Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 549/405)
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Publication number: 20090111868Abstract: The present invention provides compositions and methods for regulating the BK channel using rottlerin and derivatives thereof. In particular, the present invention provides pharmaceutical compositions for use in treating or preventing BK channel medicated disorders including hypertension and various hyperexcitability disorders. Also provided are compositions and methods for use in post-stroke neuroprotection and in treating or preventing erectile dysfunction. The present invention further provides kits for use in treating or preventing BK channel mediated disorders, comprising the compositions of the present invention.Type: ApplicationFiled: November 18, 2005Publication date: April 30, 2009Inventors: Steven O. Marx, Sergey I. Zakharov
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Patent number: 7524883Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.Type: GrantFiled: January 8, 2003Date of Patent: April 28, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Sergei Agoulnik, Kozo Akasaka, Frank Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuiness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
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Patent number: 7524975Abstract: The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and/or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenylflavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and/or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.Type: GrantFiled: October 11, 2002Date of Patent: April 28, 2009Assignee: Kaneka CorporationInventors: Tatsumasa Mae, Misuzu Tsukagawa, Mikio Kitahara, Kaku Nakagawa, Shiro Kitamura, Yasuyoshi Ueda, Minpei Kuroda, Yoshihiro Mimaki, Yutaka Sashida
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Patent number: 7514461Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: September 15, 2004Date of Patent: April 7, 2009Assignee: Edison Pharmaceuticals, Inc.Inventors: Bing Wang, Gail Walkinshaw, Sekhar Boddupalli, Arkadij M. Elizarov, Xianming Jin, Xianfeng Li, Donald R. James, Jiangao Song, Jian Chen, Wei Zhang
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Publication number: 20090076130Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-neurodegenerative diseases and human spinal muscular atrophy (SMA).Type: ApplicationFiled: September 14, 2007Publication date: March 19, 2009Applicant: NATUREWISE BIOTECH & MEDICALS CORPORATIONInventors: Chung-Yang Huang, Chia-Nan Chen, Wei-Jan Huang, Chih-Hsiang Huang, Li-Ling Chi, Chiou-Ping You
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Patent number: 7476741Abstract: The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R5, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: May 16, 2003Date of Patent: January 13, 2009Assignees: Cytovia, Inc., Shire BioChem, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Giorgio Attardo, Réal Denis, Richard Storer, Rabindra Rej
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Publication number: 20080318779Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: August 10, 2005Publication date: December 25, 2008Applicant: ISHIHARA SANGYO KAISHA LTDInventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Patent number: 7456214Abstract: Chrome compounds have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.Type: GrantFiled: May 21, 2004Date of Patent: November 25, 2008Assignees: Baylor University, OXiGENE, Inc.Inventors: Kevin G. Pinney, Phyllis Arthasary, Anupama Shirali, Klaus Edvardsen, David J. Chaplin
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Publication number: 20080207928Abstract: The invention provides a hair and/or scalp care composition comprising a flavonoid compound of general formula (I) in which: R1, R3 and R4 are each, independently, —H,—F,—Cl,—Br,—I,—OH, lower alkyl (e.g. C1-6 alkyl) or lower alkoxy (e.g. C1-6 alkoxy); and R2 is —H or an alkenyl group.Type: ApplicationFiled: February 27, 2006Publication date: August 28, 2008Inventors: Ranjit Bhogal, Jasveen Chugh, Helen Meldrum
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Patent number: 7410998Abstract: Benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase for inhibiting the growth of cancer cells.Type: GrantFiled: September 6, 2001Date of Patent: August 12, 2008Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Jeffrey Pfefferkorn, Guo-Qiang Cao, Anthony Roecker
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Publication number: 20080161520Abstract: The present invention relates to a heterocycle-containing onium salt useful as, for example, a cationic photopolymerization initiator and an acid generator for a chemically amplified resist, and provides a heterocycle-containing onium salt shown in the specification.Type: ApplicationFiled: November 20, 2007Publication date: July 3, 2008Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Masami Ishihara, Yoji Urano, Masahiro Takahashi
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Patent number: 7361774Abstract: The present invention relates to a chalcone compound represented by the following general formula: wherein R1 and R2 are taken together with the carbon atom to which they are bound, respectively, to form a hydroxydimethyl hexane ring, or where R1 is a hydroxyl group, R2 is an isohexenyl group, a derivative thereof, or a salt thereof. Also, the present invention relates to a therapeutic agent or prophylactic agent for a disease requiring neuronal protection, suppression for nitrogen monoxide (NO) production, inhibition for aldose reductase or suppression for interleukin production, and a food, beverage or feed for treatment or prevention of the above-mentioned disease, characterized in that each comprises the above-mentioned compound as an effective ingredient.Type: GrantFiled: September 29, 2003Date of Patent: April 22, 2008Assignee: Takara Bio Inc.Inventors: Hiromu Ohnogi, Katsumi Sugiyama, Nobuko Muraki, Tatsuji Enoki, Hiroaki Sagawa, Ikunoshin Kato
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Patent number: 7351737Abstract: Compounds of the formula where the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.Type: GrantFiled: March 14, 2003Date of Patent: April 1, 2008Assignee: Allergan, Inc.Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok-Yin Tsang, Yang-Dar Yuan, Roshantha A. Chandraratna
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Patent number: 7312232Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound having said structural formula.Type: GrantFiled: August 20, 2003Date of Patent: December 25, 2007Assignee: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 7226644Abstract: The present invention relates to a liquid crystal compound which has negative dielectric anisotropy and a large absolute value thereof; and a liquid crystal display element which contains the compound as a constituent element and has a negative value of dielectric anisotropy in the vertical alignment mode, IPS, or the like. The liquid-crystal display element has a structure including a pair of substrates and a liquid crystal sandwiched therebetween, and includes at least an alignment control layer, a transparent electrode, and a polarizing plate, in which the liquid crystal includes at least one compound having a partial structure represented by general formula (A): (wherein W1 and W2 each independently represents fluorine, chlorine, —CF3, —CF2H, —OCF3, or —OCF2H) and has negative dielectric anistropy.Type: GrantFiled: June 25, 2004Date of Patent: June 5, 2007Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takashi Matsumoto, Tetsuo Kusumoto, Shotaro Kawakami
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7115657Abstract: The present invention relates to novel bifunctional agents possessing antioxidant and antiarrhytmic activity, methods for the synthesis of the same and their applications in treating ischemia-reperfusion injury, as well as a variety of disorders related to free radicals and/or arrhythmias. These bifunctional drugs should preferentially segregate in the membrane and produce their antiarrhytmic effects while, at the same time, help in protecting the membrane lipids by scavenging free radicals.Type: GrantFiled: July 4, 2001Date of Patent: October 3, 2006Assignee: Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A.Inventors: Maria Koufaki, Theodora Calogeropoulou, Alexandros Makriyannis
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Patent number: 6911469Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2??(I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.Type: GrantFiled: January 17, 2002Date of Patent: June 28, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
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Publication number: 20040192762Abstract: The present invention provides a method to prepare 2H-benzo[6]pyrans, such as the anti-HIV natural product daurichromenic acid (1a), by microwave-assisted tandem aldol reaction of a phenolic enolate followed by intramolecular SN2′ type cyclization to form the 2H-benzo[6]pyran core structure.Type: ApplicationFiled: December 18, 2003Publication date: September 30, 2004Inventors: Zhendong Jin, Ying Kang
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Patent number: 6787565Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2 (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.Type: GrantFiled: January 17, 2002Date of Patent: September 7, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
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Patent number: 6756403Abstract: Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.Type: GrantFiled: July 11, 2003Date of Patent: June 29, 2004Assignee: Eli Lilly and CompanyInventors: Barbara Briggs, James Kanter, John J. G. Mullins, Gerd Ruhter, Uko Udodong, Milton Zmijewski, Jr., Daniel Verral, II
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Patent number: 6716998Abstract: This invention provides a process for the stereospecific preparation of 2-yl-chroman and -chromene derivatives of the formula: These compounds are useful for the preparation of optically active 2-aminomethyl- and 2-azaheterocyclylmethyl-chromans.Type: GrantFiled: October 4, 2002Date of Patent: April 6, 2004Assignee: WyethInventor: Jonathan L. Gross
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Patent number: 6713508Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: October 29, 2001Date of Patent: March 30, 2004Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
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Patent number: 6699860Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: GrantFiled: December 7, 2001Date of Patent: March 2, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
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Patent number: 6653488Abstract: A first process for producing a benzopyran carboxamide represented by the general formula [1] includes reacting 3-aminopropionitrile.½ sulfate, N≡CCH2CH2NH2.½(H2SO4), with a benzopyran carboxylic halide represented by the general formula [2], in the presence of a base. A second process for producing the benzopyran carboxamide includes the steps of (a) reacting 3-aminopropionitrile.½ sulfate with a base, thereby forming 3-aminopropionitrile; and (b) reacting the 3-aminopropionitrile with the benzopyran carboxylic halide [2], thereby producing the benzopyran carboxamide. A process for stabilizing 3-aminopropionitrile includes turning the 3-aminopropionitrile into a sulfate of the 3-aminopropionitrile. where R is a straight-chain or non-straight-chain perfluoroalkyl group represented by CnF2n+1 where n is an integer of 1-10; and X is fluorine, chlorine, bromine or iodine.Type: GrantFiled: August 8, 2002Date of Patent: November 25, 2003Assignee: Central Glass Company, LimitedInventors: Takeo Komata, Matsue Kawamura, Nariaki Ii
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Patent number: 6653472Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.Type: GrantFiled: April 26, 2002Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
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Patent number: 6645997Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: September 24, 2001Date of Patent: November 11, 2003Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
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Publication number: 20030207937Abstract: Compounds of the formula 1Type: ApplicationFiled: March 14, 2003Publication date: November 6, 2003Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok-Yin Tsang, Yang-Dar Yuan, Roshantha A. Chandraratna
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Patent number: 6635772Abstract: A method for producing a chroman-carboxylic acid is provided, which method includes reacting a dialkylphenol compound, a formaldehyde and an alcohol in the presence of a secondary amine and an acid to give an alkoxymethylated phenol compound (Step 1); reacting the obtained alkoxymethylated phenol compound with an ester having a carbon-carbon double bond at a temperature of not less than 100° C. to give a dialkylchroman carboxylic acid ester (Step 2); hydrolyzing the obtained dialkylchroman carboxylic acid ester to give a dialkylchroman-carboxylic acid (Step 3); and reacting the obtained dialkylchroman-carboxylic acid with an aromatic hydrocarbon in the presence of a Lewis acid (Step 4).Type: GrantFiled: August 28, 2001Date of Patent: October 21, 2003Assignee: Kuraray Co., Ltd.Inventors: Tatsuhiko Hayashibara, Junko Sato, Masahiro Torihara
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20030191181Abstract: Compounds of Formula 1 1Type: ApplicationFiled: March 19, 2002Publication date: October 9, 2003Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok-Yin Tsang, Yang-Dar Yuan, Roshantha Chandraratna
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Patent number: 6630461Abstract: A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein A selected from the group consisting of hydrogen and wherein the substituents are defined as set forth in the specification.Type: GrantFiled: June 15, 2001Date of Patent: October 7, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
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Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
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Patent number: 6620947Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: August 26, 2002Date of Patent: September 16, 2003Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
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Patent number: 6608217Abstract: The present invention relates to a first process for producing a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-carboxylic acid. The first process includes the steps of (a) reacting a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-one with a perfluoroalkanesulfonic acid anhydride in the presence of a base, thereby obtaining a perfluoroalkanesulfonic 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H- 1-benzopyran-4-yl ester; and (b) reacting the benzopyranyl ester with carbon monoxide in the presence of a palladium complex compound and a base, thereby obtaining the carboxylic acid. The present invention further relates to a second process for producing a 2-hydroxy-5-(perfluoroalkyl) acetophenone, which can be a raw material for producing the carboxylic acid.Type: GrantFiled: September 26, 2002Date of Patent: August 19, 2003Assignee: Central Glass Company, LimitedInventors: Takeo Komata, Masaki Fujiwara, Takanao Tarui, Yusuke Saito, Hiroshi Minesaki
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Patent number: 6596758Abstract: The present invention relates to benzopyrans and benzoxepines of formula (I), wherein X, A, R1, R2 and (R)p have the meanings as given in claim 1, which can be used in the treatment of dislipidaemias, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to processes allowing the preparation of these compounds.Type: GrantFiled: June 29, 2001Date of Patent: July 22, 2003Assignee: Merck Patent GmbHInventors: Michel Brunet, Jean-Jaques Zeiller, Jean-Jaques Berthelon, Francis Contard, Guy Augert, Daniel Guerrier
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Publication number: 20030109574Abstract: The present invention relates to a first process for producing a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-carboxylic acid. The first process includes the steps of (a) reacting a 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-one with a perfluoroalkanesulfonic acid anhydride in the presence of a base, thereby obtaining a perfluoroalkanesulfonic 2,2-bis(fluoromethyl)-6-(perfluoroalkyl)-2H-1-benzopyran-4-yl ester; and (b) reacting the benzopyranyl ester with carbon monoxide in the presence of a palladium complex compound and a base, thereby obtaining the carboxylic acid. The present invention further relates to a second process for producing a 2-hydroxy-5-(perfluoroalkyl)acetophenone, which can be a raw material for producing the carboxylic acid.Type: ApplicationFiled: September 26, 2002Publication date: June 12, 2003Applicant: Central Glass Company, LimitedInventors: Takeo Komata, Masaki Fujiwara, Takanao Tarui, Yusuke Saito, Hiroshi Minesaki
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Publication number: 20030083523Abstract: A compound represented by the following general formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: May 1, 2003Applicant: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
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Publication number: 20030065189Abstract: Starting, for example, from 1-fluoro-2-fluoromethyl-3-butyn-2-yl 4-trifluoromethylphenyl ether, N-(2-cyanoethyl)-5-fluoro-4-fluoromethyl-4-(4-trifluoromethylphenoxy)-2-pentynamide is produced and then cyclized to synthesize 2,2-bis(fluoromethyl)-N-(2-cyanoethyl)-6-trifluoromethyl-2H-1-benzopyran-4-carboxamide. The invention processes for producing 4-substituted benzopyran derivatives involve fewer steps, feature greater safety and allow for easier purification than the prior art processes.Type: ApplicationFiled: August 6, 2002Publication date: April 3, 2003Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Yukio Suzuki, Takenori Ishizawa, Vladimir A. Khlebnikov, Masashi Watanabe
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6492390Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.Type: GrantFiled: May 24, 2001Date of Patent: December 10, 2002Assignee: G.D. Searle & Co.Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
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Publication number: 20020082292Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: ApplicationFiled: September 24, 2001Publication date: June 27, 2002Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
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Patent number: 6399656Abstract: This invention relates to substituted heteroanilide compounds which are modulators, agonists or antagonists, of the CCR5 receptior. In addition, this invention relates to the treatment and prevention of disease states mediatd by CCR5.Type: GrantFiled: April 9, 2001Date of Patent: June 4, 2002Assignee: SmithKline Beecham CorporationInventors: William E Bondinell, Thomas W Ku, Michael J Neeb
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Patent number: 6395909Abstract: This invention relates to 6-(hydroxyalkylcarbonyl) benzopyrans and their use as anticonvulsants.Type: GrantFiled: December 19, 2000Date of Patent: May 28, 2002Inventors: David Bell, Peter J. Cox, Mervyn Thompson, Gillian Turner
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Patent number: 6384225Abstract: The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C114 C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a processType: GrantFiled: August 31, 2000Date of Patent: May 7, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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Patent number: 6355618Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: April 7, 2000Date of Patent: March 12, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
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Publication number: 20020010206Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders.Type: ApplicationFiled: May 24, 2001Publication date: January 24, 2002Applicant: G.D. Searle & Co.Inventors: Jeffery S. Carter, Mark G. Obukowicz, Balekudru Devadas, John J. Talley, David L. Brown, Matthew J. Graneto, Stephen R. Bertenshaw, Donald J. Rogier,, Srinivasan Raj Nagarajan, Cathleen E. Hanau, Susan J. Hartmann, Cindy L. Ludwig, Suzanne Metz, Donald E. Korte
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Patent number: 6258603Abstract: This invention relates to an improved method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The improvement resides in a select group of non-steroid ligands which show improved activity over known ligands.Type: GrantFiled: May 20, 1999Date of Patent: July 10, 2001Assignee: Rohm and Haas CompanyInventors: Glenn Richard Carlson, Dean Ervin Cress, Tarlochan Singh Dhadialla, Robert Eugene Hormann, Dat Phat Le
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Patent number: 6248777Abstract: It is an object of the present invention to provide novel therapeutic agents for peripheral vascular disease. The present invention provides pharmaceutical compositions comprising a benzopyran or benzoxazine derivative of the general formula (1): wherein; R1 represents a hydrogen atom, a lower alkyl group or an aryl group, or R1 directly couples with Q or R11 to form a single bond; R2represents a substituted or unsubstituted amino group, a saturated or unsaturated heterocyclic group, A—O—or —C(═X)Y; Q represents ═N—, N+—O−or C(R11)R12; R3 and R4 each represent a hydrogen atom, a lower alkyl group or a substituted lower alkyl group having a halogen atom or a lower alkoxy group as a substituent or the like; and R5 and R6 each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group or the like; and a pharmaceutically acceptable carrier.Type: GrantFiled: September 1, 1999Date of Patent: June 19, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hisanori Takanashi, Eiji Kumagai