Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Publication number: 20110172207Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.Type: ApplicationFiled: September 16, 2010Publication date: July 14, 2011Applicant: AiCuris Gmbh & Co. KGInventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
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Publication number: 20110171171Abstract: A compound of Formula 1.1A: 1.1A or salt thereof, as well as methods of making compounds of Formula 1.1A, methods of using compounds of Formula 1.1A to treat proliferative disorders such as cancer, and related compounds, composition, and methods.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Aegera Therapeutics, Inc.Inventors: Alain Laurent, Melanie Proulx, Yannick Rose, James B. Jaquith, Stephen Morris
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Patent number: 7977363Abstract: Novel biphenyl thiazole carboxamides of Formula (I) where R1, R2, R3, R4, R5 and n have the meanings specified in the description, several methods for the manufacture of these substances and their use for combating undesired microorganisms, as well as novel intermediate products and their manufacture.Type: GrantFiled: August 13, 2005Date of Patent: July 12, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20110160192Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Geoffrey Wells
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Publication number: 20110160255Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: June 30, 2011Inventors: Meagan B. Rouse, Mark A. Seefeld
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Publication number: 20110160256Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: June 30, 2011Inventors: Meagan B. Rouse, Mark A. Seefeld
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Publication number: 20110152301Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: December 22, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: David Rekosh, Marie-Louise Hammarskjöld
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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: 20110136831Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.Type: ApplicationFiled: March 20, 2007Publication date: June 9, 2011Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Haseba, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Publication number: 20110136879Abstract: The invention provides compounds of formula (I) wherein X is O or S; R1 is H, OH, SH, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, halo, haloC1-6alkyl, CN, C1-6-alkyl, OC1-6alkyl, C1-6alkylCOOH, C1-6alkylCOOC1-6alkyl, C2-6-alkenyl, C3-10cycloalkyl, C6-10aryl, C1-6alkylC6-10aryl, heterocyclyl, heteroaryl, CONH2, CONHC1-6alkyl, CON(C1-6alkyl)2, OCOC1-6alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group; R2 is as defined for R1 or R1 and R2 taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R5; R3 is H, halo (preferably fluoro), or CHal3 (preferably CF3), each R5 is defined as for R1; V1 is a covalent bond or a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; M1 is absent or is a C5-10 cyclic group or a C5-15 aromatic group; and R4 is H,Type: ApplicationFiled: October 4, 2010Publication date: June 9, 2011Applicant: Avexxin ASInventors: George Kokotos, Berit Johansen, Victoria Magrioti, Michael Tsakos
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Publication number: 20110130568Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: February 23, 2009Publication date: June 2, 2011Inventors: Roman Manetsch, Hong-Gang Wang, Xiandong Hu, Sameer Kulkami, Jiazhi G. Sun
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Publication number: 20110124663Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: November 23, 2010Publication date: May 26, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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Publication number: 20110118322Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 15, 2010Publication date: May 19, 2011Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110112070Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 12, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
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Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
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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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Publication number: 20110105491Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: July 7, 2009Publication date: May 5, 2011Inventors: Hamed Aissaoui, Christoph Boss, Julien Hazemann, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen
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Publication number: 20110105460Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Publication number: 20110105447Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 5, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20110092423Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: April 21, 2011Inventors: Meagan B. Rouse, Mark A. Seefeld
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Publication number: 20110092475Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.Type: ApplicationFiled: October 20, 2010Publication date: April 21, 2011Applicant: H. LUNDBECK A/SInventors: Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Mathivanan Packiarajan, Michel Grenon
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Publication number: 20110070196Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20110070197Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Ce Wang, Yao-Ling Qiu
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Patent number: 7910609Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: GrantFiled: September 24, 2008Date of Patent: March 22, 2011Assignee: The Trustees Of The University Of PennsylvaniaInventors: William F. DeGrado, Seth E. Snyder, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
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Publication number: 20110065726Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: ApplicationFiled: July 31, 2007Publication date: March 17, 2011Inventors: Zhuoliang CHEN, Sushil Kumar Sharma, Christopher Straub, Mark G. Charest, Feng He, Run-Ming David Wang, Leigh Zawel, Christine Hiu-Tung Chen, Miao Dai, Huangshu Lei, Ly Pham, Fan Yang
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Publication number: 20110064698Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Publication number: 20110064696Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20110064695Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Patent number: 7897626Abstract: The present invention relates to 2-substituted thiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereofType: GrantFiled: December 9, 2008Date of Patent: March 1, 2011Assignee: Bayer Schering Pharma AGInventors: Ulrich Bothe, Arne Von Bonin, Duy Nguyen, Ulf Bömer, Judith Guenther
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110009456Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: December 21, 2009Publication date: January 13, 2011Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Patent number: 7868179Abstract: The invention relates to novel thiazolylbiphenylamides of the formula (I) in which R1, R2, R3, R4, R5 and R6 are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling unwanted micro-organisms.Type: GrantFiled: October 1, 2009Date of Patent: January 11, 2011Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wahendorff-Neumann, Karl-Heinz Kuck
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Patent number: 7863304Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.Type: GrantFiled: November 20, 2007Date of Patent: January 4, 2011Assignee: Neuren Pharmaceuticals LimitedInventors: Margaret Anne Brimble, Paul William Richard Harris, Frank Sieg
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Publication number: 20100324071Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
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Patent number: 7842707Abstract: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.Type: GrantFiled: July 21, 2005Date of Patent: November 30, 2010Assignee: Nuada, LLCInventors: Susan Marie Royalty, James Ford Burns, Jan Jozef Scicinski, Gunnar Erik Jagdmann, Jr., Robert James Foglesong, Kellee Griffin Ring, Tatyana Dyakonov, David Middlemiss
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20100286116Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: ApplicationFiled: April 28, 2010Publication date: November 11, 2010Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20100286112Abstract: The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: September 10, 2008Publication date: November 11, 2010Inventors: Oscar Barba, Stuart Edward Bradley, Matthew Colin Thor Fyfe, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Christine Reynet McCormack, Karen Lesley Schofield, Donald Smyth, Alan John William Stewart, Simon Andrew Swain, Peter Widdowson
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Publication number: 20100286146Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: April 27, 2010Publication date: November 11, 2010Applicant: Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger
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Publication number: 20100286170Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.Type: ApplicationFiled: September 24, 2008Publication date: November 11, 2010Inventors: Arun K. Ghosh, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, John C. Lilly, Geoffrey M. Bilcer
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Patent number: 7825068Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: April 6, 2006Date of Patent: November 2, 2010Assignee: Bayer Cropscience AGInventors: Darren Mansfield, Heiko Rieck, Pierre-Yves Coqueron, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Publication number: 20100267688Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 15, 2010Publication date: October 21, 2010Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Patent number: 7812026Abstract: The present invention relates to novel imidazole 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 R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: GrantFiled: December 21, 2006Date of Patent: October 12, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20100239520Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 22, 2007Publication date: September 23, 2010Inventors: Natalie Dales, Zaihui Zhang
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Publication number: 20100240903Abstract: The invention relates to crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.Type: ApplicationFiled: March 22, 2010Publication date: September 23, 2010Applicant: Onyx Therapeutics, Inc.Inventors: Pasit Phiasivongsa, Louis C. Sehl
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander