Nitrogen Or Halogen In Acid Moiety Patents (Class 560/153)
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Patent number: 4780469Abstract: A (fused) benz(thio)amide of the formula: ##STR1## wherein B represents(i) a carbocyclic ring of from 4 to 8 members being unreplaced or replaced one, two or three of optional carbon atom(s) by oxygen, nitrogen and/or sulphur atom(s) or(ii) a divalent group of the formula: ##STR2## R.sup.1 represents a group of formula: ##STR3## (iv) a straight or branched alkyl, alkenyl, or alkynyl of from 1 to 20 carbon atoms,R.sup.4 represents(i) when B represents a closed ring, a group of the formula: ##STR4## (ii) when B does not represent a ring, a group of formula: ##STR5## with the proviso that compounds of formula: ##STR6## wherein A' is a vinylene or an ethylene group optionally substituted by straight or branched alkyl groups of from 1 to 4 carbon atom(s);R.sup.4' is--(CH.sub.2).sub.n --COOR.sup.8andR.sup.1' is(i) a group of the formula: ##STR7## or (ii) a group of the formula: ##STR8## are excluded, wherein A, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, U, n, m, p, q, R.sup.5', and R.sup.Type: GrantFiled: August 20, 1985Date of Patent: October 25, 1988Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
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Patent number: 4769325Abstract: 2-(Allenyl)penicillins antibiotics and intermediates thereto are disclosed. A process for making the 2-(allenyl)penicillins and the starting materials for the process are also disclosed.Type: GrantFiled: July 28, 1986Date of Patent: September 6, 1988Inventors: Jack E. Baldwin, Amit Basak
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Patent number: 4767781Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.Type: GrantFiled: December 8, 1986Date of Patent: August 30, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada
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Patent number: 4737300Abstract: The invention relates to material containing aldosemarcaptals of the formula I ##STR1## wherein n can be an integer from 2 to 6, and wherein R.sup.1 and R.sup.2 are identical or different, and in each case are C.sub.1 -C.sub.18 -alkyl, which is unsubstituted, substituted or interrupted by --O-- or --S--, or are --(CH.sub.2).sub.r --CO--N(C.sub.1 -C.sub.17 -alkyl).sub.2, r being 1 or 2, or are phenyl, benzyl or --(CH.sub.2).sub.r --CO--O--R.sup.3, in which r can be 1 or 2 and R.sup.3 is an alkali metal or C.sub.1 -C.sub.14 -alkyl; also wherein R.sup.1 and R.sup.2 are --CH.sub.2 --CH(OH)--R.sup.4, in which R.sup.4 is hydrogen, or C.sub.1 -C.sub.16 -alkyl, unsubstituted or substituted by --OH, or --CH.sub.2 --Y--(C.sub.1 -C.sub.15 -alkyl), in which Y is --O-- or --S--; or wherein R.sup.1 and R.sup.2 together form --(CH.sub.2).sub.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: Ciba-Geigy CorporationInventors: Hermann O. Wirth, Hans-Helmut Friedrich
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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: 4721803Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and an organic hydroxyl compound to produce a N-acyl-.alpha.-amino acid ester, the improvement comprising using as the organic hydroxyl compound reactant, an organic hydroxyl compound which has a chiral center that is essentially all L or D, thereby producing a reaction mixture having essentially no enantiomeric pairs and containing diastereomeric N-acyl-.alpha.-amino acid esters having two chiral centers.Type: GrantFiled: October 29, 1985Date of Patent: January 26, 1988Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, Robert A. Dubbert, James D. Burrington
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Patent number: 4713469Abstract: A fluorine-containing multifunctional ester compound represented by the formula ##STR1## wherein A is halogen atom, NO.sub.2 or N.sub.3, B is halogen atom or SR.sup.2, R.sup.1 is lower aliphatic group, aromatic group or aralkyl, R.sup.2 is lower aliphatic group or aromatic group.Type: GrantFiled: March 27, 1986Date of Patent: December 15, 1987Assignee: Daikin Industries, Ltd.Inventors: Yoshio Takeuchi, Toru Koizumi, Kozo Hori
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Patent number: 4695588Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.Type: GrantFiled: March 16, 1978Date of Patent: September 22, 1987Assignee: Merck & Co., Inc.Inventors: Janos Kollonitsch, Arthur A. Patchett
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Patent number: 4680310Abstract: Tetrahydronaphthalene derivatives of the formula ##STR1## wherein Y, m, n, R and R.sup.1 to R.sup.9 are as set forth herein, are described.These compounds have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias and high blood pressure. The compounds of formula I can be prepared by the amination of a compound of the formula ##STR2## with a corresponding N-methyl-phenylalkylamine and optional subsequent O-acylation. Compounds of formula II and IV are also described and are within the scope of the invention.Type: GrantFiled: October 10, 1985Date of Patent: July 14, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Urs Hengartner, Henri Ramuz
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Patent number: 4678806Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: September 2, 1986Date of Patent: July 7, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
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Patent number: 4675330Abstract: A compound of formula I ##STR1## wherein R.sub.1 represents ethyl or vinyl andR.sub.2 represents a five membered saturated heterocycle or aminoalkyl unsubstituted or substituted in its alkyl moiety by hydroxy,in free or in the form of an acid addition or quaternary salt, which compounds are indicated for use as chemotherapeutic agents e.g. as anti-bacterially active antibiotics and as veterinary agents e.g. in combatting microorganism infections and promoting growth in domestic animals.Type: GrantFiled: May 6, 1986Date of Patent: June 23, 1987Assignee: Sandoz Ltd.Inventors: Heinz Berner, Hermann Vyplel
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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: 4661510Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.Type: GrantFiled: October 21, 1985Date of Patent: April 28, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano
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Patent number: 4657956Abstract: Additives for rubber compositions, giving vulcanizates having improved retention of optimum physical properties, are compounds having the formula R--S--B--S--R where B is an organic bridging group and R is an electron-withdrawing group, for example CN, CCl.sub.3, a radical containing an activated methylene group linked to the sulphur atom or the enolic tautomer of a keto-activated methylene group. Also useful as stabilizing agents are oligomeric analogues of such compounds.Type: GrantFiled: September 13, 1985Date of Patent: April 14, 1987Assignee: Monsanto Europe, S. A.Inventors: Albert F. L. G. Devaux, Philippe G. Moniotte
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Patent number: 4654433Abstract: A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.Type: GrantFiled: January 14, 1985Date of Patent: March 31, 1987Assignee: Merck & Co., Inc.Inventor: David L. Hughes
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Patent number: 4649215Abstract: Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,R.sup.3 represents hydroxy, alkoxy or an optionally substituted amino group, and-X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene groupwherein the O-atom of the hydroxy group is in the transconfiguration relative to the S-atom, are effective as leucotriene-antagonists since they eliminate the contractions of smooth muscles caused by leucotrienes and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.Type: GrantFiled: June 25, 1985Date of Patent: March 10, 1987Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Ivan Ernest, Alan J. Main, Andreas Beck
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Patent number: 4622413Abstract: Amino acid ester hydrohalide is produced by reacting amino acid, alcohol, and halocarbonyl compound represented by the formula: ##STR1## in the presence of an excess of the alcohol and under substantially anhydrous conditions, wherein X.sub.1 and X.sub.2 are each independently fluoro, chloro, bromo, trichloromethoxy or tribromomethoxy.Type: GrantFiled: August 31, 1984Date of Patent: November 11, 1986Assignee: PPG Industries, Inc.Inventor: James A. Krogh
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Patent number: 4609673Abstract: The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R is a hydrogen atom, alkyl, a metal cation or an ammonium or alkylammonium ion, R.sub.1 is a hydrogen atom, a hydroxyl group or an alkyl, O-alkyl,O-benzyl or O-acyl radical, R.sub.2 is a hydrogen atom or an alkyl, aryl or aralkyl radical, n is 0, 1 or 2 and R.sub.Type: GrantFiled: December 18, 1984Date of Patent: September 2, 1986Assignee: Boehringer Mannheim GmbHInventors: Hermann Eggerer, Bernd Hagenbruch, Tran G. Nguyen, Karlheinz Stegmeier, Johannes Pill
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Patent number: 4604417Abstract: There are disclosed polymerizable thioester synergists which have utility in enhancing the antioxidative activity of phenolic and amine stabilizers. The invention is also concerned with the thioesters themselves, their use in oxidizable organics, their combination with polymerizable and/or conventional antioxidants, and with polymers which contain these thioesters as physical admixtures or segmeric units of the polymer.Type: GrantFiled: December 10, 1984Date of Patent: August 5, 1986Assignee: The Goodyear Tire & Rubber CompanyInventor: Kirkwood S. Cottman
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Patent number: 4597913Abstract: A novel fluorinated cation exchange membrane containing carboxylic acid groups and sulfonic acid groups, both in the form of a specific pendant structure, the carboxylic acid groups being at least 20% on one surface of the membrane and gradually decreasing toward the innerside of the membrane, which membrane is useful in electrolysis of an aqueous alkali metal halide solution with advantageously stable performance for a long term under more severe operational conditions than those conventionally used. The membrane can be prepared from a novel copolymer of a fluorinated olefin with a novel sulfur containing fluorinated vinylether of the formula: ##STR1## wherein k is 0 or 1, l is an integer of 3 to 5, Z is --S-- or --SO.sub.2 -- and R is C.sub.1 -C.sub.10 alkyl, an aryl, C.sub.1 -C.sub.10 perfluoroalkyl.Type: GrantFiled: August 29, 1983Date of Patent: July 1, 1986Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Kyoji Kimoto, Hirotsugu Miyauchi, Jukichi Ohmura, Mikio Ebisawa, Toshioki Hane
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Patent number: 4596819Abstract: Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.Type: GrantFiled: January 23, 1984Date of Patent: June 24, 1986Assignee: Warner-Lambert CompanyInventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
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Patent number: 4594188Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.Type: GrantFiled: May 20, 1985Date of Patent: June 10, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, Eric M. Gordon
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Patent number: 4557754Abstract: A novel compound bis-(N,N-dimethyl-N-carbodecyloxymethyl-N-ethyleneammonium)-sulphide dichloride of the formula ##STR1## A method for preparing said novel compound comprising quaternization of bis-(.beta.-dimethylaminoethyl)-sulphide with monochloroacetic acid decyl ester, molar ratio of said reagents being not more than 1:2.A chemotherapeutic antimicrobial preparation comprising said novel compound as an active principle in combination with a pharmaceutical carrier.A plant growth regulator in the form of an aqueous solution of said novel compound in a concentration of from 0.0001 to 0.1 wt. %.Type: GrantFiled: August 13, 1980Date of Patent: December 10, 1985Assignee: Institut Organicheskoi KhimiiInventors: Georgy A. Golik, Yaroslav P. Demchenko, Miron O. Lozinsky, Vladlen V. Malovik, Valery Y. Semeny
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Patent number: 4533747Abstract: The compounds represented by the formula (I) ##STR1## wherein m is 0, 1 or 2; p is 9, 10, 11, 12 or 13; R.sub.1 ' is hydrogen, ##STR2## and R.sub.2 ' is amino, --NHCH.sub.2 CO.sub.2 R.sub.3 ', ##STR3## --NHCH.sub.2 CONH.sub.2 or --OR.sub.3 ' wherein R.sub.3 ' is an alkyl radical containing one to six carbon atoms with the proviso that when m is 0, R.sub.1 ' is hydrogen are chemical intermediates in the synthesis of leukotriene antagonists of the formula (II) ##STR4## wherein m and p, are described above and R.sub.1 is hydrogen, amino or ##STR5## R.sub.2 is hydroxyl, amino, --NHCH.sub.2 CO.sub.2 H, ##STR6## --NHCH.sub.2 CONH.sub.2 ; and X is ##STR7## --CO.sub.2 H or --CH.sub.2 OH which are useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.Type: GrantFiled: March 7, 1983Date of Patent: August 6, 1985Assignee: SmithKline Beckman CorporationInventors: John G. Gleason, Ralph F. Hall, Thomas W. Ku
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Patent number: 4533500Abstract: N-acyliminodiacetic acids are manufactured by reacting formaldehyde or a formaldehyde generator compound with a N-unsubstituted amide or a generator thereof and with carbon monoxide in contact with a carbonylation catalyst, for example, a cobalt compound, the ratio of the aldehyde groups to the amide groups being at least 2:1. The formaldehyde generator can be a polymeric form of formaldehyde and the amide generator can be a carboxylic ester, acid or anhydride.Type: GrantFiled: March 17, 1983Date of Patent: August 6, 1985Assignees: Institut Francais du Petrole, Societe Nationale Elf-Aquitaine (Production)Inventors: Yves Chauvin, Dominique Commereuc, Andre Hirschauer, Dominique Reffet, Robert Stern
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Patent number: 4491547Abstract: Monofluoromethylthioacetic acid (FCH.sub.2 SCH.sub.2 COOH) or difluoromethylthioacetic acid (F.sub.2 CHSCH.sub.2 COOH), or its derivative at the carboxy group can be prepared e.g. by treating a thioglycolic acid ester with monolfuorohalomethane or difluorohalomethane in the presence of a base if required followed by a conventional modification of the produced ester e.g. to make an acid by hydrolysis, a salt by neutralization, a halide with a halogenating agent, and from acid halide or anhydride an ester with an alcohol, or an amide with an amine. These compounds are useful intermediates in the production of medicinal and agricultural chemicals.Type: GrantFiled: December 23, 1981Date of Patent: January 1, 1985Assignee: Shionogi & Co., Ltd.Inventors: Teruji Tsuji, Hisao Sato, Yoshio Hamashima
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Patent number: 4474700Abstract: .beta.-substituted polyfluoropropionate salts, derivatives and copolymers and processes for the preparation thereof.Type: GrantFiled: May 20, 1982Date of Patent: October 2, 1984Assignee: E. I. Du Pont DeNemours and CompanyInventor: Carl G. Krespan
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Patent number: 4461775Abstract: Hydroxythioether fatty acid derivatives of formula (I) ##STR1## wherein n is 2-5, m is 8-12, R.sup.1 is OH, O-loweralkyl, NH.sub.2, NH-loweralkyl or NH-carboxyalkyl, R.sup.2 is OH or O-lower-alkyl, X is H or NH.sub.2 or ##STR2## and salts thereof are useful in preventing or alleviating asthma or other allergic diseases.Type: GrantFiled: August 2, 1982Date of Patent: July 24, 1984Assignee: McNeilab, Inc.Inventors: Kerry G. Stanley, Winston Ho
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Patent number: 4460601Abstract: Dipeptides are claimed which consist of a mercaptoalkanoic acid and a derivative of said acid, namely an S-alkyl-, aralkyl-, aryl-, acyl- or aroyl derivative with methionine, a methionine ester or a methionine amide, as well as their salts with metallic cations and organic bases. These compounds have the property of protecting the liver against intoxications and have sedative and hypnotic properties.Type: GrantFiled: December 21, 1982Date of Patent: July 17, 1984Assignee: Maggioni Farmaceutici, S.p.A.Inventors: Giampaolo Picciola, Franco Ravenna, Mario Riva
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Patent number: 4456766Abstract: The subject matter of the invention is a process for the production of N-acetyl-2,3-dehydroaminocarboxylic acid esters by reaction of the corresponding 2-azido-carboxylic acid esters with a mixture of one part by volume of acetic anhydride and 1.5 to 5 parts by volume of acetic acid in the presence of rhenium VII sulfide and/or oxide and at a temperature between 50.degree. and 150.degree. C., in a given case, in the simultaneous presence of dry hydrogen chloride.Type: GrantFiled: September 16, 1982Date of Patent: June 26, 1984Assignee: Degussa AktiengesellschaftInventors: Franz Effenberger, Thomas Beisswenger
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Patent number: 4454336Abstract: This disclosure describes a novel process for the synthesis of 5-mercapto-1,2,3-thiadiazoles which are useful as intermediates in the preparation of antibacterial agents.Type: GrantFiled: September 27, 1982Date of Patent: June 12, 1984Assignee: American Cyanamid CompanyInventors: William V. Curran, Martin L. Sassiver, James H. Boothe
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Patent number: 4438270Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: wherein Y is ClCH.sub.2, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR1## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.Type: GrantFiled: June 25, 1982Date of Patent: March 20, 1984Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Michel Jung
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Patent number: 4424354Abstract: Mammalian collagenase is inhibited by compounds of the formula ##STR1## or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl;R.sub.2 is hydrogen, ##STR2## R.sub.3 is ##STR3## R.sub.4 is hydrogen, methyl, ethyl, or ##STR4## R.sub.5 and R.sub.6 are each independently selected as --OCH.sub.3 or --OCH.sub.2 CH.sub.3 or are combined as --OCH.sub.2 CH.sub.2 O-- or --O--(CH.sub.2).sub.3 --O--;R.sub.7 and R.sub.8 are each independently selected as hydrogen, methyl or ethyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --;R.sub.9 is hydrogen, methyl, ethyl ##STR5## m is an integer from 0 to 7; p is an integer from 1 to 3; AA.sub.n is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3;when p is 1, AA.sub.n is AA.sub.1 ;when p is 2, AA.sub.n is AA.sub.1 -AA.sub.2 ;when p is 3, AA.sub.n is AA.sub.1 -AA.sub.Type: GrantFiled: September 24, 1982Date of Patent: January 3, 1984Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, Tamara Dejneka
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Patent number: 4401827Abstract: Novel acyl-derivatives of the .beta.-hydroxy-.gamma.-butyrobetaine are disclosed (typically pyruvyl carnitine hydrochloride) which are useful therapeutic agents in the treatment of cardiac disorders, hyperlipidoemias and hyperlipoproteinemias.Type: GrantFiled: December 28, 1981Date of Patent: August 30, 1983Assignee: Sigma-TauInventor: Paolo de Witt
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Patent number: 4395569Abstract: A sulfonic acid salt of an acyloxyalkylamine is prepared by reaction of an organic acid or amino-acid with a sulfonic acid salt of an alkanolamine. Isocyanates are prepared therefrom by reaction with phosgene.Type: GrantFiled: December 17, 1979Date of Patent: July 26, 1983Assignee: Rohm and Haas CompanyInventors: Sheldon N. Lewis, Jerome F. Levy
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Patent number: 4384998Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.Type: GrantFiled: March 30, 1981Date of Patent: May 24, 1983Assignee: Merck & Co., Inc.Inventor: Philippe L. Durette
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Patent number: 4382031Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.Type: GrantFiled: November 23, 1981Date of Patent: May 3, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
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Patent number: 4343947Abstract: Amides of carnitine or acyl-carnitines having general formula: ##STR1## wherein X.sup.- is a halogen anion, e.g. the chloride anionR is either hydrogen or an acyl radical, such as acetyl, propionyl or butyryl; andY is the residue of an optically active esterified amino-acid (e.g. the residue of L-phenylglycine methyl ester, ##STR2## are prepared by either (a) directly condensing D,L-carnitine (or acyl-D,L-carnitine) with an ester of an optically active aminoacid, or (b) preparing the acid halogenide of D,L-carnitine or acyl-D,L-carnitine and subsequently condensing it with an ester of an optically active aminoacid.The mixture of the diastereoisomer amides thus obtained is resolved by fractional crystallization from organic solvents into the respective separated diastereoisomers.Type: GrantFiled: December 29, 1980Date of Patent: August 10, 1982Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Paolo De Witt, Maria O. Tinti
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Patent number: 4330674Abstract: Carbamoyl sulfides such as dimethyl N,N'-[2,3-butanediylidenebis[nitrilooxycarbonyl(N-methylimino)thio(N-methy limino)carbonyloxy]]bis[ethanimidothioate] useful for control of insects and nematodes.This application is a divisional of application Ser. No. 139,836, filed Apr. 24, 1980, now U.S Pat. No. 4,254,141, which is a continuation-in-part of application Ser. No. 18,293, filed Mar. 6, 1979, and now abandoned.Type: GrantFiled: October 8, 1980Date of Patent: May 18, 1982Assignee: E. I. Du Pont de Nemours and CompanyInventor: Jiin-Duey Cheng
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Patent number: 4325961Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.Type: GrantFiled: June 1, 1977Date of Patent: April 20, 1982Assignee: Merck & Co., Inc.Inventors: Janos Kollonitsch, Arthur A. Patchett
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Patent number: 4320056Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.Type: GrantFiled: March 12, 1981Date of Patent: March 16, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
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Patent number: 4313956Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.Type: GrantFiled: December 28, 1979Date of Patent: February 2, 1982Assignee: INTERx Research Corp.Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4311706Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.Type: GrantFiled: January 22, 1980Date of Patent: January 19, 1982Assignee: INTERx Research CorporationInventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4311645Abstract: A chemical synthesis of an SRS-A active compound from the reaction product of 1-halo-2-octyne and the ether of 2-penten-4-yn-1-ol including intermediates in the synthesis, some of which being antagonists of SRS-A useful for treating allergic reactions.Type: GrantFiled: March 24, 1980Date of Patent: January 19, 1982Assignee: Hoffmann-La Roche Inc.Inventor: Michael Rosenberger
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Patent number: 4303669Abstract: Novel hybrid 1,3-dione-carbamate compounds which exhibit utility as insecticides and acaricides. Also included are insecticidal and acaricidal compositions containing these compounds and a method of controlling insects and acarids.Type: GrantFiled: March 25, 1980Date of Patent: December 1, 1981Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4284557Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.Type: GrantFiled: May 15, 1980Date of Patent: August 18, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
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Patent number: 4275217Abstract: A chiral .alpha.-amino acid having a hydrogen substituent in a position alpha to the carboxylic function thereof is prepared by subjecting a corresponding optical antipode with a chiral amino acid to a strong base whereby the proton in a position alpha to the carboxylic function is removed and thereafter reacting the resulting product with a chiral protonation agent.Type: GrantFiled: July 9, 1979Date of Patent: June 23, 1981Assignee: Agence Nationale de Valorisation de la Recherche (ANVAR)Inventors: Lucette Duhamel, Jean-Christophe Plaquevent
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Patent number: 4258200Abstract: Carboxylic acid amides are produced by the catalytic reaction of an ester and an amine is shown. Organo cobalt salts are used as the catalyst. The process is particularly useful for producing dimethylacetamide by the reaction of methyl acetate and dimethylamine.Type: GrantFiled: March 11, 1980Date of Patent: March 24, 1981Assignee: Air Products and Chemicals, Inc.Inventor: Randall J. Daughenbaugh
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Patent number: 4256761Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycyclo-alkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, dialkylamino-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, or fused heteroaryl-cycloalkyl-alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or ##STR2## wherein Z is hydrogen, alkyl, hyroxyalkyl, aminoalkyl or the radical ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.Type: GrantFiled: July 13, 1979Date of Patent: March 17, 1981Assignee: USV Pharmaceutical CorporationInventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab
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Patent number: 4242516Abstract: The invention is directed to fluorinated compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxyperfluoroalkyl group, R.sup.1 is a branched or straight chain alkylene, alkylenethioalkylene, alkyleneoxyalkylene or alkyleneiminoalkylene group, X is oxygen or an amino group, Q is an organic group containing at least one amino group and y is zero or 1, and the corresponding succinimides. These compounds are useful as surfactants.Type: GrantFiled: January 12, 1978Date of Patent: December 30, 1980Assignee: Ciba-Geigy CorporationInventor: Karl F. Mueller