Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/447)
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Publication number: 20130225619Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20130217706Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Yoúng-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20130217759Abstract: The invention provides sulphonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: October 12, 2011Publication date: August 22, 2013Applicant: Zafgen Inc.Inventors: Robert Zahler, Hazel Joan Dyke, Thomas David Pallin, Susan Mary Cramp
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Patent number: 8513298Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: January 14, 2011Date of Patent: August 20, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Michael O'Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
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Publication number: 20130203706Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2012Publication date: August 8, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8501802Abstract: The present invention relates to co-crystals of duloxetine and co-crystal formers selected from COX-INHIBITORs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.Type: GrantFiled: May 20, 2009Date of Patent: August 6, 2013Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Helmut Heinrich Buschmann, Lluis Solá Carandell, Jordi Benet Buchholz, Jordi Carles Ceròn Bertran, Jesüs Ramirez Artero
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Publication number: 20130190289Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2012Publication date: July 25, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130183266Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A biological probe comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2012Publication date: July 18, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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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: 8450363Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: GrantFiled: February 5, 2010Date of Patent: May 28, 2013Assignee: Elan Pharmaceuticals, Inc.Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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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: 8436041Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica, NVInventor: Jay M. Matthews
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Publication number: 20130096106Abstract: 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: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventor: Vertex Pharmaceuticals (Canada) Incorporated
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Patent number: 8420695Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: GrantFiled: July 1, 2009Date of Patent: April 16, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
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Patent number: 8410150Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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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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Publication number: 20130079348Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 2, 2011Publication date: March 28, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8389567Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: December 10, 2008Date of Patent: March 5, 2013Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Patent number: 8383670Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1, and R4 are defined herein, and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: March 17, 2011Date of Patent: February 26, 2013Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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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: 20120322797Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.Type: ApplicationFiled: December 9, 2010Publication date: December 20, 2012Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY, ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
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Publication number: 20120302561Abstract: The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.Type: ApplicationFiled: April 27, 2012Publication date: November 29, 2012Applicants: THE PENN STATE RESEARCH FOUNDATION, THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David A. Antonetti, Paul Titchenell
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Publication number: 20120301430Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: August 10, 2012Publication date: November 29, 2012Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Real Denis
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Publication number: 20120289587Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: July 19, 2012Publication date: November 15, 2012Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, David P.M. Pleynet, Soan Cheng, Jeffrey P. Whitten
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Patent number: 8309554Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: May 14, 2009Date of Patent: November 13, 2012Assignee: Threshold PharmaceuticalsInventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Publication number: 20120276121Abstract: The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.Type: ApplicationFiled: July 13, 2012Publication date: November 1, 2012Applicants: INSTITUTO DE MEDICINA MOLECULAR, FACULDADE DE MEDICINA DA UNIVERSIDADE DE LISBOA, CENIX BIOSCIENCE GMBHInventors: MICHAEL HANNUS, CECILIE MARTIN, MARIA M. MOTA, MIGUEL PRUDENCIO, CHRISTINA DIAS RODRIGUES
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Publication number: 20120269864Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: June 11, 2012Publication date: October 25, 2012Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
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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: 20120237627Abstract: A pharmaceutical composition characterized in that the composition contains at least 4 wt % relative to the total weight of the composition of an active principle selected from among cetearyl octanoate and hexanoic acid, beeswax and optionally one or more pharmaceutically acceptable excipient(s), as well as to the use thereof for the treatment of cutaneous pre-burns or burns and for reducing pain following a thermal shock.Type: ApplicationFiled: December 10, 2010Publication date: September 20, 2012Applicant: 45 SEC. LLCInventor: Jean-Jacques Debetencourt
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Patent number: 8263641Abstract: Described herein are compounds of Formula I and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also describe herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 15, 2008Date of Patent: September 11, 2012Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, David P. M. Pleynet, Soan Cheng, Jeffrey P. Whitten
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Publication number: 20120225895Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
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Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
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Publication number: 20120202750Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: January 23, 2012Publication date: August 9, 2012Applicant: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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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: 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: 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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Patent number: 8198271Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyleType: GrantFiled: May 25, 2009Date of Patent: June 12, 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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Patent number: 8193372Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.Type: GrantFiled: March 3, 2010Date of Patent: June 5, 2012Assignee: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
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Patent number: 8188145Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.Type: GrantFiled: April 18, 2005Date of Patent: May 29, 2012Assignee: Magnachem International Laboratories, Inc.Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
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Patent number: 8183281Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Neil John Press, Simon James Watson
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Publication number: 20120122862Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: January 30, 2012Publication date: May 17, 2012Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20120115915Abstract: Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N?-diarylureas and/or N,N?-diarylthiourea compounds are described.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Applicant: President and Fellows of Harvard CollegeInventors: Bertal Huseyin Aktas, José A. Halperin, Michael Chorev
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Publication number: 20120108636Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
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Publication number: 20120108573Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
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Patent number: 8158675Abstract: 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: GrantFiled: July 24, 2009Date of Patent: April 17, 2012Assignee: 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: 20120077804Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.Type: ApplicationFiled: July 24, 2008Publication date: March 29, 2012Applicant: The Regents of the University of CaliforniaInventor: Shou-Wei Ding
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Publication number: 20120070369Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.Type: ApplicationFiled: December 10, 2009Publication date: March 22, 2012Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Othon Iliopoulos, Michael Zimmer
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Publication number: 20120065231Abstract: The present invention provides a compound represented by the formula (I) or its salt, solvate, or physiologically functional derivative; and a pharmaceutical composition which is useful for treatment or prevention of conditions or disorders having sensitivity to selective androgen receptor modulation, the composition comprising the above-described compound; among others:Type: ApplicationFiled: April 28, 2010Publication date: March 15, 2012Applicant: SUMITOMO CHEMICAL COMPANY LTD.Inventors: Koichiro Harada, Kozo Motonaga, Koichi Saito, Akio Tanaka