Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/375.1)
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Publication number: 20100234439Abstract: The present invention relates to a 1,5-diphenylpyrazole compound and its use in the treatment of obesity, psychiatric and neurological disorders, to methods for the its therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 18, 2007Publication date: September 16, 2010Inventor: Leifeng Cheng
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Publication number: 20100234438Abstract: The present invention relates to a 1,5-diphenylpyrazole compound and its use in the treatment of obesity, psychiatric and neurological disorders, to methods for the its therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 18, 2007Publication date: September 16, 2010Inventor: Leifeng Cheng
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Patent number: 7795448Abstract: Provided are compounds of Formula V and pharmaceutically acceptable salts thereof which may be useful for the treatment of cancer or other proliferative disorders.Type: GrantFiled: May 6, 2005Date of Patent: September 14, 2010Assignee: Cytokinetics, IncorporatedInventors: Xiangping Qian, Andrew I. McDonald, Han-Jie Zhou, Luke W. Ashcraft, Bing Yao, Hong Jiang, Jennifer Kuo Chen Huang, Jianchao Wang, David J. Morgans, Jr., Bradley P. Morgan, Gustave Bergnes, Dashyant Dhanak, Steven D. Knight, Nicholas D. Adams, Cynthia A. Parrish, Kevin Duffy, Duke Fitch, Rosanna Tedesco
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Patent number: 7790905Abstract: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.Type: GrantFiled: December 29, 2003Date of Patent: September 7, 2010Assignee: McNeil-PPC, Inc.Inventors: Mark Tawa, Örn Almarsson, Julius Remenar
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Patent number: 7790756Abstract: The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.Type: GrantFiled: October 10, 2007Date of Patent: September 7, 2010Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A Petillo, Michael D Kaufman
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Patent number: 7786161Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: GrantFiled: October 27, 2008Date of Patent: August 31, 2010Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20100216859Abstract: Novel curcumin-analog compounds are disclosed that are antioxidants useful in inhibition of pro-inflammation, angiogenic, and vascular permeability factors and elimination of reactive oxygen species. The curcumin compounds specifically inhibit VEGF and are useful in treating various diseases that are mediated through the oxidative stress pathway, including those that are characterized by inflammation, angiogenesis, or vascular leakage.Type: ApplicationFiled: October 14, 2009Publication date: August 26, 2010Inventor: Danyang Chen
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Publication number: 20100190981Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: ApplicationFiled: January 14, 2010Publication date: July 29, 2010Inventors: Jiacheng Zhou, Pingli Liu, Qiyan Lin, Brian W. Metcalf, David Meloni, Yongchun Pan, Michael Xia, Mei Li, Tai-Yuen Yue, James D. Rodgers, Haisheng Wang
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Publication number: 20100179203Abstract: This invention relates to novel pyrazole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: June 27, 2008Publication date: July 15, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen, David Spencer Jones
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Patent number: 7745477Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: GrantFiled: January 25, 2007Date of Patent: June 29, 2010Assignee: Hoffman-La Roche Inc.Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Publication number: 20100144812Abstract: Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.Type: ApplicationFiled: February 19, 2010Publication date: June 10, 2010Applicant: Wyeth LLPInventors: Lynn Resnick, Donna M. Huryn, Joan E. Sabalski, Joshua D. Berkowitz, Anthony Frank Kreft, Dennis Martin Kubrak, Thomas Joseph Caggiano, Koi Michele Morris
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100137322Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.Type: ApplicationFiled: April 22, 2008Publication date: June 3, 2010Applicant: ASTRAZENECA ABInventors: Yevgeni Besidski, Inger Kers, Martin Nylof, Lars Sandberg, Karin Skogholm
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Patent number: 7723370Abstract: The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2—COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.Type: GrantFiled: July 27, 2006Date of Patent: May 25, 2010Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: János Fischer, Istvánné Kis-Varga, György Szabo, János Leibinger
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Patent number: 7713974Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: GrantFiled: August 15, 2007Date of Patent: May 11, 2010Assignee: Roche Palo Alto LLCInventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
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Publication number: 20100111858Abstract: The present invention provides conjugates useful for the diagnosis and treatment of diseases associated with the over-expression of COX-2. The conjugates comprise a selective COX-2 targeting carrier, a metal coordinating moiety, and a linker chemically linking the metal coordinating moiety to the carrier. The metals coordinated by the metal coordinating moiety are selected from paramagnetic or radioisotopes. The invention also includes kits comprising a conjugate and a radioisotope solution.Type: ApplicationFiled: January 17, 2008Publication date: May 6, 2010Inventors: Carol P. Howard, Dennis A. Moore
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Patent number: 7700607Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: July 18, 2007Date of Patent: April 20, 2010Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Publication number: 20100094006Abstract: The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.Type: ApplicationFiled: September 28, 2009Publication date: April 15, 2010Inventors: Ghilsoo NAM, Kyung Il Choi, Hye Ran Kim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Hyunah Choo, Hyewhon Rhim, Yong Seo Cho, Eun Joo Roh, Gyo Chang Keum, Kee Hyun Choi, Kye Jung Shin, Hoh Gyu Hahn, Chan Seong Cheong, Jae Kyun Lee, Kee Dal Nam, Yong Koo Kang, Youngsoo Kim, Woong Seo Park, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Dong Yun Shin, Chi man Song
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Publication number: 20100062942Abstract: The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to their use as pesticides, microbicides and herbicides.Type: ApplicationFiled: November 12, 2009Publication date: March 11, 2010Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Mark Wilhelm Drewes
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Publication number: 20100041665Abstract: The present invention is related to a family of N-phenyl-prenylamine derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.Type: ApplicationFiled: August 1, 2007Publication date: February 18, 2010Applicant: NOSCIRA, S.A.Inventors: Ana Martinez Gil, Ana Castro Morera, Miguel Medina Padilla, Pilar Munoz Ruiz, Javier Lopez Ogalla, Esther Garcia Palomero, Celia De Austria De Luque, Paola Usan Egea, Rita Valenzuela Liminana, Pablo Garcia Fernandez, Elena Delgado Hernandez, Daniel Ignacio Perez Fernandez
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Publication number: 20100041709Abstract: The present invention relates to compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as defined herein. The invention further relates to preparation and therapeutic use of these compounds.Type: ApplicationFiled: June 24, 2009Publication date: February 18, 2010Applicant: SANOFI-AVENTISInventors: Francis BARTH, Christian Congy, Serge Martinez, Murielle Rinaldi-Carmona, Martine Vernhet
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Patent number: 7659298Abstract: 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: GrantFiled: June 21, 2006Date of Patent: February 9, 2010Assignee: 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: 20100022605Abstract: Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) eachindicates a point of attachment.Type: ApplicationFiled: December 4, 2006Publication date: January 28, 2010Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Publication number: 20100016612Abstract: The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same. A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like. The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.Type: ApplicationFiled: February 13, 2008Publication date: January 21, 2010Applicant: Mitsui Chemicals Agro, IncInventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
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Patent number: 7645757Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt; where the variables are as defined in the attached specification.Type: GrantFiled: August 14, 2006Date of Patent: January 12, 2010Assignee: sanofi-aventisInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Patent number: 7642263Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and prodrugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: September 2, 2008Date of Patent: January 5, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20090318703Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: ApplicationFiled: October 27, 2008Publication date: December 24, 2009Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20090306396Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: October 3, 2006Publication date: December 10, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
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Publication number: 20090306129Abstract: The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).Type: ApplicationFiled: September 11, 2006Publication date: December 10, 2009Inventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Vinayak Vasantrao Khairnar, Mandadapu Raghuramaiah, Abhijit Ray, Sunanda Ghose Dastidar
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Publication number: 20090275588Abstract: The invention relates to novel sulfonamide compounds and their use as orexin receptor antagonists.Type: ApplicationFiled: April 10, 2007Publication date: November 5, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornella Zumbrunn Acklin
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Publication number: 20090275617Abstract: Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.Type: ApplicationFiled: September 28, 2006Publication date: November 5, 2009Inventors: Hirokatsu Ito, Kensuke Kobayashi, Hisashi Ohta, Osamu Okamoto, Satoshi Ozaki, Tomohiro Tsujita
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Publication number: 20090247586Abstract: Novel carboxamides of the formula (I) The present application is further directed toward 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 5, 2006Publication date: October 1, 2009Applicant: Bayer CropScienceInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 7592338Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: August 2, 2007Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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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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Patent number: 7576116Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof, and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.Type: GrantFiled: September 28, 2007Date of Patent: August 18, 2009Assignee: The Ohio State University Research FoundationInventor: Ching-Shih Chen
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Publication number: 20090197935Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: May 17, 2007Publication date: August 6, 2009Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jingdong Xu, Ning Zou
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Publication number: 20090186924Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: ApplicationFiled: March 19, 2009Publication date: July 23, 2009Applicants: Pfizer Inc., Pfizer Products Inc..Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Publication number: 20090170873Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 17, 2008Publication date: July 2, 2009Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20090156651Abstract: 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: ApplicationFiled: April 6, 2006Publication date: June 18, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Alain Villier, Pierre Genix, Marie-Claire Grosjean-Cournoyer
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Publication number: 20090149524Abstract: The present invention relates to novel pyrazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.Type: ApplicationFiled: June 5, 2007Publication date: June 11, 2009Inventors: Paul John Beswick, Laura J. Chambers, David John Davies, David Kenneth Dean, Emmanuel Hubert Demont, Susan Roomans, Daryl Simon Walter
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Publication number: 20090143454Abstract: The present invention relates to novel pyrazoline derivatives of the formula (I) in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests, and further relates to novel intermediates and processes for their preparation.Type: ApplicationFiled: July 8, 2002Publication date: June 4, 2009Applicant: BAYER CROPSCIENCE AGInventors: Fritz Maurer, Rainer Fuchs, Christoph Erdelen, Angelika Lubos-Erdelen, Udo Reckmann, Andreas Turberg
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Patent number: 7541377Abstract: This invention provides compounds of Formula I, and N-oxides and salts thereof wherein A, B, R1 through R5, R7 through R9, X and Y are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I. Also disclosed are compositions for controlling an invertebrate pest comprising the compounds of Formula I.Type: GrantFiled: January 31, 2007Date of Patent: June 2, 2009Assignee: E.I. du Pont de Nemours and CompanyInventors: Bruce Lawrence Finkelstein, George Philip Lahm, Stephen Frederick McCann, Thomas Paul Selby, Ying Song, Thomas Martin Stevenson
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Publication number: 20090137524Abstract: This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as described herein, and one or more further biologically active compounds as described herein, particularly anti-parasitic agents.Type: ApplicationFiled: February 3, 2009Publication date: May 28, 2009Inventors: Denis Billen, Nathan Anthony Logan Chubb, David Morris Gethin, Kim Thomas Hall, Lee Richard Roberts, Nigel Derek Arthur Walshe
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Publication number: 20090131256Abstract: The present invention relates to 1-(azolin-2-yl)-amino-2-aryl-1-hetaryl-ethane compounds (I) and 1-(aminothiocarbonylamino)-2-aryl-1-hetaryl-ethane compounds (II) and their salts which are useful for combating animal pest, in particular insects, arachnids and nematodes. Furthermore, the present invention relates to a method for combating animal pests selected from insects, arachnids and nematodes, and to agricultural compositions for combating animal pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests.Type: ApplicationFiled: June 29, 2007Publication date: May 21, 2009Applicant: BASF SEInventors: Markus Kordes, Delphine Breuninger, Ronan Le Vezouet, Christopher Koradin, Livio Tedeschi, Michael Puhl, Deborah L. Culbertson
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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: 20090118335Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.Type: ApplicationFiled: March 30, 2007Publication date: May 7, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Masahiro Kajino, Haruyuki Nishida
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Publication number: 20090111996Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: April 30, 2009Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20090111860Abstract: The present invention relates to compounds of formula (I) that mediate Edg, including Edg-1, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant vascularization or inflammatory component such as in tumor-related diseases. The present invention also relates to compounds that inhibit a5bl, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: April 20, 2007Publication date: April 30, 2009Applicant: ASTRAZENECA ABInventors: Gurmit Grewal, Edward Hennessy, Victor Kamhi, Danyang Li, Vibha Oza, Jamal Carlos Saeh, Qibin Su
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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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