Additional Ring Containing Patents (Class 546/337)
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Publication number: 20100158798Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: ApplicationFiled: February 8, 2010Publication date: June 24, 2010Inventor: Emmanuel Skordalakes
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Publication number: 20100152207Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: June 17, 2010Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20100145045Abstract: Process for the protection of fish and invertebrates and all their stages of development against mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of abovementioned, selected fungicides. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms. The addition of the composition according to the invention to the water decreases fungal infections of spawn and fish.Type: ApplicationFiled: April 10, 2008Publication date: June 10, 2010Applicant: Bayer CropScience AGInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20100145056Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: ApplicationFiled: November 23, 2009Publication date: June 10, 2010Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
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Publication number: 20100144681Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: June 10, 2010Inventors: Klaus Fuchs, Christian Eickmeier, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Patent number: 7723364Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: July 19, 2004Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier, Isabelle Christian
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Publication number: 20100113536Abstract: The present invention relates to novel compounds of formula [I], wherein R1 represents heteroaryl, at least one substituent among R5, R6 and R7 represent —SR12, —S(O)R12 or —S(O)2R12 and the remaining substituents are as defined in the claims, that act as chemical uncouplers. Compounds of the invention are useful inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases associated therewith.Type: ApplicationFiled: November 15, 2007Publication date: May 6, 2010Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Flemming Elmelund Nielsen
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Patent number: 7700775Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: March 1, 2002Date of Patent: April 20, 2010Assignee: Emisphere Technologies, Inc.Inventors: Jun Liao, David Gschneidner, John J. Weidner, Nai Fang Wang
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Publication number: 20100075942Abstract: The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).Type: ApplicationFiled: January 12, 2006Publication date: March 25, 2010Applicant: ASTRAZENECA ABInventors: Keith Hopkinson Gibson, Elaine Sophie, Elizabeth Stokes, Michael James Waring, David Michael Andrews, Zbigniew Stanley Matusiak, Mark Maybury, Craig Anthony Roberts
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Publication number: 20100063267Abstract: Provided are a bi-functional compound that is positively charged at a first pH and negatively charged at a second pH, a solid support having the bi-functional compound immobilized thereon, and a method of isolating a nucleic acid, including: binding the bi-functional compound with a nucleic acid at a first pH and isolating the nucleic acid from the bi-functional compound at a second pH.Type: ApplicationFiled: September 8, 2009Publication date: March 11, 2010Applicant: SAMSUNG ELECTRONICS CO., LTDInventors: Kyu-youn HWANG, Joon-ho KIM
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Publication number: 20100056794Abstract: Process for the preparation of 2,5-bis(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)benzamide, its pharmaceutically acceptable salts and important intermediates thereof that involves 1,4-dihalotoluenes as starting material. The method involves a technique for preparing the starting material 2,5-bis(2,2,2-trifluoroethoxy)toluene in high yields by reacting 1,4-dibromotoluene with 2,2,2-trifluoroethanol in presence of a base and a copper-containing catalyst.Type: ApplicationFiled: November 2, 2007Publication date: March 4, 2010Applicant: GRINDEKS A JOINT STOCK COMPANYInventors: Daina Zicane, Janis Jaunbergs
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Publication number: 20100056585Abstract: The crystalline Polymorph B of N-(2-aminophenyl)-4-[N-(pyridine-3-yl)methoxy-carbonyaminomethyl]benzamide (MS-275) of formula I is described, as well as the process for the production of said compound, and its use as a medicament for the treatment of selected diseases.Type: ApplicationFiled: August 28, 2009Publication date: March 4, 2010Applicant: BAYER SCHERING PHARMA AGInventors: Matthias Schneider, Michael Gottfried, Jens Geisler, Gabriele Winter
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Publication number: 20100035880Abstract: This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)Type: ApplicationFiled: October 13, 2009Publication date: February 11, 2010Inventors: TAKESHI HANAZAWA, MISATO HIRANO, TADASHI INOUE, SATOSHI NAGAYAMA, KAZUNARI NAKAO, YUJI SHISHIDO, HIROTAKA TANAKA
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Publication number: 20100022781Abstract: The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.Type: ApplicationFiled: April 24, 2009Publication date: January 28, 2010Inventors: Torsten Steinmetzer, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghisch, Jochen Heinicke
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Publication number: 20100016278Abstract: The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: ApplicationFiled: June 17, 2009Publication date: January 21, 2010Applicant: SANOFI-AVENTISInventors: Hartmut STROBEL, Paulus WOHLFART, Gerhard ZOLLER, David William WILL
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Publication number: 20100016410Abstract: Disclosed are compositions and methods for regulating eosinophils.Type: ApplicationFiled: May 17, 2007Publication date: January 21, 2010Inventors: Lori A. Wagner, Katrin Szardenings, Gerald J. Gleich, Tarek Aboul-Fadl Mohamed
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Publication number: 20100016379Abstract: Described herein are compounds having a terephthalamate structural feature. Also described herein, are methods of making such compounds, methods of using such compounds to modulate the activity of HIV integase, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology of AIDS or infection with HIV.Type: ApplicationFiled: April 18, 2007Publication date: January 21, 2010Applicant: IRM LLCInventors: Yun He, Zhiwei Wang, Baogen Wu
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Publication number: 20090318497Abstract: This invention provides a compound of the formula (I): wherein A1 is N and A2 is CR7, or A1 is CR7 and A2 is N; Y1, Y2 and Y3 are each independently CH or N, Y4 and Y5 are each independently CR8 or N, with the proviso that when one of Y1, Y2, Y3, Y4 and Y5 is N, the others are not N; R1 and R2 are each independently hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; R3 and R8 are each independently hydrogen, halogen, hydroxy, (C1-C6)alkyl, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R4 is halogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; and R5, R6 and R7 are each independently hydrogen, halogen, (C1-C6)alkyl, hydroxy(C1-C6)alkyl, orType: ApplicationFiled: September 10, 2007Publication date: December 24, 2009Inventors: Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka
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Publication number: 20090318290Abstract: A compound of general formula (I) A process for preparing this compound. A fungicidal 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: ApplicationFiled: July 5, 2007Publication date: December 24, 2009Applicant: BAYER CROPSCIENCE SAInventors: Pierre-Yves Coqueron, Philippe Desbordes, Rüdiger Pulheim, Oliver Gaertzen, Pierre Genix, Marie-Chaire Grosjean-Cournoyer, Benoît Hartmann, Klaus Kunz, Darren Mansfield, Mattes Amos, Oswald Ort, Alain Villier
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Patent number: 7635715Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: GrantFiled: December 17, 2007Date of Patent: December 22, 2009Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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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: 20090312370Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: July 20, 2007Publication date: December 17, 2009Inventors: Kurt Laumen, Rainer Machauer, Marina Tintelnot-Blomley, Siem Jacob Veenstra
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Publication number: 20090312328Abstract: [Object] A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom. [Means for Solution] It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.Type: ApplicationFiled: August 9, 2007Publication date: December 17, 2009Applicant: Astellas Pharma Inc.Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
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Publication number: 20090306016Abstract: Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1i and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors.Type: ApplicationFiled: July 27, 2007Publication date: December 10, 2009Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20090291988Abstract: The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.Type: ApplicationFiled: June 14, 2006Publication date: November 26, 2009Inventor: Renata Oballa
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Publication number: 20090286786Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: March 10, 2009Publication date: November 19, 2009Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
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Publication number: 20090281103Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: July 20, 2006Publication date: November 12, 2009Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20090280230Abstract: The present invention relates to the use of certain high potency savory (“umami”) taste modifiers, as savory flavoring agents and/or enhancers of monosodium glutamate, for the preparation of foods, beverages, and other comestible compositions, and to processes for preparing food flavorant compositions for use in the preparation of comestible food and drink.Type: ApplicationFiled: April 19, 2007Publication date: November 12, 2009Inventors: Rhondi Shigemura, Qing Chen, Vincent Darmohusodo, Aaron R. Dean
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Publication number: 20090281089Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: April 8, 2009Publication date: November 12, 2009Applicant: Genentech, Inc.Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca L. LaLonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Publication number: 20090275550Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: April 11, 2007Publication date: November 5, 2009Inventors: James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20090275515Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: October 15, 2007Publication date: November 5, 2009Inventors: Yuntae Kim, Robert S. Meissner, Helen J. Mitchell, James J. Perkins, Michael A. Rossi, Jiabing Wang
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Publication number: 20090270338Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted N-cyclylalkyl-diphenylpropanamide derivatives as shown in formula (1).Type: ApplicationFiled: April 28, 2009Publication date: October 29, 2009Inventors: Robert Galemmo, JR., Richard Holland, Gabriel Hum
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Publication number: 20090270631Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which is associated with a fewer side effects such as body weight gain, adipocyte accumulation, cardiac hypertrophy and the like, and which contains a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: May 5, 2009Publication date: October 29, 2009Inventors: Hidenori Abe, Takeshi Wakabayashi, Kentarou Rikimaru
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Publication number: 20090258884Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: ApplicationFiled: April 16, 2009Publication date: October 15, 2009Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, JR.
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Publication number: 20090258906Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 18, 2008Publication date: October 15, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Josef PERNERSTORFER, Stephen SHIMSHOCK, Carolina LANTER, Raymond KOSLEY
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Publication number: 20090253755Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal 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: ApplicationFiled: July 5, 2007Publication date: October 8, 2009Applicant: Bayer Cropscience SAInventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Philippe Desbordes, Pierre Genix, Benoit Hartmann, Amos Mattes, Klaus Kunz, Rüdiger Fischer, Oliver Gaertzen, Oswald Ort, Darren Mansfield, Alain Villier
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Publication number: 20090239841Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: October 24, 2005Publication date: September 24, 2009Inventors: Alan J. Hutchison, Jun Yuan
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Patent number: 7572818Abstract: Compound of general formula (I) in which p is an integer equal to 1, 2, 3 or 4; q is an integer equal to 1, 2, 3, 4 or 5; each substituent X is chosen, independently of the others, as being halogen, alkyl or haloalkyl, at least one of the substituents being a haloalkyl; each substituent Y is chosen, independently of the others, as being halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, amino, phenoxy, alkylthio, dialkylamino, acyl, cyano, ester, hydroxy, aminoalkyl, benzyl, haloalkoxy, halosulphonyl, halothioalkyl, alkoxyalkenyl, alkylsulphonamide, nitro, alkylsulphonyl, phenylsulphonyl or benzylsulphonyl; as to the N-oxides of 2-pyridine thereof; with the exception of N-{2-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-ethyl}-2,6-dichlorobenzamide. Method for preparing the compound of general formula (I). Fungicidal composition comprising the compound of general formula (I). Method for treating phytopathogenic diseases.Type: GrantFiled: August 8, 2003Date of Patent: August 11, 2009Assignee: Bayer Cropscience S.A.Inventors: Darren James Mansfield, Tracey Cooke, Peter Stanley Thomas, Pierre-Yves Coqueron, Jean-Pierre Vors, Geoffrey Gower Briggs, Hélène Lachaise, Heiko Rieck, Philippe Desbordes, Marie-Claire Grosjean-Cournoyer
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Publication number: 20090197201Abstract: The present invention relates to the use of end groups Y, where Y stands for (formula I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r—, [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, as end group in surface-active compounds, to corresponding novel compounds, and to processes for the preparation of these compounds.Type: ApplicationFiled: July 2, 2007Publication date: August 6, 2009Inventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Publication number: 20090192172Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 8, 2005Publication date: July 30, 2009Applicant: 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: 20090186900Abstract: There is provided a compound of Formula I wherein the various symbols are as defined in the description, and a method of manufacturing a medicament for use in the therapy of a condition or disease associated with 17?-hydroxysteroid dehydrogenase (17?-HSD), comprising a compound of Formula I.Type: ApplicationFiled: August 27, 2008Publication date: July 23, 2009Inventors: Nigel VICKER, Gillian Margaret ALLAN, Harshani Rithma Ruchiranani LAWRENCE, Joanna Mary DAY, Atul PUROHIT, Michael John REED, Barry Victor Lloyd POTTER
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Publication number: 20090182020Abstract: The present invention relates to substituted bis(hetero)aromatic N-ethylpropiolamides, methods for the production thereof, medicaments containing these compounds and the use thereof for the production of medicaments.Type: ApplicationFiled: June 26, 2008Publication date: July 16, 2009Applicant: GRUNENTHAL GMBHInventors: Michael Haurand, Klaus Schiene, Sven Kuhnert, Stefan Oberborsch
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Patent number: 7560567Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal 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: December 16, 2004Date of Patent: July 14, 2009Assignee: Bayer Cropscience S.A.Inventors: Pierre-Yves Coqueron, Philippe Desbordes, Darren James Mansfield, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Alain Villier, Pierre Genix
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Publication number: 20090172897Abstract: The disclosure relates to the dyeing of keratin materials using styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dyes. Disclosed herein is a dye composition comprising a styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dye and a dyeing process with, for example, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are novel thiol/disulfide fluorescent dyes and the uses thereof in lightening keratin materials. This composition makes it possible to obtain a lightening effect which can be resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: July 9, 2009Inventors: Nicolas DAUBRESSE, Andrew GREAVES, Franco MANFRE
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Publication number: 20090124671Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4, R5, m, and n are defined in the specification are TRPV1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: October 23, 2008Publication date: May 14, 2009Applicant: ABBOTT LABORATORIESInventors: Arthur R. Gomtsyan, Robert G. Schmidt, Erol K. Bayburt, Jerome F. Daanen, Michael E. Kort
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Publication number: 20090117185Abstract: The invention relates to 2-(aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of coagulation factor Xa. The compounds are suitable for the treatment and prophylaxis of cardiovascular and thrombotic events.Type: ApplicationFiled: September 18, 2006Publication date: May 7, 2009Inventors: Torsten Steinmetzer, Daniel Doennecke, Andrea Schweinitz, Anne Stuerzebecher, Joerg Stuerzebecher
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Publication number: 20090118339Abstract: The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: ApplicationFiled: May 30, 2007Publication date: May 7, 2009Inventors: Tim Hugo Maria Jonckers, Inge Dierynck, Stefaan Julien Last, Herman De Kock