Additional Hetero Ring Attached Directly Or Indirectly To The Morpholines By Nonionic Bonding Patents (Class 514/232.2)
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Publication number: 20110098267Abstract: The invention relates to a topical composition and a method for treating psoriasis. The topical composition comprises one or more compound that inhibits the production of IL-12 and IL-23.Type: ApplicationFiled: February 6, 2009Publication date: April 28, 2011Applicant: Synta Pharmaceuticals CorporationInventors: Suresh R. Babu, Yumiko Wada, Jianhua Shen, Nhung Nguyen
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Patent number: 7915405Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: September 30, 2009Date of Patent: March 29, 2011Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
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Publication number: 20110070197Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Ce Wang, Yao-Ling Qiu
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Publication number: 20110070196Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20110064696Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20110064695Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Publication number: 20110064697Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20110053891Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 5, 2010Publication date: March 3, 2011Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Peter L. Johnson, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20110033453Abstract: The present invention relates to the use of compounds of formula (I) in the treatment of Epidermal Growth Factor Receptor (EGFR) family members dependent diseases or diseases that have acquired resistance to agents that target EGFR family members, use of said compounds for the manufacture of pharmaceutical compositions for the treatment of said diseases, combinations of said compounds with EGFR modulators for said use, methods of treating said diseases with said compounds and pharmaceutical preparations for the treatment of said diseases comprising said compounds alone or in combination, especially with an EGFR modulator.Type: ApplicationFiled: March 4, 2009Publication date: February 10, 2011Inventors: Carlos Garcia-Echeverria, Sauveur-Michel Maria
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Publication number: 20110028470Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: ApplicationFiled: July 31, 2008Publication date: February 3, 2011Applicants: TOKAI UNIVERSITY EDUCATIONAL SYSTEM, RENASCIENCE CO., LTD., MEDICAL & BIOLOGICAL LABORATORIES CO., LTD.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Publication number: 20110020338Abstract: The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: March 24, 2009Publication date: January 27, 2011Inventor: Carlos Garcia-Echeverria
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Patent number: 7872002Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 18, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
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Patent number: 7863266Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 4, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
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Patent number: 7858614Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: December 28, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Patent number: 7855199Abstract: Heterocyclic compounds represented by the formula I and anti-malignant-tumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; Y represents C1-C6 alkyl; R1 represents morpholino (which may be substituted with one to four C1-C6 alkyl); and R2 and R3 each represent hydrogen atom or C1-C6 alkyl.Type: GrantFiled: March 30, 2005Date of Patent: December 21, 2010Assignee: Zenyaku Kogyo Kabushiki KaishaInventors: Seiichiro Kawashima, Mitsuko Kawashima, legal representative, Hiroto Kawashima, legal representative, Masato Kawashima, legal representative, Toshiyuki Matsuno, Shinichi Yaguchi, Yoshio Tsuchida, Kenichi Saitoh, Tetsuo Watanabe
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Publication number: 20100298312Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: ApplicationFiled: September 3, 2008Publication date: November 25, 2010Applicant: The Scripps Research InstituteInventors: Theodore M. Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael D. Cameron, Derek R. Duckett
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Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100280009Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: December 10, 2008Publication date: November 4, 2010Inventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
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Publication number: 20100267716Abstract: Compounds of pyridinium salts and methods of their use in medicine, particularly in the prophylaxis and treatment of inflammatory conditions, infectious conditions, as well as immune disorders are disclosed. The present invention also relates to methods of controlling fungi and/or bacteria.Type: ApplicationFiled: June 29, 2010Publication date: October 21, 2010Inventors: Richard B. Klein, Jeffrey L. Selph, John J. Partridge, John Reinhard
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Publication number: 20100267667Abstract: The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto.Type: ApplicationFiled: June 4, 2008Publication date: October 21, 2010Applicant: Ben-Gurion University of the Negev Research and Development AuthorityInventors: Aviv Gazit, Shimon Slavin, Esther Priel, Sara Yitzchak
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Publication number: 20100256132Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: ApplicationFiled: March 24, 2010Publication date: October 7, 2010Applicant: Synta Pharmaceuticals CorporationInventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
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Publication number: 20100256097Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 16, 2008Publication date: October 7, 2010Inventors: Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyan Chong Woo, Jonathan Young, Anna Zabierek
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Publication number: 20100249126Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: January 22, 2007Publication date: September 30, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS INC.Inventors: Matthew Burger, Zhi-Jie Ni, Sabina Pecchi, Gordana Atallah, Sarah Bartulis, Kelly Frazier, Aaron Smith, Joelle Verhagen, Yanchen Zhang, Allan Wagman, Simon Ng, Keith Pfister, Daniel J. Poon, Alicia Louie, Teresa Pick, Paul Barsanti, Edwin Iwanowicz, Wendy Fantl, Thomas Hendrickson, Mark Knapp, Hanne Meritt, Charles Voliva, Marion Wiesmann, Xiahua Xin
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Publication number: 20100226883Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 9, 2010Inventors: Yao-Ling Qiu, Lu Ying, Ce Wang, Xiaowen Peng, Yat Sun Or
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Publication number: 20100227858Abstract: A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use intherapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.Type: ApplicationFiled: July 8, 2008Publication date: September 9, 2010Applicant: ASTRAZENECA ABInventors: Maurice Raymond, Verschoyle Finlay, Kurt Gordon Pike
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Publication number: 20100226882Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 9, 2010Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
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Publication number: 20100221216Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 2, 2010Inventors: Yat Sun Or, Datong Tang
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Publication number: 20100204219Abstract: The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R1, R2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C1-C3 alkyl group and a C1-C3 alkoxy group, R3 represents, independently from one another if p is not 0, hydrogen, halogen, a C1-C5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C1-C4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C1-C3 alkyl, a hydroxyl or a benzyl group, a C1-C6 alkylsulfonyl, a mono or disubstituted C1-C5 alkyl group, a branched or a cyclic amine, R6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF3 or a branched or unbranched C1-C4 alkyl group, if m=1Type: ApplicationFiled: December 11, 2007Publication date: August 12, 2010Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Guy Lemaillet, Leonardo Scapozza
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Publication number: 20100173413Abstract: This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.Type: ApplicationFiled: March 11, 2010Publication date: July 8, 2010Applicant: Synta Pharmaceuticals CorporationInventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Howard P. Ng, Zachary Demko
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Publication number: 20100152162Abstract: It is intended to provide an agent for treating and/or preventing sleep disorder containing as an active ingredient a thiazole derivative represented by the general formula (I) (in the formula, R1 represents a five-membered aromatic heterocyclic group containing at least one oxygen atom or the like, R2 represents halogen or the like, and R3 represents —NR10R11 (in the formula, R10 and R11 are the same or different and represent a hydrogen atom or the like) or the like) or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 2, 2006Publication date: June 17, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Shunji Ichikawa, Takao Nakajima
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Patent number: 7737141Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.Type: GrantFiled: July 25, 2007Date of Patent: June 15, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
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Publication number: 20100137275Abstract: The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synthesizing these compounds and also to therapeutic compositions containing these products and to the use thereof as medicaments.Type: ApplicationFiled: April 30, 2008Publication date: June 3, 2010Applicant: IPSEN PHARMA S.A.S.Inventors: Grégorie Prevost, Anne-Marie Liberatore, Dennis Bigg, Dominique Pons
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Publication number: 20100130465Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: May 27, 2010Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga A. Reddy, Lianyun Zhao, Shuyi Tang, Tzu T. Wong, Praveen K. Tadikonda, Luis E. Torres, M. Arshad Siddiqui, Michael P. Dwyer, Kartik M. Keertikar, Timothy J. Guzi
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Publication number: 20100130473Abstract: Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and anType: ApplicationFiled: February 24, 2006Publication date: May 27, 2010Inventors: Marc Geoffrey Hummersone, Sylvie Gomez, Keith Allan Menear, Xiao-Ling Fan Cockcroft, Graeme Cameron Murray Smith
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Publication number: 20100113435Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: ApplicationFiled: November 16, 2009Publication date: May 6, 2010Inventors: Tjeerd BARF, Rikard Emond, Guido Kurz, Jerk Vallgarda, Marianne Nilsson
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Publication number: 20100105674Abstract: The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.Type: ApplicationFiled: March 12, 2008Publication date: April 29, 2010Inventors: Felix Deanda Jr., David Harold Drewry, James Andrew Linn, Paul Reid
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Patent number: 7696202Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: November 10, 2005Date of Patent: April 13, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
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Publication number: 20100061960Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: July 16, 2009Publication date: March 11, 2010Inventors: Franz Ulrich Schmitz, Roopa Rai, Ronald Griffith, Christopher Don Roberts
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Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20100048543Abstract: The invention relates to a compound of the Formula I or salt thereof wherein Rx, Ry, Rz, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: January 27, 2006Publication date: February 25, 2010Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard Williams Arthur Luke, William McCoull
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Publication number: 20100048547Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.Type: ApplicationFiled: February 6, 2008Publication date: February 25, 2010Inventors: Gordana Atallah, Sarah Bartulis, Matthew Burger, Hanne Merritt, Simon Ng, Zhi-Jie Ni, Sabina Pecchi, Keith B. Pfister, Aaron Smith, Charles Voliva, Allan Wagman, Yanchen Zhang
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Publication number: 20100016298Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: August 29, 2006Publication date: January 21, 2010Inventor: Gerad M. Housey
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Publication number: 20100016252Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.Type: ApplicationFiled: September 21, 2009Publication date: January 21, 2010Applicant: State of Oregon Acting By and Through The Oregon State Board of Higher Education On Behalf of The UInventors: John F.W. Keana, Paul Westberg, John Curd, Alshad S. Lalani
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Publication number: 20100009961Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: June 26, 2009Publication date: January 14, 2010Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jurgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Publication number: 20090317360Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: June 11, 2008Publication date: December 24, 2009Inventors: Roopa Rai, Franz Ulrich Schmitz, Christopher Don Roberts, Irina Slobodov, Martin Robert Leivers
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Publication number: 20090291079Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: May 22, 2009Publication date: November 26, 2009Applicant: WyethInventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
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Patent number: 7618961Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 17, 2009Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
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Publication number: 20090264401Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: April 21, 2009Publication date: October 22, 2009Applicant: AstraZeneca ABInventors: Adrian Liam GILL, Andrew Leach, Martin Packer, James Stewart Scott, Pernilla Sorme, John Gibbin Swales, Paul Robert Owen Whittamore
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Patent number: 7585857Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: August 23, 2007Date of Patent: September 8, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler