The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Patent number: 7807676Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: October 23, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini, Lawrence G. Hamann
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Publication number: 20100240639Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: April 13, 2010Publication date: September 23, 2010Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Mac Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
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Publication number: 20100240668Abstract: Pyridazinyl compounds, compositions and related methods of use.Type: ApplicationFiled: May 25, 2010Publication date: September 23, 2010Inventors: D. M. Watterson, L.J. Van Eldik, Heather Behanna, Hantamalala Ralay Ranaivo
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Publication number: 20100234354Abstract: Compounds of the formula (I), in which R1, R2, R, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: April 29, 2008Publication date: September 16, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
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Publication number: 20100234389Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Mitsunori Kouno
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Patent number: 7790730Abstract: The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula (A): wherein U is N or C; X is selected from C1-C10 alkylene, C2-10 alkenylene or C2-10 alkynylene, where each may include one or more intrachain heteroatoms selected from O, S, or NR11, provided any such heteroatom is not adjacent to the N in the ring; R3 is selected from aryl, aryloxy, arylthio, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl-N(R10)—, or heterocycle, where each said substituent is optionally substituted with at least one R17, provided that for cycloalkenyl the double bond is not adjacent to a nitrogen; and the other substituents are described in the specification.Type: GrantFiled: July 26, 2005Date of Patent: September 7, 2010Assignees: Gilead Sciences, Inc., K.U. Leuven Research & DevelopmentInventors: Choung U. Kim, Johan Neyts, David A. Oare, Gerhard Puerstinger
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Publication number: 20100216793Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: ApplicationFiled: February 16, 2010Publication date: August 26, 2010Inventors: Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rose Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
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Publication number: 20100210659Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20100210590Abstract: The present invention relates to therapeutic and/or prophylactic uses of pyridazine compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disorder characterized by conduction disturbances, electroconvulsions and/or seizures, in particular epilepsy, more particularly pediatric epilepsy. In an aspect of the invention, the pyridnsine compound has the Formula (Ia) or (Ib) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.Type: ApplicationFiled: February 29, 2008Publication date: August 19, 2010Applicant: NORTHWESTERN UNIVERSITYInventors: Martin D. Watterson, Linda J. Van Eldik, Mark S. Wainwright
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Patent number: 7776863Abstract: The invention encompasses pharmaceutical compositions and methods for using Compound 1 in combination with other agents for treating patients with AIDS or HIV infection.Type: GrantFiled: February 24, 2005Date of Patent: August 17, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Pin-Fang Lin, Beata Nowicka-Sans, Gregory Yamanaka
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Publication number: 20100204209Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: May 29, 2008Publication date: August 12, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Stefan Peters, Silke Hobbie
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Publication number: 20100197690Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 4, 2008Publication date: August 5, 2010Applicant: MERCK PATENT GESELLSCHAFTInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 7767677Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: August 3, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vishnumurthy Kodumuru, Serguei Sviridov, Kashinath Sadalapure, Shifeng Liu, Shaoyi Sun, Duanjie Hou, Nagasree Chakka
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Publication number: 20100183564Abstract: The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.Type: ApplicationFiled: October 29, 2009Publication date: July 22, 2010Applicant: IRM LLCInventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
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Patent number: 7759348Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.Type: GrantFiled: February 25, 2008Date of Patent: July 20, 2010Assignees: Xenon Pharmaceuticals Inc., Novartis Pharma AGInventors: Andreas Billich, Michael D. Winther, Yigal Paul Goldberg
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Publication number: 20100179148Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 2, 2008Publication date: July 15, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20100179144Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.Type: ApplicationFiled: June 12, 2008Publication date: July 15, 2010Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Steven David Knight, Kenneth Allen Newlander, Lance H. Ridgers, Stanley J. Schmidt
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Publication number: 20100179149Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 2, 2008Publication date: July 15, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 7754711Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: February 9, 2005Date of Patent: July 13, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Nagasree Chakka, Mikhail Chafeev, Sultan Chowdhury, Jian-Min Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Michael D. Winther, Zaihui Zhang, Melwyn Abreo, Mark W. Holladay, Wenbao Li, Sengen Sun, Chi Tu, Heinz W. Gschwend
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Patent number: 7754713Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: October 15, 2008Date of Patent: July 13, 2010Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Gunter Muller, Cecile Combeau, Christine Delaisi, Anke Steinmetz, Ingrid Sassoon
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Patent number: 7750011Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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: GrantFiled: February 13, 2006Date of Patent: July 6, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100168120Abstract: The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ?S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ?S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.Type: ApplicationFiled: April 27, 2007Publication date: July 1, 2010Applicant: NEUROMEDIX INC.Inventors: D.Martin Watterson, Linda Van Eldik, Wenhui Hu
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Publication number: 20100168076Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: August 29, 2007Publication date: July 1, 2010Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellenk Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco
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Patent number: 7745437Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, ??K, T??2, ???, ?NK2?2, MKK4, c-RAF, MKK6, SAPK2? and SAPK2? kinases.Type: GrantFiled: June 9, 2005Date of Patent: June 29, 2010Assignee: IRM LLCInventors: Pingda Ren, Xia Wang, Guobao Zhang, Qiang Ding, Shuli You, Qiong Zhang, Greg Chopiuk, Pamela A. Albaugh, Taebo Sim, Nathanael Schiander Gray
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Publication number: 20100160311Abstract: The present invention relates to azolopyrimidines of the formula I in which the substituents are defined according to the description, to processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling phytopathogenic harmful fungi.Type: ApplicationFiled: July 5, 2007Publication date: June 24, 2010Applicant: BASF SEInventors: Jochen Dietz, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou
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Publication number: 20100158992Abstract: There is disclosed a method for treating or preventing fungal infections comprising the administration of at least one glucan synthase inhibitor of a formula as described above in the specification or a pharmaceutically acceptable salt thereof; also claimed are methods of preparing pharmaceutical compositions comprising a compound as described above in the specification and a carrier, method of treating or preventing fungal infections comprising administration of combinations of glucan synthase inhibitor of a formula as described above in the specification and other antifungal agents, and method of treating or preventing fungal infections comprising administration of pharmaceutical compositions prepared according to a method described above in the specification, and a method of preparing a kit in a single package of the above described pharmaceutical composition and other antifungal agents.Type: ApplicationFiled: March 12, 2008Publication date: June 24, 2010Applicant: Schering CorporationInventors: Todd A. Black, Paul M. McNicholas, Scott S. Walker, Yiming Xu, Pauline C. Ting
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Publication number: 20100144747Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: September 29, 2009Publication date: June 10, 2010Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20100137329Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Applicant: SANOFI-EVENTISInventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Patent number: 7727988Abstract: The present invention relates to novel compounds of formula (I)? or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P1 or a group P2 wherein P1 is and the other groups are define in herein.Type: GrantFiled: March 30, 2007Date of Patent: June 1, 2010Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Giorgio Bonanomi, Anna Maria Capelli, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Giovanna Tedesco, Silvia Terreni
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates 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: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100120783Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: ApplicationFiled: November 10, 2009Publication date: May 13, 2010Applicant: LG LIFE SCIENCE LTD.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Publication number: 20100113464Abstract: The present invention relates to novel pyridazine derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is hydrogen, C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is an optionally substituted heteroaryl; R3 is an optionally substituted aryl; and R4 is hydrogen, halogen, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, (VCehaloalkoxy, hydroxy or cyano; or an agrochemically usable salt form thereof.Type: ApplicationFiled: July 16, 2007Publication date: May 6, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephan Trah, Clemens Lamberth, Sebastian Volker Wendeborn
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Publication number: 20100105693Abstract: 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: ApplicationFiled: January 5, 2010Publication date: April 29, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani
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Patent number: 7704998Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: October 29, 2007Date of Patent: April 27, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
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Publication number: 20100093703Abstract: The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Ruediger Streicher, Matthias Eckhardt, Annette Schuler-Metz, Alexander Pautsch, Corinna Schoelch
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Patent number: 7696207Abstract: A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.Type: GrantFiled: August 17, 2007Date of Patent: April 13, 2010Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Qun Sun
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Patent number: 7687503Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: GrantFiled: June 22, 2006Date of Patent: March 30, 2010Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Patent number: 7687502Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 23, 2005Date of Patent: March 30, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Morihiro Mitsuya, Makoto Bamba, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki, Keisuke Arakawa
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Publication number: 20100069394Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: ApplicationFiled: February 11, 2008Publication date: March 18, 2010Inventors: Gregor James MacDonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Publication number: 20100069351Abstract: The present invention aims to provide a novel SCD inhibitor. The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.Type: ApplicationFiled: February 5, 2008Publication date: March 18, 2010Inventors: Takahiko Taniguchi, Kenichi Miyata, Osamu Kubo
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Patent number: 7678796Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: GrantFiled: April 25, 2007Date of Patent: March 16, 2010Assignee: AstraZeneca ABInventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
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Publication number: 20100063031Abstract: Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: January 18, 2008Publication date: March 11, 2010Applicant: XCOVERY, INC.Inventor: Congxin Liang
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Publication number: 20100056532Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: March 4, 2010Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20100041663Abstract: The present invention relates generally to novel compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders. The present invention includes novel compounds, novel compositions, methods of their use and methods of their manufacture, where such compounds are generally pharmacologically useful as agents in therapies whose mechanism of action involve methods of inhibiting tumorigenesis, tumor growth and tumor survival using agents that inhibit the Hedgehog and Smo signaling pathway.Type: ApplicationFiled: July 15, 2009Publication date: February 18, 2010Inventors: Feng HE, Stefan Peukert, Karen Miller-Moslin, Naeem Yusuff, Zhuoliang Chen, Bharat Lagu
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Patent number: 7662812Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. 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: GrantFiled: February 13, 2006Date of Patent: February 16, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B Timmermann, Gunnar Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100034827Abstract: The invention is related to compounds of Formula (I), (II), or (III); or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 24, 2007Publication date: February 11, 2010Applicants: GILEAD SCIENCES, INC., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Hongyan Guo, Choung U. Kim, Thorsten A. Kirschberg, Iii Young Lee, Michael L. Mitchell, Jong Chan Son, Lianhong Xu
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Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20100022549Abstract: The synthesis of new ?-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available dimethyl pyridazine-3,6-dicarboxylate building block. These scaffolds may be thought of as synthetic counterparts of amphiphilic ?-helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.Type: ApplicationFiled: July 23, 2009Publication date: January 28, 2010Applicant: The Scripps Research InstituteInventors: Julius Rebek, JR., Lionel Moisan, Alexandre Carella, Enrique Mann
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Publication number: 20100022538Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 7, 2009Publication date: January 28, 2010Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Carla J.R. Klittich, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao