Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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Patent number: 7592352Abstract: This invention relates to newly identified compounds for treating and preventing tumors and cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate activity of tyrosine kinases implicated in proliferative diseases.Type: GrantFiled: April 29, 2004Date of Patent: September 22, 2009Assignee: SmithKline Beecham CorporationInventor: Yasushi Miyazaki
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Publication number: 20090209544Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: May 11, 2007Publication date: August 20, 2009Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Ann E. Weber
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Patent number: 7576072Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X, Y and Z are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: November 18, 2004Date of Patent: August 18, 2009Assignee: Array BioPharma Inc.Inventors: Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, T. Brian Hurley, Allison L. Marlow, James Blake
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Publication number: 20090156803Abstract: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.Type: ApplicationFiled: January 29, 2009Publication date: June 18, 2009Inventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Tatsuya Watanabe, Jun Murakami, Takashi Mitsui
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Patent number: 7547709Abstract: Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.Type: GrantFiled: November 2, 2004Date of Patent: June 16, 2009Assignee: Vanderbilt UniversityInventors: Derek A. Pratt, Luca Valgimigli, Gino A. DiLabio
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Publication number: 20090137586Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: May 28, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Aneta M. Micula, Robert Feltz
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Publication number: 20090136448Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: December 20, 2006Publication date: May 28, 2009Inventors: John Andrew Corfield, Richard Martin Grimes, David Harrison, Charles David Hartley, Peter David Howes, Joelle Le, Malcolm Lees Meeson, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Patent number: 7538220Abstract: A compound having the formula in racemic form, enantiomerically enriched form or enantiomerically pure form; wherein X is a radical precursor; R5 is a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group; R6 is an alkyl group, —Si(R8R9R10) or —(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a —(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SRc or a nitro group; and R13 is H, F or —CH3.Type: GrantFiled: May 22, 2007Date of Patent: May 26, 2009Assignee: University of Pittsburgh - of the Commonwealth System of Higher EducationInventors: Dennis P. Curran, Bom David, Thomas G. Burke
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Publication number: 20090131468Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
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Publication number: 20090124625Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: June 17, 2005Publication date: May 14, 2009Applicant: Addex Pharmaceuticals SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Publication number: 20090105259Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors.Type: ApplicationFiled: September 8, 2006Publication date: April 23, 2009Inventors: Jae U. Jeong, Robert W. Marquis
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Publication number: 20090099227Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.Type: ApplicationFiled: December 23, 2005Publication date: April 16, 2009Inventors: Matthew Colin Thor Fyfe, Gerard Hugh Thomas, Lisa Sarah Bertram, Stuart Edward Bradley, William Gattrell, Chrystelle Marie Rasamison, Vilasben Kanji Shah
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Publication number: 20090099170Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: February 15, 2008Publication date: April 16, 2009Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Patent number: 7514449Abstract: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.Type: GrantFiled: January 8, 2004Date of Patent: April 7, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Tatsuya Watanabe, Jun Murakami, Takashi Mitsui
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Publication number: 20090076001Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compound corresponding to formula I, methods for producing them, to medicaments containing these compounds, the use of these compounds for producing medicaments and related treatment methodsType: ApplicationFiled: April 5, 2006Publication date: March 19, 2009Applicant: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann, Jorg Holenz, HagenHeinrich Hennies
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Publication number: 20090076067Abstract: The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, leishmania, African sleeping sickness, Chagas disease, toxoplasmosis lymphatic filariasis, babesiosis, and coccidiosis, and a novel compound contained therein.Type: ApplicationFiled: June 5, 2006Publication date: March 19, 2009Applicants: JAPAN SCIENCE AND TECHNOLOGY AGENCY, FUJIFILM CORPORATIONInventors: Masataka Ihara, Kiyosei Takasu, Kanitha Pudhom, Masayuki Kawakami, Hiroshi Kitaguchi, Kouzou Satou
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Publication number: 20090075978Abstract: The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
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Patent number: 7498349Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.Type: GrantFiled: August 1, 2003Date of Patent: March 3, 2009Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Jacob A. Kaizerman, Dustin L. McMinn
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Publication number: 20090054418Abstract: 2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.Type: ApplicationFiled: April 5, 2007Publication date: February 26, 2009Inventors: William Henry Miller, Alan T. Price
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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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Patent number: 7491733Abstract: The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1. These compounds may be used in the treatment of pathologies associated with insulin resistane syndrome.Type: GrantFiled: February 27, 2002Date of Patent: February 17, 2009Assignee: Merck Patent GmbHInventors: Gerard Moinet, Daniel Cravo
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Publication number: 20090035810Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090035809Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090029987Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: ApplicationFiled: July 28, 2006Publication date: January 29, 2009Applicant: RESVERLOGIX CORP.Inventors: Norman C.W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Publication number: 20090023728Abstract: Compounds of general formula (I) wherein D, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: December 20, 2004Publication date: January 22, 2009Applicant: ASTRAZENECA ABInventors: Justin Ripper, Ian Jenkins, Phuc Van Le, Ron Quinn, Christian Janssen
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Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Patent number: 7470693Abstract: The invention is directed to compounds having the following Formula I: and methods of using them for the treatment of proliferative diseases.Type: GrantFiled: April 19, 2006Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Gretchen M. Schroeder, Lyndon A. M. Cornelius
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Publication number: 20080306108Abstract: Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue.Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: MEDICURE INTERNATIONAL INC.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Wenlian Zhang
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Patent number: 7459468Abstract: Aryl sulfonic pyridoxine compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxines.Type: GrantFiled: October 28, 2004Date of Patent: December 2, 2008Assignee: Medicure International, Inc.Inventors: Wasimul Haque, James Diakur
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Patent number: 7456192Abstract: The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3-thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.Type: GrantFiled: October 30, 2002Date of Patent: November 25, 2008Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Barbara Monse, Wouter Koek
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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
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Publication number: 20080269227Abstract: The present invention is related to fused pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: September 2, 2005Publication date: October 30, 2008Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Thomas Rueckle, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Publication number: 20080269279Abstract: 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: April 7, 2008Publication date: October 30, 2008Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh, Andrey V. Peresypkin, Roy Helmy
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Patent number: 7439247Abstract: The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.Type: GrantFiled: November 30, 2005Date of Patent: October 21, 2008Assignee: Roche Palo Altop LLCInventors: Jian Jeffrey Chen, Nolan James Dewdney, Christoph Martin Stahl
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Patent number: 7439246Abstract: In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.Type: GrantFiled: December 1, 2005Date of Patent: October 21, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhong Chen, Tram N. Huynh, Wayne Vaccaro, Xiao-Tao Chen, Kyoung S. Kim, Zhen-wei Cai
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Patent number: 7429584Abstract: This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C1-C3)alkoxy halo, OH, CF3, CN, NO2 and (C1-C3)alkyl, said alkyl being optionally substituted with CF3; Ar2 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each independently selected from halo, OH, CN, NO2, CF3, (C1-C6)alkoxy, NR1R1, S(O)2R2, C(O)R3, and (C1-C6)alkyl optionally substituted with R4, and its use in treating hyper-proliferative disorders.Type: GrantFiled: July 11, 2003Date of Patent: September 30, 2008Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Gaetan Ladouceur, Michael J. Burke
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Patent number: 7425562Abstract: Compounds of general formula (I) or general formula (II) wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.Type: GrantFiled: January 17, 2002Date of Patent: September 16, 2008Assignee: Amura Therapeutics Ltd.Inventor: Martin Quibell
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Patent number: 7423048Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1?a2-a3?a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alType: GrantFiled: February 16, 2006Date of Patent: September 9, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristol Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Maria Encamacion Matesanz-Ballesteros, José Manuel Bartolomé-Nebreda
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Publication number: 20080214562Abstract: The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.Type: ApplicationFiled: July 5, 2006Publication date: September 4, 2008Inventor: Kristjan Gudmundsson
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Publication number: 20080207634Abstract: There is provided novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.Type: ApplicationFiled: December 16, 2005Publication date: August 28, 2008Inventor: Kristjan Gudmundsson
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Publication number: 20080207907Abstract: The invention relates to a novel process for the Pd catalysed formation of C—N bonds between an aryl halide or an aryloxysulphonyl compound and an amine in specific solvent systems, and also to the use of these solvent systems for C—N couplings.Type: ApplicationFiled: November 23, 2005Publication date: August 28, 2008Applicant: UCB PHARMA, S.A.Inventors: Björn Schlummer, Ulrich Scholz, Ian Smith
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Publication number: 20080207666Abstract: 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: ApplicationFiled: January 16, 2008Publication date: August 28, 2008Inventors: John S. Debenham, Jeffrey J. Hale, Pei Huo, Christina B. Madsen-Duggan, Thomas F. Walsh, Lin Yan
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Publication number: 20080188478Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2 represents halo; Ring A represents a 5- or 6-membered heterocyclic ring containing at least one N atom (the ring being optionally bridged with two or more carbon atoms); R3 represents a 5- or 6-membered heterocyclic ring containing at least one atom selected from N, O or S, the heterocyclic ring being optionally substituted by one or more groups selected from C1-6 alkyl oxo or NH2, the heterocyclic ring being further optionally fused to a 5- or 6-membered aryl or heterocyclic ring containing at least one atom selected from N, O or S, the fused aryl or heterocyclic ring being substituted by one or more halo atoms; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhea.Type: ApplicationFiled: April 18, 2006Publication date: August 7, 2008Inventors: Justin Stephen Bryans, Mark Edward Bunnage, Patrick Stephen Johnson, Helen Janet Mason, Lee Richard Roberts, Thomas Ryckmans, Alan Stobie, Toby James Underwood
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Patent number: 7407967Abstract: The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.Type: GrantFiled: April 18, 2007Date of Patent: August 5, 2008Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Alfredo C. Castro, Michael A. Foley, Somarajan Nair Janardanan Nair, Marta Nevalainen, James R. Porter, Martin R. Tremblay
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Publication number: 20080167339Abstract: 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: December 5, 2007Publication date: July 10, 2008Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MULLER, Hubert HEUER, Norbert TENNAGELS
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Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
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Publication number: 20080138656Abstract: Provided is a novel heterocyclic compound which is useful as a material for an organic electroluminescent device. The heterocyclic compound is represented by the general formula [I]: wherein X represents a nitrogen atom or a carbon atom; Y represents O or S; R1 and R2 each represent, independently of one another, a group selected from the group consisting of a substituted or unsubstituted alkyl group and the like; a represents 0 or more and 3 or less; b represents 0 or more and 3 or less; and Ar1 represents a substituted or unsubstituted heterocyclic ring or the like; and n represents an integer of 2 to 10.Type: ApplicationFiled: November 14, 2007Publication date: June 12, 2008Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Akihiro Senoo, Tetsuya Kosuge, Taiki Watanabe
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Patent number: 7358365Abstract: The invention relates to novel cyclic hydroxylamine esters and to the use of known hydroxylamine esters selected from the group consisting of HALS (sterically hindered amine) compounds and the novel hydroxylamine esters achieving a controlled increase in the molecular weight of polyethylene.Type: GrantFiled: January 25, 2006Date of Patent: April 15, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Michael Roth, Rudolf Pfaendner, Peter Nesvadba, Marie-Odile Zink
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Publication number: 20080045526Abstract: The present invention provides a compound represented by the formula: wherein the variables R1, b, R6, Y, Z, X, R and a are defined in the specification. Said compound may be used in a method for treating diseases related to unregulated tyrosine kinase signal transduction, wherein said disease is selected from the group consisting of cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, and metabolic diseases.Type: ApplicationFiled: March 16, 2007Publication date: February 21, 2008Inventors: Sougato Boral, Xialing Guo, Shimiao Wang, Julie A. Wurster, Thomas C. Malone
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Patent number: 7332504Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: September 22, 2004Date of Patent: February 19, 2008Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji