The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Publication number: 20100093814Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specfication, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: November 19, 2008Publication date: April 15, 2010Applicant: ABBOTT LABORATORIESInventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
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Publication number: 20100093690Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Inventors: Ian Bruce, Peter Finan, Catherine LeBlanc, Clive McCarthy, Lewis Whitehead, Nicola Press, Graham Charles Bloomfield, Judy Hayler, Louise Kirman, Mrinalini Sachin Oza, Lena Shukla
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Patent number: 7687637Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: February 27, 2003Date of Patent: March 30, 2010Assignee: Novartis AGInventors: Ian Bruce, Peter Finan, Catherine Leblanc, Clive McCarthy, Lewis Whitehead, Nicola Press, Graham Charles Bloomfield, Judy Hayler, Louise Kirman, Mrinalini Sachin Oza, Lena Shukla
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Publication number: 20100061960Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: July 16, 2009Publication date: March 11, 2010Inventors: Franz Ulrich Schmitz, Roopa Rai, Ronald Griffith, Christopher Don Roberts
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Publication number: 20100063022Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: September 4, 2009Publication date: March 11, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
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Publication number: 20100063051Abstract: 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: ApplicationFiled: October 31, 2007Publication date: March 11, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T.G. Murali Dhar
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Patent number: 7674912Abstract: The invention relates to compounds of the formula I A-B-Z ??I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.Type: GrantFiled: April 24, 2006Date of Patent: March 9, 2010Assignee: H. Lundbeck A/SInventors: Anette Graven Sams, Benny Bang-Andersen, Gitte Mikkelsen, Mogens Larsen
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Publication number: 20100022542Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1-W1??(I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted phenylene or the like; and W1 is a group represented by the below formula: wherein R1, R2, R3, and R4 are each independently a hydrogen atom, optionally substituted lower alkyl or the like, a broken line (---) represents the presence or absence of bond.Type: ApplicationFiled: July 16, 2009Publication date: January 28, 2010Inventors: Hiroshi TAKEMOTO, Takeshi SHIOTA, Masami TAKAYAMA
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Publication number: 20100022772Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: ApplicationFiled: July 28, 2004Publication date: January 28, 2010Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Yusheng Wu, Chen Shili, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Publication number: 20100016304Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2007Publication date: January 21, 2010Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Patent number: 7645783Abstract: A method of treating viral infections by the administration of a halogenated benzamide derivative according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds.Type: GrantFiled: October 1, 2007Date of Patent: January 12, 2010Assignee: Romark Laboratories L.C.Inventor: Jean Francois Rossignol
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Publication number: 20100004441Abstract: Disclosed are compounds having Formula (I) and the compositions and methods thereof for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: ApplicationFiled: August 20, 2009Publication date: January 7, 2010Inventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers, Irina Slobodov, Roopa Rai
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Publication number: 20100004219Abstract: 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 metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to whType: ApplicationFiled: October 31, 2007Publication date: January 7, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko
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Publication number: 20090325961Abstract: Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: ApplicationFiled: August 18, 2009Publication date: December 31, 2009Inventors: Jingwu Duan, Bin Jiang
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Publication number: 20090312314Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: June 10, 2009Publication date: December 17, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090306156Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: August 4, 2009Publication date: December 10, 2009Inventors: Allen HOPPER, Robert Francis Dunn, Erik Mikal Kuester, Richard Dennis Conticello, Ruiping Liu, Ashok Tehim
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Publication number: 20090298832Abstract: The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.Type: ApplicationFiled: August 15, 2006Publication date: December 3, 2009Inventors: Song Li, Changbin Guo, Xiancheng Jiang, Junhai Xiao, Zhong Wu
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Publication number: 20090291969Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 5-membered heterocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 12, 2007Publication date: November 26, 2009Inventors: Isabelle Christian, Maria-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
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Publication number: 20090286800Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: May 15, 2009Publication date: November 19, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20090281154Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: ApplicationFiled: June 7, 2007Publication date: November 12, 2009Inventors: James B. Doherty, Swaminathan R. Natarajan, Dong-Ming Shen, Fengqi Zhang
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Publication number: 20090281142Abstract: [Problem] To provide a compound which is useful as a GK activator. [Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention. Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.Type: ApplicationFiled: August 30, 2006Publication date: November 12, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Takahiro Nigawara, Kazuyuki Tsuchiya, Naoki Ishibashi, Mitsuaki Okumura, Yuichiro Kawamoto, Akira Nagayoshi
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Publication number: 20090258915Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: ApplicationFiled: April 8, 2009Publication date: October 15, 2009Inventors: Yun Yen, David Horne, Yate-Ching Yuan
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Patent number: 7598392Abstract: The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below: in which R1, R2, R3, Y, m, n, and p are as defined in the disclosure; as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic use thereof.Type: GrantFiled: April 18, 2007Date of Patent: October 6, 2009Assignee: sanofi-aventisInventors: Pierre Casellas, Daniel Floutard, Pierre Fraisse, Samir Jegham
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Publication number: 20090247500Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: ApplicationFiled: March 11, 2009Publication date: October 1, 2009Applicant: Abbott LaboratoriesInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rosemarie Tietje, Sridhar Peddi, William A. Carroll
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Publication number: 20090247593Abstract: The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are A2A-receptor ligands, such as antagonists, agonists, reverse agonists or partial agonists, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.Type: ApplicationFiled: December 19, 2008Publication date: October 1, 2009Applicant: H. Lundbeck A/SInventors: Anette Graven Sams, Mogens Larsen, Gitte Mikkelsen
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Patent number: 7595398Abstract: Disclosed are compounds having Formula (I) and the compositions and methods thereof for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: GrantFiled: December 12, 2006Date of Patent: September 29, 2009Assignee: SmithKline Beecham CorporationInventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers, Irina Slobodov, Roopa Rai
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Patent number: 7592461Abstract: Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: GrantFiled: December 20, 2006Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang
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Patent number: 7582769Abstract: Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes.Type: GrantFiled: July 7, 2006Date of Patent: September 1, 2009Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedso, Marit Kristiansen, Lone Jeppesen
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Patent number: 7582632Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: GrantFiled: April 16, 2007Date of Patent: September 1, 2009Assignee: Prosidion LimitedInventors: Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Karen Lesley Schofield, Vilasben Kanji Shah, Kosuke Yasuda
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Publication number: 20090215800Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.Type: ApplicationFiled: May 4, 2006Publication date: August 27, 2009Applicant: CHROMA THERAPEUTICS LTDInventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
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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: 20090203745Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.Type: ApplicationFiled: May 14, 2007Publication date: August 13, 2009Applicant: Jerini AGInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 7563903Abstract: Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5? represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5? form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, inType: GrantFiled: July 21, 2005Date of Patent: July 21, 2009Assignee: Sanofi-AventisInventors: Pierre Despeyroux, Daniel Frehel, Bruno Schoentjes, Viviane Van Dorsselaer
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Publication number: 20090176756Abstract: The present invention relates to substituted thiazoles, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: July 9, 2009Applicant: GRUNENTHAL GMBHInventors: Michael Haurand, Klaus Schiene, Sven Kuhnert, Melanie Reich
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Patent number: 7553974Abstract: Crystals of (2R,4R)-monatin potassium salt which exhibit an X-ray powder diffraction pattern having characteristic peaks at diffraction angles 2? of 5.5°, 7.2°, 8.1°, 8.9°, and 16.3°, by powder X-ray diffraction (Cu—K? radiation), are superior in sweetness, preservation stability, solubility, and color stability.Type: GrantFiled: July 14, 2005Date of Patent: June 30, 2009Assignee: Ajinomoto Co., Inc.Inventors: Ken-ichi Mori, Eriko Ono, Tadashi Takemoto
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Publication number: 20090163470Abstract: The invention relates to novel thiazolylidine urea and amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: December 18, 2008Publication date: June 25, 2009Applicant: ABBOTT LABORATORIESInventors: Ramin Faghih, Gregory A. Gfesser, Kathleen H. Mortell, Murali Gopalakrishnan
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Patent number: 7550493Abstract: A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds and where at least two of R2-R6 are not hydrogen and where at least one of R2-R6 are hydroxy or acyloxy.Type: GrantFiled: October 1, 2007Date of Patent: June 23, 2009Assignee: Romark Laboratories, LCInventor: Jean Francois Rossignol
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Publication number: 20090156554Abstract: New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.Type: ApplicationFiled: February 5, 2009Publication date: June 18, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen BREITFELDER, Udo MAIER, Trixi BRANDL, Christoph HOENKE, Matthias GRAUERT, Alexander PAUTSCH, Matthias HOFFMANN, Frank KALKBRENNER, Anne T. JOERGENSEN, Gerhard SCHAENZLE, Stefan PETERS, Frank BUETTNER, Eckhart BAUER
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Publication number: 20090156574Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.Type: ApplicationFiled: January 27, 2009Publication date: June 18, 2009Applicant: SANOFI-AVENTISInventors: Pierre CARAYON, Pierre CASELLAS, Daniel FLOUTARD, Pierre FRAISSE, Samir JEGHAM, Bernard LABEEUW
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Publication number: 20090137642Abstract: The Invention relates to compounds of the formula I, wherein the variables are as defined in the claims, for use as a medicament. The compounds are A2A-receptor legends and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.Type: ApplicationFiled: September 20, 2005Publication date: May 28, 2009Applicant: H. LUNDBECK A/SInventors: Mogens Larsen, Anette Graven Sams, Gitte Mikkelsen, Benny Bang-Andersen
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Patent number: 7534918Abstract: This invention relates to hydroxamic acid derivatives having a sulfonamide linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: GrantFiled: July 8, 2005Date of Patent: May 19, 2009Assignee: Merck & Co., Inc.Inventors: Sandro Belvedere, Joey Lee Methot, Thomas A. Miller, David J. Witter, Jiaming Yan
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Publication number: 20090118291Abstract: This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: ApplicationFiled: August 22, 2005Publication date: May 7, 2009Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Publication number: 20090105250Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, FGFR3, PDGFR? and b-Raf kinases.Type: ApplicationFiled: January 19, 2006Publication date: April 23, 2009Applicant: IRM LLCInventors: Taebo Sim, Nathanael Schiander Gray, Hyun Soo Lee, Yi Liu, Pingda Ren, Shuli You, Qiong Zhang, Qiang Ding, Xia Wang, Songchun Jiang, Pamela A. Albaugh
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Publication number: 20090093485Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: April 9, 2009Applicant: ASTRAZENECA ABInventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
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Publication number: 20090093530Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.Type: ApplicationFiled: May 17, 2007Publication date: April 9, 2009Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Andrea Aramini, Alessio Moriconi
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Patent number: 7514439Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 10, 2006Date of Patent: April 7, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
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Publication number: 20090082396Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Inventors: Josephus H.M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Publication number: 20090075995Abstract: 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, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substitutedType: ApplicationFiled: August 8, 2007Publication date: March 19, 2009Inventors: David S. Weinstein, Ping Chen, T.G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Bingwei Vera Yang, Arthur M. Doweyko
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Publication number: 20090054463Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2008Publication date: February 26, 2009Inventors: Pierre Deprez, Christopher Fotsch, Paul Harrington, Sarah Lively, Kanaka Pattabiraman, David St. Jean, Taoues Temal-Laib
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Publication number: 20090048258Abstract: The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: January 31, 2006Publication date: February 19, 2009Inventors: Masaki Ogino, Yoshihisa Nakada, Mitsuyuki Shimada, Kouhei Asano, Norikazu Tamura, Minori Masago