Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/233)
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Publication number: 20110160225Abstract: 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: November 19, 2010Publication date: June 30, 2011Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: Mark G. Currie, John Jeffrey Talley, Brian Cali
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Patent number: 7968577Abstract: 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 inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Patent number: 7968707Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 27, 2007Date of Patent: June 28, 2011Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Publication number: 20110152318Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: ApplicationFiled: July 2, 2009Publication date: June 23, 2011Applicant: Amorepacific CorporationInventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
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Publication number: 20110144057Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.Type: ApplicationFiled: February 8, 2011Publication date: June 16, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee
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Publication number: 20110144333Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are 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: February 24, 2011Publication date: June 16, 2011Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20110124647Abstract: The present invention relates to novel derivatives of substituted benzylamines, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 28, 2008Publication date: May 26, 2011Applicant: Bayer CropScience AGInventors: Christian Arnold, Ulrich Görgens, Hans-Georg Schwarz, Graham Holmwood, Roland Andree, Olga Malsam, Otto Schallner, Eva-Marie Franken, Horst-Peter Antonicek, Stefan Werner
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Patent number: 7928036Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: GrantFiled: February 10, 2010Date of Patent: April 19, 2011Assignee: Divergence, Inc.Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman
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Patent number: 7902237Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of the disease or disorder directly or indirectly related to the activity of the receptors.Type: GrantFiled: August 9, 2005Date of Patent: March 8, 2011Assignee: Exelixis, Inc.Inventors: Richard Martin, Brenton Todd Flatt, Jeffrey Dean Kahl
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Patent number: 7902238Abstract: 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: GrantFiled: February 8, 2008Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20110028523Abstract: Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclosed.Type: ApplicationFiled: July 1, 2010Publication date: February 3, 2011Applicant: ALLERGAN, INC.Inventors: Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Wenkui K. Fang, Santosh C. Sinha, Michael E. Garst, Daniel W. Gil
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Publication number: 20110015241Abstract: The invention relates to substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: May 25, 2007Publication date: January 20, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Tobias Wunberg, Susanne Röhrig, Stefan Heitmeier
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Publication number: 20100311798Abstract: The invention relates to compounds of formula wherein R1, R2, R2?, X, Y, andn are as defined in the specification or to a pharmaceutically suitable acid addition salt thereof. The compounds of formula I are active on the TAAR1 receptor and are therefore suitable for the treatment of 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: May 28, 2010Publication date: December 9, 2010Inventors: Guillaume Décoret, Guido Galley, Katrin Groebke Zbinden, Roger Norcross
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Patent number: 7838681Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.Type: GrantFiled: April 30, 2004Date of Patent: November 23, 2010Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris SudInventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
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Publication number: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20100280036Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100280085Abstract: The use of a compound of formula (I) wherein X is (i), (ii) or (iii), where the substituents have the meanings assigned to them in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: August 6, 2007Publication date: November 4, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Christoph Luthy, Anthony Cornelius O'Sullivan, Jurgen Harry Schaetzer
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100280078Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.Type: ApplicationFiled: July 2, 2008Publication date: November 4, 2010Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecile Ebuenga
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Patent number: 7807690Abstract: A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.].Type: GrantFiled: September 19, 2008Date of Patent: October 5, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
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Publication number: 20100249129Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
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Publication number: 20100210849Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: ApplicationFiled: February 10, 2010Publication date: August 19, 2010Applicant: DIVERGENCE, INC.Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, JR., Al Wideman
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100120864Abstract: 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: December 16, 2009Publication date: May 13, 2010Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20100076029Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 22, 2009Publication date: March 25, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Alessandra BARTOLOZZI, Eugene Richard HICKEY, Doris RIETHER, Lifen WU, Renee M. ZINDELL, Stephen Peter EAST, Monika ERMANN
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Publication number: 20100041686Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are 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: July 17, 2009Publication date: February 18, 2010Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20100041720Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein Y, X1, X2, X3, R1, and R2 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Steven P. Latshaw, Bo Liu, Meena V. Patel, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20100029589Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are 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: September 14, 2009Publication date: February 4, 2010Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Patent number: 7655600Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the general formula (I) wherein A is a radical of the formulae A? or A2: NRA?A2 and wherein m is 0, 1, 2, 3, 4 or 5, n is 0, 1, 2, 3, 4 or 5, X is sulfur or oxygen, and wherein the variables R1, R2, R3, R4, R5a, R5b, R5c, R5d are as defined in the claims, and to the agriculturally acceptable salts thereof. The invention relates also to a method of combating animal pests, selected from insects, arachnids and nematodes and to a method for protecting crops from attack or infestation by insects, arachnids or nematodes, which comprises contacting a crop with a pesticidally effective amount of a 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the general formula I and/or at least one salt thereof.Type: GrantFiled: December 22, 2004Date of Patent: February 2, 2010Assignee: BASF AktiengesellschaftInventors: Markus Kordes, Michael Hofmann, Michael Puhl, Norbert Götz, Michael Rack, Ernst Baumann, Wolfgang von Deyn, Thomas Schmidt, Livio Tedeschi, Michael F. Treacy, Deborah L. Culbertson, Toni Bucci, David G. Kuhn
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Publication number: 20100010060Abstract: The invention relates to novel isoindolin-1-one, isoindolin-3-one and isoindoline-1,3-dione derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: May 26, 2007Publication date: January 14, 2010Applicant: Bayer Healthcare AGInventors: Susanne Röhrig, Mario Jeske, Elisabeth Prezborn, Mark Jean Gnoth
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Publication number: 20090275627Abstract: Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both ?2B and ?2C adrenergic agonists. Methods of synthesis and administration of the compounds are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: November 5, 2009Applicant: ALLERGAN, INC.Inventors: Janet A. Takeuchi, Ken Chow, Ling Li, Liming Wang
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Patent number: 7608619Abstract: Substituted oxazole derivatives corresponding to formula I: 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: GrantFiled: June 20, 2008Date of Patent: October 27, 2009Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Heinz Graubaum
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Publication number: 20090209529Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
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Patent number: 7576108Abstract: According to the present invention there is provided a compounds of formula (I): and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 16, 2003Date of Patent: August 18, 2009Assignee: Eli Lilly and CompanyInventors: Andreas Gerhard Weichert, David Gene Barrett, Stefan Heuser, Rainer Riedl, Mark Joseph Tebbe, Andrea Zaliani
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Publication number: 20090192317Abstract: The present invention relates to a process for synthesizing in good yield substituted 2-aminoaryloxazole compounds of formula I which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit, bcr-abl, Flt-3 and mutant forms thereof.Type: ApplicationFiled: May 11, 2007Publication date: July 30, 2009Applicant: AB SCIENCEInventor: Abdellah Benjahad
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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: 20090137817Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: ApplicationFiled: August 25, 2008Publication date: May 28, 2009Inventors: Pierre Deslongchamps, Yves Dory, Kamel Benakli, Eric Marsault, Luc Ouellet, Mahesh Ramaseshan, Martin Vezina, Daniel Fortin, Ruoxi Lan, Shigui Li, Gerald Villeneuve, Hamid R. Hoveyda, Sylvie Beaubien, Mark L. Peterson
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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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Patent number: 7504520Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.Type: GrantFiled: May 10, 2006Date of Patent: March 17, 2009Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee
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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: 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: 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: 20080312435Abstract: An imine compound represented by the formula: wherein A represents a heterocyclic group; R1, R2, an R3 each represent a hydrogen atom, a halogen atom, a C1-10 alkyl group optionally substituted with an aryl group(s) substituted with a halogen atom(s), a C3-10 cycloalkyl group, a C1-6 haloalkyl group, a C1-10 alkoxy group, etc.; R4 represents an optionally substituted C1-10 alkyl, C2-6 alkenyl, or aryl group; R5 represents a hydrogen atom, a C1-10 alkoxy group, a C1-6 haloalkyl group, an optionally substituted C1-10 alkyl or C2-6 alkenyl group, an optionally substituted aryl or heterocyclic group, etc.; W represents —CO—, —CO—CO—, —CO—NH—, —CS—NH—, or —SO2—, or a cannabinoid-receptor agonist comprising said imine compound as an active ingredient. The imine compound of the present invention has a cannabinoid-receptor agonist effect, and is useful as a therapeutic or prophylactic drug for pains and autoimmune diseases.Type: ApplicationFiled: October 31, 2005Publication date: December 18, 2008Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Shiuji Saito, Hiroshi Ohta, Tomoko Ishizaki, Mitsukane Yoshinaga, Makoto Tatsuzuki, Yuji Yokobori, Yasumitsu Tomishima, Aki Morita, Yoshihisa Toda, Kimiko Tokugawa, Ayaka Kaku, Tomomi Murakami, Hiromitsu Yoshimura, Shingo Sekine, Takao Yoshimizu
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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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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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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: 20080194833Abstract: A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided. A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.Type: ApplicationFiled: February 23, 2006Publication date: August 14, 2008Applicant: Kowa Co., Ltd.Inventors: Yukiyoshi Yamazaki, Takaaki Araki, Minoru Koura, Kimiyuki Shibuya