Plural 1,4-diazine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/252.11)
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Publication number: 20110237584Abstract: Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.Type: ApplicationFiled: November 9, 2009Publication date: September 29, 2011Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kinpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
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Publication number: 20110224211Abstract: 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: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110224185Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: May 23, 2011Publication date: September 15, 2011Inventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
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Patent number: 8017611Abstract: The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.Type: GrantFiled: October 23, 2008Date of Patent: September 13, 2011Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Craig Steven Harris, Christine Marie Paul Lambert, Gilles Ouvry, Justin Fairfield Bower, Benedicte Delouvrie, Gary Fairley, Jon James Gordon Winter
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Publication number: 20110218184Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: March 9, 2011Publication date: September 8, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Johnny Yasuo NAGASAWA, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
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Publication number: 20110212080Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: July 28, 2009Publication date: September 1, 2011Inventors: Umar Faruk Mansoor, Panduranga Adulla Reddy, M. Arshad Siddiqui
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Publication number: 20110212955Abstract: The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo.Type: ApplicationFiled: July 2, 2009Publication date: September 1, 2011Applicant: CANCER RESEARCH INITIATIVES FOUNDATIONInventors: Hong Boon Lee, Kevin Burgess, Siang Hui Lim, Liangxing Wu
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Publication number: 20110195963Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: August 11, 2011Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Publication number: 20110195973Abstract: The present invention relates to sodium channel blockers. The present Invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: June 11, 2007Publication date: August 11, 2011Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross Johnson
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Publication number: 20110189130Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: ApplicationFiled: March 22, 2011Publication date: August 4, 2011Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
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Patent number: 7989446Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: GrantFiled: September 22, 2010Date of Patent: August 2, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Publication number: 20110183967Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.Type: ApplicationFiled: September 25, 2009Publication date: July 28, 2011Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
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Publication number: 20110172238Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: July 16, 2010Publication date: July 14, 2011Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110160182Abstract: Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: AMGEN INC.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Publication number: 20110152256Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: June 23, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110152272Abstract: The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.Type: ApplicationFiled: November 5, 2010Publication date: June 23, 2011Inventors: Gordon McMurray, Wesley Dennis Miner
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Publication number: 20110142796Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: December 18, 2008Publication date: June 16, 2011Applicant: Amgen IncInventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang, Dustin L. Mcminn, Jeffrey T. Mihalic, Jeffrey Deignan
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Publication number: 20110144060Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: February 16, 2011Publication date: June 16, 2011Inventors: Philip D. Stein, Sharon N. Bisaha, Saleem Ahmad, Khehyong Ngu, William N. Washburn
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Publication number: 20110136799Abstract: Compounds of formula (I): wherein A, B, C, D, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, m, n, p, q, r, t, u, and v are defined herein. Also disclosed is a method for treating hepatitis C virus infection with these compounds.Type: ApplicationFiled: December 2, 2010Publication date: June 9, 2011Applicant: National Health Research InstitutesInventors: Jyh-Haur Chern, Yu-Sheng Chao
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Publication number: 20110136820Abstract: Compounds of formula (I) Q-L-W—C(?X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions.Type: ApplicationFiled: February 1, 2011Publication date: June 9, 2011Applicant: ASTRAZENECA ABInventors: Justin Fairfield Bower, Jeffrey Philip Poyser, Paul Turner, David Waterson, Jon Winter
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Patent number: 7951955Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: May 1, 2008Date of Patent: May 31, 2011Assignee: Biota Scientific Management Pty LtdInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Publication number: 20110124628Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 22, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
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Publication number: 20110124653Abstract: The invention relates to dimeric aryl-sulphonamido compounds endowed with inhibitory activity against metalloproteases MMP, having formula (I) below (M)-L-(M?) (I), wherein M and M?, the same or different from each other, represent the residues of the metalloproteases inhibitors of formula (II), wherein R, R1, R2, R3, G and n have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.Type: ApplicationFiled: July 21, 2009Publication date: May 26, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Tiziano Tuccinardi, Elisabetta Orlandini
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Publication number: 20110117015Abstract: The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.Type: ApplicationFiled: July 21, 2009Publication date: May 19, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Stanislava Ivanova Avramova, Fulvio Uggeri, Alessandro Maiocchi
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Publication number: 20110118233Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: May 6, 2009Publication date: May 19, 2011Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
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Publication number: 20110118264Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammalType: ApplicationFiled: January 28, 2011Publication date: May 19, 2011Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
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Publication number: 20110118275Abstract: The present invention relates to a compound of formula (I) wherein R1 is hydrogen or methyl, or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, as well as intermediates.Type: ApplicationFiled: November 12, 2010Publication date: May 19, 2011Applicant: ASTRAZENECA ABInventors: Kristofer Ahlin, Per I. ARVIDSSON, Ulrika YNGVE, Fernando HUERTA
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Publication number: 20110112110Abstract: Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases.Type: ApplicationFiled: March 30, 2009Publication date: May 12, 2011Applicants: UNIVERSITA' DEGLISTUDI DI MILANO- BICOCCA, UNIVERSITE ' DE GENEVE, UNIVERSITE ' CLAUDE BERNARD DE LYON 1Inventors: Carlo Gambacorti Passerini, Rosalind Helen Gunby, Alfonso Zambon, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Cerric Schneider
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Publication number: 20110112077Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: January 15, 2009Publication date: May 12, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. KUDUK, Ronald K, CHANG
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Publication number: 20110112051Abstract: 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: January 13, 2011Publication date: May 12, 2011Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Publication number: 20110112111Abstract: The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. The present invention also relates to novel DGAT inhibitors. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicament of said compounds.Type: ApplicationFiled: June 3, 2009Publication date: May 12, 2011Inventors: Joannes Theodorus Maria Linders, Peter Walter Maria Roevens, Brian Joel Hrupka
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Patent number: 7932247Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.Type: GrantFiled: November 15, 2005Date of Patent: April 26, 2011Assignee: Glaxo Group LimitedInventors: Brian W. Budzik, Anthony W. J. Cooper, Jian Jin, Dramane I. Laine, Brent W. McCleland, Michael R. Palovich, Ralph A. Rivero, Yonghui Wang, Haibo Xie, Chongjie Zhu
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Publication number: 20110082142Abstract: A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Inventors: MICHELLE LEANNE STYLES, JUN ZENG, HERBERT RUDOLF TREUTLEIN, ANDREW FREDERICK WILKS, MARCEL ROBERT KLING, XIANYONG BU, CHRISTOPHER JOHN BURNS
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Patent number: 7919489Abstract: The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: August 20, 2007Date of Patent: April 5, 2011Assignee: Aicuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Ulrich Rosentreter, Martin Hendrix, Joerg Keldenich, Dieter Lang, Martin Radtke, Daniela Paulsen, Armin Kern
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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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Patent number: 7910588Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N? and R1-7 are as defined herein.Type: GrantFiled: September 30, 2008Date of Patent: March 22, 2011Assignee: Eli Lilly and CompanyInventors: Valentina O Badescu, Sandra Ann Filla, Peter Thaddeus Gallagher, Maria Ann Whatton
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Patent number: 7910585Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: August 26, 2005Date of Patent: March 22, 2011Assignee: Novartis AGInventors: Eiji Kawahara, Takahiro Miyake, Johannes Roesel
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Publication number: 20110065690Abstract: The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Jolanta Grembecka, Tomasz Cierpicki, Jay Hess
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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: 20110065693Abstract: 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: ApplicationFiled: November 18, 2010Publication date: March 17, 2011Applicant: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20110065651Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: ApplicationFiled: November 23, 2010Publication date: March 17, 2011Applicants: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Seong Heon Kim, Gopinadhan N. Anilkumar, Michael K. C. Wong, Qingbei Zeng, Stuart B. Rosenblum, Joseph A. Kozlowski, Yuefei Shao, Brian F. McGuinness, Douglas W. Hobbs
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Publication number: 20110065706Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Applicant: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, David Stephen Clarke, Andrew Leach, Philip Alexander MacFaul, Charles John O'Donnell, James Stewart Scott, Paul Robert Owen Whittamore, Dan Anders Broo, Öjvind Percy Davidsson, Kjell Erik Johansson, Hanna De La Motte
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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: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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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: 20110065687Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.Type: ApplicationFiled: April 17, 2008Publication date: March 17, 2011Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
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Patent number: 7906645Abstract: Compounds of formula (I) Q-L-W—C(?X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C-C chemokine mediated conditions.Type: GrantFiled: December 19, 2005Date of Patent: March 15, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Jeffrey Philip Poyser, David Waterson
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Patent number: 7906515Abstract: The present invention relates to a method of treatment of a tumour cell which comprises administering to a subject in need of treatment an effective amount of a topoisomerase-II poison, e.g. etoposide, in combination with a bis-dioxypiperazine, e.g. dexrazoxane wherein said subject is further treated with radiation.Type: GrantFiled: March 2, 2005Date of Patent: March 15, 2011Assignee: Topotarget A/SInventors: Kenneth Hofland, Maxwell Sehested, Paul Kristjansen, Annemette Thougaard, Peter Buhl Jensen