At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
-
Publication number: 20130131087Abstract: The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1?, 2?, 3?(1S*,2R*),5?]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Applicant: AstraZeneca ABInventor: Simon Banks
-
Publication number: 20130116236Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 6, 2012Publication date: May 9, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
-
Publication number: 20130109702Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: October 31, 2012Publication date: May 2, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
-
Publication number: 20130072503Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: March 19, 2012Publication date: March 21, 2013Applicant: AstraZenecaInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
-
Publication number: 20130045962Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.Type: ApplicationFiled: November 6, 2008Publication date: February 21, 2013Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
-
Publication number: 20130040970Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).Type: ApplicationFiled: December 3, 2010Publication date: February 14, 2013Applicant: AstraZeneca ABInventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
-
Patent number: 8372852Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: May 11, 2012Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
-
Publication number: 20130030176Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.Type: ApplicationFiled: February 15, 2011Publication date: January 31, 2013Applicant: ACTAVIS GROUP PTC EHFInventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
-
Patent number: 8354414Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: GrantFiled: November 4, 2010Date of Patent: January 15, 2013Assignee: Cephalon, IncInventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg A. Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
-
Publication number: 20120316161Abstract: The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: ApplicationFiled: December 20, 2010Publication date: December 13, 2012Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Gunter Carlens, Patrick Chaltin, Frauke Christ, Zeger Debyser, Arnaud Marchand, Damien Marchand, Arnout Voet, Marc De Maeyer
-
Publication number: 20120301458Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereofType: ApplicationFiled: July 27, 2010Publication date: November 29, 2012Applicant: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
-
Patent number: 8273877Abstract: Substituted tetraazapentalenes have two benzenoid rings and eight substitutable positions. Substitutions are made of hydrogen or C—H groups in favor of amino groups, nitro groups or nitrogen atoms. The tetraazapentalenes are synthesized through an intermediate azo, which is made from a 1:1:1 molar ratio of a nitroaniline, sodium nitrite and an amine.Type: GrantFiled: November 18, 2011Date of Patent: September 25, 2012Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Alfred G. Stern, Patrick A. Caruana
-
Publication number: 20120232073Abstract: The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Santhosh Francis Neelamkavil, Dipshikha Biswas, Samuel Chackalamannil, Bernard R. Neustadt, Andrew Stamford, Hong Liu
-
Substituted 1,2,3-triazolopyrimidines for the inhibition of NAD(P)H oxidases and platelet activation
Patent number: 8236809Abstract: The invention relates to compounds of formula het-X-AB containing a N-heteroaryl moiety “het”, which is linked via X=sulfur to the 1,2,3-triazolo[4,5-d]pyrimidine-7-yl moiety AB of the formula (II). The invention also relates to a process for the preparation of said compounds and the use thereof in drugs for the treatment of NAD(P)H oxidase-related diseases and disorders and inhibition of platelet activation.Type: GrantFiled: May 13, 2005Date of Patent: August 7, 2012Assignee: Vasopharm GmbHInventors: Frank Tegtmeier, Ulrich Walter, Reinhard Schinzel, Kirstin Wingler, Peter Scheurer, Harald Schmidt -
Patent number: 8232275Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: GrantFiled: July 15, 2011Date of Patent: July 31, 2012Assignees: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
-
Publication number: 20120190697Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substitutedType: ApplicationFiled: March 2, 2012Publication date: July 26, 2012Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
-
Patent number: 8227601Abstract: This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: May 5, 2006Date of Patent: July 24, 2012Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Stephanie Shaw, Hong Woo Kim, Zhi Hong
-
Publication number: 20120172591Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: February 17, 2012Publication date: July 5, 2012Applicant: ICOS CORPORATIONInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
-
Publication number: 20120165348Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: July 21, 2011Publication date: June 28, 2012Applicant: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
-
Patent number: 8207178Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: December 12, 2008Date of Patent: June 26, 2012Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
-
Publication number: 20120157453Abstract: Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: June 21, 2012Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Steven Mark Wenglowsky
-
Publication number: 20120135994Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Applicant: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
-
Publication number: 20120122892Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Applicant: AstraZeneca ABInventors: Michelle Lamb, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
-
Publication number: 20120101274Abstract: The present invention is directed to a process for preparing [1S-[1?,2?,3?(1S*,2R*),5?]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol and to intermediates useful in the process.Type: ApplicationFiled: September 8, 2009Publication date: April 26, 2012Applicant: ASTRAZENECA ABInventors: Martin Hans Bohlin, Helena Hellström, Peter W. Johansson, Ulf G. Larsson, Mikaela Recknagel, Rhony Aufdenblatten, Andreas Weiss, Ursula Weiss
-
Patent number: 8158634Abstract: The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: GrantFiled: October 26, 2005Date of Patent: April 17, 2012Assignee: IRM LLCInventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David Woodmansee, Zhicheng Wang, David Archer Ellis, Baogen Wu, Yun He, Truc Ngoc Nguyen
-
Patent number: 8148385Abstract: The present invention is directed to novel bicyclic triazolopyrimidine compounds of Formula (I) or a form thereof: wherein X1, X2, R1, R2, R3 and R4 are as defined herein, and their methods of preparation and use as ADP inhibitors.Type: GrantFiled: October 31, 2007Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye, Cailin Chen
-
Publication number: 20120077826Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: John M. Fevig, Dean A. Wacker
-
Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
-
Patent number: 8093257Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.Type: GrantFiled: April 30, 2008Date of Patent: January 10, 2012Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Dean A. Wacker
-
Publication number: 20120004203Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 29, 2009Publication date: January 5, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
-
Patent number: 8080547Abstract: The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 6, 2009Date of Patent: December 20, 2011Assignee: Sanofi-AventisInventors: Luc Even, Christian Hoornaert
-
Publication number: 20110269778Abstract: This invention relates to novel (6-phenyl-5-amino/nitro-pyrimidin-4-yl)-phenyl-amines, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 8, 2009Publication date: November 3, 2011Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
-
Publication number: 20110237565Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 29, 2011Applicant: KALYPSYS, INC.Inventors: Allen Borchardt, Robert Davis, Stewart A. Noble
-
Patent number: 8022083Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 1, 2008Date of Patent: September 20, 2011Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang
-
Publication number: 20110218330Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.Type: ApplicationFiled: March 24, 2011Publication date: September 8, 2011Applicant: AstraZeneca ABInventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
-
Publication number: 20110183992Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
-
Publication number: 20110172252Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: ApplicationFiled: June 25, 2009Publication date: July 14, 2011Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
-
Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
-
Patent number: 7960394Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.Type: GrantFiled: May 30, 2005Date of Patent: June 14, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
-
Publication number: 20110118285Abstract: Selected fused imidazole or triazole derivatives are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: May 22, 2009Publication date: May 19, 2011Inventors: Brian K. Albrecht, Steven Bellon, Christiane Bode, Alessandro Boezio, Deborah Choquette, Jean-Christophe Harmange
-
Publication number: 20110118286Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.Type: ApplicationFiled: July 15, 2009Publication date: May 19, 2011Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Joel M. Harris, Andre Stamford, Jinsong Hao, Bernard R. Neustadt, Samuel Chackalamannil, Yan Xia, Wiliam J. Greenlee
-
Publication number: 20110110927Abstract: In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.Type: ApplicationFiled: April 21, 2009Publication date: May 12, 2011Inventors: Andrew W. Stamford, Zhaoning Zhu, Mihirbaran Mandal, Xiaoxiang Liu
-
Patent number: 7863279Abstract: The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 13, 2009Date of Patent: January 4, 2011Assignee: sanofi-aventisInventors: Luc Even, Christian Hoornaert
-
Publication number: 20100324074Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: February 28, 2009Publication date: December 23, 2010Inventor: Junhu Zhang
-
Patent number: 7851468Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: GrantFiled: May 14, 2007Date of Patent: December 14, 2010Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
-
Patent number: 7816350Abstract: The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of such compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease. Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.Type: GrantFiled: February 4, 2005Date of Patent: October 19, 2010Assignees: Institute of Experimental Botany ASCR, Univerzita Palackeho v OlomouciInventors: Kveta Fuksova, Libor Havlicek, Vladimir Krystof, Rene Lenobel, Miroslav Strnad
-
Patent number: 7799795Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.Type: GrantFiled: June 26, 2006Date of Patent: September 21, 2010Assignee: Amgen Inc.Inventors: Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Julio C. Medina, Jeffrey T. Mihalic, George R. Tonn
-
Publication number: 20100197684Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 9, 2010Publication date: August 5, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
-
Publication number: 20100197692Abstract: Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: July 18, 2008Publication date: August 5, 2010Inventors: Yeeman K. Ramtohul, Chun Sing Li, Jean-Philippe Leclerc
-
Publication number: 20100173914Abstract: Compounds that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: ApplicationFiled: January 2, 2008Publication date: July 8, 2010Inventors: Hexi Chang, Benjamin Lane, Weirong Chen, Slawomir Janicki, Richard Todd, William F. Kiesman