Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
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Publication number: 20110224078Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyridines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyridine compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: October 14, 2009Publication date: September 15, 2011Applicant: BASF SEInventors: Dschun Song, Eike Hupe, Christian Pilger, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andrea Vescovi, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Robert Reinhard, Anja Simon, Ricarda Niggeweg, Bernd Sivernich, Thomas Seitz
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Patent number: 7999107Abstract: 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, Huntington's disease movement disorders, and schizophrenia.Type: GrantFiled: January 16, 2008Date of Patent: August 16, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: John S. Debenham, Jeffrey J. Hale, Pei Huo, Christina B. Madsen-Duggan, Thomas F. Walsh, Lin Yan
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110190334Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.Type: ApplicationFiled: November 3, 2010Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
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Patent number: 7985594Abstract: The present invention provides methods for performing dynamic nuclear polarization using biradicals with a structure of formula (I) as described herein. In general, the methods involve (a) providing a frozen sample in a magnetic field, wherein the frozen sample includes a biradical of formula (I) and an analyte with at least one spin half nucleus; (b) polarizing the at least one spin half nucleus of the analyte by irradiating the frozen sample with radiation having a frequency that excites electron spin transitions in the biradical; (c) optionally melting the sample to produce a molten sample; and (d) detecting nuclear spin transitions in the at least one spin half nucleus of the analyte in the frozen or molten sample. The present invention also provides biradicals with a structure of formula (I) with the proviso that Q1 and Q2 are different when X1 and X2 are —O—. The present invention also provides methods for making biradicals with a structure of formula (IA) as described herein.Type: GrantFiled: May 10, 2007Date of Patent: July 26, 2011Assignee: Massachusetts Institute of TechnologyInventors: Robert G. Griffin, Kan-Nian Hu, Timothy M. Swager, Changsik Song, Eric Dane
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Publication number: 20110150864Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110092706Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, a novel bicyclic compound of formula IV.Type: ApplicationFiled: October 15, 2010Publication date: April 21, 2011Applicant: CarboDesign LLCInventor: Milan Soukup
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Publication number: 20110092700Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: December 3, 2010Publication date: April 21, 2011Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Publication number: 20110046175Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20110046176Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20110039883Abstract: The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I wherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Hubert Heuer, Norbert Tennagels
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Publication number: 20110021557Abstract: The present invention relates to deuterium-enriched pyridinone carboxamides and their derivatives of the formula I, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT4) receptor subtype 4, and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, speech improvement in autistic children, sleep apnea in Alzheimer's patients, irritable bowel syndrome, gastroesophageal reflux disease, Crobn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, arterial fibrillation, arrhythmia, ischemic stroke, gastric emptying disorders, gastritis,Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Inventor: Daljit Singh Dhanoa
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Publication number: 20110008288Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: January 13, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Publication number: 20110008461Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.Type: ApplicationFiled: July 12, 2010Publication date: January 13, 2011Inventors: Gerald Carlson, Todd Holyoak, Sarah Sullivan, Rose Mary Stiffin
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Publication number: 20110009398Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.Type: ApplicationFiled: July 18, 2008Publication date: January 13, 2011Inventors: Toshiyuki Sakai, Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100303928Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: ApplicationFiled: December 2, 2008Publication date: December 2, 2010Applicant: FibroGen, Inc.Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100261736Abstract: The present application relates to novel substituted bicyclic heteroaryl compounds, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: June 3, 2008Publication date: October 14, 2010Inventors: Thomas Lampe, Raimund Kast, Hartmut Beck, Friederike Stoll, Eva-Maria Becker, Mario Jeske, Joachim Schuhmacher
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100204240Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: September 15, 2008Publication date: August 12, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Tumer, Eli M. Wallce
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Patent number: 7750151Abstract: The present invention is directed to compounds which contain substituted napthyridines 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: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, John C. Hartnett, Essa H. Hu, Peter J. Manley, Lou Anne Neilson, Lida R. Tehrani, Zhicai Wu
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Patent number: 7700611Abstract: The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1?-cyclohexane]-4?-carboxamide and novel salts, hydrates and polymorphs thereof.Type: GrantFiled: July 24, 2006Date of Patent: April 20, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Russell R. Ferlita, Yuji Haga, Makoto Ishikawa, Keisuke Kamei, Shinji Kato, Hisaki Kojima, Aaron Moment, Nobuaki Nonoyama, Nobuya Satake, Kazuki Shigemori, Toshihiro Wada, Yaling Wang, Steven A. Weissman, Robert M. Wenslow
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Patent number: 7691857Abstract: Muscarinic agonists of the formula (I) with M1 selectivity which are useful as agents for stimulating the cognitive functions of the brain.Type: GrantFiled: December 6, 2004Date of Patent: April 6, 2010Assignee: Muscagen LimitedInventors: Maxime Buffat, James Eric Thomas, Harvard Robin Davies
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Publication number: 20100081686Abstract: It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(?O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.Type: ApplicationFiled: September 2, 2009Publication date: April 1, 2010Inventors: Yukio TADA, Yasuyoshi ISO, Kohji HANASAKI
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Patent number: 7674907Abstract: The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof.Type: GrantFiled: July 18, 2005Date of Patent: March 9, 2010Assignee: Amgen Inc.Inventors: Joseph J. Nunes, Matthew W. Martin, Ryan White, David McGowan, Jean E. Bemis, Frank Kayser, Jiasheng Fu, Jinqian Liu, XianYun Jiao
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Publication number: 20100048591Abstract: The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.Type: ApplicationFiled: December 11, 2007Publication date: February 25, 2010Applicant: Bionomics LimitedInventors: Bernard Luke Flynn, Jason Hugh Chaplin, Dharam Paul, Damian Wojciech Grobelny, Brian Kelly
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Publication number: 20100029678Abstract: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating, hypertension.Type: ApplicationFiled: July 27, 2009Publication date: February 4, 2010Inventors: Amjad ALI, Iyassu K. Sebhat, Cristopher L. Franklin, Kathleen M. Rupprecht, Robert K. Baker, Ravi P. Nargund, Lin Yan, Pei Huo, Dong-Ming Shen, Nicoletta Almirante, Stefano Biondi, Massimiliano Ferrario, Alessia Nicotra
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Publication number: 20090318439Abstract: Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.Type: ApplicationFiled: January 9, 2008Publication date: December 24, 2009Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert Guzzo, Matthew David Surman
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Patent number: 7622479Abstract: The present invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by formula: (wherein, R1b is a C6-10 aryl group which has substituent(s), and the like; Ta is a single bond, a C1-6 alkyl group, —CH2O—, and the like; X and Y are the same or different, and each is a nitrogen atom which may have substituent(s), and the like; the broken line is a single bond or a double bond; Za is a nitrogen atom or CH; W is a single bond, an oxygen atom, and the like; Q is a C6-10 aryl group which may have substituent(s) or an aromatic heterocyclic group which may have substituent(s)); or a salt thereof and a pharmaceutical composition comprising thereof.Type: GrantFiled: November 25, 2002Date of Patent: November 24, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Oda, Takashi Imada, Kenichiro Naito, Toshiya Tamura, Shuichi Furuya
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Patent number: 7601736Abstract: The invention relates to novel pyridine derivatives having an inhibitory effect on production of cytokines, which are involved in inflammatory responses, thus suggesting its usefulness as therapeutic agents for treating diseases related to inflammation, immune, chronic inflammation as well as an agent having an anti-inflammatory and analgesic effect. Further, this invention relates to a method of manufacturing the same and a pharmaceutical composition containing the same.Type: GrantFiled: December 30, 2004Date of Patent: October 13, 2009Assignee: SK Chemicals Co., Ltd.Inventors: Hyung Ook Kim, Nam Kyu Lee, Joo Hyon Kim, Hae In Rhee, Yong-Baik Cho, Je Ho Ryu, Nam Ho Kim, Keun Ho Ryu, Jung Bum Yi, Jae Yoon Jung
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090247566Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I: or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: March 19, 2009Publication date: October 1, 2009Inventors: Alexander Kornienko, Igov V. Magedov, Snezna Rogelj
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Patent number: 7576213Abstract: A hitherto unknown class of chemical compounds, 2H-furo[2,3-c]pyran-2-ones including derivatives and analogues thereof are disclosed herein. Methods for making compounds within said class are disclosed herein and includes, without limitation, at least the intermediates employed in the generation of said compounds. The invention also relates to the use of vinylogous 4H-pyrones, including but not limited to the hitherto unknown 2H-furo[2,3-c]pyran-2-ones. Disclosed herein are methods comprising the step of exposing biological plant material to at least a compound of the invention to promoting bioactivity within said material. In another aspect in methods for promoting growth of plant material in, for example, smoke-responsive plant species by exposing said material to a compound of the invention are disclosed herein. More specifically, methods comprising the use of these compounds for promoting seed germination of a plant, for example, a smoke-responsive plant, are disclosed herein.Type: GrantFiled: June 19, 2006Date of Patent: August 18, 2009Assignee: The University of Western AustraliaInventors: Gavin Ray Flematti, Emilio Luciano Ghisalberti, Kingsly Wayne Dixon, Robert Donald Trengove
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Publication number: 20090197864Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.Type: ApplicationFiled: February 6, 2009Publication date: August 6, 2009Inventors: An-Hu Li, Arno G. Steinig, Andrew Kleinberg, Qinghua Weng, Mark J. Mulvihill, Jing Wang, Xin Chen, Ti Wang, Hanqing Dong, Meizhong Jin
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Publication number: 20090181947Abstract: The present invention relates to novel bicyclic enamino(thio)carbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 19, 2007Publication date: July 16, 2009Applicant: Bayer CropScience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Michael Edmund Beck, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Christian Arnold, Erich Sanwald
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Publication number: 20090143335Abstract: The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.Type: ApplicationFiled: October 17, 2008Publication date: June 4, 2009Applicant: H. LUNDBECK A/SInventors: Mie Larsen, Carsten Uhd Nielsen, Birger Brodin Larsen, Rene Holm
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Publication number: 20090124595Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: MarK Adams, Qing Dong, Toufike Kanouni, Stephen W. Kaldor, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090118324Abstract: Compounds are provided for use with MEK that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 17, 2008Publication date: May 7, 2009Inventors: Qing DONG, Toufiko Kanounl, Michael B. Wallace
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Publication number: 20090088420Abstract: Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the treatment of HIV/AIDS and related infections either alone or in combination with all the known antiretroviral therapeutics are described.Type: ApplicationFiled: April 14, 2008Publication date: April 2, 2009Applicant: University of Southern CaliforniaInventors: Nouri Neamati, Raveendra S. Dayam
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Publication number: 20090076068Abstract: The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments.Type: ApplicationFiled: September 22, 2008Publication date: March 19, 2009Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Stefan Petry, Markus Follmann, Gunter Muller, Norbert Tennagels
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Publication number: 20090062547Abstract: The present invention provides a concise synthetic method for generating lactam-fused beta-lactones that feature, in some embodiments, a tertiary fused carbinol, quaternary carbons, and a reactive beta-lactone moiety available for further reactions. The present invention further provides compounds synthesized by this method as well as methods of using these compounds as inhibitors of the proteasome and fatty acid synthase.Type: ApplicationFiled: July 9, 2007Publication date: March 5, 2009Inventors: Daniel Romo, Huda Henry-Riyad, Changsuk Lee, Henry Nguyen, Seongho Oh, Vikram C. Purohit
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Patent number: 7498438Abstract: A compound having the general structure shown in Formula 1: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: GrantFiled: April 6, 2005Date of Patent: March 3, 2009Assignee: Schering CorporationInventors: Dong Xiao, Anandan Palani, Cheng Wang, Hon-Chung Tsui, Neng-Yang Shih, Gregory A. Reichard
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Patent number: 7495101Abstract: A process for manufacturing a 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 9-acyloxy-1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin (I) and optionally for manufacturing pyridoxine involves performing an addition reaction between a 4-methyl-5-alkoxy-oxazole (II) and a 2-unsubstituted, 2-monosubstituted or 2,2-disubstituted 4,7-dihydro-(1,3)-dioxepin (III) in the substantial absence of a solvent and a catalyst to give a product mixture consisting essentially of the appropriate Diels-Alder adduct (IV) in a major proportion and the appropriate 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin 9-ol (V) in a minor proportion, removal of a substantial proportion of the unreacted oxazole and dioxapin starting materials from the product mixture by distillation under reduced pressure, addition of a substantially anhydrous organic acid to said product mixture and rearrangement of the Diels-Alder adduct IV to further V in the presence of said substantiallyType: GrantFiled: November 9, 2004Date of Patent: February 24, 2009Assignee: DSM IP Assets B.V.Inventors: Jocelyn Fischesser, Helmut Fritsch, Andrew George Gum, Reinhard Karge, Ralf Keuper
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Publication number: 20090048276Abstract: The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 26, 2007Publication date: February 19, 2009Inventors: Mark T. Goulet, Benito Munoz, Alexey A. Rivkin
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Patent number: 7449472Abstract: The present invention discloses compounds corresponding to the formula wherein A, X, Y, R, R1 and R2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.Type: GrantFiled: August 12, 2005Date of Patent: November 11, 2008Assignee: Roche Palo Alto LLCInventors: Jian Jeffrey Chen, Nolan James Dewdney, Christoph Martin Stahl