1,2-oxazoles (including Hydrogenated) Patents (Class 546/272.1)
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Publication number: 20090048306Abstract: The present invention relates to compounds of the formula (I): and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: ApplicationFiled: May 2, 2008Publication date: February 19, 2009Applicant: Pfizer, Inc.Inventors: Sharanjeet Kaur Bagal, Karl Richard Gibson, Mark Ian Kemp, Cedric Poinsard, Blanda Luzia Christa Stammen, Stephen Martin Denton, Melanie Susanne Glossop
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Publication number: 20090042945Abstract: The present invention relates to substituted benzo[d]isoxazol-3-yl-amine compounds, methods for their production, medicaments containing these compounds and the use of these compounds to produce medicaments.Type: ApplicationFiled: May 18, 2006Publication date: February 12, 2009Applicant: Gruenenthal GmbHInventors: Robert Frank, Beatrix Merla, Melanie Reich, Ruth Jostock
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Publication number: 20090042726Abstract: Compounds of formula I: wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.Type: ApplicationFiled: November 21, 2006Publication date: February 12, 2009Applicant: SYNGENTA LIMITEDInventors: Janice Black, Jutta Elisabeth Boehmer, Ewan James Turner Chrystal, Anthony Marian Kozakiewicz, Andrew Plant
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Patent number: 7488824Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.Type: GrantFiled: March 5, 2004Date of Patent: February 10, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: David Anthony Jackson, Martin Charles Bowden
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Publication number: 20090036450Abstract: The pyrazole compound of the present invention is represented by the following general formula (I). The pyrazole compound of the present invention or a salt thereof or a solvate thereof potently inhibits liver glycogen phosphorylase, and, therefore, is useful as a therapeutic or prophylactic agent for diabetes. wherein each symbol denotes as described in the specifications.Type: ApplicationFiled: November 20, 2007Publication date: February 5, 2009Applicant: JAPAN TOBACCO, INC.Inventors: Masaki Takagi, Takeshi Nakamura, Isamu Matsuda, Toshihiro Kiguchi, Naoki Ogawa, Hidekazu Ozeki
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Publication number: 20090018160Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof wherein the heterocycle comprises two double bonds which may be present at several positions, and which are represented by the dashed lines (---); the heterocycle contains two heteroatoms, W is N or NH; Y is CH, O or NH, wherein if Y is O, X1 is CH and X2 is C-Z-R2 or C—R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, wherein if X1 is CH or N, X2 is C-Z-R2 or C—R3, and if X2 is CH or N, X1 is C-Z-R2 or C—R3, wherein Z is NH or S; R1 is chosen from structures (a), (b) and (c): R2 is chosen from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally sType: ApplicationFiled: April 23, 2008Publication date: January 15, 2009Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
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Patent number: 7476684Abstract: The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.Type: GrantFiled: September 20, 2006Date of Patent: January 13, 2009Assignee: AstraZeneca ABInventors: Alexander Minidis, David Wensbo, Methvin Isaac, Abdelmalik Slassi, Jalaj Arora, Tao Xin, Louise Edwards, Caroline Eriksson, Veronica Profir, Per-Olov Bergstrom
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Patent number: 7476683Abstract: The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: GrantFiled: July 31, 2003Date of Patent: January 13, 2009Assignee: Merck Patent GmbHInventors: Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell
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Publication number: 20090005370Abstract: The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.Type: ApplicationFiled: June 16, 2008Publication date: January 1, 2009Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
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Patent number: 7456200Abstract: The present invention relates to new compounds of formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing compounds of the formula I and to the use of compounds of the formula I in therapy.Type: GrantFiled: November 14, 2005Date of Patent: November 25, 2008Assignee: Astrazeneca ABInventors: Jalaj Arora, Louise Edwards, Methvin Isaac, Donald A. McLeod, Abdelmalik Slassi, Tomislav Stefanac, Thomas M. Stormann, David Wensbo, Tao Xin, Helena Gyback, Martin Johansson, Annika Kers, John Malmberg, Alexander Minidis, Karin Oscarsson, Mangus Waldman, Ulrika Yngve, Christoffer Osterwall
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Publication number: 20080274891Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: May 23, 2008Publication date: November 6, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
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Patent number: 7446199Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: September 7, 2004Date of Patent: November 4, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Pan Li, Ronald C. Tomlinson
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Publication number: 20080269267Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof aType: ApplicationFiled: April 18, 2008Publication date: October 30, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20080262028Abstract: The present invention is directed to a compound of formula I: or any stereoisomeric form of the compound of the formula I or a mixture of these forms in any ratio or a physiologically acceptable salt of the compound of the formula I which inhibit the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor), and to a process for their preparation and to their use to treat described diseases where the substituents are as described in the specification.Type: ApplicationFiled: April 14, 2008Publication date: October 23, 2008Applicant: SANOFI-AVENTISInventors: Christopher KALLUS, Holger HEITSCH, Volkmar WEHNER
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Publication number: 20080255155Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds, compositions and methods for the inhibition of kinase activity. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: October 18, 2007Publication date: October 16, 2008Inventors: Stephane Raeppel, Oscar Saavedra, Stephen Claridge, Arkadii Vaisburg, Frederic Gaudette, Ljubomir Isakovic, Robert Deziel
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Publication number: 20080233102Abstract: Administering an effective dose of a tTGase inhibitor to a Celiac or dermatitis herpetiformis patient reduces the toxic effects of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.Type: ApplicationFiled: November 12, 2004Publication date: September 25, 2008Inventors: Chaitan Khosla, Kihang Choi
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Publication number: 20080227824Abstract: The present invention is directed to novel compounds of formula (I)/(II)/(III), their use in therapy and pharmaceutical compositions comprising said novel compounds.Type: ApplicationFiled: September 20, 2006Publication date: September 18, 2008Applicant: Astrazeneca ABInventors: Alexander Minidis, David Wensbo, Abdelmalik Slassi, Methvin Isaac, Caroline Ericsson, Veronica Profir, Per-Olov Bergstrom, Louise Edwards, Jalaj Arora, Tao Xin
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Publication number: 20080214623Abstract: The present invention relates to a novel compound, processes for its preparation, compositions comprising the same and its use in the treatment of condition or diseases mediated by p38 kinase activity.Type: ApplicationFiled: June 16, 2006Publication date: September 4, 2008Inventors: Amrik Chandi, Trevor Raymond Keel, Vipulkumar Kantibhai Patel, Ann Louise Walker
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Patent number: 7414061Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: December 18, 2006Date of Patent: August 19, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Bo Han, Henner Knust, Andrew Thomas
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Publication number: 20080194586Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dylipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.Type: ApplicationFiled: March 3, 2006Publication date: August 14, 2008Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
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Publication number: 20080171754Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: December 19, 2007Publication date: July 17, 2008Applicant: Millennium Pharmaceuticals, Inc.Inventors: Ruth S. Adams, Matthew Duffey, Alexandra E. Gould, Paul D. Greenspan, Bheemashankar A. Kulkarni, Tricia J. Vos
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Publication number: 20080167350Abstract: The present invention provides compounds of formula I: along with methods of making the same, compositions thereof, and methods of use thereof, particularly methods of use as fungicides.Type: ApplicationFiled: March 3, 2008Publication date: July 10, 2008Applicant: SYNGENTA LIMITEDInventors: Shy-Fuh Lee, Micah Gliedt
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Publication number: 20080153838Abstract: The invention relates to a compound of the Formula I. or salt, prodrug or solvate thereof, wherein R1, R5, R6, D, A, B, L, n, m and p are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: February 2, 2006Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard Williams Arthur Luke, William McCoull
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080139561Abstract: This invention relates to novel compounds having the Formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: February 1, 2006Publication date: June 12, 2008Applicant: ASTRAZENECA ABInventors: Audrey Davies, Michelle Lamb, Paul Lyne, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
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Publication number: 20080132551Abstract: The invention provides compounds of Formula I: wherein A, B, and X are described herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which ?7 nAChR is known to be involved.Type: ApplicationFiled: March 24, 2004Publication date: June 5, 2008Inventors: Bruce Nelsen Rogers, David Walter Piotrowski, Brandon J. Margolis, Jason K. Myers, Vincent Edward Groppi, Daniel G. Rudmann
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Publication number: 20080132706Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: ApplicationFiled: June 18, 2007Publication date: June 5, 2008Applicant: AVENTIS PHARMA LIMITEDInventors: Garry FENTON, Tahir Nadeem MAJID, Malcolm Norman PALFREYMAN
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Patent number: 7381687Abstract: 3-Heteroaryl-substituted isoxazolines of the formula I where: X is substituted 5-membered heteroaryl having one to four nitrogen atoms or one to three nitrogen atoms and one oxygen or sulfur atom or one oxygen or sulfur atom; or substituted 6-membered heteroaryl having one to four nitrogen atoms; where the abovementioned 5-membered heteroaryl is not pyrazolyl or thienyl; R1-R7 are hydrogen, alkyl or haloalkyl; Y is unsubstituted or substituted aryl, or benzo[1,4]dioxonyl, benzo[1,3]dioxolanyl, 2,3-dihydrobenzofuranyl or benzimidazole; or unsubstituted or substituted 5- to 6-membered heteroaryl; and their agriculturally useful salts, processes and intermediates for their preparation, and the use of these compounds or of the compositions comprising these compounds for controlling unwanted plants are described.Type: GrantFiled: April 23, 2003Date of Patent: June 3, 2008Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Michael Rack, Matthias Witschel, Cyrill Zagar, Andreas Landes
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Publication number: 20080113988Abstract: The present invention relates to novel isoxazoline-indole derivatives according to 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, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.Type: ApplicationFiled: November 25, 2005Publication date: May 15, 2008Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jose Ignacio Andres-Gil, Jose Manuel Bartolome-Nebreda, Manuel Jesus Alcazar-Vaca, Maria de las Mercedes Garcia-Martin, Antonius Adrianus Hendrikus Petrus Megens
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Patent number: 7354919Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: July 24, 2003Date of Patent: April 8, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao
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Publication number: 20080064689Abstract: Compounds of the formula (I): or a pharmaceutically-acceptable salt or pro-drug thereof: wherein R1 is selected for example from hydrogen, halogen, optionally substituted methyl; R2 and R3 are independently selected from hydrogen, fluoro, chloro and trifluoromethyl; R4 and R5 are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl, C(O)R6 or R4 and R5 together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.Type: ApplicationFiled: May 24, 2004Publication date: March 13, 2008Applicant: AstraZeneca ABInventors: Daniel Robert Carcanague, Michael Barry Gravestock
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Patent number: 7338967Abstract: The present invention provides compounds of formula I: along with methods of making the same, compostions thereof, and methods of use thereof, particularly methods of use as fungicides.Type: GrantFiled: September 8, 2005Date of Patent: March 4, 2008Assignee: Syngenta LimitedInventors: Shy-Fuh Lee, Micah Gliedt
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Patent number: 7332602Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.Type: GrantFiled: November 21, 2006Date of Patent: February 19, 2008Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, John Partridge, Henry H. Lu
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Publication number: 20070259923Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: April 25, 2007Publication date: November 8, 2007Applicants: AstraZeneca AB, NPS PHARMACEUTICALS, INC.Inventors: Methvin Isaac, Abdelmalik Slassi, Louise Edwards, Tao Xin, Andreas Wallberg, Tomislav Stefanac
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Patent number: 7259175Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethylType: GrantFiled: February 13, 2003Date of Patent: August 21, 2007Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Patent number: 7253187Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.Type: GrantFiled: February 3, 2004Date of Patent: August 7, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
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Patent number: 7229999Abstract: The present invention relates to compounds of the formula wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.Type: GrantFiled: April 4, 2006Date of Patent: June 12, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Hans Iding, Matthias Heinrich Nettekoven, Ulrike Obst, Stephan Roever, Beat Wirz
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7211595Abstract: Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.Type: GrantFiled: November 30, 2001Date of Patent: May 1, 2007Assignee: Abbott LaboratoriesInventors: Akiyo K. Claiborne, Stephen L. Gwaltney, II, Lisa A. Hasvold, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Todd W. Rockway, Hing L. Sham, Gerard M. Sullivan, Yunsong Tong, Gary Wang, Le Wang, Xilu Wang, Wei-Bo Wang
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Patent number: 7196103Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: March 27, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, Kurt Ritter, Volker Laux
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Patent number: 7179804Abstract: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykininsType: GrantFiled: April 22, 2003Date of Patent: February 20, 2007Assignee: Eli Lilly and CompanyInventors: Albert Kudzovi Amegadzie, Kevin Matthew Gardinier, Erik James Hembre, Jian Eric Hong, Louis Nickolaus Jungheim, Michael Alan Robertson, Kenneth Allen Savin
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Patent number: 7169798Abstract: The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: February 13, 2004Date of Patent: January 30, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Guy Bemis, Anne-Laure Grillot, Mark Ledeboer, Francesco G. Salituro, Edmund Harrington, Huai Gao, Christopher Baker, Jingrong Cao, Michael Hale
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Patent number: 7125865Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.Type: GrantFiled: July 21, 2003Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, Alan D. Adams, Ahren I. Green, Shaei Y. Huang, Bruno Tse, Clare E. Gutteridge, Yuan Cheng
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Patent number: 7119104Abstract: A compound represented by the formula (I) or a salt of the compound, and a PPAR-? activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B1 represents N, etc.; B2 represents O, etc.; each of X1 and X2 represents O, S, a bond, etc.; Y represents C1-8 alkylene chain; Z represents O or S; R1 represents aryl, etc. which can have substituents; R2 represents C1-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; each of R4 and R5 represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that each of Z and R3 is attached to the benzene ring, and X2 is not attached to the benzene ring).Type: GrantFiled: October 9, 2002Date of Patent: October 10, 2006Assignee: Nippon Chemiphar, Co., Ltd.Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
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Patent number: 7105549Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: September 6, 2002Date of Patent: September 12, 2006Assignee: Euro-Celtique S.A.Inventors: Bin Shao, R. Richard Goehring, Samuel F Victory, Qun Sun
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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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: 7087598Abstract: This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered nonaromatic heterocyclic ring; K is taken together with the two contiguous linking carbon atoms to form a phenyl ring or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted; and R1, R2, and R3 are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).Type: GrantFiled: May 21, 2002Date of Patent: August 8, 2006Assignee: E. I. du Pont de Nemours and CompanyInventor: David Alan Clark
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Patent number: 7081538Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are describedType: GrantFiled: November 28, 2000Date of Patent: July 25, 2006Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Michael John Betts
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley