Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/376.1)
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Publication number: 20120213758Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Publication number: 20120165382Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: June 28, 2011Publication date: June 28, 2012Applicant: ALLERGAN, INC.Inventors: William L. Carling, Jose L. Martos, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmesta
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Publication number: 20120053173Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.Type: ApplicationFiled: March 4, 2009Publication date: March 1, 2012Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Publication number: 20120028938Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.Type: ApplicationFiled: January 24, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Ralf ANDERSKEWITZ, Dieter Wolfgang HAMPRECHT, Christoph HOENKE, Domnic MARTYRES, Wolfgang RIST, Peter SEITHER
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Publication number: 20120022119Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 16, 2009Publication date: January 26, 2012Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
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Publication number: 20110319430Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(?O) or C(?S); and R1, R1a, R2, R4, R15, R16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 3, 2010Publication date: December 29, 2011Applicant: E.I. Du pont Nemours and CompanyInventors: Jeffrey Keith Long, Wonpyo Hong, Andrew Edmund Taggi
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Patent number: 8071782Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: GrantFiled: October 2, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Neelakandha S. Mani
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Patent number: 8071565Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: July 11, 2007Date of Patent: December 6, 2011Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20110275813Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, Y, X, and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: Bayer Cropscience AGInventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Stefan Hillebrand, Arnd Voerste
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Patent number: 8048897Abstract: A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity.Type: GrantFiled: July 26, 2005Date of Patent: November 1, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Tsutomu Sato, Masahiro Nishimoto, Nobuo Shimma
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Publication number: 20110237640Abstract: The invention relates to compounds of the formula I: wherein one of R5, R6 and R7 is and X1, X2, R1 to R15 and n are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR ? and/or PPAR? agonists.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Publication number: 20110224262Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: November 24, 2009Publication date: September 15, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
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Patent number: 7977367Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: GrantFiled: September 9, 2009Date of Patent: July 12, 2011Assignee: Pfizer IncInventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20110152532Abstract: The present invention relates to a process for the preparation of 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives comprising the reaction of substituted 1,3-dioxolanes and 1,4-dioxanes with alkyl- or arylhydrazines to give 1-alkyl- or 1-aryl-substituted dihydro-1H-pyrazoles, and their further reaction to give 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives, which can be used as valuable intermediates for producing insecticidally effective anthranilamides.Type: ApplicationFiled: December 15, 2010Publication date: June 23, 2011Applicant: Bayer CropScience AGInventors: Sergii PAZENOK, Norbert Lui, Igor Gerus
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Patent number: 7947687Abstract: This invention comprises antineoplastic curcumin derivatives and methods of preparation and use thereof. Particular reference is made to the following isomeric compounds wherein R1, R2, and R3 are selected from the group consisting of H, OH, OCH3, and COOH.Type: GrantFiled: October 29, 2007Date of Patent: May 24, 2011Inventor: Byron C Robinson
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Patent number: 7939531Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: May 10, 2011Assignee: Roche Palo AltoInventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Publication number: 20110104305Abstract: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.Type: ApplicationFiled: June 30, 2010Publication date: May 5, 2011Inventors: Brian J. DAY, Remy KACHADOURIAN
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Publication number: 20110092539Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: June 3, 2009Publication date: April 21, 2011Inventors: Jonathan Gillespie, Craig Jamieson, Zoran Rankovic
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110053980Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: July 4, 2008Publication date: March 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
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Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110039852Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 29, 2009Publication date: February 17, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
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Patent number: 7879897Abstract: The invention relates to 5-sub-stituted-oxyalkylaminopyrazole derivatives of the formula or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests including arthropods and helminths.Type: GrantFiled: August 21, 2004Date of Patent: February 1, 2011Assignee: Merial LimitedInventors: David Teh-Wei Chou, Stefan Schnatterer, Werner Knauf, Karl Seeger
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Publication number: 20110009638Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.Type: ApplicationFiled: April 8, 2009Publication date: January 13, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventor: Gary David Annis
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Publication number: 20100331295Abstract: Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: June 26, 2006Publication date: December 30, 2010Applicant: EXELIXIS, INC.Inventors: Brett B Busch, Brenton T. Flatt, Xiao Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin Schweiger, William C. Stevens, JR., Tie Lin Wang, Yinong Xie
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Publication number: 20100331381Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: December 30, 2010Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Nils Damann, Sven Frormann, Bernhard Lesch, Jeewoo Lee, Yong-Soo Kim, Myeong-Seop Kim
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Patent number: 7820709Abstract: The invention relates to polar 5-aminopyrazole carbamate derivatives of formula (I) or salts thereof: (I), wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: GrantFiled: December 22, 2006Date of Patent: October 26, 2010Assignee: Merial LimitedInventors: Stefan Schnatterer, Michael Maier, Friederike Lochhaas, Werner Knauf, Karl Seeger
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Publication number: 20100267714Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2010Publication date: October 21, 2010Inventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20100261758Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.Type: ApplicationFiled: March 28, 2007Publication date: October 14, 2010Applicant: NOVARTIS AGInventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
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Publication number: 20100240634Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: October 9, 2009Publication date: September 23, 2010Applicant: JAPAN TOBACCO INC.Inventors: Takahisa Motomura, Hironobu Nagamori, Koichi Suzawa, Hirotsugu Ito, Toru Morita, Satoru Kobayashi, Hisashi Shinkai
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Publication number: 20100221186Abstract: Cardiovascular tissue mRNA expression profiles in monkeys treated with coxibs was analyzed. Genomic data indicated that the animals showing vasculitis exhibit a specific mRNA expression pattern. The pattern includes gene expression changes involved in blood and endothelial cell (EC) activation, interaction of blood cells with EC, activation of INF? pathway, and release of pro-inflammatory cytokines and chemo-attractants. These results provide direct evidence of minimal vasculitis together with corresponding genomic signature and peripheral biomarkers for minimal vasculatis. These results also suggest that treatment might triggers/aggravate a clinically latent cardiovascular disorder in the context of an endothelium tropic viral infection and/or an autoimmune vascular disorder. The histopathological examination revealed marginal vascular changes consistent with the genomic findings.Type: ApplicationFiled: March 10, 2006Publication date: September 2, 2010Inventors: Hueseyin Firat, Julie Boisclair, Olivier Grenet, Perentes Elias, Martin M. Schumacher
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Publication number: 20100216827Abstract: Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: October 20, 2009Publication date: August 26, 2010Inventors: Jingyuan Ma, Aaron Novack, Imad Nashashibi, Phuongly Pham, Christopher J. Rabbat, Jiangao Song, Dong Fang Shi, Zuchun Zhao, Yun-Jung Choi, Xin Chen
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Patent number: 7750032Abstract: The invention provides trisubstituted pyrazoles and imidazoles of Formula I: wherein L2, q, R13, R14, R15, R16, Z1 and Z2 are as described in the Summary of the Invention; and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the peroxisome proliferator-activated receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: February 3, 2006Date of Patent: July 6, 2010Assignee: IRM LLCInventors: Christopher Cow, Robert Epple, Xing Wang, Yongping Xie, Hans Martin Seidel
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Patent number: 7714025Abstract: Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an ?,?-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.Type: GrantFiled: May 3, 2007Date of Patent: May 11, 2010Assignee: Arizona Biomedical Research CommissionInventors: Seth D. Rose, Rosemarie F. Hartman
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Patent number: 7709658Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: July 21, 2006Date of Patent: May 4, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
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Publication number: 20100069367Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: December 7, 2007Publication date: March 18, 2010Applicant: EXELIXIS, INC.Inventors: Brant Clayton Boren, Brett B. Busch, Xiao-Hui Gu, Vasu Jammalamadaka, Shao Po Lu, Richard Martin, Raju Mohan, Edwin Schweiger, William C. Stevens, Tie-Lin Wang, Yinong Xie, Wei Xu
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Publication number: 20100056595Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R2 represents hydrogen, halogen, C1-6 alkyl or C3-6 cycloalkyl; and either of said C1-6 alkyl or C3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.Type: ApplicationFiled: April 10, 2008Publication date: March 4, 2010Applicant: Glaxo Group LimitedInventors: Paul John Beswick, David Kenneth Dean, Daryl Simon Walter
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Publication number: 20090286976Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: ApplicationFiled: August 15, 2008Publication date: November 19, 2009Inventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Publication number: 20090275598Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: July 10, 2009Publication date: November 5, 2009Applicant: Amgen Inc.Inventors: Michelle Akerman, Sean Brown, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Wei Qiu, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang, Liusheng Zhu
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Publication number: 20090270361Abstract: The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same.Type: ApplicationFiled: March 25, 2009Publication date: October 29, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Mitsuhiro Ito, Naoki Tomita, Tomohiro Kaku, Tomohiko Suzaki
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Publication number: 20090270460Abstract: Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.Type: ApplicationFiled: May 22, 2007Publication date: October 29, 2009Inventors: Michael Gregory Bell, Robert Anthony Doti, Michael James Genin, Peter Ambrose Lander, Tianwei Ma, Peter Rudolph Manninen, Jason Matthew Ochoada, Fucheng Qu, Lindsay Scott Stelzer, Ryan Edward Stites, Alan M. Warshawsky
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Patent number: 7608633Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.Type: GrantFiled: February 6, 2004Date of Patent: October 27, 2009Assignee: Merckle GmbHInventors: Matthias Lehr, Joachim Ludwig
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Patent number: 7576115Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or is pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: August 13, 2007Date of Patent: August 18, 2009Assignee: Nissan Chemical Industries, Ltd.Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Publication number: 20090156592Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 27, 2007Publication date: June 18, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
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Publication number: 20090136473Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: May 28, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao, Timothy Hagen
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Patent number: 7531669Abstract: In accordance with the present invention, there are provided novel compounds that protect neurons and/or promote neuroregeneration and/or promote memory formation. Such compounds are useful for treatment of a variety of neural disorders and conditions. In another aspect of the present invention, there are also provided formulations containing one or more of the above-described compounds, optionally further containing additional neurologically active compound(s) and/or adjuvants to facilitate delivery thereof across the blood/brain barrier. In still another aspect of the present invention, there are further provided methods for treating a wide variety of neurological indications, e.g., acute neural injuries, chronic injuries, promoting memory formation, and the like.Type: GrantFiled: December 30, 2005Date of Patent: May 12, 2009Assignee: The Salk Institute for Biological StudiesInventors: David R. Schubert, Yuanbin Liu, Thomas Baiga
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Publication number: 20090093637Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Inventors: Xiaohu Deng, Neelakandha S. Mani
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Patent number: 7452899Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.Type: GrantFiled: July 29, 2004Date of Patent: November 18, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Michela Bettati, Amanda Louise Boase, Ian Churcher, Tamara Ladduwahetty, Kevin John Merchant, Abdul Quddus
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Publication number: 20080221127Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: March 5, 2008Publication date: September 11, 2008Inventors: Jack Lin, Patrick Womack, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang