Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Nitrogen Of The Hetero Ring Patents (Class 540/607)
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Patent number: 9947204Abstract: A connection validation apparatus includes a connector engagement mechanism configured to physically engage a connector to connect the connector to a connector interface. The apparatus further includes a connection indication detector located on the connector engagement mechanism and configured to detect at least one of a sound and a vibration corresponding to a secure connection of the connector with the connector interface. The apparatus also includes a connection indicator output unit configured to provide an indication to a user that the connector is securely connected with the connector interface based on the detection of the at least one of the sound and the vibration by the connection indication detector.Type: GrantFiled: September 30, 2014Date of Patent: April 17, 2018Assignee: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Alan F. Benner, Benjamin V. Fasano
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Publication number: 20150087823Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.Type: ApplicationFiled: April 26, 2013Publication date: March 26, 2015Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
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Publication number: 20150038493Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.Type: ApplicationFiled: October 5, 2012Publication date: February 5, 2015Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
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Patent number: 8901295Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: February 21, 2014Date of Patent: December 2, 2014Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Montpellier 1, Universite Paris-EST Creteil val de Marne, Assistance Publique-Hopitaux de Paris, Centre National de la Recherche ScientifiqueInventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Patent number: 8889683Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: September 23, 2011Date of Patent: November 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
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Patent number: 8822679Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: California Institute of TechnologyInventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
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Publication number: 20140228354Abstract: Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.Type: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Applicant: Vivolux ABInventors: Stig Linder, Rolf Larsson
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Patent number: 8802666Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140179687Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: February 21, 2014Publication date: June 26, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Patent number: 8623863Abstract: The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Mark E. Fraley, John D. Schreier
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Patent number: 8624022Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: October 7, 2011Date of Patent: January 7, 2014Assignee: UCB Pharma, S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Patent number: 8609659Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: GrantFiled: December 13, 2010Date of Patent: December 17, 2013Assignee: Neuroscienze Pharmaness S.C.A.R.L.Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Gabriele Murineddu, Luca Pani, Gerard Aime Pinna
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Publication number: 20130203738Abstract: The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g.Type: ApplicationFiled: February 9, 2011Publication date: August 8, 2013Applicants: NAGOYA CITY UNIVERSITY, NAGASAKI UNIVERSITYInventors: Yoshifumi Nishimura, Aritaka Nagadoi, Yuuka Hirao, Yoshio Goshima, Naoya Yamashita, Naoki Miyata, Takayoshi Suzuki, Ryuta Hiraishi, Hiroshi Ueda
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Patent number: 8481527Abstract: The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: GrantFiled: October 27, 2007Date of Patent: July 9, 2013Assignee: Richter Gedeon Nyrt.Inventors: Istvan Vago, Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Monika Vastag
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Patent number: 8470850Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: May 6, 2010Date of Patent: June 25, 2013Assignee: MethylGene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
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Publication number: 20130018044Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: December 21, 2010Publication date: January 17, 2013Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20130012701Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8278329Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH?CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C?C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.Type: GrantFiled: October 26, 2007Date of Patent: October 2, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
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Publication number: 20120228151Abstract: An extraction component enabling the concurrent recovery of gold and/or palladium selectively from a hydrochloric acid media containing the base metals and other contaminants. The disclosed extractant disclosed eliminates the conventional multi-step process for such extraction by providing for an extraction method which uses a single solvent extraction reagent. Further enhancing the conventional multi step process, the conventional scrubbing stage is eliminated by a single stripping stage. The resulting solutions can be obtained from leaching many types of material such as copper anode slimes, the treatment of scrap such as electronic circuit boards and plating effluents, PGM, or refractory gold ores.Type: ApplicationFiled: March 7, 2011Publication date: September 13, 2012Inventors: Loghman Moradi, Hiwa Salimi, Mohammad Piltan, Issa Yavari
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Publication number: 20120184438Abstract: This invention relates to agrochemical compositions comprising a benzamide compound of formula (I) where R1 is fluoro, methoxy or C1-4 alkyl; R2 and R3 are each independently optionally substituted C1-6 alkyl or optionally substituted C2-6 alkenyl; or R3 is hydrogen and R3 is optionally substituted C5-8 alkyl or optionally substituted C4-6 alkenyl or optionally substituted benzyl; or R2 and R3 and the nitrogen atom to which they are both attached together form an optionally substituted 5-, 6- or 7-membered ring, which ring optionally contains at least one further heteroatom selected from O, N and S; to the use of those benzamide compounds as solvents; to certain novel compounds of formula (I); and to a process for preparing those novel compounds.Type: ApplicationFiled: July 15, 2010Publication date: July 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Gordon Alistair Bell, David Stock, Jeffrey Steven Wailes
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Patent number: 8173638Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: November 15, 2007Date of Patent: May 8, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Publication number: 20120065193Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: James Arnold, Andrew Todd Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
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Publication number: 20120029188Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Applicant: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20110257130Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Inventor: Desikan Rajagopal
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Publication number: 20110172208Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Publication number: 20110086311Abstract: A photosensitive resin composition which is excellent in resolution, low in cost, and usable in a wide range of structures of polymer precursors each of which is reacted into a final product by a basic substance or by heating in the presence of a basic substance. The photosensitive resin composition includes a base generator which has a specific structure and generates a base by exposure to electromagnetic radiation and heating, and a polymer precursor which is reacted into a final product by the base generator and by a basic substance or by heating in the presence of a basic substance.Type: ApplicationFiled: March 30, 2009Publication date: April 14, 2011Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori
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Publication number: 20110021358Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.Type: ApplicationFiled: July 20, 2010Publication date: January 27, 2011Applicant: Marrone Bio Innovations, Inc.Inventors: Huazhang Huang, Ratnakar Asolkar
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Publication number: 20100266717Abstract: Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from Pseudomonas and/or Erwinia. Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions.Type: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Applicant: Marrone Bio Innovations, Inc.Inventors: Ratnakar Asolkar, Sarahann Dow, Huazhang Huang, Marja Koivunen, Pamela Marrone, Stephanie Shu
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Patent number: 7772247Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: July 28, 2005Date of Patent: August 10, 2010Assignee: Methylgene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Naomy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Llewellyn
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Patent number: 7754709Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: GrantFiled: June 7, 2004Date of Patent: July 13, 2010Assignee: Solvay Pharmaceuticals BVInventors: Kristiina Waehaelae, Annamaria Lilienkampf, Sari Alho, Kaisa Huhtinen, Nina Johansson, Pasi Koskimies, Kimmo Vihko
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Publication number: 20100168083Abstract: Novel substituted adamantane based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: March 20, 2007Publication date: July 1, 2010Inventor: Soren Ebdrup
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Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 7678785Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: July 24, 2007Date of Patent: March 16, 2010Assignee: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20100035861Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both ACHE and A? aggregation. The most potent compound inhibited both ACHE and BCHE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.Type: ApplicationFiled: July 24, 2007Publication date: February 11, 2010Inventors: Zhuibai Qiu, Qiong Xie, Hongzhuan Chen, Hao Wang, Zheng Xia, Meiyan Lu
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Publication number: 20090281085Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 3, 2009Publication date: November 12, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20090264414Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: June 29, 2009Publication date: October 22, 2009Applicant: High Point Pharmaceuticals, LLCInventors: Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen, John Paul Kilburn
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Publication number: 20090209520Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2? together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is formula (ii): where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F.Type: ApplicationFiled: June 15, 2007Publication date: August 20, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Sylvie Gomez, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090203675Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: December 6, 2005Publication date: August 13, 2009Applicant: SIGA TECHNOLOGIES, INC.Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
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Publication number: 20090181951Abstract: A compound of the formula (I), and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRC1RC2—(CH2)m—, where m is 0 or 1, Rc1 is selected from CH3 and CF3, and Rc2 is selected from H and CH3, or RC1 and RC2 together with the carbon atom to which they are attached form the 1,1-cyclopropylene group (a), RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocyclic ring; Het is selected from: (i), where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and (ii), where Q is O or S.Type: ApplicationFiled: June 15, 2007Publication date: July 16, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Sylvie Gomez, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090018116Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: May 20, 2005Publication date: January 15, 2009Applicant: ASTRAZENECA ABInventors: Shujuan Jin, Ziping Liu, Claire Milburn, Miroslaw Tomaszewski, Christopher Walpole, Zhong-Yong Wei, Hua Yang
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Publication number: 20080207898Abstract: The present invention provides processes and intermediates for the preparation of aminoethoxybenzyl alcohols of Formula I useful in the production of pharmaceutically useful compounds.Type: ApplicationFiled: April 17, 2008Publication date: August 28, 2008Applicant: WYETHInventors: Pietro ALLEGRINI, Giuseppe BARRECA, Giorgio SORIATO
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Publication number: 20080119459Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: ApplicationFiled: February 16, 2006Publication date: May 22, 2008Inventors: Bruno Roux, Isabelle Berard
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Patent number: 7291738Abstract: The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods, and processes and intermediates useful for preparing compounds of formula I.Type: GrantFiled: February 27, 2003Date of Patent: November 6, 2007Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 7285547Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.Type: GrantFiled: December 20, 2001Date of Patent: October 23, 2007Assignee: LEK Pharmaceuticals d.d.Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomaz Solmajer, Gregor Mlinsek
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Patent number: 7241902Abstract: Compounds which are the reaction product of allicin and ACE-inhibiting compounds are useful in treating hypertension, elevated triglycerides, and elevated insulin.Type: GrantFiled: May 30, 2002Date of Patent: July 10, 2007Assignee: Yeda Research and Development Co. Ltd.Inventors: Talia Miron, Aharon Rabinkov, David Mirelman, Meir Wilchek
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6921822Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.Type: GrantFiled: June 9, 2003Date of Patent: July 26, 2005Assignee: Bayer AktiengesellschaftInventors: Hans-Christian Militzer, Boris Bosch, Markus Eckert, Benjamin Meseguer
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher