Additional Hetero Ring Patents (Class 514/444)
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Patent number: 8513297Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: GrantFiled: January 18, 2012Date of Patent: August 20, 2013Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Laurence Clary, Corinne Millois Barbuis
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Publication number: 20130210828Abstract: The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity.Type: ApplicationFiled: July 13, 2011Publication date: August 15, 2013Inventors: David G. Whitten, Kirk S. Sehanze, Anand Parthsaray, Eunkyung Ji, Motokatsu Ogawa, Thomas S. Corbitt, Dimitri Dascier, Ying Wang, Linnea K. Ista
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Publication number: 20130184277Abstract: The present invention provides adamantyl diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: February 1, 2013Publication date: July 18, 2013Applicant: H. Lundbeck A/SInventor: H. Lundbeck A/S
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Publication number: 20130183388Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: LANKENAU INSTITUTE FOR MEDICAL RESEARCHInventor: Lankenau Institute for Medical Research
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 8476309Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: GrantFiled: August 20, 2010Date of Patent: July 2, 2013Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20130149314Abstract: Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying anti-tumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed.Type: ApplicationFiled: February 9, 2011Publication date: June 13, 2013Inventors: Jörn Bullerdiek, Dominique N. Markowski
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Publication number: 20130136719Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: May 25, 2012Publication date: May 30, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson
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Patent number: 8449914Abstract: A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, including a human, in such a manner that a prolonged residence of carvedilol is obtained in the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(?) carvedilol for obtaining the desired therapeutic effect.Type: GrantFiled: March 13, 2008Date of Patent: May 28, 2013Assignee: Egalet Ltd.Inventors: Christine Andersen, Gina Fischer, Daniel Bar-Shalom, Lillian Slot, Anne-Marie Lademann
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Patent number: 8436013Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.Type: GrantFiled: July 9, 2009Date of Patent: May 7, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: Chen Liu, David A. Ostrov
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Publication number: 20130096129Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).Type: ApplicationFiled: July 20, 2012Publication date: April 18, 2013Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Patent number: 8410163Abstract: Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.Type: GrantFiled: February 9, 2010Date of Patent: April 2, 2013Assignee: Telik, Inc.Inventors: Paul P. Beroza, Komath V. Damodaran, Stella Lui, Wenli Ma, Zhuo Wang, Hua Xu
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Patent number: 8404855Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: December 22, 2011Date of Patent: March 26, 2013Assignee: Bayer CropScience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald
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Patent number: 8404859Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: GrantFiled: February 17, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Publication number: 20130065849Abstract: The invention relates to compounds of formula (I) wherein the groups A and B represent independently from each other —CH?CH—, or —C?C—, the terms t, u, v, w represent, independently from each other, values ranging from 0 to 9, the groups Y1 and Y2 can represent independently from each other an alkyl group (linear, branched or substituted) carrying from 1 to 9 carbon atoms, the groups Z1, Z2, Z3, and Z4 can represent independently from each other a chemically reactive group W, such as OH, NH2, SH, the groups Z5 and Z6 represent independently from each other a hydrogen atom, silica nanoparticles functionalized by these compounds, and their use as drugs.Type: ApplicationFiled: December 7, 2010Publication date: March 14, 2013Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, UNIVERSITE DE RENNES 1Inventors: David Brevet, Laurence Raehm, Mireille Blanchard-Desce, Olivier Mongin, Magali Gary-Bobo-Sable-Teychene, Marcel Garcia, Alain Morere, Jean-Olivier Durand
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Publication number: 20130053417Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.Type: ApplicationFiled: March 21, 2012Publication date: February 28, 2013Applicant: JAPAN TOBACCO INC.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
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Publication number: 20130053380Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 28, 2011Publication date: February 28, 2013Applicant: PHENEX PHARMACEUTICALS AGInventors: Olaf Kinzel, Christoph Steeneck, Gerald Klaymann, Michael Albers, Thomas Hoffman, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
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Publication number: 20130039945Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 14, 2013Applicant: Kineta, Inc.Inventors: Shawn P. Iadonato, Kristin Bedard
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Publication number: 20130035323Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Abbott GmbH & Co. KGInventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
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Publication number: 20130030027Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.Type: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Patent number: 8357718Abstract: Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.Type: GrantFiled: February 4, 2008Date of Patent: January 22, 2013Assignee: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thumkunta Jagadeeswar Reddy, Zhang Ming-Qiang
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Publication number: 20130005767Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20120322823Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.Type: ApplicationFiled: August 28, 2012Publication date: December 20, 2012Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
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Patent number: 8334317Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: GrantFiled: October 15, 2008Date of Patent: December 18, 2012Assignee: Amgen Inc.Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St. Jean, Jr., David J. Semin
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Publication number: 20120316197Abstract: This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 22, 2011Publication date: December 13, 2012Applicant: RAQUALIA PHARMA INC.Inventors: Kiyoshi Kanazawa, Kazuhiko Nonomura, Takako Okumura, Shinichi Koizumi
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Publication number: 20120309768Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Applicant: BIONOMICS LIMITEDInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Patent number: 8318772Abstract: The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.Type: GrantFiled: June 23, 2009Date of Patent: November 27, 2012Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Bohua Zhong, Youzhi Zhang, Yanping Zhang, Rui Xue, Xinhua He, Yunfeng Li, Hongxia Chen, Nan Zhao, Meiying Li
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Publication number: 20120295966Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: February 12, 2010Publication date: November 22, 2012Applicant: N30 PHARMACEUTICALS, LLCInventors: Xicheng Sun, Jian Qiu, Jan Wasley
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Publication number: 20120289570Abstract: The present invention concerns methods and compositions for the inhibition or reduction of the primary tumor and metastasis by inhibition of fatty acid binding proteins.Type: ApplicationFiled: March 16, 2012Publication date: November 15, 2012Inventors: Ernst Lengyel, Kristin Nieman, Hilary Kenny
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Publication number: 20120289555Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: February 10, 2011Publication date: November 15, 2012Applicant: N30 PHARMACEUTICALS, LLCInventors: Xicheng Sun, Jian Qiu
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Publication number: 20120283222Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: May 31, 2012Publication date: November 8, 2012Applicant: Ajinomoto Co., Inc.Inventors: Atsushi KONISHI, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
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Publication number: 20120277222Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: May 24, 2012Publication date: November 1, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20120264736Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Applicant: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8288380Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1—W2 represents CH—CH, or Y represents a single bond and W1—W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.Type: GrantFiled: April 17, 2012Date of Patent: October 16, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20120258965Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: ApplicationFiled: June 22, 2012Publication date: October 11, 2012Applicants: The Johns Hopkins University, Cardioxyl PharmaceuticalsInventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Patent number: 8278290Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.Type: GrantFiled: February 14, 2006Date of Patent: October 2, 2012Assignee: Biononics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20120238569Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: ApplicationFiled: February 17, 2012Publication date: September 20, 2012Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Patent number: 8268862Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: January 24, 2011Date of Patent: September 18, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Patent number: 8242159Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.Type: GrantFiled: October 31, 2008Date of Patent: August 14, 2012Assignee: Dong-A Pharmaceutical. Co., LtdInventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
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Patent number: 8222288Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: June 14, 2010Date of Patent: July 17, 2012Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jianyong Chen, Shanghai Yu
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120178780Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20120178697Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.Type: ApplicationFiled: April 1, 2005Publication date: July 12, 2012Inventors: Jie Zheng, Jufang Shan, Dianqing Wu
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Publication number: 20120172351Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.Type: ApplicationFiled: June 8, 2010Publication date: July 5, 2012Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
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Publication number: 20120172345Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 5, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Patent number: 8211893Abstract: Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.Type: GrantFiled: August 18, 2009Date of Patent: July 3, 2012Assignee: The Penn State Research FoundationInventors: David A. Antonetti, Jeffrey M. Sundstrom, Charles D. Smith
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Publication number: 20120164103Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: March 9, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Publication number: 20120157516Abstract: The present invention relates to novel substituted thiophene derivatives useful in therapy of diseases related to misfolded and aggregated proteins.Type: ApplicationFiled: October 19, 2009Publication date: June 21, 2012Inventors: Peter Åsberg, Leif Johansson, Anna Herland, Andreas Åslund, Peter Konradsson