1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
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Patent number: 8389508Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: April 28, 2011Date of Patent: March 5, 2013Assignee: Glaxo Group LimitedInventors: Guanghui Deng, Xichen Lin, Feng Ren, Baowei Zhao
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Patent number: 8377574Abstract: An organic light-emitting device which has high emission efficiency and high durability even at low drive voltage is provided. An organic light-emitting device including an anode, a cathode, and an organic compound layer which is interposed between the anode and the cathode, wherein the organic compound layer include at least one dibenzo[c,g]fluorene compound represented by the following General Formula (1).Type: GrantFiled: May 14, 2009Date of Patent: February 19, 2013Assignee: Canon Kabushiki KaishaInventors: Shigemoto Abe, Jun Kamatani, Chiaki Nishiura
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Patent number: 8372982Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: February 16, 2010Date of Patent: February 12, 2013Assignee: Bayer Cropscience AGInventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20130030180Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).Type: ApplicationFiled: December 13, 2010Publication date: January 31, 2013Applicant: GeneCode ASInventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
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Publication number: 20120329811Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Inventors: Christelle Boléa, Sylvain Celanire
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Patent number: 8334235Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.Type: GrantFiled: June 19, 2009Date of Patent: December 18, 2012Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Jörg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Günther Tietjen, Hiroyuki Hadano
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Patent number: 8324257Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders.Type: GrantFiled: October 3, 2007Date of Patent: December 4, 2012Assignee: Array Biopharma Inc.Inventors: Kateri Ahrendt, Robert Kirk Delisle, Jeremy Hans, Joseph P. Lyssikatos, John E. Robinson, Eli M. Wallace, Qian Zhao
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Patent number: 8309584Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: GrantFiled: September 25, 2008Date of Patent: November 13, 2012Assignee: Green Cross CorporationInventors: Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
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Patent number: 8299103Abstract: 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: June 1, 2010Date of Patent: October 30, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
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Patent number: 8293919Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.Type: GrantFiled: July 23, 2008Date of Patent: October 23, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20120258990Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein G1 and G2 are independently O or S; T is —C(R9R10)—, —C(R11)?C(R12)—, —C?C—, NR13 or O; Y1 and Y2 are independently CR14 or N; Q is —C(?O)—N(R15)-z, —C(?S)—N(R16)-z, —C(?O)—O-z, —N(R17)—C(?O)-z, —N(R18)—C(?S)-z, —N(R19)—C(?O)—O-z or —N(R20)—C(?O)—N(R21)-z, in each case z indicates the bond that is connected to R8; n is 1, 2, 3 or 4 when T is —C(R9R10)—, NR13 or O; n is 1, 2, 3 when T is —C(R11)?C(R12)— or —C?C—; R1, R2, R3, R4, R11, R12 and R14 each independently are hydrogen, halogen, cyano, C1-C4alkyl, or C1-C4haloalkyl; R5, R13, R15, R16, R17, R18, R19, R20 and R21 each independently are hydrogen, C1-C4alkyl or C1-C4alkoxy; R6 and R7 each independently are hydrogen, halogen, cyano, hydroxy, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, C1-C4haloalkyl, C1-C4haloalkoxy, C1-C4haloalkylthio or together from a carbonyl group (?O); R9 and R10 each independentType: ApplicationFiled: November 25, 2010Publication date: October 11, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer, Clemens Lamberth
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Publication number: 20120225879Abstract: The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.Type: ApplicationFiled: October 4, 2010Publication date: September 6, 2012Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFACAS ( CSIC)Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Valle Palomo Ruiz, Daniel Perez Fernandez, Concepción Perez Martín, Ana María Perez Castillo, María Isabel Loza Garcia, María Isabe Cadavid Torres, José Brea Floriani
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Patent number: 8252782Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).Type: GrantFiled: December 18, 2009Date of Patent: August 28, 2012Assignee: Pfizer Inc.Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
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Publication number: 20120149679Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: February 20, 2012Publication date: June 14, 2012Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20120142666Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: June 8, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Publication number: 20120142700Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
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Patent number: 8168567Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.Type: GrantFiled: April 8, 2008Date of Patent: May 1, 2012Assignee: Bayer Cropscience AGInventors: Klaus Kunz, Ralf Dunkel, Jörg Nico Greul, Oliver Guth, Hartmann Benoit, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Ronald Ebbert, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Eva-Maria Franken, Olga Malsam, Klaus Tietjen
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Publication number: 20120101136Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.Type: ApplicationFiled: June 24, 2010Publication date: April 26, 2012Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Jia-Ning Xiang
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Publication number: 20120101134Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.Type: ApplicationFiled: June 24, 2010Publication date: April 26, 2012Applicant: GLAXO GROUP LIMITEDInventors: Guanghui Deng, Xichen Lin, Qinghua Meng, Feng Ren, Jia-Ning Xiang, Heng Xu, Haibo Zhang, Baowei Zhao
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Publication number: 20120101137Abstract: The object of the present invention is to provide a compound having a glucokinase-activating effect. A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.Type: ApplicationFiled: June 26, 2010Publication date: April 26, 2012Applicant: SANWA KAGAKU KENKYUSHO CO., LTD.Inventors: Tokuyuki Yamashita, Kaori Chikamatsu, Naoki Takahashi, Hisakazu Iwai, Masakazu Kogami, Masao Sakairi, Nobuhide Watanabe, Hiroki Fujieda, Daisuke Kataoka, Mitsuhiro Makino, Noriyasu Kato, Toshiyuki Miyazawa, Kazushige Nagai, Nobuyoshi Kasugai, Hiroyo Kataoka, Naoki Hiramatsu, Nobuaki Tsuruta, Yurie Yamada, Mika Miyoshi, Sei Murakami, Izumi Goto, Tohru Izuchi, Kimie Suzuki, Satoko Harada, Martin Lang, Markus Hans-Juergen Seifert, Kristina Kaarina Wolf
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Patent number: 8148380Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: GrantFiled: July 23, 2008Date of Patent: April 3, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120071663Abstract: The present invention relates to various processes for the preparation of N?-(4-{[3-(4-chloro-benzyl)-1,2,4-thiadiazol-5-yl]oxy}-2,5-dimethylphenyl)-N-ethyl-N-methylimidoformamide.Type: ApplicationFiled: August 10, 2011Publication date: March 22, 2012Applicant: Bayer CropScience AGInventors: Frank VOLZ, Thomas Himmler, Klaus Kunz, Jörg Greul, Ulrich Heinemann, Thomas Seitz, Pierre Cristau, Oswald Ort
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Publication number: 20120064181Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: March 15, 2010Publication date: March 15, 2012Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
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Publication number: 20120046273Abstract: Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.Type: ApplicationFiled: March 5, 2010Publication date: February 23, 2012Applicant: MITHRIDION, INC.Inventors: Trevor M. Twose, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Melinda L. Verdone
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Patent number: 8110577Abstract: The present invention provides histone deacetylase inhibitors of general formula (I), a process for the preparation of such compounds and uses of the compounds in medicine, especially in the treatment of cancers and the inhibition of histone deacetylase activity.Type: GrantFiled: October 19, 2007Date of Patent: February 7, 2012Assignee: Queen Mary & Westfield CollegeInventors: Simon Peter Joel, Charles Michael Marson
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Publication number: 20120015988Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: May 4, 2009Publication date: January 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Renee M. Zindell, Patricia Amouzegh, Monika Ermann, Christopher Francis Palmer, Mark Whittaker
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Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20110319379Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.Type: ApplicationFiled: March 4, 2010Publication date: December 29, 2011Inventors: Jeffrey W. Corbett, Angel Guzman-Perez, Jeffrey A. Pfefferkorn, Meihua Tu
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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Patent number: 8071631Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof:Type: GrantFiled: August 16, 2007Date of Patent: December 6, 2011Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University Of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20110269738Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: April 28, 2011Publication date: November 3, 2011Applicant: Glaxo Group LimitedInventors: Guanghui Deng, Xichen Lin, Feng Ren, Baowei Zhao
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Publication number: 20110237589Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: ApplicationFiled: February 4, 2011Publication date: September 29, 2011Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
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Publication number: 20110230477Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.Type: ApplicationFiled: December 7, 2009Publication date: September 22, 2011Applicant: Euroscreen S.A.Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
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Publication number: 20110224259Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: March 3, 2011Publication date: September 15, 2011Applicant: PROBIODRUG AGInventors: Ulrich HEISER, Daniel RAMSBECK, Torsten HOFFMANN, Livia BOEHME, Hans-Ulrich DEMUTH
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Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20110207935Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.Type: ApplicationFiled: October 14, 2009Publication date: August 25, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Masato Iizuka, Hideki Fujikura, Yasushi Takigawa, Masahiro Hiratochi
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Patent number: 8003675Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.Type: GrantFiled: July 6, 2007Date of Patent: August 23, 2011Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
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Publication number: 20110200557Abstract: The present disclosure relates to 2-amidothiadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.Type: ApplicationFiled: October 13, 2009Publication date: August 18, 2011Inventors: Pedro Manuel Grima Poveda, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Manuel Lopez Martinez
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Publication number: 20110178140Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: September 25, 2008Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
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Publication number: 20110172236Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
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Publication number: 20110160211Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: April 27, 2009Publication date: June 30, 2011Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
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Patent number: 7968157Abstract: A discotic nematic material comprising a compound of R1—H1—Ar—H2—R wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon ring; H1 and H2 represent an aromatic hetero ring; and R1 and R2 represent a substituent having from 1 to 30 carbon atoms. The discotic nematic material contains a discotic liquid-crystal compound having a smaller number of side branches and capable of expressing an ND phase.Type: GrantFiled: February 6, 2007Date of Patent: June 28, 2011Assignee: Fujifilm CorporationInventor: Makoto Takahashi
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Publication number: 20110152080Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.Type: ApplicationFiled: June 19, 2009Publication date: June 23, 2011Applicant: Bayer Cropscience AGInventors: Pierre Cristau, Joerg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Guenther Tietjen, Hiroyuki Hadano
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Patent number: 7960556Abstract: The invention provides novel 1,2,4-thiadiazole derivatives useful for preventing or treating an ?-synucleopathy such as Parkinson's disease, as well as pharmaceutical compositions including them as biologically active ingredients, and methods for manufacturing them.Type: GrantFiled: November 22, 2007Date of Patent: June 14, 2011Assignee: NV reMYNDInventors: Gerard Griffioen, Stefaan Wera, Hein Roger Duhamel, Ellen Gommé, Nele Van Damme
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Publication number: 20110136869Abstract: 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: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki