAS DAUTZENBERG, GREGOR JAMES MACDONALD, SHRILEY ELIZABETH PULLAN, ROBERT JOHANNES LUTJENS, GUILLAUME ALBERT JACQUES DUVEY, VANTHEA NHEM, TERRY PATRICK FINN, GAGIK MELIKYAN
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Publication number: 20140315913Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.Type: ApplicationFiled: March 11, 2014Publication date: October 23, 2014Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
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Publication number: 20140315917Abstract: 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 23, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Michael D. Kaufman, Thiwanka Samarakoon, Timothy Malcolm Caldwell, Lakshminarayana Vogeti, YuMi Ahn, William C. Patt, Karen M. Yates
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Publication number: 20140309225Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.Type: ApplicationFiled: June 27, 2014Publication date: October 16, 2014Applicant: FUJIFILM CorporationInventors: Hideyasu FUJIWARA, Shinsuke MIZUMOTO, Yohei KUBO, Hiyoku NAKATA, Shinji HAGIWARA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Tomoyuki MASHIKO, Mari YAMAMOTO
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Publication number: 20140309237Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Publication number: 20140309234Abstract: The present invention provides methods for treating fibrotic diseases by administering a compound having the general structural formula (I)Type: ApplicationFiled: March 10, 2014Publication date: October 16, 2014Applicant: ANGION BIOMEDICA CORPInventors: Lambertus J.W.M Oehlen, Bijoy Panicker, Latha Paka
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Patent number: 8859760Abstract: Described herein are methods and compositions for killing or preventing the growth of microbes. It has been discovered that a class of porphyrins can kill or prevent the growth of microbes. The porphyrins can be used in a number of different applications where microbes grow.Type: GrantFiled: December 12, 2013Date of Patent: October 14, 2014Assignee: Frontier Scientific, Inc.Inventors: Glenn Prestwich, Jerry C. Bommer, Charles Testa
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Patent number: 8859768Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 10, 2011Date of Patent: October 14, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
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Publication number: 20140303206Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (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: October 9, 2014Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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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: 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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Publication number: 20140296200Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
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Publication number: 20140296237Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: June 12, 2014Publication date: October 2, 2014Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
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Publication number: 20140296266Abstract: 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 2, 2014Inventors: Yunfeng Eric HU, John O. LINK, Qi LIU, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140296239Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
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Publication number: 20140296208Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: April 1, 2014Publication date: October 2, 2014Applicants: Topivert Pharma Limited, Respivert LimitedInventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
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Patent number: 8846931Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: GrantFiled: June 7, 2011Date of Patent: September 30, 2014Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
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Publication number: 20140288107Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20140288076Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Cheng Hu, Jeff Jin, Robert Keyes, Robert Kucejko, Xiaodong Lin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8841287Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: June 11, 2009Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20140275118Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Christine F. GELIN, Terry P. LEBOLD, Brock T. SHIREMAN
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Publication number: 20140274950Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: March 13, 2013Publication date: September 18, 2014Applicant: Medical University of South CarolinaInventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Publication number: 20140275057Abstract: The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.Type: ApplicationFiled: September 2, 2011Publication date: September 18, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
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Publication number: 20140275065Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
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Publication number: 20140275084Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
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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: 20140271591Abstract: This invention provides pharmaceutical compositions for the allosteric modulation of hemoglobin (S) and methods for their use in treating disorders mediated by hemoglobin (S) and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Global Blood Therapeutics, Inc.Inventors: Uma Sinha, Brian W. Metcalf, Donna Oksenberg
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Publication number: 20140275008Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Publication number: 20140275011Abstract: Disclosed are compound of Formula (Ia), wherein R2, R12, R16, J, Q, X, Y and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (Ia).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: AbbVie Inc.Inventors: Anthony Mastracchio, Milan Bruncko, Chunqiu Lai, Julie M. Miyashiro, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers
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Publication number: 20140283218Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.Type: ApplicationFiled: June 27, 2012Publication date: September 18, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
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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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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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Publication number: 20140249024Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.Type: ApplicationFiled: July 13, 2012Publication date: September 4, 2014Applicant: BASF SEInventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
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Publication number: 20140249185Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: ApplicationFiled: December 17, 2013Publication date: September 4, 2014Applicant: PURDUE PHARMA L.P.Inventors: QUN SUN, XIN WEN
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Publication number: 20140249135Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: May 9, 2014Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
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Publication number: 20140248347Abstract: The present invention relates to pharmaceutical compositions containing axitinib, which is known as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide or 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-E-[2-(pyridin-2-yl)ethenyl]indazole, or crystalline forms thereof, that protect axitinib from degradation, including photodegradation, as well as the therapeutic use of such compositions. The present invention also relates to novel photodegradants of axitinib.Type: ApplicationFiled: September 26, 2012Publication date: September 4, 2014Inventors: Daniel Scott Gierer, James Eric Morgado, Brendan John Murphy, Daryl Michael Simmons
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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: 20140249154Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.Type: ApplicationFiled: October 4, 2012Publication date: September 4, 2014Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
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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: 8822489Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.Type: GrantFiled: February 27, 2013Date of Patent: September 2, 2014Assignee: Acura PharmaceuticalsInventors: Vijai Kumar, David Dixon, Divya Tewari, Dilip B. Wadgaonkar
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Publication number: 20140243390Abstract: Novel RET fusion molecules and uses are disclosed.Type: ApplicationFiled: February 23, 2014Publication date: August 28, 2014Applicant: FOUNDATION MEDICINE, INC.Inventors: Sean R. Downing, Matthew J. Hawryluk, Doron Lipson, Alexander N. Parker, Philip James Stephens
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Publication number: 20140243331Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.Type: ApplicationFiled: May 7, 2014Publication date: August 28, 2014Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Dixon
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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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Publication number: 20140243339Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Amgen Inc.Inventors: Teresa L. Burgess, Angela Coxon, Isabelle Dussault, Paula Kaplan-Lefko, Anthony J. Polverino, Darrin Beaupre
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Metal-catalyzed copolymerization of imines and carbon monoxide as a route to synthesize polypeptides
Patent number: 8815913Abstract: Polypeptides of formula (I): wherein R1 and R2 are substituents independently selected from substituted and un-substituted alkyl groups and substituted and un-substituted aryl groups, and n is an integer greater than or equal to 2. Synthesis methods are also provided that do not use amino acids as starting materials, but instead employ imines and carbon monoxide as monomers that undergo transition metal-catalyzed alternating copolymerization to directly provide polypeptides using an acylcobalt catalyst with the following structural formula: wherein R is selected from the group consisting of alkyl, phenyl, and substituted phenyl groups.Type: GrantFiled: June 8, 2009Date of Patent: August 26, 2014Assignee: Nankai UniversityInventors: Huailin Sun, Jian Zhang, Qiuhua Liu, Lei Yu, Jiangyu Zhao -
Patent number: 8815915Abstract: The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: March 1, 2013Date of Patent: August 26, 2014Assignee: Allergan, Inc.Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20140235652Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: November 13, 2013Publication date: August 21, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Publication number: 20140235647Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
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Patent number: 8809372Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: GrantFiled: September 30, 2012Date of Patent: August 19, 2014Assignee: Asana Biosciences, LLCInventors: Roger Astbury Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Patent number: 8809371Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: GrantFiled: December 28, 2012Date of Patent: August 19, 2014Assignee: FUJIFILM CorporationInventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto