The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 549/447)
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Publication number: 20150073157Abstract: Discloses is a process for preparation of a compound of formula 7, or a derivative thereof, wherein PG1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 7 can be useful in the preparation of halinchondrin analogs such as Eribulin.Type: ApplicationFiled: December 14, 2012Publication date: March 12, 2015Applicant: ALPHORA RESEARCH INC.Inventors: Fabio E.S. Souza, Jason A. Bexrud, Ricardo Orprecio, Boris Gorin
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Publication number: 20140249192Abstract: The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: February 12, 2014Publication date: September 4, 2014Applicant: Allergan, Inc.Inventors: Jose L. Martos, William R. Carling, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmetsa
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Publication number: 20140249199Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.Type: ApplicationFiled: July 19, 2012Publication date: September 4, 2014Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITYInventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8450313Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: May 22, 2012Date of Patent: May 28, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20130096209Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.Type: ApplicationFiled: April 15, 2011Publication date: April 18, 2013Applicants: Kraft Foods Global Brands LLC, Chromocell CorporationInventors: David Hayashi, William P. Jones, Jane V. Leland, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Louise Slade, Kambiz Shekdar, Jessica Langer
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 8088936Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: GrantFiled: March 10, 2010Date of Patent: January 3, 2012Assignee: Hoffman-La Roche Inc.Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 7981460Abstract: The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I?) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group.Type: GrantFiled: December 29, 2008Date of Patent: July 19, 2011Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Yoshinobu Takino
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Publication number: 20100298347Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.Type: ApplicationFiled: December 1, 2008Publication date: November 25, 2010Applicant: MERCK FROSST CANADA LTDInventors: Michel Belley, Denis Deschenes, Rejean Fortin, Jean-Francois Fournier, Sebastien Gagne, Yves Gareau, Jacques Yves Gauthier, Lianhai Li, Joel Robichaud, Michel Therien, Geoffrey K. Tranmer, Zhaoyin Wang
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100240678Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.Type: ApplicationFiled: March 10, 2010Publication date: September 23, 2010Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20100121085Abstract: Disclosed are: (1) a method for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal, which comprises the step of providing a reaction mixture containing 1-acetoxy-2-methyl-3-(3,4-methylenedioxyphenyl)-1-propene by a process for reacting 1,2-methylenedioxybenzene with 2-methyl-3,3-diacetoxypropene or a process for reacting 1,2-methylenedioxybenzene, methacrolein and acetic anhydride with one another; subjecting the reaction mixture to hydrolysis or transesterification with an alcohol to provide a reaction mixture containing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; and purifying by distilling the reaction mixture, wherein a high boiling point compound contained in the reaction mixture is removed by a specific procedure; and (2) 2-methyl-3-(3,4-methylenedioxyphenyl)-propanal produced by the method, which has an acetic acid content of a less than 40 ppm, is useful as a perfume, and has a high purity.Type: ApplicationFiled: February 14, 2008Publication date: May 13, 2010Applicant: UBE INDUSTRIES, LTD.Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
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Publication number: 20100121069Abstract: An electron withdrawing group substituted ?-arylolefin derivative represented by general formula (I) (in the formula, Ar1 represents an aryl group, E represents a formyl, acyl and so on) is allowed to react with an arylboronic acid represented by general formula (II) Ar2—BXmMn in the general formula (IV) RhYoL1p (Chiraphos)q (in the formula, Y represents ClO4, BF4, PF6, SbF6, OTf, halogen atom, hydroxyl group, alkoxy group or acyloxy group, L1 represents an organic ligand) to produce an optically active ?-diaryl electron withdrawing group substituted compound represented by general formula (V)Type: ApplicationFiled: July 13, 2007Publication date: May 13, 2010Inventors: Norio Miyaura, Yasunori Yamamoto, Takashi Nishikata, Takahiro Itoh
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Publication number: 20100035849Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: August 5, 2009Publication date: February 11, 2010Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
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Publication number: 20090252685Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Inventors: Chongxi Yu, Lina Xu
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Publication number: 20090203774Abstract: The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I?) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group.Type: ApplicationFiled: December 29, 2008Publication date: August 13, 2009Applicant: AJINOMOTO CO., INC.Inventors: Yusuke AMINO, Yoshinobu Takino
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Patent number: 7544682Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.Type: GrantFiled: January 8, 2007Date of Patent: June 9, 2009Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
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Publication number: 20090137567Abstract: Methods of treating blood disorders are described.Type: ApplicationFiled: September 17, 2008Publication date: May 28, 2009Applicant: HEMAQUEST PHARMACEUTICALS, INC.Inventors: Susan P. Perrine, Regine Bojacek
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Patent number: 7459568Abstract: Alpha crystalline form of strontium ranelate of formula (I): characterized by its powder X-ray diffraction diagram and by a water content of from 22 to 24%. Medicinal products containing the same which are useful in the treatment of osteoporosis and arthrosis.Type: GrantFiled: May 31, 2005Date of Patent: December 2, 2008Assignee: Les Laboratoires ServierInventors: Stéphane Horvath, Isabelle Demuynck, Gérard Damien
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Patent number: 7319101Abstract: The present invention relates to compounds of formula I wherein R1 is as defined in the specification and to esters thereof which are hydrolyzable under physiological conditions and to the pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of COMT and, thus, are useful for the treatment of diseases for which COMT inhibition is beneficial. The invention further relates to the treatment, control, or prevention of diseases such as depression, schizophrenia, Parkinson's disease, and to improve cognition.Type: GrantFiled: December 14, 2004Date of Patent: January 15, 2008Assignee: Hoffmann-La Roche Inc.Inventors: François Diederich, Roland Jakob-Roetne, Christian Lerner, Ralph Paulini
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Patent number: 7220752Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.Type: GrantFiled: November 28, 2001Date of Patent: May 22, 2007Assignees: Karo Bio AB, Abbott LaboratoriesInventors: Benjamin Pelcman, Annika Gustafsson, Philip R. Kym
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Patent number: 7037914Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 7019028Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.Type: GrantFiled: July 25, 2003Date of Patent: March 28, 2006Assignees: Aventis Pharma Deutschland GmbH, Aventis Pharmaceuticals Inc.Inventors: Claudia Eder, Herbert Kogler, Sabine Haag-Richter
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Patent number: 6867218Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: February 20, 2003Date of Patent: March 15, 2005Assignee: Novo Nordisk A/SInventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Patent number: 6559179Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.Type: GrantFiled: February 5, 2002Date of Patent: May 6, 2003Assignee: SmithKline Beecham CorporationInventors: Dimitri Gaitanopoulos, Jack D. Leber, Mei Li, Joseph Weinstock
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Patent number: 6531485Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: December 16, 1999Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
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Publication number: 20030008895Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: December 16, 1999Publication date: January 9, 2003Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
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Patent number: 6498187Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.Type: GrantFiled: February 19, 2002Date of Patent: December 24, 2002Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Robert A. Daines, Jack D. Leber, Israil Pendrak, Joseph Weinstock
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Patent number: 6448260Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: July 10, 2001Date of Patent: September 10, 2002Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6300514Abstract: Pharmaceutical composition containing aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (1) and the salts thereof as active ingredient (wherein R1 is H, alkyl; R2 is COOR7, CONHOR8; E is —CONR9—, —NR9CO—, —OCO—,—COO—, —CH2—O—, —(CH2)2—, vinylene, ethynylene; J is bond, alkylene; A is H, alkyl, Ar, alkyl-OH ; R3, R4 is H, alkyl, COOR19, hydroxy, —NR20R21, Ar1 etc.); R5, R6 is H, methyl) and the novel aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (I).Type: GrantFiled: January 15, 1999Date of Patent: October 9, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6288247Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.Type: GrantFiled: March 8, 2000Date of Patent: September 11, 2001Assignee: SmithKline Beecham CorporationInventors: Yemane Woldeselassie Andemichael, Neil Howard Baine, William Morrow Clark, Conrad John Kowalski, Michael Anthony McGuire, Robert John Mills
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Patent number: 6271399Abstract: Indane and indene compounds are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6211197Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.Type: GrantFiled: October 4, 1999Date of Patent: April 3, 2001Assignee: Merck Frosst Canada & Co.Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
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Patent number: 6143907Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylen edioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyph eyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.Type: GrantFiled: February 4, 1997Date of Patent: November 7, 2000Assignee: SmithKline Beecham CorporationInventors: William Morrow Clark, Ivan Lantos, Robert John Mills, Lendon Norwood Pridgen, Ann Marie Tickner
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Patent number: 6107339Abstract: The derivatives of esters of carboxylic acids represented by the general formula I: ##STR1## wherein: R.sub.1 is an alkyl group having a chain or branched chain of 1 to 4 carbon atoms; andR.sub.2 is a group represented by the following general formulae II, III or IV; ##STR2## wherein: R.sub.3 is a hydrogen atom or a methyl group;X is an oxygen atom or a methylidene group;R.sub.4 is an hydrogen atom or an ethynyl group;R.sub.5 and R.sub.6 are alike or differently selected from the group consisting of hydrogen, fluorine, chlorine atoms or methyl group;R.sub.7 is a hydrogen atom or a trifluoromethyl group;R.sub.8 is selected from the group consisting of propargyl, methoxymethyl or methylthio groups; orR.sub.7 and R.sub.8 may combine with each other to form a methylenedioxy chain; and the process for manufacturing the same, and the insecticides and the insect proofing agents containing the same as an active ingredient.Type: GrantFiled: November 1, 1996Date of Patent: August 22, 2000Assignee: Dainihon Jochugiku Co., Ltd.Inventors: Yoshio Katsuda, Koji Nakayama, Yoshihiro Minamite
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Patent number: 6043241Abstract: Compounds of the Formula I ##STR1## are nonpeptide antagonists of endothelin which are useful in treating a variety of diseasses such as elevated levels of endothelin, acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon etc. The compounds are prepared by reacting an alpha-hydroxy butenolide with one or more equivalents of a suitable base, and exposing the solution to UV light.Type: GrantFiled: July 31, 1998Date of Patent: March 28, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, Timothy Robert Hurley, Michael James Lovdahl, William Chester Patt, Joseph Thomas Repine
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Patent number: 5962688Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.Type: GrantFiled: August 8, 1997Date of Patent: October 5, 1999Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Paul N. Devine, Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen, Yoshiaki Kato
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Patent number: 5945548Abstract: Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II).Type: GrantFiled: May 21, 1998Date of Patent: August 31, 1999Assignee: Societe Civile BioprojectInventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
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Patent number: 5817693Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: November 9, 1994Date of Patent: October 6, 1998Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5814657Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.Type: GrantFiled: November 21, 1997Date of Patent: September 29, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5786494Abstract: Process for the synthesis of a-substituted acrylic acids and their application.Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II).Type: GrantFiled: March 1, 1996Date of Patent: July 28, 1998Assignee: Societe Civile BioprojetInventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5716984Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott
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Patent number: 5708186Abstract: This invention relates to a method for the stereoselective synthesis of a 2-aryloxycarboxylic acid using a chiral auxiliary to enhance the stereoselectivity of the alkylation of the .alpha.-halo acid with an aryloxy group.Type: GrantFiled: December 6, 1996Date of Patent: January 13, 1998Inventors: Paul N. Devine, David M. Tschaen, Richard M. Heid, Jr.
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Patent number: 5686633Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.Type: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5686478Abstract: Novel derivatives of the general structural Formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, complications of diabetes, migraine, bone resorption, and inflammatory diseases, including Raynaud's disease and asthma.Type: GrantFiled: July 7, 1994Date of Patent: November 11, 1997Assignee: Merck & Co. Inc.Inventors: William J. Greenlee, Thomas F. Walsh
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Patent number: 5547983Abstract: Aromatic bicyclic compounds of formula (I) ##STR1## where R.sub.1 is specifically --H, CH.sub.3, --CH.sub.2 OH, --OH, --CHO, --CONH.sub.2, --COOH, --COOalkyl, --SH, S-alkyl, etc. . . . ; R.sub.2 is H; R.sub.3 is H, aryl, aralkyl or lower alkyl optionally substituted by a hydroxyl, a lower alkoxy or a --CO--R.sub.12, R.sub.12 being specifically H, lower alkyl, hydroxyl, lower alkoxy, or R.sub.2 and R.sub.3 together form a naphthalene ring with the benzene ring; R.sub.4 is a linear branched or unbranched alkyl having 1 to 15 carbon atoms or a cycloaliphatic radical; R.sub.5 represents specifically --(CH.sub.2).sub.n --R.sub.13, --CH.dbd.CH--(CH.sub.2).sub.n --R.sub.13, n being 0 or 1 to 6, R.sub.13 representing --COR.sub.15, monohydroxyalkyl, polyhydroxyalkyl, epoxy lower alkyl or --O--CO--R.sub.16, R.sub.15 representing specifically --OH, --Oalkyl, --Oaryl, R.sub.16 being specifically H, lower alkyl, aryl, or aralkyl; R.sub.6 and R.sub.7 are H, a halogen, lower alkyl or --OR.sub.Type: GrantFiled: August 22, 1994Date of Patent: August 20, 1996Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)Inventor: Bruno Charpentier
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Patent number: 5493032Abstract: The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.Type: GrantFiled: March 6, 1995Date of Patent: February 20, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Ackermann, Hans-Ruedi Kanel, Bruno Schaub
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Patent number: 5475132Abstract: R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated or hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: May 27, 1994Date of Patent: December 12, 1995Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat