The Additional Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/61)
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Publication number: 20110159563Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, JR., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Patent number: 7951807Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substituents A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: July 13, 2005Date of Patent: May 31, 2011Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Herve Geneste
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Publication number: 20110124634Abstract: The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.Type: ApplicationFiled: May 8, 2009Publication date: May 26, 2011Inventors: Connie L. Sun, Xiaoyuan Li
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Patent number: 7939531Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: May 10, 2011Assignee: Roche Palo AltoInventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7902182Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: November 10, 2006Date of Patent: March 8, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson, Yasutsugu Ueda, John D. Matiskella, Michael A. Walker
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7897593Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: May 29, 2007Date of Patent: March 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Patent number: 7893256Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: April 8, 2010Date of Patent: February 22, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 7858620Abstract: 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: GrantFiled: September 11, 2008Date of Patent: December 28, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Morten Langgaard
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Publication number: 20100324024Abstract: The present invention is directed to compounds of formula (I) (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: February 3, 2009Publication date: December 23, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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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
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Publication number: 20100311729Abstract: The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.Type: ApplicationFiled: May 9, 2008Publication date: December 9, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet, Jiong Lan, Sabrina Pecchi, Joseph Schoepfer
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Publication number: 20100305113Abstract: The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.Type: ApplicationFiled: May 7, 2008Publication date: December 2, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet
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Publication number: 20100298297Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: ApplicationFiled: March 20, 2007Publication date: November 25, 2010Applicant: BAYER HEALTHCARE AGInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaeten Ladouceur, Qian Zhao, Zheng Liu, Kristen Allegue, Chetan Darne, Jason Newcom
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Publication number: 20100280021Abstract: The present invention comprises pyridopyrimidinediamine compounds of the general formula I: The compounds of the present invention are potent inhibitors of PTP1B. Accordingly, the invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.Type: ApplicationFiled: July 16, 2010Publication date: November 4, 2010Inventors: Steven Joseph Berthel, Adrian Wai-Hing Cheung, Kyungjin Kim, Shiming Li, Kshitij Chhabilbhai Thakkar, Weiya Yun
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Publication number: 20100249118Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: June 21, 2006Publication date: September 30, 2010Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Shumeye Mamo, Chao Zhang, Jiazhong Zhang, James Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Shenghua Shi
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Publication number: 20100216763Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: November 27, 2007Publication date: August 26, 2010Applicant: H. LUNDBECK A/SInventors: Alan J. Hutchison, Hongbin Li, Jianmin Mao, David J. Wustrow, Jun Yuan, He Zhao
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Patent number: 7776867Abstract: The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 29, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: John Laird Buchanan, William H. Buckner, Simon A. Burkitt, Erin F. DiMauro, Christopher N. Farthing, Alexander D. Frenkel, Martin J. Harrison, Frank Kayser, Jinqian Liu, Sarah E. Lively, Teresa L. Marshall, David C. McGowan, Rajiv Sharma, Stephen J. Shuttleworth, Xiaotian Zhu
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Patent number: 7763624Abstract: The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.Type: GrantFiled: August 18, 2006Date of Patent: July 27, 2010Assignee: Amgen Inc.Inventors: John L. Buchanan, William H. Buckner, Mario G. Cardozo, Erin F. DiMauro, Jiasheng Fu, Xiaolin Hao, Xian Yun Jiao, Frank Kayser, David J. Kopecky, Craig E. Masse, Susan A. Tomlinson, Ryan White, Xiaotian Zhu
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Patent number: 7732441Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: February 7, 2008Date of Patent: June 8, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Publication number: 20100137294Abstract: The present application discloses the Tv-stp-1 serine/threonine phosphatase gene from Trichostrongylus vitrinus, and compounds that are useful as invertebrate control agents.Type: ApplicationFiled: November 15, 2007Publication date: June 3, 2010Applicants: GENETIC TECHNOLOGIES LIMITED, MEAT & LIVESTOCK AUTRALIA LIMITEDInventors: Robin Beat Gasser, Adam McCluskey
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Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
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Publication number: 20100105668Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-Type: ApplicationFiled: November 24, 2009Publication date: April 29, 2010Inventors: Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Gaston Stanislas Marcella Diels, Werner Constant Johan Embrechts, Peter ten Holte, Frederik Jan Rita Rombouts, Carsten Schultz-Fademrecht
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Publication number: 20100093998Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straighted or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2008Publication date: April 15, 2010Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca AktiebolagInventors: Yoshiaki Isobe, Tomoaki Nakamura
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Publication number: 20100093702Abstract: This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.Type: ApplicationFiled: June 5, 2009Publication date: April 15, 2010Inventors: J. Kent Barbay, Devraj Chakravarty, Brian Christopher Shook, Aihua Wang
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Publication number: 20100063032Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia.Type: ApplicationFiled: March 24, 2008Publication date: March 11, 2010Inventors: John S. Debenham, Christina B. Madsen-Duggan, Thomas F. Walsh
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Patent number: 7674788Abstract: The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds.Type: GrantFiled: May 22, 2007Date of Patent: March 9, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Horst Dollinger, Domnic Martyres, Juergen Mack, Rolf Goeggel, Birgit Jung, Peter Nickolaus
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Publication number: 20100036118Abstract: The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.Type: ApplicationFiled: August 11, 2009Publication date: February 11, 2010Inventors: William D. Arnold, Pierre Bounaud, Chixu Chen, Brian Eastman, Andreas Gosberg, Stefan N. Gradl, Stephanie Hopkins, Zhe Li, Ian McDonald, Paul A. Sprengeler, Ruo W. Steensma, Mark E. Wilson
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Publication number: 20100029619Abstract: The present invention provides a compound represented by the formula (I): wherein ring A is a ring which is optionally further substituted; R1 is a hydrogen atom or a substituent; R2 is a hydrogen atom or a substituent; R3 is a hydrogen atom or a substituent; R4 is a hydrogen atom or a substituent; R5 is a hydrogen atom or a substituent; R6 is a hydrogen atom or a substituent; X is ?N— or ?C(Z)- (Z is a hydrogen atom or a substituent); when X is ?C(Z)-, Z and R6 are optionally bonded to each other to form, together with the carbon atom bonded thereto, an optionally substituted ring, provided that when X is ?CH—, then R6 is not optionally substituted 2-piperidinyl, excluding N-imidazo[1,2-a]pyridin-2-yl-4-methyl-benzamide, N-imidazo[1,2-a]pyridin-2-yl-benzamide and N-(7-methylimidazo[1,2-a]pyridin-2-yl)-benzamide, or a salt thereof, and a pharmaceutical agent containing same.Type: ApplicationFiled: August 3, 2007Publication date: February 4, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTEDInventors: Osamu Uchikawa, Nozomu Sakai, Yoshito Terao, Hideo Suzuki
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Patent number: 7648988Abstract: Described are new pteridine compounds of the formula 1, where the variables are as described herein. The compounds are useful for the treatment of: respiratory or gastrointestinal complaints or diseases; inflammatory diseases of the joints, skin or eyes; diseases of the peripheral or central nervous system; and cancers. Also described are pharmaceutical compositions which contain these compounds.Type: GrantFiled: February 14, 2008Date of Patent: January 19, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Horst Dollinger, Domnic Martyres, Juergen Mack, Peter Nickolaus, Birgit Jung
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Patent number: 7642350Abstract: This invention relates to purine derivatives, to processes for their preparation, to compositions containing them and to their use. The present invention provides compounds of formula (I) wherein R1, R2, R3, R9, R9a and Y are defined in the description. More particularly, the present invention relates to the use of purine derivatives in the treatment of a variety of viral infections and immune or inflammatory disorders, including those in which the modulation, in particular agonism, of Toll-Like Receptors (TLRs) is implicated. Accordingly, the compounds of the invention are useful in the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infections, inflammatory diseases such as asthma and arthritis, and cancer.Type: GrantFiled: May 3, 2006Date of Patent: January 5, 2010Assignee: Pfizer LimitedInventor: David Pryde
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Publication number: 20090325945Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc.Type: ApplicationFiled: April 26, 2007Publication date: December 31, 2009Inventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Richard Malcolm Marais, Harmen Dijkstra, Delphine Menard, Ion Niculescu-Duvaz, Lawrence Davies, Arnaud Nourry
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Publication number: 20090324543Abstract: 2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a patient in a therapeutically effective amount.Type: ApplicationFiled: December 24, 2007Publication date: December 31, 2009Applicant: Gilead Sciences, IncInventors: William John Watkins, Lee Shung Chong, Jennifer R. Zhang
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Patent number: 7625890Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: June 27, 2007Date of Patent: December 1, 2009Assignee: SmithKline Beecham Corp.Inventors: Dirk A. Heerding, Tammy J. Clark, Jack Dale Leber, Igor Safonov
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Patent number: 7618963Abstract: A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-14C)aryl or (4-13C)heteroaryl; R3 is (1-8C)alkyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1-X2 is C?C, C(O)—NH, NH—C(O), C(O)—O, O—C(O), C?N, N?C or S or O. The compounds of the invention can be used in fertility regulation therapies.Type: GrantFiled: April 23, 2007Date of Patent: November 17, 2009Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Johan Karstens
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Patent number: 7612063Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: January 14, 2008Date of Patent: November 3, 2009Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Patent number: 7605154Abstract: The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.Type: GrantFiled: August 2, 2006Date of Patent: October 20, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Eva Binnun, Peter J. Connolly, Sigmond G. Johnson, Ronghui Lin, Steven A. Middleton, Sandra J. Moreno-Mazza, Niranjan B. Pandey, Steven K. Wetter
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Publication number: 20090253679Abstract: The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.Type: ApplicationFiled: March 31, 2009Publication date: October 8, 2009Applicant: sanofi-aventisInventors: Vincent Leroy, Eric Bacque, Emmanuel Conseiller, Anke Steinmetz, Baptiste Ronan, Jean-Philippe Letallec
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Patent number: 7582627Abstract: Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, heterocyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 13, 2006Date of Patent: September 1, 2009Assignee: Warner-Lambert CompanyInventors: Paul Bird, Edmund Lee Ellsworth, Dai Quoc Nguyen, Joseph Peter Sanchez, Howard Daniel Hollis Showalter, Rajeshwar Singh, Michael Andrew Stier, Tuan Phong Tran, Brian Morgan Watson, Judy Yip
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Publication number: 20090203673Abstract: The present invention encompasses compounds of general Formula (I) wherein X and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: July 5, 2007Publication date: August 13, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
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Patent number: 7557112Abstract: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.Type: GrantFiled: October 5, 2005Date of Patent: July 7, 2009Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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Publication number: 20090149452Abstract: A compound represented by the following formula (I) is used as a xanthine oxidase inhibitor: in which R1 is phenyl or pyridyl each optionally having, as a substituent, C1-8 alkyl, C1-8 haloalkyl, C1-8 alkoxy, carboxyl, halogeno, hydroxyl, nitro, cyano, amino, etc.; R2 is cyano, nitro, etc.; X is oxygen, sulfur, etc.; and Y is sulfur, NH, etc.Type: ApplicationFiled: June 29, 2006Publication date: June 11, 2009Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Takeshi Nishino, Shinichi Yoshida, Atsushi Tendo, Tomio Yamakawa, Tadashi Kobayashi, Yoriko Shinohara
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Publication number: 20090143352Abstract: The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity.Type: ApplicationFiled: April 10, 2007Publication date: June 4, 2009Applicant: SGX Pharmaceuticals, Inc.Inventors: William D. Arnold, Pierre Bounaud, Chixu Chen, Brian Eastman, Andreas Gosberg, Stefan N. Gradl, Stephanie Hopkins, Zhe Li, Ian McDonald, Paul A. Sprengeler, Ruo W. Steensma, Mark E. Wilson
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Patent number: 7528140Abstract: The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and are therefore expected to be useful as therapeutic or prophylactic agents for conditions in which GSK-3 is implicated, such as diabetes, diabetes complications, Alzheimer's disease, neurodegenerative diseases, manic depression, traumatic encephalopathy, alopecia, inflammatory diseases, cancer and immune deficiency.Type: GrantFiled: February 24, 2003Date of Patent: May 5, 2009Assignee: Teijin LimitedInventors: Kenichiro Kataoka, Tomomi Kosugi, Toshihiro Ishii, Takahiro Takeuchi, Takaharu Tsutsumi, Akira Nakano, Gen Unoki, Masanori Yamamoto, Yuri Sakai
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Patent number: 7524852Abstract: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(?O)—, —SO2—, —OC(?O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided.Type: GrantFiled: June 6, 2003Date of Patent: April 28, 2009Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Tsutomu Matsumura, Hiroshi Ishida, Yosuke Yamaura, Seiji Aratake, Etsuo Ohshima, Koji Yanagawa, Motoki Miyama, Koji Suzuki, Ari Kawabe, Satoshi Nakanishi, Katsuya Kobayashi, Takashi Sato, Ichiro Miki, Kimihisa Ueno, Shinya Fujii, Miho Iwase
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Publication number: 20090069298Abstract: The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 20, 2006Publication date: March 12, 2009Applicant: TANABE SEIYAKU CO., LTD.Inventors: Yasunori Moritani, Kimihiro Shirai, Mariko Oi