Cyclobutyl In Acid Moiety Patents (Class 560/123)
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Patent number: 5126345Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.Type: GrantFiled: February 8, 1991Date of Patent: June 30, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: William A. Slusarchyk, Robert Zahler
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Patent number: 5102911Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: July 6, 1990Date of Patent: April 7, 1992Assignee: Merck & Co, Inc.Inventors: Ta J. Lee, Wilbur J. Holtz
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Patent number: 5099067Abstract: The present invention relates to a method of converting .beta.-nitro compounds, specifically alcohols, into the corresponding hydroxy amines with retention of configuration by the use of ammonium formate.Type: GrantFiled: August 15, 1991Date of Patent: March 24, 1992Assignee: Northwestern UniversityInventors: Anthony G. M. Barrett, Christopher D. Spilling
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Patent number: 5095137Abstract: The amides of cyclomethylen-1,2-bicarboxylic acids having the formula: ##STR1## wherein A represents ##STR2## R.sup.1 represents --H, --CH.sub.3, --CH.sub.2 --CH.sub.3, --CH(CH.sub.3).sub.2, ##STR3## R.sup.2 represents --H, CH.sub.3, --CH.sub.2 --CH.sub.3, --CH(CH.sub.3).sub.2, --CH.sub.2 --CH.sub.2 --CH.sub.3, --CH.sub.2 --CH(CH.sub.3).sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.3, --CH.sub.2 --C.sub.6 H.sub.5, --C.sub.6 --H.sub.5 ;R.sup.3 represents --H, --CH.sub.3, --C.sub.2 H.sub.5, ##STR4## R.sup.5 represents --H, --CH.sub.3, --C.sub.2 H.sub.5, --CH.sub.2 C.sub.6 H.sub.5, ##STR5## Y=--H, --CH.sub.3, --CH(CH.sub.3).sub.2 Z=--H,--CH.sub.3, --C(CH.sub.3).sub.3, --CH(C.sub.2 H.sub.5).sub.2, ##STR6## R.sup.4 =R.sup.5, ##STR7## m is 0 or 1 and n is an integer varying between 0 and 3, are endowed with ACE-inhibiting activity and are thus therapeutically useful as anti-hypertension agents.Type: GrantFiled: October 9, 1990Date of Patent: March 10, 1992Assignee: Laboratori Guidotti SpAInventors: Luigi Turbanti, Guido Cerbai, Marco Criscuoli
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Patent number: 5026898Abstract: A process for regioselectively preparing phosphorylated cyclitols, in particular phosphorylated inositols such as myo-inositol 1,4,5-tris(phosphate) and muo-inositol 1,3,4,5-tetrakis(phosphate). Novel cyclitols produced by means of this process are also described.Type: GrantFiled: January 31, 1990Date of Patent: June 25, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Frank W. Hobbs, James L. Meek
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Patent number: 5026899Abstract: The invention relates to novel 2-acyl-1,3-cyclohexanediones and the oxime ethers thereof with herbicidal and plant growth regulating properties.The novel 2-acyl-1,3-cyclohexanediones and the oxime ethers thereof are of the formula I ##STR1## wherein A is a 2- or 7-membered alkylene bridge, or a 3- to 7-membered alkenylene bridge which may be mono- or polyunsaturated,n is 0, 1 or 2,R.sub.1 is C.sub.1 -C.sub.4 alkyl or benzyl,R.sub.2 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; or is C.sub.3 -C.sub.6 cycloalkyl; or phenyl, benzyl or phenylethyl, the phenyl ring of each of which may be substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, cyano or nitro,X is oxygen or a radical --NOR.sub.3, andR.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.Type: GrantFiled: December 13, 1989Date of Patent: June 25, 1991Assignee: Ciba-Geigy CorporationInventor: Hans Tobler
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Patent number: 5025003Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthetis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.Type: GrantFiled: September 18, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Scott A. Biller
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Patent number: 5025017Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.Type: GrantFiled: September 28, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5021453Abstract: Compounds of formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: June 6, 1990Date of Patent: June 4, 1991Assignee: Merck & Co., Inc.Inventors: Henry Joshua, Kenneth E. Wilson, Michael S. Schwartz, Ta J. Lee, Gerald E. Stokker
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Patent number: 5021602Abstract: Novel compounds have at least one perfluorocyclobutane ring and at least two functional groups suitable for forming condensation polymers. Preferably the compounds have a structures represented by Formula II: ##STR1## wherein R and R' independently represent optionally inertly substituted groups; X and X' represent any molecular structures which link R and R' with the perfluorocyclobutane ring; n and n' are the number of G and G' groups, respectively; and G and G' independently represent any reactive functional groups or any groups convertible into reactive functional groups. The compound are preferably prepared by a process of thermally dimerizing trifluorovinyl compound to form a compounds of Formula IG.sub.n --R--X--CF.dbd.CF.sub.2wherein G represents G or G' in Formula II; X represents X or X' of Formual II; and n represents n or n' of Formula II, to form a compound having a perfluorocyclobutane group.Type: GrantFiled: June 9, 1989Date of Patent: June 4, 1991Assignee: The Dow Chemical CompanyInventors: Katherine S. Clement, David A. Babb, Bobby R. Ezzell
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Patent number: 5010105Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: May 9, 1990Date of Patent: April 23, 1991Assignee: Merck & Co., Inc.Inventor: Ta J. Lee
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4997977Abstract: This invention provides multistep process embodiments for the production of novel esters which exhibit nonlinear optical response.A process embodiment is illustrated by the reaction of a Schiff base with a substituted acetic acid to form a stilbene alcohol intermediate: ##STR1## The stilbene alcohol intermediate is decarboxylated, and then is esterified in the presence of a pyridine type catalyst to provide an ester with a conjugated structure.Type: GrantFiled: September 11, 1989Date of Patent: March 5, 1991Assignee: Hoechst Celanese Corp.Inventors: Thomas M. Leslie, Bernice I. Feuer, Mark J. Sebastian
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Patent number: 4997978Abstract: Alkyl carboxylates of the formula:R--CO--O--CH.sub.2 R'are prepared by hydrocarbonylating a compound of the formula:R--CO--O--R'in the simultaneous presence, in the reaction medium, of cobalt, ruthenium, an alkyl iodide and an ionic iodide, the atomic ratio Co/Ru being less than or equal to 1, and the total amount of iodine-containing promoters present in the medium being such that I/Ru is greater than or equal to 5.Type: GrantFiled: October 24, 1988Date of Patent: March 5, 1991Assignee: Rhone-Poulenc IndustriesInventors: Jean Gauthier-Lafaye, Robert Perron
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Patent number: 4970331Abstract: Vinyl ethers having a carboxyl group in a form of salt are stable and is usable as materials for fluorine-containing copolymers. The vinyl ethers can provide sable monomer compositions by mixing with vinyl ethers having a free carboxyl group when the former vinyl ethers are present in an amount of not less than 1% by mole of the latter vinyl ethers. The fluorine-containing copolymer prepared by copolymerizing fluoroolefins with the vinyl ethers are useful as aqueous coatings particularly electro dip coatings.Type: GrantFiled: March 9, 1988Date of Patent: November 13, 1990Assignee: Daikin Industries, Ltd.Inventors: Tatsushiro Yoshimura, Nobuyuki Tomihashi, Tsutomu Terada, Masayuki Yamana, Kazuhiro Nakai, Takayuki Araki
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Patent number: 4966915Abstract: An L-dopa derivative represented by formula (I) ##STR1## wherein one of R.sup.1 and R.sup.2 denotes a hydrogen atom and the other denotes a group of formula R--CO-- in which R denotes an alkyl, alkenyl, optionally substituted cycloalkyl, optionally substituted phenyl, optionally substituted aralkyl, lower alkoxy or optionally substituted aralkyloxy group,and its acid addition salt. The compounds are useful in the medical field, especially in the treatment of a series of diseases called Parkinson's disease or Parkinsonism.Type: GrantFiled: September 16, 1988Date of Patent: October 30, 1990Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshimi Tsuchiya, Masahiro Hayashi, Hiroshi Takehana, Akihiro Hisaka, Yoshio Sawasaki, Masaki Ihara
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Patent number: 4946864Abstract: Novel HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: February 1, 1988Date of Patent: August 7, 1990Assignee: Merck & Co., Inc.Inventors: John Prugh, Albert A. Deana, Clarence S. Rooney
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Patent number: 4931582Abstract: Novel fluorinated, acrylamide monomers are prepared from 2-alkenyl azlactones reacted with fluorinated alcohols. The novel monomers have the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen or methyl;R.sup.2 and R.sup.3 independently can be an alkyl, cycloalkyl, or aryl group, or R.sup.2 and R.sup.3 taken together with the carbon to which they are joined can form a carbocyclic ring containing 4 to 12 ring atoms;R.sup.4 and R.sup.5 are independently hydrogen or lower alkyl;a is 0 or 1;b is 1 or 2;X is a single bond, CH.sub.2, CH.sub.2 OCH.sub.2, and CH.sub.2 CH.sub.2 OCH.sub.2 ; andR.sub.F is a substantially perfluorinated alkyl, cycloalkyl, or aryl group when b is 1 and perfluorinated alkylene when b is 2.Novel polymers and copolymers can be prepared from the monomers of the invention.Type: GrantFiled: November 4, 1988Date of Patent: June 5, 1990Assignee: Minnesota Mining and Manufacturing CompanyInventors: Steven M. Heilmann, Larry R. Krepski, Dean M. Moren, Jerald K. Rasmussen, Howell K. Smith, II
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Patent number: 4929751Abstract: A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.Type: GrantFiled: October 19, 1987Date of Patent: May 29, 1990Assignee: Yale UniversityInventors: Harry H. Wasserman, Natesan Murugesan, John H. Van Duzer
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Patent number: 4927964Abstract: An advantageous method of producing in large amounts on a commercial scale 2-substituted oxyimino-3-oxobutyric acids, which are useful as intermediates in the synthesis of e.g. aminothiazole cephalosporins, is characterized by reacting a tert-butyl 2-substituted oxyimino-3-oxobutyrate with a hydrogen halide in an anhydrous organic solvent.Type: GrantFiled: January 11, 1989Date of Patent: May 22, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Kenzo Naito, Yukio Ishibashi, Haruo Shinbo
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Patent number: 4916156Abstract: The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.Type: GrantFiled: April 6, 1988Date of Patent: April 10, 1990Assignee: SanofiInventors: Madeleine Mosse, Vincenzo Proietto
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Patent number: 4902818Abstract: The manufacture of optically active bifunctional compounds of the general formula ##STR1## wherein R represents protected hydroxymethyl, protected formyl or alkoxycarbonyl and R.sup.1 represents a group of the formula ##STR2## in which R.sup.2 and R.sup.3 represents lower alkyl or cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom represent a heterocyclic ring, by isomerizing compounds of the general formula ##STR3## wherein R, R.sup.2 and R.sup.3 have the above significance and R.sup.3 can additionally signify hydrogen, is described.The compounds of formula I are potential intermediates in the manufacture of, interalia, natural vitamin E and natural vitamin K.sub.1.Type: GrantFiled: October 5, 1988Date of Patent: February 20, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Hans-Jurgen Hansen, Rudolf Schmid, Max Schmid
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Patent number: 4876279Abstract: Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 26, 1988Date of Patent: October 24, 1989Assignee: Merck & Co., Inc.Inventors: Ta J. Lee, William F. Hoffman, Clarence S. Rooney
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Patent number: 4874822Abstract: The present invention provides a dramatically improved process for the preparation of acrylamide and methacrylamide functional monomers, oligomers, and polymers that avoids the use of acidic catalysts which can cause undesired side reactions. The present invention process involves reacting an alkenyl azlactone with a hydroxy functional compound in the presence of a catalytic amount of either a bicyclic amidine or a trivalent phosphorus compound. These efficient basic catalysts provide unexpectedly increased reaction rates under mild conditions.Type: GrantFiled: April 7, 1988Date of Patent: October 17, 1989Assignee: Minnesota Mining and Manufacturing CompanyInventors: Jerald K. Rasmussen, Steven M. Heilmann, Larry R. Krepski, Dean M. Moren
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Patent number: 4835304Abstract: Esters having the general formula: ##STR1## where X is a halogen, n is 1-5, Y is an alkyl, ether, ester, or nitro substituent, m is 0-2, Z is an ester linkage --OCO-- or --CO.sub.2 --, R' is a haloalkyl group, and p is 1-3, constitute high density flotation fluids for inertial instruments such as gyroscopes and accelerometers. Synthetic methods are disclosed for production of such fluids from available starting materials.Type: GrantFiled: May 1, 1987Date of Patent: May 30, 1989Assignee: Charles Stark Draper LaboratoryInventor: John R. Williams
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Patent number: 4831184Abstract: This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure ##STR1## wherein R and R.sub.9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino;R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are independently hydrogen, alkyl, alkenyl or alkynyl containing up to 20 carbon atoms, aryl or aryl-lower alkyl having from 7 to 12 carbon atoms, heterocyclic or heterocyclic-lower alkyl having from 6 to 12 carbon atoms, cycloalkyl or cycloalkyl-alkyl containing up to 20 carbon atoms in the cycloalkyl group, provided that each of R.sub.1 and R.sub.2 and R.sub.4 and R.sub.Type: GrantFiled: February 14, 1983Date of Patent: May 16, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
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Patent number: 4816604Abstract: The compounds of formula I, ##STR1## where the substituents have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterifield form, are useful as cardioselective .beta.-adrenoceptor blocking agents.Type: GrantFiled: March 9, 1987Date of Patent: March 28, 1989Assignee: William J. LouisInventors: William J. Louis, Richard Berthold, Andre Stoll
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Patent number: 4816598Abstract: The invention relates to 4-amino-butanoic acid derivatives of general formula: ##STR1## in which: M represents an alkali metal atom,R represents a protected amino group,R.sub.1 represents a labile group,R.sub.2 represents hydrogen, a branched- or straight-chain alkyl radical having from 1 to 6 carbon atoms, a lower methyloxyalkyl, a lower methylthioalkyl, a lower (lower alkyl)-aminoalkyl, a lower di-(lower alkyl)-aminoalkyl or a lower hydroxyalkyl radical or R.sub.2 represents one of the radicals of general formulae:Cy--A--, Cy--O--A'--, R--A'-- or R.sub.Type: GrantFiled: June 16, 1987Date of Patent: March 28, 1989Assignee: SanofiInventors: Marcel Descamps, Walter Verstraeten
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Patent number: 4812592Abstract: The invention concerns a process for the preparation of the esters of an alkyltartronic acid by direct oxidation, with O.sub.2 or the like, at 30.degree.-200.degree. C., of the corresponding alkyl-malonic esters, in the presence of a catalytic system, comprising a salt of a transition metal, selected from Mn, Fe, Co and Cu, and an alkali-metal salt of an aliphatic carboxylic acid, optionally in the presence of a polar solvent.Type: GrantFiled: January 8, 1987Date of Patent: March 14, 1989Assignees: Istituto Guido Donegani, S.p.A., Consiglio Nazionale Delle RicercheInventors: Roberto Santi, Giuseppe Cometti, Anselmo Pagani
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Patent number: 4788218Abstract: Novel compounds having the general formula: ##STR1## wherein: R.sup.1 is hydrogen or an acyl substituent of the formula:--(C.dbd.O)--R.sup.2wherein:R.sup.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkylene, haloalkyl, aryl, haloaryl or arylalkylene are described. These compounds have both gonadotropic and antigonadotropic properties depending upon the dosage level, and are therefore useful in therapy in the control of male fertility in mammals, particularly in human beings. These compounds combine gonadotropic, antigonadotropic and androgenic properties in the same compound. Their use with LHRH antagonists on male fertility control is also disclosed.Type: GrantFiled: April 28, 1986Date of Patent: November 29, 1988Assignee: SRI InternationalInventors: Masato Tanabe, David F. Crowe, George Detre, Peters, Richard H., Mitchell A.g34 Avery
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Patent number: 4766246Abstract: Sweeteners of the formula: ##STR1## and food-acceptable salts thereof, where the substituents are disclosed herein.Type: GrantFiled: August 19, 1986Date of Patent: August 23, 1988Assignee: General Foods CorporationInventors: Paul R. Zanno, Ronald E. Barnett, Glenn M. Roy
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Patent number: 4755619Abstract: Compounds of formula (II) ##STR1## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen, alkyl, alkenyl and alkynyl groups having up to a maximum of four carbon atoms and being unsubstituted, and alkyl, alkenyl and alkynyl groups having up to a maximum of three carbon atoms and being substituted by one, or in the case of fluoro by one or more, substitutents but with the proviso that when R.sub.1 is hydrogen then R.sub.2 is hydrogen or methyl, or R.sub.1 and R.sub.2 together constitute an ethylene bridging group, and R.sub.3 is a group which under physiological conditions undergoes elimination with the formation of a 3,5-dioxopiperazinyl ring, with the further proviso that the compound is in the meso or erythro configuration when each of R.sub.1 and R.sub.Type: GrantFiled: March 24, 1986Date of Patent: July 5, 1988Assignee: National Research Development CorporationInventors: Andrew M. Creighton, William A. Jeffery
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Patent number: 4740331Abstract: Salts having the formula:Y--NH.sub.3.sup..sym..RCO.sub.2.sup..crclbar. Iin which Y is a group of formula R.sup.1 XCH.sub.2 CH(OH)CH.sub.2 --, R and R.sup.1 are the same or different and each is a straight- or branched chain alkyl group having from 1 to 18 carbon atoms, a straight- or branched chain alkenyl group having from 2 to 18 atoms, a cycloalkyl group having from 4 to 12 ring atoms, an aryl group having 6-10 ring atoms, or an aralkyl group having from 7 to 10 carbon atoms; and X is O,CO.sub.2, NR.sup.2 or S and R.sup.2 is hydrogen, a straight- or branched chain alkyl group having from 1 to 18 carbon atoms or an alkenyl group having from 2 to 18 C atoms. These salts are useful as corrosion inhibitors.Type: GrantFiled: February 7, 1986Date of Patent: April 26, 1988Assignee: Ciba-Geigy CorporationInventors: Emyr Phillips, David Wilson
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Patent number: 4739107Abstract: Process for the preparation of dicarboxylate esters by reacting an optionally substituted ethylenically unsaturated hydrocarbon having two carbon atoms less than said dicarboxylic acid, CO and an alcohol in the presence of a Group VIII noble metal or a compound thereof, a quinone and optionally, a redox agent and molecular oxygen.Type: GrantFiled: January 12, 1987Date of Patent: April 19, 1988Assignee: Shell Oil CompanyInventor: Eit Drent
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Patent number: 4734120Abstract: Dipeptides containing C-terminal phosphinothricin of the formula ##STR1## in which phosphinothricin is attached to a--preferably natural--amino acids at the amino group are effective herbicides in the pre-emergence and post-emergence techniques. The compounds are obtained, for example, by reacting phosphinothricin with the hydroxysuccinimide ester of an amino acids which is protected at the amino group in the presence of a base and subsequently splitting off the protective groups.Type: GrantFiled: December 12, 1986Date of Patent: March 29, 1988Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Klaus Bauer, Hermann Bieringer
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Patent number: 4727151Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.Type: GrantFiled: November 22, 1978Date of Patent: February 23, 1988Assignee: INTERx Research CorporationInventor: Nicolae S. Bodor
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Patent number: 4709081Abstract: The invention relates to a process for the preparation of compounds of formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or the group COR.sup.2, whereinR.sup.2 stands for a straight or branched chained alkyl having 1 to 8 carbon atoms optionally substituted with phenyl, naphthyl, tetrahydronaphthyl or m-phenoxy-benzyl, cycloalkyl having 3 to 6 carbon atoms optionally substituted with one or more straight or branched chained alkyl or alkenyl having 1 to 6 carbon atoms, phenyl or naphthyl.The compounds of formula (I) are prepared according to the invention by(a) reacting esters of formula (II) ##STR2## wherein X stands for chlorine or bromine andR.sup.2 has the same meanings as defined above with a phenol alkali metal salt and(b) if desired converting the diphenyl ethers so obtained to a specific compound of formula (I), m-phenoxybenzyl alcohol by the hydrolysis of the ester group.Type: GrantFiled: September 26, 1985Date of Patent: November 24, 1987Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.Inventors: Gergely Heja, Dezso Korbonits, Endre Palosi, Pal Kiss, Csaba Gonczi, Ida Szvoboda nee Kanzel, Ede Marvanyos, Judit Kun, Maria Szomor nee Wundele, Gabor Szabo, Tamas Kallay, Laszlo Ledniczky
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Patent number: 4708954Abstract: Pharmaceutical compositions containing an oxaluric acid derivative of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen; an alkyl group or a cycloalkyl group; or R.sub.1 and R.sub.2 are joined to form a heterocyclic ring with the nitrogen atom to which they are both attached; and R.sub.3 is hydrogen or an alkyl group. These compounds have excellent hypoglycemic effects with low toxcicity and safety.Type: GrantFiled: February 7, 1986Date of Patent: November 24, 1987Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kazuharu Ienaga, Ko Nakamura, Akira Ishii
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Patent number: 4691048Abstract: The invention concerns a process for reducing carbonylation of an aldehyde wherein the aldehyde is used as hemiacetalester, the reaction being conducted in the presence of a catalyst consisting of a cobalt carbonyl complex.The hemiacetal-ester may be formed in situ by reacting an acetal with an anhydride of acid.The process preferentially yields alkylene-glycol mono-esters, free of esterified, for a ratio H.sub.2 /CO ranging from 1:1 to 3:1 and preferentially 2-alkoxy aldehydes, for a ratio H.sub.2 /CO ranging from 0.1:1 to 0.5:1.Type: GrantFiled: May 10, 1985Date of Patent: September 1, 1987Assignee: Institut Francais du PetroleInventors: Francois Hugues, Dominique Commereuc, Yves Chauvin
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Patent number: 4691047Abstract: A process for the carbonylation of a conjugated diene with CO and an alcohol or water in the presence of an aprotic solvent is carried out in the presence of a dissolved catalytic system prepared by combining a Pd(II) compound, at least 5 mol of a triarylphosphine per gram atom of Pd and at least 1 mol of HC1 per gram atom of trivalent P.Type: GrantFiled: March 26, 1986Date of Patent: September 1, 1987Assignee: Shell Oil CompanyInventor: Eit Drent
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Patent number: 4681953Abstract: Novel syntheses of dihalovinylcyclopropanecarboxylates, including potent insecticides, are described. The processes begin with the reaction between an alkenol and an orthoester to produce a .gamma.-unsaturated carboxylate, followed by the catalyzed addition of a carbon tetrahalide to the double bond and dehydrohalogenation to produce a cyclopropane derivative.Type: GrantFiled: August 22, 1975Date of Patent: July 21, 1987Assignee: Sagami Chemical Research CenterInventors: Kiyoshi Kondo, Kiyohide Matsui, Akira Negishi, Yuriko Takahatake
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Patent number: 4680388Abstract: Antibacterial activity is exhibited by compounds having the formula and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 31, 1986Date of Patent: July 14, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, William H. Koster, Robert Zahler
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Patent number: 4677129Abstract: 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.Type: GrantFiled: June 20, 1985Date of Patent: June 30, 1987Assignee: Ciba-Geigy CorporationInventors: Alex Alder, Jaroslav Stanek, Daniel Bellus
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Patent number: 4665193Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: June 27, 1986Date of Patent: May 12, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4659372Abstract: 2-Aryl-1,3-cyclohexanedione enol ester compounds exhibit outstanding miticidal, mite ovicidal and herbicidal activity.Type: GrantFiled: November 28, 1983Date of Patent: April 21, 1987Assignee: Union Carbide CorporationInventor: Thomas N. Wheeler
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Patent number: 4638071Abstract: The following dipeptides possess a high order of sweetness: ##STR1## wherein X=O or S;R is alkyl containing 1-3 carbon atoms;R.sub.1 is cycloalkyl, cycloalkenyl, lower alkyl-substituted cycloalkyl or cycloalkenyl, bicycloalkyl, bicycloalkenyl, tricycloalkyl, cyclic ether, cyclic thioether, cyclic sulfoxides, cyclic sulfones, aryl, benzyl, alkylaryl, aromatic heterocyclic or alkyl substituted aromatic heterocyclic containing up to 10 ring carbon atoms and up to a total of 12 carbon atoms;R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are each H or lower alkyl;R.sub.5 is H, lower alkyl or cycloalkyl containing 3-5 ring carbons;each n=0, 1 or 2;m=0 or 1;Z is an alkylene chain containing 0-2 carbon atoms in the principal chain and up to a total of 6 carbon atoms;and food-acceptable salts.Type: GrantFiled: December 27, 1984Date of Patent: January 20, 1987Assignee: General Foods CorporationInventors: Ronald E. Barnett, Paul R. Zanno, Glenn M. Roy
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Patent number: 4633006Abstract: Novel 3-hydroxy-4-alkyloxyphenyl aliphatic carboxylate compounds particularly well suited as sweeteners in foodstuff.Type: GrantFiled: August 14, 1985Date of Patent: December 30, 1986Assignee: General Foods CorporationInventors: Ronald E. Barnett, Jed A. Riemer, Paul R. Zanno
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Patent number: 4622418Abstract: Amides of .alpha.-aminodicarboxylic acids and .beta.-aminoethers are low calorie sweetners.Type: GrantFiled: April 4, 1985Date of Patent: November 11, 1986Assignee: General Foods CorporationInventors: Ronald E. Barnett, Paul R. Zanno, Glenn M. Roy
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Patent number: 4622417Abstract: Dipeptides of certain .alpha.-amino dicarboxylic acids and etherified hydroxy .alpha.-amino-mono-carboxylic acid esters possess a high order of sweetness. These dipeptides have the following formula: ##STR1## wherein R is alkyl containing 1-3 carbon atoms;R.sub.1 is cycloalkyl, cycloalkenyl, lower alkyl substituted cycloalkyl or cycloalkenyl, bicycloalkyl, bicycloalkenyl or tricycloalkyl containing up to 10 ring carbon atoms and up to a total of 12 carbon atoms;R.sub.2 and R.sub.4 are each H or alkyl containing 1-3 carbon atoms;R.sub.3 is H, alkyl containing 1-6 carbon atoms or cycloalkyl containing 3-5 ring carbons;n=0, 1 or 2; andm=0 or 1;and food acceptable salts thereof.Type: GrantFiled: December 27, 1984Date of Patent: November 11, 1986Assignee: General Foods CorporationInventors: Ronald E. Barnett, Paul R. Zanno, Glenn M. Roy
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Patent number: 4619782Abstract: Sweeteners of the formula: ##STR1## and food-acceptable salts thereof, where the substituents are disclosed herein.Type: GrantFiled: April 15, 1985Date of Patent: October 28, 1986Assignee: General Foods CorporationInventors: Paul R. Zanno, Ronald E. Barnett, Glenn M. Roy