Sulfur In Acid Moiety Patents (Class 560/9)
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Patent number: 5235100Abstract: A process for the separation of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process comprises:i) separating a racemic mixture of an aliphatic carboxylic acid or ester thereof having the formula: ##STR1## where R.sub.1 is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; cycloalkyl; alkyl-substituted cycloalkyl; C.sub.6 to C.sub.14 aryl; C.sub.1 to C.sub.6 alkylthio; C.sub.2 to C.sub.8 cycloalkylthio; C.sub.6 to C.sub.10 arylthio; C.sub.6 to C.sub.10 arylcarbonyl; C.sub.4 to C.sub.8 cycloalkenyl; trifluoromethyl; halo; or C.sub.4 to C.sub.Type: GrantFiled: January 24, 1992Date of Patent: August 10, 1993Assignee: Ethyl CorporationInventors: Azfar A. Choudhury, Abbas Kadkhodayan, Deepak R. Patil
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Patent number: 5235095Abstract: An improved process for the separation of enantiomers of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process involves: (i) forming a salt solution comprising said racemic mixture of a C.sub.1 to C.sub.6 linear or branched aliphatic carboxylic acid and an organic or inorganic base; (ii) treating said salt solution with one-half molar equivalent of a chiral organic nitrogenous base having a base strength no stronger than said organic or inorganic base; and (iii) precipitating from the reaction solution formed in step (ii) the less soluble diastereomeric salt, the improvement being adding to the salt solution of step (ii) an inert organic or inorganic base that is soluble in the salt solution.Type: GrantFiled: January 24, 1992Date of Patent: August 10, 1993Assignee: Ethyl CorporationInventors: Abbas Kadkhodayan, Deepak R. Patil, Azfar A. Choudhury
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Patent number: 5223529Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.Type: GrantFiled: May 11, 1990Date of Patent: June 29, 1993Assignee: Rhone-Poulenc SanteInventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Gerard Roussel, Franco Manfre
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Patent number: 5223645Abstract: Unsaturated phenone derivatives of the general formula I ##STR1##whereR.sup.1 is C.sub.1 -C.sub.4 -alkyl, cyclopropyl, cyclopentyl, cyclohexyl, indanonyl, tetralonyl, phenyl or phenyl in which some or all of the hydrogen atoms have been replaced by a C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -thioalkyl group, or together with R.sup.2 or R.sup.6 forms an ethylene or propylene bridge,R.sup.2 to R.sup.6 are each hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -thioalkyl, and R.sup.3, R.sup.4 and R.sup.5 may each additionally be hydroxyl, R.sup.2 or R.sup.6 may additionally together with R.sup.1 form an ethylene or propylene bridge and one or more, but not more than three, of the radicals R.sup.2 to R.sup.6 are a group of the general formula II ##STR2##whereK is C.sub.1 -C.sub.10 -alkylene which may contain 1 or 2 oxygen or sulfur atoms,Y is straight-chain or branched C.sub.1 -C.sub.10 -alkylene or is C.sub.1 -C.sub.Type: GrantFiled: September 23, 1991Date of Patent: June 29, 1993Assignee: BASF AktiengesellschaftInventors: Juergen Barwich, Gerd Rehmer, Kaspar Bott
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Patent number: 5214191Abstract: 2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.Type: GrantFiled: May 22, 1990Date of Patent: May 25, 1993Assignee: Cortech, Inc.Inventors: Gary P. Kirschenheuter, Lyle W. Spruce, John C. Cheronis
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Patent number: 5202458Abstract: Compounds of the formula I or II ##STR1## in which R, R.sup.0, R.sup.1 and R.sup.2 are as defined in claim 1. The compounds, some of which are novel, are light stabilizers for color photographic recording materials.Type: GrantFiled: August 5, 1991Date of Patent: April 13, 1993Assignee: Ciba-Geigy AGInventor: David G. Leppard
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Patent number: 5202471Abstract: Retinoid like activity is exhibited by compounds of the formula ##STR1## where R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and B independently are hydrogen, lower alkyl cycloalkyl, lower alkenyl, SR* or OR* where R* is lower alkyl, cycloalkyl or lower alkenyl; Y is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl or (CH.sub.2).sub.n where n is 0-6; and Z is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR' or a ketal derivative where R' is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.Type: GrantFiled: February 6, 1990Date of Patent: April 13, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5202451Abstract: Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.Type: GrantFiled: February 17, 1988Date of Patent: April 13, 1993Assignee: NeoRx CorporationInventors: Alan R. Fritzberg, Ananthachari Srinivasan
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Patent number: 5196423Abstract: Unsaturated cyclohexylacetic acid derivatives of the formula I ##STR1## where U is.dbd.NOCH.sub.3, .dbd.CHOCH.sub.3, .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.N--NH--CH.sub.3 or .dbd.CH--S--CH.sub.3,n is from 0 to 10,A is hydrogen or substituted or unsubstituted alkyl, cycloalkyl, aryl or hetaryl, andX is a single bond when n is 0, and oxygen, sulfur or a single bond when n is not 0, and the plant-compatible acid addition products and base addition products thereof, and fungicides and insecticides containing these compounds.Type: GrantFiled: June 15, 1992Date of Patent: March 23, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5191113Abstract: A cinnamoylamide derivative of general formula: ##STR1## [wherein, (i) in case that R.sup.2 represents a methyl group and R.sup.3 represents a hydrogen atom,(R.sup.1).sub.n represents a group selected out of3-pentyl group,4-pentyl group,4-neopentyl group,4-(2-ethylbutyl) group,4-(2-methylpentyl) group,2-fluoro-4-pentyloxy group,4-butylthio group,4-cyclobutylmethyl group,4-cyclohexylmethyl group,4-(4-phenylbutyl) group and4-phenoxy group, and(ii) in case that R.sup.2 represents a hydrogen atom and R.sup.3 represents a methyl group,(R.sup.1).sub.n represents a group selected out of3-pentyl group and4-phenethyl group.]or non-toxic salts thereof possess an inhibitory activity on 5.alpha.-reductase, and therefore be useful for treating and/or preventing agent for alopecia, acnes or prostatic hypertrophy.Type: GrantFiled: December 5, 1991Date of Patent: March 2, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5180744Abstract: Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 29, 1991Date of Patent: January 19, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5179105Abstract: A phenoxyacetic acid compound represented by the general formula I: ##STR1## wherein X is one member selected from the class consisting of hydrogen atom, halogen atoms, lower alkyl groups, trifluoromethyl group, alkoxy groups, hydroxy group, and cyano group, R.sup.1 is one member selected from the class consisting of hydrogen atom, methyl group, and ethyl group, n is an integer in the range of from 0 to 2, and Y is ##STR2## wherein R.sup.2 is hydrogen atom or n-propyl group and m is an integer in the range of from 1 to 5, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 15, 1991Date of Patent: January 12, 1993Assignee: Terumo Kabushiki KaishaInventors: Azuma Igarashi, Sachiko Maeda, Yasuhiro Hirakawa, Katsuyoshi Sugisaki, Shinji Ozawa
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Patent number: 5179229Abstract: A process for the preparation of 2,2-diorgano-3-arylpropionic acids is disclosed by the carbonylation of corresponding 2,2-diorgano-1-aryl ethanol in the presence of a Lewis acid catalyst. Furthermore, a process for the production of 2,2-diorgano-3-arylpropionic esters is disclosed by reacting a corresponding 2,2-diorgano-1-aryl ethanol with carbon monoxide and an alcohol in the presence of a Lewis acid catalyst.Type: GrantFiled: April 24, 1992Date of Patent: January 12, 1993Assignee: Hoechst Celanese CorporationInventor: Varadaraj Elango
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Patent number: 5177106Abstract: Novel 4-amino substituted phenoxyalkyl carboxylic acid, ester, and alcohol derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: June 21, 1991Date of Patent: January 5, 1993Assignee: Warner-Lambert CompanyInventor: Paul L. Creger
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Patent number: 5162405Abstract: The present invention comprises novel single-functional and mixtures of multi-functional oligomeric performance additive compounds having one or more components of Structure A R1 ? ? ##STR1## (The definitions of R, Z1, Z2, Z3, A1, A2, A3 and y are given in the Summary Section), their uses and polymeric compounds and compositions containing them which have enhanced oxidative stabilities, enhanced ultraviolet (UV) and light stabilites and/or enhanced flame retardance. An example is the bis sulfonic acid bispotassium salt reaction product from an oligomeric caprolactone diol (TONE.RTM. 260), 2-sulfobenzoic acid anhydride and potassium carbonate, and use of this product, at levels up to about 3.0%, in a general purpose bisphenol A polycarbonate resin, to enhance the fire resistance or flame retardance of the polycarbonate resin.Type: GrantFiled: March 22, 1991Date of Patent: November 10, 1992Assignee: ELF Atochem North America, Inc.Inventors: Ronald E. MacLeay, Jose Sanchez, Daryl L. Stein
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Patent number: 5157143Abstract: A diastereoselective process for the preparation of compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification and the asterisks show the asymmetric carbon atoms) starting from the corresponding N-protected 2-amino-3-aryl-propan-1-ol is described.The compounds of formula I are intermediates useful for the synthesis of pharmacologically active peptides.Type: GrantFiled: May 11, 1989Date of Patent: October 20, 1992Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Dario Chiarino, Angelo Carenzi
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Patent number: 5152826Abstract: An herbicide compound of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, nitro; cyano; C.sub.1 -C.sub.2 haloalkyl, or R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together are oxo;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.5 and R.sup.6 together are alkylene having 2 to 5 carbon atoms;R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n --wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.Type: GrantFiled: October 16, 1991Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventor: Christopher G. Knudsen
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Patent number: 5147893Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof.Type: GrantFiled: May 9, 1991Date of Patent: September 15, 1992Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 5145874Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: February 25, 1991Date of Patent: September 8, 1992Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, by Vera M. Wallach, legal representative
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Patent number: 5144057Abstract: 3-Oxocarboxylic acid esters are produced by acylation of the magnesium enolates of acetoacetic acid esters with carboxylic acid chlorides and cleavage of the acetyl group from the acylacetoacetic acid esters formed as the intermediate product. The yields and purity of the products are considerably improved by adding a tertiary amine during the acylation.Type: GrantFiled: October 11, 1991Date of Patent: September 1, 1992Assignee: Lonza Ltd.Inventor: Martin Eyer
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Patent number: 5140044Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.Type: GrantFiled: March 27, 1990Date of Patent: August 18, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
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Patent number: 5135940Abstract: Compounds of the Formulae: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 20, 1991Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Joshua Rokach, Rejean Fortin, Christiane Yoakim, Yvan Guindon
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Patent number: 5132312Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: July 21, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent E. Neuenschwander
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Patent number: 5126476Abstract: A process for making aryl-, heteroaryl-, or cycloalkyl-substituted alkyl urethanes is disclosed. The urethanes are prepared by electrophilic carbamylation of aromatic compounds with alkylene bis(carbamic acid esters) or the equivalent in the presence of an acidic catalyst and a polar aprotic solvent. The alkyl urethanes may be cracked to give the corresponding substituted alkyl isocyanates.Type: GrantFiled: January 25, 1991Date of Patent: June 30, 1992Assignee: Arco Chemical Technology, L.P.Inventors: Mahmoud K. Faraj, Haven S. Kesling, Jr., John G. Zajacek
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5112862Abstract: 3-Methoximinopropionic esters of the formula ##STR1## where the radicals R (m=1 to 5) are each hydrogen, halogen, cyano, nitro, alkyl, cycloalkyl, alkenyl, alkoxy, haloalkyl, haloalkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, unsubstituted or substituted benzyl or unsubstituted or substituted benzyloxy, or the group ##STR2## is naphthyl, and X is methyleneoxy, oxymethylene, ethylene, ethenylene, thiomethylene or oxygen, and fungicides containing these compounds.Type: GrantFiled: July 2, 1990Date of Patent: May 12, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5109000Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine; CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 --AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12) O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.5 is hydrogen; alkyl; or --CH(R.Type: GrantFiled: April 30, 1990Date of Patent: April 28, 1992Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
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Patent number: 5100654Abstract: A phosphorylated derivative of L-dopa of the formula ##STR1## wherein when X is ##STR2## wherein Z is --CH.sub.2, N, S or a linkage other than oxygen which renders the phosphate group resistant to hydrolysis by phosphatase enzymes in tissues and biological fluids,then Y is OQ, wherein Q is H or an alkyl with one to twelve carbon atoms, orwherein X is OQ, then Y is ##STR3## wherein R' is hydrogen or a pharmaceutically acceptable cation and R is a moiety which increases hydropobicity. The phosphorylated derivative of L-dopa is useful as an agent to increase the melanin content in mammalian skin and hair.Type: GrantFiled: April 7, 1989Date of Patent: March 31, 1992Assignee: Yale UniversityInventors: John M. Pawelek, Michael P. Osber
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Patent number: 5099030Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: June 27, 1991Date of Patent: March 24, 1992Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5096925Abstract: Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazoly or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.o independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.Type: GrantFiled: April 11, 1990Date of Patent: March 17, 1992Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 5095133Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of alkoxides of the formulaM.sup.1 OR.sup.10 (IV)where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.10, X.sup.- and M.sup.1 have the meaning mentioned in the description.Type: GrantFiled: July 16, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz U. Blank, Helmut Kraus
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Patent number: 5073552Abstract: Substituted benzophenones are disclosed having the following formula ##STR1## where R.sub.A and R.sub.B are each independently COOH, C.sub.1 to C.sub.12 linear or branched alkyl or taken together to form an anhydride ring, R is nitro or amino unsubstituted or substituted with at least one C.sub.1 to C.sub.6 linear or branched alkyl, phenyl or substituted phenyl, the substituents being one or more C.sub.1 to C.sub.6 linear or branched alkyl or C.sub.6 to C.sub.10 aryl, Y and Y' are the same or different and are a chemical bond ##STR2## and m is 0 or 1 with the proviso that both R.sub.A and R.sub.B can not be hydrogen.Processes to produce these benzophenones are also disclosed.Type: GrantFiled: September 4, 1990Date of Patent: December 17, 1991Assignee: Ethyl CorporationInventors: Mark W. Beltz, Venkataraman Ramachandran
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Patent number: 5066675Abstract: There are described new phenylacetic acid derivatives of general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: August 31, 1990Date of Patent: November 19, 1991Assignee: Schering AktiengesellschaftInventors: Ulrich Buhmann, Hartmut Joppien, Dietrich Baumert
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Patent number: 5066823Abstract: A process for the preparation of 5-acylamino-2,4,6-triiodo or tribromo-benzoic acid derivatives of formula (I), wherein X is I or Br, R is H or a variously substituted alkyl, or a group of formula (II), wherein X has the above meanings; Y is hydroxy, alkoxy, hydroxyalkoxy, alkylamino or hydroxyalkylamino; Z may be the same as COY or it is hydroxylalkylaminocarbonyl provided that at least one of the two acyl or R groups is hydroxy-substituted, which process comprises the rearrangement of the corresponding 5-(alkylaminocarbonyl-alkoxy)-2,4,6-trioodo ro tribromo-benzoic acid derivatives, in the presence of bases.Type: GrantFiled: October 10, 1989Date of Patent: November 19, 1991Assignee: Bracco Industria Chemica S.p.A.Inventors: Ernest Felder, Carlo Musu, Luciano Fumagalli, Fulvio Uggeri
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5051447Abstract: Oxime ethers of the general formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or alkyl,R.sup.3 is hydrogen, halogen, cyano, aryl or aryloxy, the aromatic ring being unsubstituted or substituted, or R.sup.3 is heteroaryl, adamantyl, fluorenyl or cycloalkyl or cycloalkenyl, these radicals being unsubstituted or substituted,X is saturated or unsaturated C.sub.1 -C.sub.12 -alkylene which is unsubstituted or substituted, andn is 0 or 1,and fungicides containing these compounds.Type: GrantFiled: July 20, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Franz Schuetz, Siegbert Brand, Hubert Sauter, Eberhard Ammermann, Gisela Lorezn
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Patent number: 5045565Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: September 8, 1989Date of Patent: September 3, 1991Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5036053Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, composition containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertensions, or hyperaldosteronism.Type: GrantFiled: March 15, 1989Date of Patent: July 30, 1991Assignee: Warner-Lambert CompanyInventors: Richard Himmelsbach, John C. Hodges, James S. Kaltenbronn, William C. Patt, Joseph T. Repine, Ila Sircar
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Patent number: 5028256Abstract: A composition for protecting culture plants from the phytotoxic action of herbicidally active chloracetanilides contains as active ingredient an acylamine derivative of the formula I ##STR1## wherein X is oxygen, sulfur, --SO-- or --SO.sub.2 --,Q is an alkyl, alkenyl, alkinyl group, which may be interrupted by oxygen sulfur sulfonyl or sulfonyl, or a test 1,3-dioxolan-2-yl-alkyl, 1,3-dioxolan-4-alkyl, 2,2-dialkyl-1,3-dioxolan-4-ylalkyl, 1,3-dioxan-2-ylalkyl, 2-benzopyranylalkyl, alkoxycarbonyl alkenyloxycarbonyl or tetrahydrofurylalkyl, or the groupQ--X represents also a halogenoalkyl radical,n is 1, 2 or 3,Z is hydrogen, halogen, alkyl or dioxymethylene, alkoxy, alkenyloxy or alkinyloxy, A is a C.sub.1 -C.sub.8 -hydrocarbon radical which may be straight-chained, branched or cyclic and which is unsubstituted or substituted by alkoxy, alkylthio, cyano or halogen,R is halogenoalkyl or halogenoalkenyl,R.sub.1 is hydrogen, a C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.Type: GrantFiled: December 22, 1988Date of Patent: July 2, 1991Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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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: 5026896Abstract: Novel trisubstituted benzoic acid intermediates which are useful in the preparation of certain herbicidal 2-(2,3,4-trisubstituted benzoyl)-1,3-cyclohexanediones are described.Type: GrantFiled: May 8, 1990Date of Patent: June 25, 1991Assignee: ICI Americas Inc.Inventor: William J. Michaely
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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: 5017583Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: February 23, 1988Date of Patent: May 21, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
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Patent number: 5015762Abstract: Aralkylphenylureas of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen, alkoxy or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together are unsubstituted or substituted alkylene which may or may not be interrupted by oxygen or sulfur, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 chain which is fused to the benzene ring to give a substituted or unsubstituted naphthyl ring, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl and n is 1, 2, 3 or 4, and herbicides containing these ureas.Type: GrantFiled: May 28, 1981Date of Patent: May 14, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
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Patent number: 5013861Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.Type: GrantFiled: October 6, 1986Date of Patent: May 7, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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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: 5008438Abstract: Ortho-substituted phenol ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio or amino which is unsubstituted or mono- or disubstituted by C.sub.1 -C.sub.4 -alkyl,R.sup.2 is C.sub.1 -C.sub.4 -alkyl,R.sup.3 is aryloxy, arylthio or arylalkoxy, the aromatic ring being unsubstituted or substituted by one or more of the following radicals: halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.2 -haloalkyl, aryl, aryl-C.sub.1 -C.sub.2 -alkoxy, C.sub.1 -C.sub.4 -alkylcarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylsubstituted amino, cyano, nitro,X is CH or N, andY is saturated or unsaturated C.sub.2 -C.sub.12 -alkylene,and fungicides containing these compounds.Type: GrantFiled: March 13, 1989Date of Patent: April 16, 1991Assignee: BASF AktiengesellschaftInventors: Franz Schuetz, Siegbert Brand, Bernd Wenderoth, Hubert Sauter, Eberhard Ammermann, Cisela Lorenz
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Patent number: 5006159Abstract: The present disclosure is directed to substituted cyclohexanedione compounds, the preparation of said compounds, compositions containing said compounds and the use of said compositions in the selective pre- and postemergent kill and control of grassy weeds in the presence of various crop plants.Type: GrantFiled: March 30, 1990Date of Patent: April 9, 1991Assignee: DowElancoInventors: Lowell D. Markley, Christopher T. Hamilton, Beth A. Swisher, Jacob Secor