Piperidinyl Or Tetrahydropyridyl Patents (Class 514/266.22)
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Publication number: 20100323019Abstract: Microparticle-bioactive agent based treatments for local treatment of diseased tissues/organs are disclosed.Type: ApplicationFiled: August 19, 2010Publication date: December 23, 2010Applicant: Abbott Cardiovascular Systems Inc.Inventors: Florencia Lim, Mikael Trollsas, Michael Ngo, Thierry Glauser, Jinping Wan
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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: 20100317607Abstract: Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.Type: ApplicationFiled: June 24, 2008Publication date: December 16, 2010Applicant: INFECTIOUS DISEASE RESEARCH INSTITUTEInventors: Graham Michael Wynne, Olivier De Moor, Peter David Johnson, Richard John Vickers
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Patent number: 7851630Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 29, 2004Date of Patent: December 14, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Samuel David, Daniel Jasserand, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra
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Publication number: 20100305144Abstract: Prevention of recurrence of urethral stricture after a conventional treatment. Composition applicable to the prevention of recurrence of urethral stricture after a conventional treatment, including a pharmaceutically effective amount of halofuginone. Urethral stricture, a common disease, appears secondary to urethritis, urethral infection, urethral inflammation, urethral instrumentation, urethral catheterization, urethral trauma, urethral surgery and all types of urethral lesions. Conventional treatments by internal urethrotomy, urethral dilation or surgical urethroplasty are available and can cure urethral stricture, but with a relatively high rate of recurrence of the stricture. Halofuginone can prevent the recurrence of urethral stricture after a conventional treatment via internal urethrotomy, urethral dilation or surgical urethroplasty.Type: ApplicationFiled: October 23, 2008Publication date: December 2, 2010Applicant: WINDGAN TRADING LTDInventor: Mehdi Jaidane
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Publication number: 20100298289Abstract: The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 7, 2008Publication date: November 25, 2010Applicant: UCB PHARMA, S.A.Inventors: Gilles Raphy, Cecile Pegurier, Hans Meissner, Roland Knight, David Alan Owen
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Publication number: 20100298298Abstract: The invention relates to quinazolinedione derivatives, processes for the preparation thereof and their therapeutic applications.Type: ApplicationFiled: April 5, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTISInventors: Annie CLAUSS, Christophe GLAESS, Gilbert MARCINIAK, Nicolas MUZET, Jean-Francois NAVE, André SEYER, Bertrand VIVET
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Patent number: 7838530Abstract: The invention concerns quinazoline derivatives of Formula (I), wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: GrantFiled: September 22, 2004Date of Patent: November 23, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Publication number: 20100286111Abstract: The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.Type: ApplicationFiled: November 2, 2009Publication date: November 11, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Zhi-Liang Chu, James N. Leonard, Hussien A. Al-Shamma, Robert M. Jones
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Patent number: 7829566Abstract: Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: December 14, 2005Date of Patent: November 9, 2010Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaeger, Richard Soll
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Patent number: 7829573Abstract: The invention concerns the use of a combination of an anti-angiogenic agent and an anti-hypertensive agent for use in the manufacture of a medicament for the treatment of a disease state associated with angiogenesis in a warm-blooded mammal, such as a human being. The invention also relates to pharmaceutical compositions comprising an anti-angiogenic agent and an anti-hypertensive agent, to kits thereof and to a method of treatment of a disease state associated with angiogenesis which comprises the administration of an effective amount of a combination of an anti-angiogenic agent and an anti-hypertensive agent to a warm-blooded animal, such as a human being.Type: GrantFiled: April 2, 2001Date of Patent: November 9, 2010Assignee: AstraZeneca ABInventors: Jon Owen Curwen, Donald James Ogilvie
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Publication number: 20100273778Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a histamine H3 receptor antagonist, described herein, a salt thereof, or a composition comprising such compound or salt.Type: ApplicationFiled: April 26, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Gin C. Hsieh, Jorge D. Brioni, James P. Sullivan
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Publication number: 20100267678Abstract: The present invention is drawn to adhesive solidifying formulations, methods of drug delivery, and solidified layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can include a volatile solvent system comprising at least one volatile solvent, and a non-volatile solvent system comprising at least one non-volatile solvent, wherein at least one non-volatile solvent is a flux-enabling non-volatile solvent(s) capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.Type: ApplicationFiled: April 16, 2010Publication date: October 21, 2010Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
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Publication number: 20100256120Abstract: The invention concerns a compound of the Formula I wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is, (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: August 7, 2006Publication date: October 7, 2010Inventors: Dearg Sutherland Brown, Ian Alun Nash, Steve Swallow
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Publication number: 20100249100Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 29, 2010Publication date: September 30, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Publication number: 20100249146Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: November 10, 2008Publication date: September 30, 2010Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asia
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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: 20100240649Abstract: A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).Type: ApplicationFiled: May 26, 2010Publication date: September 23, 2010Inventor: Hesheng ZHANG
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Publication number: 20100215773Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with a platinum anti-tumour agent; to a pharmaceutical composition comprising ZD6474 and a platinum anti-tumour agent; to a combination product comprising ZD6474 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and a platinum anti-tumour agent; to the use of ZD6474 and a platinum anti-tumour agent in the manufacture of a medicament for use in the production of all antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.Type: ApplicationFiled: November 24, 2009Publication date: August 26, 2010Applicant: AstraZeneca ABInventors: Stephen Robert Wedge, Anderson Joseph Ryan
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Publication number: 20100204227Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 12, 2010Inventors: George W. MULLER, Alexander L. Ruchelman
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Publication number: 20100204226Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: February 10, 2010Publication date: August 12, 2010Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, JR., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Patent number: 7772244Abstract: The present invention relates to compounds of Formula (I) as 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: March 28, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, Xiaojun Han, Gene M. Dubowchik, John E. Macor, Stephen E. Mercer
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Publication number: 20100179176Abstract: The present invention relates to a V3 antagonist for use in the treatment of chronic pain, in particular neuropathic pain.Type: ApplicationFiled: December 13, 2007Publication date: July 15, 2010Inventor: Inga Neumann
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Publication number: 20100179152Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.Type: ApplicationFiled: January 4, 2010Publication date: July 15, 2010Applicant: NYCOMED GmbHInventors: Torsten Dunkern, Christian Schudt, Friedrich Grimminger, Hossein Ardeschir Ghofrani, Manfred Kaps, Bernhard Rosengarten
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Publication number: 20100179144Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.Type: ApplicationFiled: June 12, 2008Publication date: July 15, 2010Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Steven David Knight, Kenneth Allen Newlander, Lance H. Ridgers, Stanley J. Schmidt
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Patent number: 7750041Abstract: The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water ?0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.Type: GrantFiled: December 20, 2001Date of Patent: July 6, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Speck, Brunn Scheller
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Publication number: 20100166765Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R2, R3, R4, Q, X and Y are as defined in the specification, is useful in the treatment of bone conditions related to increased calcium depletion or resorption.Type: ApplicationFiled: August 14, 2006Publication date: July 1, 2010Inventors: Sandra Ammon, Rene Beerli, Leo Widler
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Publication number: 20100168143Abstract: The invention provided a compound of formula (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.Type: ApplicationFiled: January 17, 2007Publication date: July 1, 2010Applicant: ASTRAZENECA ABInventor: Michael Kevin Foote
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Publication number: 20100160316Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 1, 2010Publication date: June 24, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus E. Gonzalez, III, Dean M. Wilson, Andreas P. Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin J. Petzoldt, Lev Tyler Dewey Fanning, Timothy D. Neubert, Roger D. Tung, Esther Martinborough, Nicole Zimmerman
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Publication number: 20100152169Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: February 25, 2010Publication date: June 17, 2010Applicant: ASTRAZENECA ABInventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
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Publication number: 20100152176Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: February 22, 2010Publication date: June 17, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Dennis J. Hurley, Gabriel Raffai
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Publication number: 20100152171Abstract: CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.Type: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS
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Publication number: 20100144731Abstract: Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.Type: ApplicationFiled: September 3, 2009Publication date: June 10, 2010Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
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Publication number: 20100144766Abstract: A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy; and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl; and n is either 1 or 2; and pharmaceutically acceptable salts thereof; for use in treatment of or prevention of skeletal muscle fibrosis and/or for inducing skeletal muscle regeneration.Type: ApplicationFiled: January 21, 2008Publication date: June 10, 2010Inventors: Mark Pines, Arnon Nagler
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Publication number: 20100143459Abstract: A pharmaceutical dosage form comprises a solid dispersion product of at least one tyrosine kinase inhibitor, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer.Type: ApplicationFiled: November 8, 2007Publication date: June 10, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Bernd Liepold, Jörg Rosenberg, Martin Knobloch, Christian Nehen
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Publication number: 20100137297Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: May 12, 2008Publication date: June 3, 2010Inventors: Joan M. Fletcher, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Publication number: 20100130520Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises one of: the administration of ZD6474 in combination with 5-FU; the administration of ZD6474 in combination with CPT-11; and the administration of ZD6474 in combination with 5-FU and CPT-11; to a pharmaceutical composition comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to a combination product comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, for use in a method of treatment of a human or animal body by therapy; to a kit comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to the use of one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, iType: ApplicationFiled: July 13, 2009Publication date: May 27, 2010Inventors: Stephen Robert WEDGE, Anderson Joseph Ryan
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Publication number: 20100125078Abstract: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: November 9, 2009Publication date: May 20, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Patent number: 7718658Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 31, 2005Date of Patent: May 18, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Patent number: 7713984Abstract: The invention relates to the pharmaceutical use of specific substance P antagonists, in particular 1-acylpiperidine substance P antagonists, especially N-benzoyl-2-benzyl-4-(azanaphthoyl-amino)-piperidines, e.g. of formula wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and pharmaceutically acceptable salts thereof for treatment of chronic fatigue syndrome (CFS) in the absence of serotonin agonist/selective serotonin reuptake inhibitory therapy, or for the treatment of fibromyalgia or associated functional symptoms.Type: GrantFiled: January 14, 2008Date of Patent: May 11, 2010Assignees: Novartis AGInventors: Lothar Färber, Wolfgang Mueller, Thomas Stratz
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Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
Publication number: 20100113411Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as 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 preparing them.Type: ApplicationFiled: August 6, 2009Publication date: May 6, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS -
Patent number: 7705005Abstract: The invention disclosed herein relates to compounds of formula (I) where the various groups are defined herein, and which are useful for treating inflammatory diseases such as atherosclerosis.Type: GrantFiled: January 25, 2007Date of Patent: April 27, 2010Assignee: Glaxo Group LimitedInventor: Colin Andrew Leach
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Publication number: 20100099658Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.Type: ApplicationFiled: July 4, 2008Publication date: April 22, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Yutaka Kondoh, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
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Publication number: 20100099651Abstract: The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK1 antagonists, anticholinergics and endothelin antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.Type: ApplicationFiled: October 23, 2007Publication date: April 22, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Birgit Jung, Frank Himmelsbach, Gerald Pohl
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Publication number: 20100093774Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: December 11, 2009Publication date: April 15, 2010Inventors: George W. MULLER, Hon-Wah MAN
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Publication number: 20100092490Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.Type: ApplicationFiled: August 2, 2006Publication date: April 15, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Toshimitsu Uenaka, Yuji Yamamoto, Junji Matsui
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Patent number: 7687502Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 23, 2005Date of Patent: March 30, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Morihiro Mitsuya, Makoto Bamba, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki, Keisuke Arakawa
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Publication number: 20100075916Abstract: The present invention relates to new substituted quinazoline inhibitors of vascular endothelial growth factor receptor tyrosine kinase, epidermal growth factor receptor tyrosine kinase, and/or REarranged during Transfection tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 4, 2009Publication date: March 25, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar, Manouchehr M. Shahbaz
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Publication number: 20100069414Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
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Publication number: 20100069412Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: ApplicationFiled: April 28, 2009Publication date: March 18, 2010Applicant: ASTRAZENECA ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri JUNG, Georges Rene PASQUET