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)
  • Publication number: 20150073157
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: March 12, 2015
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Fabio E.S. Souza, Jason A. Bexrud, Ricardo Orprecio, Boris Gorin
  • Publication number: 20140249199
    Abstract: 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: Application
    Filed: July 19, 2012
    Publication date: September 4, 2014
    Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITY
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
  • Publication number: 20140249192
    Abstract: 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: Application
    Filed: February 12, 2014
    Publication date: September 4, 2014
    Applicant: Allergan, Inc.
    Inventors: Jose L. Martos, William R. Carling, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmetsa
  • Publication number: 20130172335
    Abstract: 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: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8450313
    Abstract: 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: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20130096209
    Abstract: 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: Application
    Filed: April 15, 2011
    Publication date: April 18, 2013
    Applicants: Kraft Foods Global Brands LLC, Chromocell Corporation
    Inventors: David Hayashi, William P. Jones, Jane V. Leland, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Louise Slade, Kambiz Shekdar, Jessica Langer
  • Publication number: 20120232071
    Abstract: 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: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Patent number: 8088936
    Abstract: 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: Grant
    Filed: March 10, 2010
    Date of Patent: January 3, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 7981460
    Abstract: 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: Grant
    Filed: December 29, 2008
    Date of Patent: July 19, 2011
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yusuke Amino, Yoshinobu Takino
  • Publication number: 20100298347
    Abstract: 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: Application
    Filed: December 1, 2008
    Publication date: November 25, 2010
    Applicant: MERCK FROSST CANADA LTD
    Inventors: 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
  • Publication number: 20100249124
    Abstract: 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: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20100240678
    Abstract: 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: Application
    Filed: March 10, 2010
    Publication date: September 23, 2010
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Publication number: 20100121085
    Abstract: 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: Application
    Filed: February 14, 2008
    Publication date: May 13, 2010
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Takashi Doi, Yoshihiro Yoshida, Eiji Sajiki, Satoru Fujitsu
  • Publication number: 20100121069
    Abstract: 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: Application
    Filed: July 13, 2007
    Publication date: May 13, 2010
    Inventors: Norio Miyaura, Yasunori Yamamoto, Takashi Nishikata, Takahiro Itoh
  • Publication number: 20100035849
    Abstract: 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: Application
    Filed: August 5, 2009
    Publication date: February 11, 2010
    Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.
    Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
  • Publication number: 20090252685
    Abstract: 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: Application
    Filed: April 2, 2009
    Publication date: October 8, 2009
    Inventors: Chongxi Yu, Lina Xu
  • Publication number: 20090203774
    Abstract: 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: Application
    Filed: December 29, 2008
    Publication date: August 13, 2009
    Applicant: AJINOMOTO CO., INC.
    Inventors: Yusuke AMINO, Yoshinobu Takino
  • Patent number: 7544682
    Abstract: 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: Grant
    Filed: January 8, 2007
    Date of Patent: June 9, 2009
    Assignee: Sanofi-Aventis
    Inventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
  • Publication number: 20090137567
    Abstract: Methods of treating blood disorders are described.
    Type: Application
    Filed: September 17, 2008
    Publication date: May 28, 2009
    Applicant: HEMAQUEST PHARMACEUTICALS, INC.
    Inventors: Susan P. Perrine, Regine Bojacek
  • Patent number: 7459568
    Abstract: 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: Grant
    Filed: May 31, 2005
    Date of Patent: December 2, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Stéphane Horvath, Isabelle Demuynck, Gérard Damien
  • Patent number: 7319101
    Abstract: 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: Grant
    Filed: December 14, 2004
    Date of Patent: January 15, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: François Diederich, Roland Jakob-Roetne, Christian Lerner, Ralph Paulini
  • Patent number: 7220752
    Abstract: 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: Grant
    Filed: November 28, 2001
    Date of Patent: May 22, 2007
    Assignees: Karo Bio AB, Abbott Laboratories
    Inventors: Benjamin Pelcman, Annika Gustafsson, Philip R. Kym
  • Patent number: 7037914
    Abstract: 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: Grant
    Filed: September 23, 2002
    Date of Patent: May 2, 2006
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
  • Patent number: 7019028
    Abstract: 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: Grant
    Filed: July 25, 2003
    Date of Patent: March 28, 2006
    Assignees: Aventis Pharma Deutschland GmbH, Aventis Pharmaceuticals Inc.
    Inventors: Claudia Eder, Herbert Kogler, Sabine Haag-Richter
  • Patent number: 6867218
    Abstract: 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: Grant
    Filed: February 20, 2003
    Date of Patent: March 15, 2005
    Assignee: Novo Nordisk A/S
    Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
  • Patent number: 6559179
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: May 6, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dimitri Gaitanopoulos, Jack D. Leber, Mei Li, Joseph Weinstock
  • Patent number: 6531485
    Abstract: 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: Grant
    Filed: December 16, 1999
    Date of Patent: March 11, 2003
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
  • Publication number: 20030008895
    Abstract: 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: Application
    Filed: December 16, 1999
    Publication date: January 9, 2003
    Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
  • Patent number: 6498187
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: December 24, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Robert A. Daines, Jack D. Leber, Israil Pendrak, Joseph Weinstock
  • Patent number: 6448260
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: July 10, 2001
    Date of Patent: September 10, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 6300514
    Abstract: 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: Grant
    Filed: January 15, 1999
    Date of Patent: October 9, 2001
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kanji Takahashi, Tsuneyuki Sugiura
  • Patent number: 6288247
    Abstract: 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: Grant
    Filed: March 8, 2000
    Date of Patent: September 11, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Yemane Woldeselassie Andemichael, Neil Howard Baine, William Morrow Clark, Conrad John Kowalski, Michael Anthony McGuire, Robert John Mills
  • Patent number: 6271399
    Abstract: Indane and indene compounds are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: August 7, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 6211197
    Abstract: 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: Grant
    Filed: October 4, 1999
    Date of Patent: April 3, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
  • Patent number: 6143907
    Abstract: 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: Grant
    Filed: February 4, 1997
    Date of Patent: November 7, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: William Morrow Clark, Ivan Lantos, Robert John Mills, Lendon Norwood Pridgen, Ann Marie Tickner
  • Patent number: 6107339
    Abstract: 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: Grant
    Filed: November 1, 1996
    Date of Patent: August 22, 2000
    Assignee: Dainihon Jochugiku Co., Ltd.
    Inventors: Yoshio Katsuda, Koji Nakayama, Yoshihiro Minamite
  • Patent number: 6043241
    Abstract: 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: Grant
    Filed: July 31, 1998
    Date of Patent: March 28, 2000
    Assignee: Warner-Lambert Company
    Inventors: Xue-Min Cheng, Annette Marian Doherty, Timothy Robert Hurley, Michael James Lovdahl, William Chester Patt, Joseph Thomas Repine
  • Patent number: 5962688
    Abstract: 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: Grant
    Filed: August 8, 1997
    Date of Patent: October 5, 1999
    Assignees: 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
  • Patent number: 5945548
    Abstract: 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: Grant
    Filed: May 21, 1998
    Date of Patent: August 31, 1999
    Assignee: Societe Civile Bioproject
    Inventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
  • Patent number: 5817693
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: October 6, 1998
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5814657
    Abstract: 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: Grant
    Filed: November 21, 1997
    Date of Patent: September 29, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5786494
    Abstract: 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: Grant
    Filed: March 1, 1996
    Date of Patent: July 28, 1998
    Assignee: Societe Civile Bioprojet
    Inventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
  • Patent number: 5719182
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 17, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
  • Patent number: 5716984
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: February 10, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, John Duncan Elliott
  • Patent number: 5708186
    Abstract: 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: Grant
    Filed: December 6, 1996
    Date of Patent: January 13, 1998
    Inventors: Paul N. Devine, David M. Tschaen, Richard M. Heid, Jr.
  • Patent number: 5686478
    Abstract: 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: Grant
    Filed: July 7, 1994
    Date of Patent: November 11, 1997
    Assignee: Merck & Co. Inc.
    Inventors: William J. Greenlee, Thomas F. Walsh
  • Patent number: 5686633
    Abstract: 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: Grant
    Filed: December 31, 1991
    Date of Patent: November 11, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Eric Vieira, Hugh Stephen Laver
  • Patent number: 5547983
    Abstract: 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: Grant
    Filed: August 22, 1994
    Date of Patent: August 20, 1996
    Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)
    Inventor: Bruno Charpentier
  • Patent number: 5493032
    Abstract: 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: Grant
    Filed: March 6, 1995
    Date of Patent: February 20, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Ackermann, Hans-Ruedi Kanel, Bruno Schaub
  • Patent number: 5475024
    Abstract: A new benzodioxole derivative has a substituent in the phenyl ring which is a carboxyalkylthioalkyl or the like and is effective to treat a liver disease.
    Type: Grant
    Filed: October 14, 1993
    Date of Patent: December 12, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshitake Ogata, Makoto Ikeda, Seiichiro Nomoto, Makoto Okita, Naoyuki Shimomura, Toshihiko Kaneko, Takashi Yamanaka, Ieharu Hishinuma, Junichi Nagakawa, Kazuo Hirota, Kaname Miyamoto, Toru Horie, Tsuneo Wakabayashi