Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/377)
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Publication number: 20090163497Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: June 25, 2009Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Patent number: 7544808Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: July 5, 2007Date of Patent: June 9, 2009Assignee: Bristol-Myers Squibb CompanyInventors: David S. Weinstein, John L. Gilmore, James Sheppeck, Bingwei Vera Yang, Soong-Hoon Kim, Wayne Vaccaro
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Publication number: 20090124666Abstract: Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV 1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: October 23, 2008Publication date: May 14, 2009Applicant: ABBOTT LABORATORIESInventors: Richard J. Perner, John R. Koenig, Stanley Didomenico, JR., Erol K. Bayburt, Jerome F. Daanen, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Anil Vasudevan, Eric Voight
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Publication number: 20090105307Abstract: The invention relates to compounds of formula wherein R1, R2, and R3 are as defined herein and to a pharmaceutically suitable acid addition salts thereof for the treatment of CNS disorders.Type: ApplicationFiled: February 8, 2008Publication date: April 23, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090093452Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein RQ, R7, n, Q2, Q3, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: April 9, 2009Inventors: Kenneth He Huang, Steven E. Hall, James Veal
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Publication number: 20090069330Abstract: Substituted oxazole derivatives corresponding to formula 1: a method for producing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds to treat pain, depression, urinary incontinence, diarrhoea, pruritus, alcohol and drug misuse, drug dependency, lethargy and/or anxiety.Type: ApplicationFiled: June 20, 2008Publication date: March 12, 2009Applicant: Gruenenthal GMBHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Heinz Graubaum
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Patent number: 7498352Abstract: The present invention provides a TGF-? superfamily production/secretion promoter comprising a compound represented by the formula wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of dysautonomia, bladder dysfunction, hearing impairment, bone disease and the like.Type: GrantFiled: June 25, 2002Date of Patent: March 3, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Yasuo Sugiyama, Masatoshi Hazama, Asae Shintani
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Publication number: 20090054450Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.Type: ApplicationFiled: June 17, 2008Publication date: February 26, 2009Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Mark G. CURRIE, John Jeffrey TALLEY, Brian CALI
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Publication number: 20090036306Abstract: Certain substituted benzylamino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (1): wherein R, R1, R2, R3, and R4 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (1), and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: May 19, 2006Publication date: February 5, 2009Applicant: Bayer CropScience AGInventors: John A. Dixson, George Theodoridis, Zeinab M. Elshenawy, Benjamin J. Dugan, Manorama M. Patel, Edward J. Barron, Stephen F. Donovan
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Publication number: 20090018150Abstract: Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.Type: ApplicationFiled: July 23, 2004Publication date: January 15, 2009Applicant: ASTERAND UK LIMITEDInventors: Richard Anthony Borman, Robert Alexander Coleman, Kenneth Lyle Clark, Alexander William Oxford, George Hynd, Janet Ann Archer, Amanda Aley, Neil Victor Harris
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Publication number: 20090005323Abstract: This invention relates to the treatment of obesity, the treatment of obesity related disorders, prevention of weight gam, prevention of weight regain or for weight maintenance by the use of a cathepsin K inhibitor as active ingredient, alone or in conjunction with other anti-obesity agents The invention also relates to the pharmaceutical compositions comprising cathepsin K inhibitor as active ingredient, pharmaceutically acceptable carriers or excipients, and optionally one or more anti-obesity agents.Type: ApplicationFiled: January 17, 2006Publication date: January 1, 2009Inventor: Michael David Percival
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Publication number: 20080312291Abstract: The present invention relates to novel thiazole and oxazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein X1 and X2 are selected from 0 and N or S and N and R1, R2 and Y are as defined in the description. For example, R1 may be alkyl, alkoxy, thioalkoxy or aryl, R2 may be alkoxy and Y may be a carbonylamino-linked substituent containing an aryl or heteroaryl group.Type: ApplicationFiled: December 21, 2006Publication date: December 18, 2008Inventors: Udo Bauer, Linda Gustafsson, Maria Saxin, Tor Svensson
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Publication number: 20080305082Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.Type: ApplicationFiled: September 14, 2005Publication date: December 11, 2008Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
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Patent number: 7462635Abstract: The present invention provides a VDAC regulator comprising a compound represented by the formula (I): wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group; a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of Down's syndrome and the like.Type: GrantFiled: March 13, 2003Date of Patent: December 9, 2008Assignees: Takeda Pharmaceutical Company Limited, Tokyo Institute of TechnologyInventors: Yasuo Sugiyama, Masatoshi Hazama, Norihisa Iwakami
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Publication number: 20080293569Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.Type: ApplicationFiled: November 15, 2006Publication date: November 27, 2008Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20080261920Abstract: The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: January 25, 2008Publication date: October 23, 2008Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20080242704Abstract: The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Fit-3 inhibitors.Type: ApplicationFiled: April 4, 2006Publication date: October 2, 2008Inventors: David Grierson, Abdellah Benjahad, Alain Moussy, Martine Croisy
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Patent number: 7429607Abstract: The present invention relates to compounds of formula I: wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either: (i) independently selected from H, R, R?, SO2R, C(?O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R? is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT2B receptor.Type: GrantFiled: February 12, 2003Date of Patent: September 30, 2008Assignee: Asterand UK LimitedInventors: Alexander William Oxford, Richard Anthony Borman, Robert Alexander Coleman, Kenneth Lyle Clark, George Hynd, Janet Ann Archer, Amanda Aley, Neil Victor Harris
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Publication number: 20080214547Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.Type: ApplicationFiled: October 2, 2007Publication date: September 4, 2008Inventors: Rakesh K. Srivastava, Sharmila Shankar
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Publication number: 20080207572Abstract: The present invention relates to a method for treating Multiple Myeloma (MM), FGFR3+ myeloma, especially relapsed or refractory multiple myeloma (4/14) expressing FGFR3, comprising administering a dual C-KIT/FGFR3 inhibitor, such as 2-aminoarylthiazoles and 2-aminoaryloxazoles.Type: ApplicationFiled: July 13, 2006Publication date: August 28, 2008Inventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20080176899Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 11, 2005Publication date: July 24, 2008Inventors: Sarah Hadida Ruah, Peter Grootenhuis, Mark Miller, Matthew Hamilton
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Patent number: 7329682Abstract: A benzoxazole derivative is disclosed for inhibiting 5-lipoxygenase.Type: GrantFiled: February 27, 2004Date of Patent: February 12, 2008Assignee: EWHA University-Industry Collaboration FoundationInventors: Hea Young Park Choo, Hyeun Wook Chang, Ju Hee Yoon, Hye Kyung Ju
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Patent number: 7317024Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 12, 2006Date of Patent: January 8, 2008Assignee: Bristol-Myers Squibb Co.Inventor: Bingwei V. Yang
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Patent number: 7317030Abstract: The present invention relates to novel compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Z is NH, or CH2 if Y is SO2 Y is C?O, C?S, or SO2 if Z is CH2; A is phenyl or indolyl, N-methyl-indolyl R1 is —CN, wherein the bond between CR3 and CR7 is a single or double bond; m is 0 or 1; n is 0 or 1; p is 0 or 1; and to their use as medicaments.Type: GrantFiled: February 28, 2005Date of Patent: January 8, 2008Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7244752Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6Type: GrantFiled: April 9, 2002Date of Patent: July 17, 2007Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Dominique Louis Nestor Ghislain Surleraux, Sandrine Marie Helene Vendeville, Wim Gaston Verschueren, Marie-Pierre T. M. M. G. De Bethune, Herman Augustinus De Kock, Abdellah Tahri, Montserrat Erra Solà
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Patent number: 7202257Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: GrantFiled: July 6, 2004Date of Patent: April 10, 2007Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 7189712Abstract: Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: October 10, 2003Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: Matthew Lee Brown, Mui Cheung, Scott Howard Dickerson, Cassandra Gauthier, Philip Anthony Harris, Robert Neil Hunter, Gregory Pacofsky, Michael Robert Peel, Jeffrey Alan Stafford
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Patent number: 7183276Abstract: The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.Type: GrantFiled: February 27, 2003Date of Patent: February 27, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Nozomu Sakai, Yu Momose, Katsuhito Murase, Masatoshi Hazama
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Patent number: 7183300Abstract: Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.Type: GrantFiled: November 10, 2005Date of Patent: February 27, 2007Inventors: Michael F. Summers, Atul Agarwal, Xi Chen, Milind Deshpande
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Patent number: 7166625Abstract: Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I:Type: GrantFiled: December 31, 2001Date of Patent: January 23, 2007Assignee: Alteon, Inc.Inventors: John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond J. LaVoie
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Patent number: 7163952Abstract: The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.Type: GrantFiled: December 3, 2002Date of Patent: January 16, 2007Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Tomoyuki Ikemoto, Shohei Sakata, Hiroshi Maegawa, Atsunori Kashiwagi
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Patent number: 7148249Abstract: The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: September 5, 2003Date of Patent: December 12, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Joerg Kley, Frank Hilberg, Armin Heckel, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Ulrike Tontsch-Grunt, Jacobus C. A. Van Meel
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Patent number: 7125893Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.Type: GrantFiled: May 1, 2000Date of Patent: October 24, 2006Assignee: Schering AGInventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
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Patent number: 7119113Abstract: The invention relates to carboxamide derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as mGluR1 enhancers in the treatment and prevention of neurological disorders and diseases, such as Alzheimer's disease and dementia.Type: GrantFiled: December 18, 2003Date of Patent: October 10, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Joerg Huwyler, Frederic Knoflach, Eric Vieira, Juergen Wichmann
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Patent number: 7112599Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R6, R7, and Z, and other variables enumerated under one or more of R3, R5, R6, R7, and Z, are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: August 5, 2004Date of Patent: September 26, 2006Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 7109224Abstract: Acyl guanidine compounds of the following Formula wherein R1, R2, R3, R4 and L are described herein, and pharmaceutical compositions thereof, are useful in treating leukocyte activation-associated disorders.Type: GrantFiled: November 6, 2003Date of Patent: September 19, 2006Assignee: Bristol-Myers Squibb Co.Inventors: James Kempson, William J. Pitts
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Patent number: 7105551Abstract: The present invention provides compounds of formula (I).Type: GrantFiled: December 19, 2001Date of Patent: September 12, 2006Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Romain Luc Marie Gosmini, Millard Hurst Lambert, III, Michael Lawrence Sierra
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Patent number: 6995181Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.Type: GrantFiled: July 17, 2003Date of Patent: February 7, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Wayne Vaccaro, Bingwei Vera Yang, Soong-Hoon Kim, Tram Huynh, David R. Tortolani, Kenneth J. Leavitt, Wenying Li, Arthur M. Doweyko, Xiao-Tao Chen, Lidia Doweyko
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Patent number: 6992083Abstract: The invention relates to compounds of formula wherein R is phenyl, unsubstituted or substituted by halogen or —CH2N(CH3)(CH2)nOCH3, or is benzyl, lower alkyl, lower alkoxy, —(CH2)nOCH3, or is pyridin 3 -or 4-yl, unsubstituted or substituted by lower alkyl, halogen, morpholinyl, —(CH2)n-halogen, —(CH2)nOCH3, —(CH2)n-morpholin-4-yl, or —(CH2)n-pyrrolidin-1-yl; R1 is phenyl, unsubstituted or substituted by halogen, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl or morpholin-4-yl; n is independently from each other 1 or 2; and to pharmaceutically acceptable salts thereof for the treatment of diseases related to the adenosine A2A-receptor.Type: GrantFiled: January 9, 2004Date of Patent: January 31, 2006Assignee: Hoffman-La Roche Inc.Inventor: Roger David Norcross
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6951873Abstract: Methods for the treatment of age-related behavioral disorders in companion animals are disclosed. These comprise administering to a companion animal in need of such treatment a therapeutically effective amount of an acetylcholinesterase inhibitor. A preferred acetylcholinesterase inhibitor is a compound of Formula 1: Pharmaceutical compositions and dosage forms comprising a compound of Formula 1 are also disclosed.Type: GrantFiled: March 3, 2000Date of Patent: October 4, 2005Assignee: Pfizer Inc.Inventor: Kristin M. Lundy
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Patent number: 6916814Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.Type: GrantFiled: July 1, 2002Date of Patent: July 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Neil Moss, John Robinson Regan
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Patent number: 6900202Abstract: There is provided di-substituted iminoheterocyclic compounds of the following formula (I): in which, A is optionally substituted alkyl group, optionally substituted aryl group or optionally substituted heterocyclic group; X is oxygen atom, sulfur atom, carbon atom or nitrogen atom; the group —X—Y— represents optionally substituted alkylene or cyclic alkenylene bond; and B1 and B2 are, hydrogen atom, optionally substituted alkyl group, optionally substituted aryl group or optionally substituted heterocyclic group, independent from each other, or a pharmaceutically acceptable salt thereof. These compounds have good affinity for ?4?2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.Type: GrantFiled: March 21, 2001Date of Patent: May 31, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Masahiro Imoto, Tatsuya Iwanami, Minako Akabane, Yoshihiro Tani
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Patent number: 6867226Abstract: This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators.Type: GrantFiled: August 16, 2002Date of Patent: March 15, 2005Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Sato, Megumi Yamada, Kazuko Kobayashi, Katsuyoshi Iwamatsu, Fukio Konno, Koichi Shudo
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Patent number: 6846838Abstract: Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.Type: GrantFiled: June 17, 2003Date of Patent: January 25, 2005Assignee: Bristol-Myers Squibb CompanyInventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley