Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
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Patent number: 7915267Abstract: The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. wherein each symbol is as defined in the specification.Type: GrantFiled: October 27, 2006Date of Patent: March 29, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroshi Nara, Akira Kaieda, Kenjiro Sato, Jun Terauchi
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Publication number: 20110070190Abstract: The invention discloses 1-N-substituted-6-(hetero)aryl-1H-thieno[3,2-d]pyrimidin-4-one derivatives of formula wherein R1, R2, R3 and R4 are as defined herein that inhibit Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: September 24, 2010Publication date: March 24, 2011Applicant: Roche Palo Alto LLCInventors: Chris Allen Broka, Robert Than Hendricks, Hans Maag, David Bernard Smith, Jutta Wanner
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Publication number: 20110065714Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Kim Hirst
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Publication number: 20110065690Abstract: The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Jolanta Grembecka, Tomasz Cierpicki, Jay Hess
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Patent number: 7906513Abstract: The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: April 26, 2007Date of Patent: March 15, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joel D. Moore, Eric L. Elliott, Yat Sun Or, Zhe Wang
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Publication number: 20110046163Abstract: Furanopyrimidine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20110046096Abstract: The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4?, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 16, 2008Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Christoph Hoenke, Peter Nickolaus, Rolf Goeggel, Thomas Fox, Dennis Fiegen, Klaus Klinder
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Publication number: 20110028496Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the treatment of pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, Alzheimer's disease, cognition impairment, memory decline, and schizophrenia, and depression.Type: ApplicationFiled: August 3, 2010Publication date: February 3, 2011Inventor: Daljit Singh Dhanoa
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Publication number: 20110028472Abstract: Novel thienopyrimidines of the formula (I), in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: March 23, 2009Publication date: February 3, 2011Applicant: MERCK PATENT CESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Guenter Hoelzemann, Hartmut Greiner, Christiane Amendt, Frank Zenke
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Publication number: 20110028441Abstract: The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2, but preferably SO, and either R3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 13, 2008Publication date: February 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Christoph Hoenke, Peter Nickolaus, Rolf Goeggel, Thomas Fox, Dennis Fiegen, Klaus Klinder
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Publication number: 20110009435Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.Type: ApplicationFiled: May 19, 2008Publication date: January 13, 2011Applicant: Pfizer, Inc.Inventors: Mark E. Schnute, Peter G. Ruminski, Cathleen E. Hanau, Joseph W. Stobach, Jeffery Carroll, Kirby Sample
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Publication number: 20110009366Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.Type: ApplicationFiled: April 23, 2010Publication date: January 13, 2011Applicant: AVEXA LIMITEDInventors: Eric Dale Jones, Jonathan Alan Victor Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherinie Macfarlane
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Publication number: 20110002886Abstract: The invention provides compounds of formula (I), as described herein, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula (I) are useful as anti-viral agents and/or as anti-cancer agents.Type: ApplicationFiled: May 8, 2008Publication date: January 6, 2011Applicant: BIOCRYST PHARMACEUTICALS, INC.Inventors: Yarlagadda S. Babu, Pooran Chand
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Patent number: 7863270Abstract: The invention relates to cyclic hydrazone compounds and compositions including the cyclic hydrazone compounds according to formula (I): The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: May 12, 2006Date of Patent: January 4, 2011Assignee: Synta Pharmaceuticals Corp.Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100331305Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Cuong Ly, Joseph P. Lyssikatos, Zhonghua Pei, Wendy Lee, Xianrui Zhao
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Publication number: 20100331348Abstract: Compounds of formula (I) wherein the substituents have the meanings assigned to them in claim 1, are useful as pesticides.Type: ApplicationFiled: July 10, 2008Publication date: December 30, 2010Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Patrice Selles, Eric Daniel Clarke, Alison Clare Elliot, Delphine Fawke, Ottmar Franz Hueter, Urs Mueller, Peter Renold, Sarah Targett, William Guy Whittingham
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Patent number: 7858635Abstract: The present invention relates to spiro compounds of formula XX as modulators of muscarinic receptors, wherein R1, R2, R3, Z1, Z2, L, G, n, m, t and p are defined herein. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: December 22, 2006Date of Patent: December 28, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Patent number: 7855194Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: March 15, 2007Date of Patent: December 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas Christ, Hans-Peter Maerki, Rainer Eugen Martin
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Publication number: 20100311966Abstract: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.Type: ApplicationFiled: December 26, 2008Publication date: December 9, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20100305102Abstract: The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 16, 2008Publication date: December 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Publication number: 20100298331Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. 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 compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: March 24, 2008Publication date: November 25, 2010Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Publication number: 20100286166Abstract: The present invention relates to the use of specific types of compounds acting as pharmacological chaperones having a stabilizing activity on the phenylalanine hydroxylase (PAH) enzyme for the prophylaxis and/or treatment of hyperphenylalaninemia (HPA) and phenylketonuria PKU) and diseases, disorders and conditions related thereto. Further, the present invention relates to pharmaceutical compositions containing the compounds according to the present invention as well as to methods of treatment of HPA, in particular, PKU and diseases, disorders and conditions related thereto.Type: ApplicationFiled: June 27, 2008Publication date: November 11, 2010Applicant: UNIVERSIDAD DE ZARAGOZAInventors: Ángel Pey Rodríguez, Aurora Martínez Ruiz, Javier Sancho Sanz, Nunilo Cremades Casasín, Adrián Velázquez Campoy, Ming Ying
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Publication number: 20100273815Abstract: The present invention discloses novel compounds of the Formula (1), containing thieno-[2,3-d]pyrimidin-4(3H)-one moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: ApplicationFiled: September 5, 2008Publication date: October 28, 2010Inventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmesher Prabhakar Sawargave, Sheerang Vidhyadhar Joshi, Sharangi Vaiude, Mohan Anand Chandavarkar
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Patent number: 7820631Abstract: A nucleoside analogue compound is provided which has a six-membered aromatic ring system, the aromatic ring system being substituted in the para position with an unbranched unsubstituted alkyl or alkoxy moiety, wherein the alkyl or alkoxy moiety, in total, has from 3 to 8 carbon atoms. This compound shows anti-vira1 activity, for example with respect to varicella zoster virus and can thus be used in therapeutic methods for the prophylaxis and treatment of viral infections such as varicella zoster virus.Type: GrantFiled: April 12, 2001Date of Patent: October 26, 2010Assignees: Rega Foundation, University College Cardiff Consultants LimitedInventors: Christopher McGuigan, Jan Balzarini
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Patent number: 7820658Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)_, —NRASO2- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: GrantFiled: August 26, 2004Date of Patent: October 26, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute Of Cancer ResearchInventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Publication number: 20100261736Abstract: The present application relates to novel substituted bicyclic heteroaryl compounds, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: June 3, 2008Publication date: October 14, 2010Inventors: Thomas Lampe, Raimund Kast, Hartmut Beck, Friederike Stoll, Eva-Maria Becker, Mario Jeske, Joachim Schuhmacher
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Publication number: 20100249114Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: February 25, 2010Publication date: September 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Henri DOODS, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Fabio PALEARI
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Publication number: 20100247517Abstract: The present invention relates to the use of modulators of the kinase activity of Mnk1 and/or Mnk2 the diagnosis, alleviation, treatment and/or prevention of a tauopathy. Particularly, the present invention relates to the use of a modulator of Mnk1 and/or Mnk2 kinase for the diagnosis, alleviation, treatment and/or prevention of Alzheimer's disease. Preferably, the compounds are condensed pyrimidines.Type: ApplicationFiled: November 21, 2008Publication date: September 30, 2010Applicant: Boehringer Ingelheim Internationational GmbHInventors: Matthias Austen, Marcus Geese, Martin Schneider
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Patent number: 7799795Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.Type: GrantFiled: June 26, 2006Date of Patent: September 21, 2010Assignee: Amgen Inc.Inventors: Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Julio C. Medina, Jeffrey T. Mihalic, George R. Tonn
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Publication number: 20100227873Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: ApplicationFiled: April 30, 2010Publication date: September 9, 2010Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brian A. McKittrick, Syliva J. Degrado
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Patent number: 7790750Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each indepenType: GrantFiled: October 20, 2006Date of Patent: September 7, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20100222352Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.Type: ApplicationFiled: September 25, 2006Publication date: September 2, 2010Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
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Publication number: 20100222342Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: December 28, 2005Publication date: September 2, 2010Inventors: Junhu Zhang, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
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Publication number: 20100222343Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: ApplicationFiled: January 8, 2010Publication date: September 2, 2010Inventors: Xiong Cai, Haixiao Zhai, Cheng-Jung Lai, Changgeng Qian
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Publication number: 20100222585Abstract: The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO2, preferably SO, and wherein RA, R1, R2, R3, R4 and R5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said pounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.Type: ApplicationFiled: October 15, 2008Publication date: September 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Rogelio Frutos, Dhileepkumar Krishnamurthy, Jason Alan Mulder, Sonia Rodriguez, Chris Hugh Senanayake, Thomas G. Tampone
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Publication number: 20100216789Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: ApplicationFiled: January 15, 2010Publication date: August 26, 2010Inventors: Dhanapalan NAGARATHNAM, Uday Khire, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Chunguang Wang, Barry Hart, Olaf Weber, Mark Lynch, Lei Zhang, Lei Wang
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Publication number: 20100216820Abstract: The current invention provides compounds of formula (1): wherein: one of Q1, Q2 and Q3 is S, and the other of two of Q1, Q2 and Q3 are —CR1—, which are inhibitors of PI3K-delta. These compounds are useful for treatment of conditions mediated by PI3K-delta, such as hematopoietic cancers, immune disorders, and bone resorption disorders. The invention further provides pharmaceutical compositions comprising a compound of formula (1) and methods of using these compounds and compositions to treat conditions mediated by PI3K-delta.Type: ApplicationFiled: November 13, 2007Publication date: August 26, 2010Inventors: Stephen L. White, Edward A. Kesicki, Eugene Thorsett, Fuqiang Ruan, Francine Farouz
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Patent number: 7776867Abstract: The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 29, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: John Laird Buchanan, William H. Buckner, Simon A. Burkitt, Erin F. DiMauro, Christopher N. Farthing, Alexander D. Frenkel, Martin J. Harrison, Frank Kayser, Jinqian Liu, Sarah E. Lively, Teresa L. Marshall, David C. McGowan, Rajiv Sharma, Stephen J. Shuttleworth, Xiaotian Zhu
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Patent number: 7776868Abstract: The present invention relates to novel compounds that are A2A adenosine receptor antagonists having the structure of Formula I and to their use in treating mammals for various disease states, such as obesity, CNS disorders, including the “movement disorders” (Parkinson's disease, Huntington's Chorea, and catelepsy), and cerebral ischemia, excitotoxicity, cognitive and physiological disorders, depression, ADHD, and drug addiction (alcohol, amphetamine, cannabinoids, cocaine, nicotine, and opioids) and to their use in the enhancement of immune response. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.Type: GrantFiled: November 29, 2007Date of Patent: August 17, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Tetsuya Kobayashi, Rao Kalla, Elfatih Elzein, Jeff Zablocki, Brent Blackburn
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Publication number: 20100204221Abstract: Compounds represented by Formula (I): are useful in treating diseases, such as cancer, that are mediated and/or associated (at least in part) with Axl kinase. The compounds can be formulated as pharmaceutically acceptable compositions for administration to a subject in need thereof.Type: ApplicationFiled: February 8, 2010Publication date: August 12, 2010Inventors: Hariprasad Vankayalapati, Xiao-Hui Liu, William Merton Hewitt, Eric Scott Gourley, Yong Xu, Bhasker Aavula
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Patent number: 7772247Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: July 28, 2005Date of Patent: August 10, 2010Assignee: Methylgene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Naomy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Llewellyn
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Publication number: 20100190746Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: November 20, 2009Publication date: July 29, 2010Applicant: ICAGEN, INC.Inventors: Grant A. McNaughton-Smith, James B. Thomas, JR., George S. Amato
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Patent number: 7763623Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.Type: GrantFiled: January 17, 2007Date of Patent: July 27, 2010Assignee: Schering CorporationInventors: Anandan Palani, Jun Qin, Dong Xiao, Ying R. Huang, Xiao Chen, Zhidan Liu, Sylvia J. Degrado, Robert G. Aslanian, Xianhai Huang
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Publication number: 20100179123Abstract: The present invention provides compounds having the formula: wherein R1, R2, X1, X2, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.Type: ApplicationFiled: October 8, 2009Publication date: July 15, 2010Applicant: Sunesis Pharmaceuticals, Inc.Inventors: Willard Lew, Subramanian Baskaran, Johan D. Oslob, Joshua C. Yoburn, Min Zhong
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Patent number: 7750015Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: GrantFiled: November 15, 2006Date of Patent: July 6, 2010Assignee: Schering CorporationInventors: Anandan Palani, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Jun Qin, Ying R. Huang, Robert G. Aslanian, Sylvia J. Degrado