Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/233.5)
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Publication number: 20090012081Abstract: An agent for promoting the proliferation or differentiation of a stem cell and/or neural progenitor cell, comprising a compound represented by Formula: wherein each of R1 and R2 is H, a hydrocarbon group or a heterocyclic group, or taken together with the adjacent carbon atom to form a ring, R3 is H, a hydrocarbon group or a heterocyclic group, W is a group represented by Formula: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R4 is an acyl group having an aliphatic hydrocarbon group, which is substituted by an aromatic group and may have a further substitutent, or aromatic group, R5 is H, C1-6 alkyl or acyl, R4c is an aromatic group, an aliphatic hydrocarbon group or acyl, and X is O or S; Y is O, S or NH, Ring C is an optionally substituted benzene ring, or a salt or prodrug thereof is provided.Type: ApplicationFiled: December 14, 2007Publication date: January 8, 2009Applicant: Takeda Pharmaceutical Company Ltd.Inventors: Shigenori Okawa, Masaomi Miyamoto, Masahiro Okura
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Publication number: 20090012083Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
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Publication number: 20090005375Abstract: The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors.Type: ApplicationFiled: March 21, 2008Publication date: January 1, 2009Inventors: Edcon Chang, Matthew H. McNeill
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Publication number: 20080318944Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: December 25, 2008Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
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Publication number: 20080318945Abstract: 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 piperazines, according to Formula I A compound of formula I wherein Z is bond or NH; R1 is aryl or optionally substituted heteroaryl; R2 is H, optionally substituted C1-6alkyl, or optionally substituted C2-6alkenyl; R3 and R7 are independently H, optionally substituted C1-6alkyl, or aryl; R4 is H or optionally substituted C1-6alkyl; R5 is H or C1-6alkyl; R6 is H or C1-6alkyl; and X and X? are independently O or H2; or wherein R3 and R4 together form a part of morpholinyl, piperadinyl, or aziridinyl ring; and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 15, 2006Publication date: December 25, 2008Inventors: Linda N. Casillas, Robert W. Marquis, JR.
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Patent number: 7456173Abstract: The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.Type: GrantFiled: October 26, 2006Date of Patent: November 25, 2008Assignee: Sepracor Inc.Inventors: Thomas P. Jerussi, Qun K. Fang
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Patent number: 7449460Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.Type: GrantFiled: February 16, 2005Date of Patent: November 11, 2008Assignee: WyethInventors: Dan Maarten Berger, Dennis William Powell, Biqi Wu
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Patent number: 7449461Abstract: The present invention relates to compounds of the general formula wherein R1 is cycloalkyl, substituted by OR or is 2-(7-oxa-bicyclo[2.2.1]hept-1-yl)-ethyl; R is hydrogen, lower alkyl or C(O)-lower alkyl; X is —CHR?—; and R? is hydrogen or lower alkyl; and pharmaceutically acceptable acid addition salts, optically pure enantiomeres, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.Type: GrantFiled: July 14, 2005Date of Patent: November 11, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Claus Riemer
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Publication number: 20080242664Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groType: ApplicationFiled: June 5, 2008Publication date: October 2, 2008Applicants: KUDOS PHARMACEUTICALS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Keith Allan Menear, Marc Geoffrey Hummersone, Laurent Jean Martin Rigoreau, Roger John Griffin, Bernard Thomas Golding, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Ian Robert Hardcastle, Kappusamy Saravanan
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Publication number: 20080207610Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.Type: ApplicationFiled: January 24, 2008Publication date: August 28, 2008Inventors: Jeff Zablocki, Matthew Abelman, Michael Organ, Yaroslav Bilokin, Robert Jiang, Elfatih Elzein, Tetsuya Kobayashi, Rao Kalla, Thao Perry, Xiaofen Li, Ivan Diamond, Lina Yao, Peidong Fan, Maria Pia Arolfo, Zhan Jiang
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Publication number: 20080206312Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.Type: ApplicationFiled: January 24, 2008Publication date: August 28, 2008Inventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
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Publication number: 20080199449Abstract: The invention includes methods and compositions for use in treating or preventing vascular disease or promoting vascular growth or development. The methods and compositions can be used, for example, in the treatment of diseases associated with ischemia, such as heart attack and stroke.Type: ApplicationFiled: August 11, 2006Publication date: August 21, 2008Applicant: The General Hospital CorporationInventors: Randall T. Peterson, Charles C. Hong
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Publication number: 20080188423Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: ApplicationFiled: December 21, 2007Publication date: August 7, 2008Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Publication number: 20080139547Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: February 7, 2008Publication date: June 12, 2008Applicant: PHARMACYCLICS, INC.Inventor: Martin SENDZIK
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Patent number: 7371749Abstract: The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with the N atom to which they are attached form a heterocyclic ring; R3 is hydrogen or lower alkyl; R4 is lower alkyl; hetaryl is 3H-imidazole-2,4-diyl or 1H-pyrazole-1,4-diyl; n is 1 or 2; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.Type: GrantFiled: July 18, 2005Date of Patent: May 13, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Claus Riemer
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Publication number: 20080108610Abstract: The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds, and especially their use as anti-infectives.Type: ApplicationFiled: December 13, 2005Publication date: May 8, 2008Applicant: Arpida AGInventors: Sorana Greiveldinger-Poenaru, Khalid Islam, Dieter Gillessen, Kaspar Burri
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Patent number: 7358244Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: May 27, 2004Date of Patent: April 15, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 7338949Abstract: The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R8 is oxo; or R7 and R8 taken together form the radical —CH?CH—N?; Z isType: GrantFiled: January 21, 2005Date of Patent: March 4, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier
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Patent number: 7304058Abstract: The present invention relates to a compound of formula I wherein R, X and n are defined hereinabove, and to a pharmaceutically acceptable salt thereof. The compound may be used for the treatment of diseases related to the A2A receptor.Type: GrantFiled: May 18, 2004Date of Patent: December 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7297692Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.Type: GrantFiled: August 3, 2006Date of Patent: November 20, 2007Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7285548Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are described herein, and their pharmaceutically acceptable salts thereof for the treatment of diseases, related to the A2A receptor.Type: GrantFiled: May 26, 2004Date of Patent: October 23, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7282497Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: March 17, 2006Date of Patent: October 16, 2007Assignee: Glaxo Group LimitedInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
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Patent number: 7256188Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity.Type: GrantFiled: May 8, 2002Date of Patent: August 14, 2007Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Patent number: 7247627Abstract: The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The invention further relates to pharmaceutical compositions of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide salts, and methods of treating disorders such as cancer using such compositions.Type: GrantFiled: September 30, 2004Date of Patent: July 24, 2007Assignee: Pharmacia & Upjohn CompanyInventors: Andrei Blasko, Qingwu Jin, Qun Lu, Michael A. Mauragis, Dian Song, Brenda S. Vonderwell
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7196082Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: October 14, 2003Date of Patent: March 27, 2007Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
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Patent number: 7189714Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and pharmaceutical compositions and methods of treatment utilising such compounds.Type: GrantFiled: October 31, 2001Date of Patent: March 13, 2007Assignee: Astrazeneca ABInventors: Marc Chapdelaine, Lucius Kemp, John McCauley
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Patent number: 7189715Abstract: The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.Type: GrantFiled: October 24, 2003Date of Patent: March 13, 2007Assignee: Sepracor Inc.Inventors: Thomas P. Jerussi, Qun K. Fang
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Patent number: 7186715Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: March 6, 2007Assignee: Eli Lilly and CompanyInventors: Karin Briner, Christopher William Doecke, Vincent Mancuso, Michael John Martinelli, Timothy Ivo Richardson, Roger Ryan Rothhaar, Qing Shi, Chaoyu Xie
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Patent number: 7169777Abstract: The present invention relates to melanocortin receptor agonist of the formula I useful in the treatment of obesity, diabetes, and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 30, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Ivan Collado Caño, Oscar De Frutos Garcia, Christopher William Doecke, Matthew Joseph Fisher, Cristina Garcia-Paredes, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Ana Isabel Mateo Herranz, Jeffrey Thomas Mullaney, Paul Leslie Ornstein, Zhipei Wu, Chaoyu Xie
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Patent number: 7157463Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunctionType: GrantFiled: January 23, 2002Date of Patent: January 2, 2007Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Karin Briner, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Chaoyu Xie
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Patent number: 7148252Abstract: This invention relates to methods for using benzopyranones, or their pharmaceutically acceptable salts, for treating or preventing a primary brain cancer or a brain metastasis. The benzopyranones have the formula: wherein R1, R2, R3, n and p are as defined herein.Type: GrantFiled: September 30, 2002Date of Patent: December 12, 2006Assignee: Signal Pharmaceuticals, LLCInventor: Jerome B. Zeldis
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Patent number: 7129240Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.Type: GrantFiled: April 29, 2004Date of Patent: October 31, 2006Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
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Patent number: 7101875Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: WyethInventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
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Patent number: 7091199Abstract: The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: September 13, 2000Date of Patent: August 15, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: George E. Lee, John G. Jurcak, Timothy A. Ayers
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Patent number: 7067516Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: December 12, 2001Date of Patent: June 27, 2006Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Martin James Harrison, Neil Jason Naylor, Christopher Neil Farthing, Bohdan Waszkowycz
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Patent number: 7064123Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: December 24, 2001Date of Patent: June 20, 2006Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.Inventors: Michael Graupe, John W. Patterson, Stephen D. Pickett, John O. Link, Jiayao Li, David Aldous, Sukanthini Thurairatnam, Andreas P. Timm, Frank Halley, Justine Lai Yeun Quai
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Patent number: 7041664Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.Type: GrantFiled: June 14, 2004Date of Patent: May 9, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, George Maynard, Alan Hutchison
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Patent number: 7030139Abstract: Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of painType: GrantFiled: April 18, 2002Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 7018986Abstract: The invention provides methods of using beta glucans to treat conditions associated with bone loss or low bone density as well as methods for promoting bone growth in situations where enhanced bone growth is desirable. In the invention methods beta glucans are administered so as to enhance the development of osteoblasts and the inhibition of the development and recruitment of osteoclasts. The inhibition of the recruitment and development of osteoclasts, coupled with the enhancement of osteoblast maturation by beta glucans leads to decreased bone resorption and increased bone formation, making beta glucans ideal agents for the treatment of osteoporosis and other bone resorption diseases.Type: GrantFiled: February 12, 2003Date of Patent: March 28, 2006Assignee: ImmudyneInventors: Nino Sorgente, Harald L. Guenther, Hannelore E. Guenther, Arun K. Bahl
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Patent number: 6903095Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N? or —CH?, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.Type: GrantFiled: September 9, 2003Date of Patent: June 7, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 6903094Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.Type: GrantFiled: May 10, 2002Date of Patent: June 7, 2005Assignee: Japan Tabacco, Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6861439Abstract: A method of treating a cerebrovascular disease, particularly stroke, is described. A method of treating a cerebrovascular disease includes administering pyridoxal-5?-phosphate, pyridoxal, pyridoxine, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, or pharmaceutical compositions thereof.Type: GrantFiled: September 24, 2002Date of Patent: March 1, 2005Assignee: Medicure International, Inc.Inventors: Wasimul Haque, Rajat Sethi
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Patent number: 6849622Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 6846817Abstract: The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, methods for preparing such a compound or salt, and methods for modulating (e.g. antagonizing or activating) nicotine receptors with such a compound or salt.Type: GrantFiled: November 30, 2001Date of Patent: January 25, 2005Assignee: Regents of the University of MinnesotaInventor: S. Mbua Ngale Efange
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Patent number: 6844336Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.Type: GrantFiled: March 15, 2001Date of Patent: January 18, 2005Assignee: Schering AGInventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier