Plural Diazine Rings Patents (Class 544/357)
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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: 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: 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: 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: 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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Publication number: 20110098286Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: July 10, 2007Publication date: April 28, 2011Applicant: H. LUNDBECK A/SInventor: Jan Kehler
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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: 20110069130Abstract: A multifunctional Type II photoinitiator according to Formula (I): wherein X represents a structural moiety according to Formula (II): wherein: A represents a Norrish Type II initiating group; and L represents a divalent linking group positioning the Norrish Type II initiating group A and the CR2R3-group in a 1-5 to a 1-9 position wherein position 1 is defined as the first atom in the aromatic or alicyclic ring of A to which L is covalently bonded and the position 5 to 9 is defined as the carbon atom of the CR2R3-group to which L is covalently bonded, with the proviso that L does not contain an amine. Radiation curable compositions and inks include the multifunctional Type II photoinitiator.Type: ApplicationFiled: May 28, 2009Publication date: March 24, 2011Applicant: AGFA GRAPHICS NVInventors: Johan Loccufier, Jaymes Van Luppen
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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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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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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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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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Publication number: 20110059946Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: September 10, 2010Publication date: March 10, 2011Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
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Publication number: 20110059969Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: March 10, 2011Applicant: ASTRAZENECA ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20110053916Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis
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Publication number: 20110046135Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: November 1, 2010Publication date: February 24, 2011Applicant: ASTRAZENECA AB (PUBL)Inventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20110039841Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.Type: ApplicationFiled: May 3, 2005Publication date: February 17, 2011Applicants: Novo Nordisk A/SInventors: Zdenék Polivka, Karel Sindelar, Per Sauerberg, Ingrid Pettersson
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Publication number: 20110033411Abstract: The invention relates to novel compounds, in particular ammonium-polyurethane and/or polycarbonate compounds, in particular ammonium-polyurethane-polydiorganosiloxane and/or polycarbonate-polydiorganosiloxane compounds, methods for their production as well as their use.Type: ApplicationFiled: March 5, 2009Publication date: February 10, 2011Applicant: MOMENTIVE PERFORMANCE MATERIALS GMBHInventors: Roland Wagner, Karl-Heinz Sockel, Walter Simon
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Patent number: 7879838Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. 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.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: February 14, 2006Date of Patent: February 1, 2011Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Qingbei Zeng, De-Yi Yang, Stuart B. Rosenblum, Michael K. C. Wong, Gopinadhan N. Anilkumar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Lisa Guise Zawacki, Doublas W. Hobbs
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Publication number: 20110021533Abstract: The present invention provides cysteine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: October 4, 2010Publication date: January 27, 2011Applicants: Marquette University, University of Wisconsin- MilwaukeeInventors: James M. Cook, David A. Baker, Edward Merle Johnson, III, Wenyuan Yin
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Publication number: 20110015156Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: June 24, 2010Publication date: January 20, 2011Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20110009381Abstract: Provided herein are novel sirtuin-modulating compounds Structural Formula (I): and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 7, 2008Publication date: January 13, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Jeremy S. Disch, Bruce Szczepankiewicz, Giovanna Gualtieri, Rebecca L. Casaubon
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Patent number: 7868005Abstract: 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: and the pharmaceutically acceptable salts, solvates and esters thereof. 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: GrantFiled: February 14, 2006Date of Patent: January 11, 2011Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Seong Heon Kim, Qingbei Zeng, Michael K. C. Wong, Gopinadhan N. Anilkumar, Yueheng Jiang, Wensheng Yu, Joseph A. Kozlowski, Neng-Yang Shih, Bandarpalle B. Shankar, Brian F. McGuinness, Guizhen Dong, Lisa Guise Zawacki, Douglas W. Hobbs, John J. Baldwin, Yuefei Shao
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Patent number: 7868006Abstract: 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: GrantFiled: February 14, 2006Date of Patent: January 11, 2011Assignees: 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: 20110003759Abstract: 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: September 14, 2010Publication date: January 6, 2011Inventors: Philip D. Stein, Sharon N. Bisaha, Saleen Ahmad, Khehyong Ngu, William N. Washburn
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Publication number: 20110003812Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.Type: ApplicationFiled: October 15, 2008Publication date: January 6, 2011Applicant: SYMPHONY EVOLUTION, INC.Inventors: Sriram Naganathan, JoAnn Wilson, Daniel Dickman
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Publication number: 20100324061Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: September 1, 2010Publication date: December 23, 2010Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20100305122Abstract: 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: May 26, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa 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 A. Mantei, Todd M. Hansen
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Patent number: 7842693Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: December 9, 2003Date of Patent: November 30, 2010Assignee: ChemoCentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J. J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Valeri V. Martichonok
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Patent number: 7842694Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: September 3, 2008Date of Patent: November 30, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20100298323Abstract: 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: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Publication number: 20100298316Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: March 22, 2007Publication date: November 25, 2010Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Erik Knud Andersen
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Publication number: 20100298314Abstract: Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: November 25, 2010Inventors: Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Praveen K. Tadikonda, Umar Faruk Mansoor, Gerald W. Shipps, JR., David B. Belanger, Lianyun Zhao
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Publication number: 20100298343Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: ApplicationFiled: September 12, 2008Publication date: November 25, 2010Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda, Nicholas Simon Stock, Jeffrey Roger Roppe, Bowei Wang
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Patent number: 7834007Abstract: The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: August 23, 2006Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Han, Prasad V. Chaturvedula
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Patent number: 7834001Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: GrantFiled: November 8, 2005Date of Patent: November 16, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
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Publication number: 20100286161Abstract: This invention relates to novel pyrazine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: September 16, 2008Publication date: November 11, 2010Inventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Publication number: 20100286133Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Hubert HEUER, Norbert TENNAGELS
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Publication number: 20100286160Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: June 25, 2008Publication date: November 11, 2010Inventors: Eric J. Gilbert, William J. Greenlee, Sarah Wei Li, Michael W. Miller, Jack D. Scott, Adrew Stamford, Chander Shekher Celly
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Patent number: 7829567Abstract: Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives, their synthetic precursors and their uses in the manufacture of pharmaceutical compositions for use in the treatment of cancers.Type: GrantFiled: October 31, 2007Date of Patent: November 9, 2010Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Chih-Hua Tseng, Pei-Jung Lu
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Patent number: 7829709Abstract: The present invention provides cysteine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: GrantFiled: August 11, 2008Date of Patent: November 9, 2010Assignees: Marquette University, University of Wisconsin - MilwaukeeInventors: James M. Cook, David A. Baker, Edward Merle Johnson, II, Wenyuan Yin
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Publication number: 20100280012Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventor: On LEE
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Patent number: 7820817Abstract: The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases.Type: GrantFiled: May 31, 2005Date of Patent: October 26, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani