1,4-diazine Ring Patents (Class 544/120)
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Publication number: 20110144084Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.Type: ApplicationFiled: August 4, 2009Publication date: June 16, 2011Applicant: PFIZER INCInventors: John Frederick Braganza, Michael Raymond Collins, John Charles Kath, Sacha Ninkovic, Hui Li, Daniel Tyler Richter
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Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 7947830Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 23, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Sven Franciscus Anna Van Brandt, Kristof Van Emelen, Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Janine Arts
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Publication number: 20110118233Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: May 6, 2009Publication date: May 19, 2011Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110082142Abstract: A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Inventors: MICHELLE LEANNE STYLES, JUN ZENG, HERBERT RUDOLF TREUTLEIN, ANDREW FREDERICK WILKS, MARCEL ROBERT KLING, XIANYONG BU, CHRISTOPHER JOHN BURNS
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Publication number: 20110034454Abstract: A compound of formula (I) or a salt, ester or prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.Type: ApplicationFiled: January 8, 2007Publication date: February 10, 2011Inventors: Allan Paul Dishington, Shaun Michael Fillery, Maurice Raymond Verschoyle Finlay, Kurt Gordon Pike
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Patent number: 7879838Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: February 14, 2006Date of Patent: February 1, 2011Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Qingbei Zeng, De-Yi Yang, Stuart B. Rosenblum, Michael K. C. Wong, Gopinadhan N. Anilkumar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Lisa Guise Zawacki, Doublas W. Hobbs
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Publication number: 20110021520Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: ApplicationFiled: July 23, 2010Publication date: January 27, 2011Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LUEOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Publication number: 20100331328Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: February 19, 2009Publication date: December 30, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Michael Cherry
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Publication number: 20100311730Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisi?q radiation.Type: ApplicationFiled: October 6, 2008Publication date: December 9, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Patent number: 7834007Abstract: The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: August 23, 2006Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Han, Prasad V. Chaturvedula
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Publication number: 20100273757Abstract: The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.Type: ApplicationFiled: June 4, 2010Publication date: October 28, 2010Inventors: Bernat Vidal Juan, Cristina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
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Publication number: 20100249405Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:Type: ApplicationFiled: December 7, 2007Publication date: September 30, 2010Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20100240648Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.Type: ApplicationFiled: June 2, 2010Publication date: September 23, 2010Inventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
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Publication number: 20100222318Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: December 18, 2009Publication date: September 2, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
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Publication number: 20100210627Abstract: The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.Type: ApplicationFiled: August 15, 2007Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Wang Mao, Tina Marie Morwick, Anthony S. Prokopowicz, III
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Publication number: 20100190766Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Publication number: 20100173909Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 10, 2009Publication date: July 8, 2010Applicant: ASTRAZENECA ABInventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
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Publication number: 20100168108Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.Type: ApplicationFiled: January 18, 2010Publication date: July 1, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
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Publication number: 20100160280Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: December 16, 2009Publication date: June 24, 2010Applicant: AMGEN INC.Inventors: Jennifer R. Allen, Ning Chen, James R. Falsey, Michael Frohn, Paul Harrington, Essa Hu, Matthew R. Kaller, Roxanne Kunz, Stephanie J. Mercede, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Aaron C. Siegmund, Christopher M. Tegley, Guomin Yao
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Publication number: 20100160292Abstract: Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.Type: ApplicationFiled: September 11, 2007Publication date: June 24, 2010Applicant: CGI PHARMACEUTICALS, INCInventors: James A. Whitney, Julie Di Paolo, Mark Velleca, David R. Brittelli, Kevin S. Currie, James W. Darrow, Jeffrey E. Krope, Seung H. Lee, Steven L. Gallion, Scott A. Mitchell, Doughlas A.I. Pippen, Peter A. Blomgren, Doughlas Gregory Stafford
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Publication number: 20100152178Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.Type: ApplicationFiled: September 5, 2007Publication date: June 17, 2010Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
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Patent number: 7737143Abstract: A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating kinase-associated disease states using the compound of formula (I) is also described.Type: GrantFiled: December 3, 2004Date of Patent: June 15, 2010Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Xianyong Bu
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Publication number: 20100137278Abstract: Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 16, 2009Publication date: June 3, 2010Applicant: AMGEN INC.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Patent number: 7727985Abstract: This invention provides beta-carboline compounds of formula I: wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.Type: GrantFiled: April 9, 2004Date of Patent: June 1, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Publication number: 20100130447Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: November 15, 2007Publication date: May 27, 2010Inventors: Christopher John Burns, Michael Francis Harte, James T. Palmer
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Publication number: 20100105899Abstract: This invention is directed to the general method of transforming non-photoactive bioactive small molecule compounds of known structure and function into photoactive analogs of the small molecules which exhibit both photoactivity and the original biological targeting activity. The general method for the design of the photoactive analogs of the small molecules includes: (a) selecting a desired bioactive molecule; (b) identifying the region of the molecule that contains an aromatic or a heteroaromatic motif; and (c) either replacing said motif with a photoactive functional group of similar size, or modifying said motif to make it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof.Type: ApplicationFiled: February 26, 2008Publication date: April 29, 2010Inventors: William L. Neumann, Raghavan Rajagopalan, Dennis A. Moore, Richard B. Dorshow
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Publication number: 20100093703Abstract: The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Ruediger Streicher, Matthias Eckhardt, Annette Schuler-Metz, Alexander Pautsch, Corinna Schoelch
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Patent number: 7696202Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: November 10, 2005Date of Patent: April 13, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
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Publication number: 20100081658Abstract: Compounds having the formula I wherein R1, R2a, R2b, R2c, R3, Y and p are as defined herein and C2-C3 is a single or double bond are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: September 25, 2009Publication date: April 1, 2010Inventors: Elbert Chin, Jim Li, Francisco Xavier Talamas, Beihan Wang
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Publication number: 20100069388Abstract: A compound having the following formula (I): wherein —R1 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with —OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.Type: ApplicationFiled: December 14, 2007Publication date: March 18, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Yoshikazu Inoue, Yoshiteru Eikyu, Fumiyuki Shirai
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Publication number: 20100056509Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: October 20, 2009Publication date: March 4, 2010Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20100004231Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: ApplicationFiled: July 1, 2009Publication date: January 7, 2010Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
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Publication number: 20090306076Abstract: The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin 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 prokineticin receptors are involved.Type: ApplicationFiled: December 4, 2006Publication date: December 10, 2009Inventors: Wayne J. Thompson, Jeffrey Y. Melamed
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Publication number: 20090281099Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: May 21, 2007Publication date: November 12, 2009Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernàndez, Juan Antonio Vega Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Drinkenburg
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Patent number: 7615550Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.Type: GrantFiled: October 14, 2003Date of Patent: November 10, 2009Assignee: Glaxo Group LimitedInventors: Thomas Daniel Heightman, Simon Teanby Hodgson, Matthew J Lindon, David Matthew Wilson
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Publication number: 20090239847Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.Type: ApplicationFiled: March 4, 2009Publication date: September 24, 2009Inventors: Ian BRUCE, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM
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Publication number: 20090233907Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.Type: ApplicationFiled: March 20, 2007Publication date: September 17, 2009Applicant: ASTRAZENECA ABInventors: Rupert Austin, Roger Victor Bonnert, Simon Fraser Hunt, Grigorios Nikitidis, Hitesh Jayantilal Sanganee, Peter Olof Sjo, Dan Warner
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Publication number: 20090198053Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas (I) and (II) below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.Type: ApplicationFiled: June 20, 2007Publication date: August 6, 2009Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
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Publication number: 20090143357Abstract: Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.Type: ApplicationFiled: March 29, 2006Publication date: June 4, 2009Applicant: ICOS CORPORATIONInventors: Frank Diaz, Francine S. Farouz, Ryan Coatsworth Holcomb, Edward A. Kesicki, Hua Chee Ooi, Alexander Rudolph, Frank Stappenbeck, Eugene D. Thorsett, John Joseph Gaudino, Kimba Lee Fischer, Adam Wade Cook
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Publication number: 20090124619Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted morpholines and piperidines, according to Formula I wherein: X is O or CH2; R1 is optionally substituted C3-7cycloalkyl, C3-6cycloalkyl-C0-6alkyl, optionally substituted C4-7cycloalkenyl, optionally substituted Het-C0-7alkyl, optionally substituted Het-C0-7alkenyl, optionally substituted aryl, optionally substituted heterocycloalkyl, or optionally substituted heteroaryl; R2 is H, branched or optionally substituted C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar—C0-6alkyl, or Het-C0-6alkyl; and R3 is optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; or pharmaceutically acceptable salts, hydrates, solvates and physiologically functional derivatives thereof.Type: ApplicationFiled: March 31, 2006Publication date: May 14, 2009Inventor: Maria CICHY-KNIGHT
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Publication number: 20090111801Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: April 19, 2007Publication date: April 30, 2009Applicant: Janssen Pharmaceutica N.V.Inventors: Jose Ignacio Andres-Gil, Manuel Jesus Alcazar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernandez, Juan Antonio Vega Ramiro, Francisca Delgado-Jimenez, Wilhelmus Helena Ignatius Maria Drinkenburg
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Publication number: 20090105210Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 18, 2006Publication date: April 23, 2009Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
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Publication number: 20090082330Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Inventors: Peter A. BLOMGREN, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
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Publication number: 20090029977Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: July 18, 2008Publication date: January 29, 2009Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20090022688Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.Type: ApplicationFiled: July 8, 2008Publication date: January 22, 2009Inventors: Luc J. Farmer, Robert B. Perni, Govinda Rao Bhisetti, Keith P. Wilson