Sulfur In Acid Moiety Patents (Class 560/147)
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Patent number: 5068445Abstract: The invention relates to the preparation of organic disulphides and polysulphides by the action of sulphur on a mercaptan or on a polysulphide which is lower in sulphur, in the presence of a basic catalyst.In the process according to the invention, an anion exchange resin is used as catalyst.Type: GrantFiled: April 3, 1989Date of Patent: November 26, 1991Assignee: Societe Nationale Elf Aquitaine (Production)Inventor: Emmanuel Arretz
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Patent number: 5041617Abstract: Multifunctional dithiodialkanoic acid esters useful in the stabilization of organic materials normally susceptible to oxidative degradation are prepared by contacting a selected dithiodialkanoic acid chloride with a selected 4-(3-hydroxypropyl)(mono- or di-alkyl) phenol under ester-forming reaction conditions. In a preferred embodiment, the ester is bis-3-(3',5'-di-t-butyl-4'-hydroxyphenyl)propyl dithiodipropionate.Type: GrantFiled: February 19, 1988Date of Patent: August 20, 1991Assignee: Mallinckrodt Specialty Chemicals CompanyInventors: Neil Dunski, Ali A. Bazzi, Henry J. Buehler
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Patent number: 5026910Abstract: The invention relates to polyfluoroaklyl nitrogen compounds of general formula:R.sub.F --(CH.sub.2).sub.2 --Xin which X denotes an isothiocyanate --N.dbd.C.dbd.S, carbodiimide --N.dbd.C.dbd.N(CH.sub.2).sub.2 --R'.sub.F or thiourea --NH--CS--A group, A denoting an optionally substituted amino group, and each of the symbols R.sub.F and R'.sub.F denotes a perfluoroalkyl radical.these compounds, prepared from the corresponding axides R.sub.F (CH.sub.2).sub.2 N.sub.3 or amines R.sub.F(CH.sub.2).sub.2 NH.sub.2, can be used as surface-active agents or precursors of such agents.Type: GrantFiled: May 22, 1990Date of Patent: June 25, 1991Assignee: Societe AtochemInventors: Eric Bollens, Francois Szonyi, Aime Cambon
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Patent number: 5011975Abstract: A (trans 1-propenyl)disulfide derivative having a distinguished anti-tumor effect, represented by the following general formula: ##STR1## , wherein R is a lower alkylene group and R' is a hydrogen atom or a carboxyl protective group, is prepared by allowing a carboxylic acid thiol derivative, represented by the following general formula:AS--R--COOR', wherein R and R' have the same meanings as defined above and A is a thiol protective group releasable by a halogenating agent, to react with a trans 1-propenethiol derivative represented by the following general formula: ##STR2## , wherein A has the same meanings as defined above, in the presence of a halogenating agent.Type: GrantFiled: July 17, 1989Date of Patent: April 30, 1991Assignee: Nippon Miktron LimitedInventors: Tokiyuki Hiramitsu, Ken-ichi Sakamoto
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Patent number: 5010097Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; 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 a group ##STR3## 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; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.Type: GrantFiled: December 20, 1988Date of Patent: April 23, 1991Assignee: Beecham PharmaceuticalsInventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes, Laramie M. Gaster
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Patent number: 5010189Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonization of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: October 24, 1989Date of Patent: April 23, 1991Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 5010103Abstract: New compounds having utility for enhancing the activity of antifolates are disclosed of the formula: ##STR1## wherein X is selected from hydrogen ##STR2## and R" ; R' is selected from alkyl, alkenyl, alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heterocyclic aryl; R" is selected from ##STR3## and R'S; M is selected from OR and secondary amine; and R is selected from hydrogen, alkyl, acyloxymethyl, substituted and unsubstituted aryl, substituted and unsubstituted heterocyclic aryl, amino cation and metal cation.Type: GrantFiled: January 17, 1990Date of Patent: April 23, 1991Assignee: The Research Foundation of State University of N.Y.Inventor: Thomas I. Kalman
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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: 5008432Abstract: Activated olefinically unsaturated organic compounds such as esters, acids, ketones, nitriles, and the like, are reacted with hydrogen sulfide in the presence of at least one of magnesium oxide and anion exchange resins catalysts to produce saturated sulfur-containing compounds. In a specific embodiment, unsaturated carboxylates are converted in high yields to mercaptoalkanoates.Type: GrantFiled: July 11, 1985Date of Patent: April 16, 1991Assignee: Phillips Petroleum CompanyInventor: John S. Roberts
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Patent number: 5002964Abstract: The invention relates to novel nitroso compounds having the formula: ##STR1## wherein, R is hydroxy, NH.sub.2, NHR.sup.4, NR.sup.4 R.sup.5 or C.sub.1 -C.sub.7 alkoxy, wherein R.sup.4 and R.sup.5 are C.sub.1 -C.sub.4 alkyl, aryl, or C.sub.1 -C.sub.4 alkyl substituted by aryl;R.sup.1 is hydrogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkyl substituted by phenyl, amino, guanidino, NHR.sup.6 or NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 are methyl, or C.sub.1 -C.sub.4 acyl;R.sup.3 is hydrogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkyl substituted by phenyl;n is 0 to 2;A is hydrogen,lower C.sub.1 -C.sub.7 alkyl,lower C.sub.2 -C.sub.7 alkylene,lower C.sub.2 -C.sub.7 alkylene substituted by hydroxy, C.sub.1 -C.sub.4 alkyl, aryl, ora C.sub.4 -C.sub.7 ring which may be fused to a benzene ring;B is hyrogen,lower C.sub.1 -C.sub.7 alkyl,phenyl,lower C.sub.1 -C.sub.7 substituted by phenyl, hydroxy, guanidino, amino, imidazoyl, indolyl, mercapto, mercapto substituted by lower C.sub.1 -C.sub.Type: GrantFiled: June 15, 1988Date of Patent: March 26, 1991Assignee: Brigham & Women's HospitalInventor: Joseph Loscalzo
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Patent number: 4994150Abstract: The present invention provides a process to recover esters of mercapto acids from solutions containing water by mixing an extraction mixture comprising cycloalkane, arene, and an aqueous inorganic salt solution with an ester of mercapto acid and water solution followed by separating and distilling the resultant organic phase to recover the ester of mercapto acid.Type: GrantFiled: August 24, 1989Date of Patent: February 19, 1991Assignee: Phillips Petroleum CompanyInventor: James E. Shaw
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Patent number: 4935510Abstract: Ammonium hydroxide is used in the recovery of a thiono compound prepared by reacting an organic carbonyl compound with phosphorus pentasulfide to improve the product yield.Type: GrantFiled: June 7, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4935514Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of an adjuvant selected from diatomaceous earth, zeolites, and molecular sieves.Type: GrantFiled: June 6, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4935513Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of a Group IIA metal fluoride as an adjuvant.Type: GrantFiled: June 7, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4927966Abstract: New compounds having utility for enhancing the activity of antifolates are disclosed of the formula: ##STR1## wherein X is selected from hydrogen ##STR2## and R"--; R' is selected from alkyl, alkenyl, alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heterocyclic aryl; R" is selected from ##STR3## and R'S; M is selected from OR and secondary amine; and R is selected from hydrogen, alkyl, acyloxymethyl, substituted and unsubstituted aryl, substituted and unsubstituted heterocyclic aryl, amino cation and metal cation.Type: GrantFiled: June 4, 1987Date of Patent: May 22, 1990Assignee: The Research Foundation of State University of New YorkInventor: Thomas I. Kalman
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Patent number: 4927808Abstract: .gamma.-L-glutamyl-L-cysteine ethyl ester which has an activity to increase glutathione levels in tissues and a drug for treating liver diseases, cataracts, and kidney diseases containing it as the effective ingredient.Type: GrantFiled: March 7, 1988Date of Patent: May 22, 1990Assignee: Teijin LimitedInventors: Shigehisa Kitahara, Akira Ohtsu, Katsuhiko Fujii
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Patent number: 4919831Abstract: Ester-type ashless dispersants containing additional integral sulfur-ester moieties which have been found to possess enhanced thermal oxidative stability are claimed.Type: GrantFiled: September 30, 1988Date of Patent: April 24, 1990Assignee: Mobil Oil CorporationInventor: Andrew G. Horodysky
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Patent number: 4916237Abstract: Intermediates useful for synthesis of cephalosporins are disclosed, which intermediates are concerned with 1,2,3-thiadiazole-4-thiolates and the preparation of such thiolates.Type: GrantFiled: August 26, 1988Date of Patent: April 10, 1990Assignee: American Cyanamid CompanyInventors: Ving J. Lee, William V. Curran
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Patent number: 4914223Abstract: A composition of matter comprising an acrylamido-acyl or methacrylamido-acyl oligomer derived from at least one nucleophilic oligomer having at least one amino-, hydroxyl-, or thio-substituted polyoxyalkylene, polyalkyleneimine, polyester, polyolefin, polyacrylate, or polysiloxane oligomer, said nucleophilic oligomer having a molecular weight in the range of 200 to 20,000 is disclosed. Also disclosed are free radically polymerizable monomer-containing compositions containing said oligomers as well as acrylamido- and methacrylamido-acylated polymers which are the thermal or photocured products of said oligomers. In addition, a process is disclosed for providing said acrylamido- and methacrylamido-acylated oligomers which are useful, for example, in coatings, films, printing inks, adhesives, and saturants.Type: GrantFiled: August 17, 1988Date of Patent: April 3, 1990Assignee: Minnesota Mining and Manufacturing CompanyInventors: Jerald K. Rasmussen, Steven M. Heilmann, Frederick J. Palensky
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Patent number: 4898977Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 4889950Abstract: Carboxylic esters are prepared by reacting carboxylic acids with low-boiling alcohols by charging the reaction mixture to a 1st distillation column, withdrawing the reaction components carboxylic ester, water and unconverted alcohol as overhead product and charging this overhead product to a 2nd distillation column, from which(a) the overhead product comprises the alcohol or an azeotropic mixture of alcohol and water or alcohol and esteer, this overhead product being recycled into the esterification reaction(b) a liquid side product comprising carboxylic ester and water is withdrawn from the stripping section and separated in a phase separating vessel into water and carboxylic ester and the carboxylic ester is returned into the distillation column below the side takeoff point, and(c) the bottom product removed is the carboxylic ester.Type: GrantFiled: August 24, 1988Date of Patent: December 26, 1989Assignee: BASF AktiengesellschaftInventors: Kaspar Bott, Horst Hartmann, Josef Guth
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Patent number: 4882341Abstract: The invention relates to amino substituted propenoates and their use against fungi.Type: GrantFiled: September 9, 1988Date of Patent: November 21, 1989Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Ian T. Kay
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Patent number: 4879314Abstract: Dihaloformaldoximes of the formula: ##STR1## wherein R, X, X.sup.1 and Y are as defined herein having biocidal, fungicidal and pesticidal activity are disclosed.Type: GrantFiled: January 8, 1986Date of Patent: November 7, 1989Inventor: Adam C. Hsu
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Patent number: 4845257Abstract: A method of producing a 4-halo-2-(substituted or unsubstituted)hydroxyimino-3-oxobutyric acid ester or amide, which is a synthetic intermediate of value for the production of cephalosporins containing an aminothiazole group, characterized by reacting a 2-(substituted or unsubstituted)-hydroxyimino-3-oxobutyric acid or an ester or amide thereof with a silylating agent and reacting the resulting novel 2-(substituted)hydroxyimino-3-silyloxy-3-butenoic acid ester or amide with a halogenating agent.Type: GrantFiled: May 18, 1987Date of Patent: July 4, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Kenzo Naito, Yukio Ishibashi
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Patent number: 4812478Abstract: L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.Type: GrantFiled: June 29, 1987Date of Patent: March 14, 1989Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Maria O. Tinti, Carlo A. Bagolini, Domenico Misiti, Carlo Scolastico
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Patent number: 4808628Abstract: An amide derivative of the formula (I): ##STR1## or a tautomeric form thereof, wherein R is a phenyl group substituted in the 4-position by a group of R.sup.1 XCH.sub.2--, where R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkynyl, C.sub.1 -C.sub.4 alkylcarbonyl, or H, and X is oxygen or sulphur; E is CN, or CSNH.sub.2, or CONH.sub.2 ; and Y is C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.3 -C.sub.4 alkynyloxy, 1-pyrazolyl or 2-furyl. Compositions and processes for using these derivatives to combat plant fungi are also disclosed.Type: GrantFiled: November 12, 1987Date of Patent: February 28, 1989Assignee: Imperial Chemical Industries PLCInventors: Margaret C. Shephard, Patrick J. Crowley
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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: 4755528Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.Type: GrantFiled: April 17, 1987Date of Patent: July 5, 1988Assignee: Alcon Laboratories, Inc.Inventors: Mark T. DuPriest, Billie M. York, Jr.
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Patent number: 4742067Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: July 30, 1986Date of Patent: May 3, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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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: 4727199Abstract: Active-hydrogen compounds, for example, primary and secondary alcohols or diols, are alkoxylated, for example, ethoxylated, using solid anion-bound metal oxide catalysts, such as, zirconium oxysulfate catalyst. Hydrous zicronium oxide is treated with solutions of sulfate phosphate, nitrate or tetrafluoroborate and calcined in air at 300.degree. to 950.degree. C. to produce highly active heterogeneous alkoxylation catalysts. The amorphous catalysts afford narrow molecular weight products. The catalyst can be removed from the product by filtration and reused with no significant loss in activity. Reaction temperatures of 50.degree. to 140.degree. C. are employed for alkoxylation.Type: GrantFiled: July 10, 1985Date of Patent: February 23, 1988Assignee: Union Carbide CorporationInventor: Stephen W. King
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Patent number: 4701282Abstract: This invention provides smoking compositions which contain a .beta.-hydroxy-.gamma.-ketoester compound as a flavorant-release additive.In one of its embodiments, this invention provides tobacco compositions which contain a flavorant-release additive such as dodecyl 3-hydroxy-2,2,3-trimethyl-4-oxopentanoate: ##STR1## Under cigarette smoking conditions the above illustrated .beta.-hydroxy-.gamma.-keto ester pyrolyzes into 2,3-butanedione and other products which enhance the flavor of the mainstream smoke and the aroma of sidestream smoke.Type: GrantFiled: August 30, 1985Date of Patent: October 20, 1987Assignee: Philip Morris IncorporatedInventors: W. Geoffrey Chan, Yoram Houminer
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Patent number: 4699972Abstract: Aliphatic polyesters containing sulphur, which contain the sulphur as structural units in the form of sulphide or disulphide groups in both the acid component and the diol component, a process for the preparation of these polyesters, and also polymers containing these polyesters.Type: GrantFiled: August 22, 1986Date of Patent: October 13, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz Hammer, Herbert Eichenauer, Ernst Roos, Eberhard Jurgens
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Patent number: 4684644Abstract: The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine.Type: GrantFiled: March 21, 1986Date of Patent: August 4, 1987Assignee: Gruppo Lepetit S.p.A.Inventors: Adriano Malabarba, Bruno Cavalleri
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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: 4677223Abstract: Described is the genus of mercapto-C.sub.2 -C.sub.3 -alkanoic acid esters of citronellol, geraniol, homologues thereof and partially saturated derivatives thereof defined according to the structure: ##STR1## wherein N represents 0 or 1; M represents 0, 1 or 2; P represents 0 or 1; and the dashed line represents a carbon-carbon single bond or a carbon-carbon double bond with the proviso that when N is 0 then the dashed line represents a carbon-carbon single bond and uses thereof in augmenting or enhancing the aroma or taste of foodstuffs.Type: GrantFiled: March 21, 1986Date of Patent: June 30, 1987Assignee: International Flavors & Fragrances Inc.Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock
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Patent number: 4659733Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.Type: GrantFiled: December 6, 1984Date of Patent: April 21, 1987Assignee: Alcon Laboratories, Inc.Inventors: Mark T. DuPriest, Billie M. York, Jr.
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Patent number: 4656308Abstract: Ethylenically unsaturated monomers containing activated ester groups are used to make polymers and copolymers which are useful in coatings, adhesives and moldings.Type: GrantFiled: September 5, 1985Date of Patent: April 7, 1987Assignee: American Cyanamid CompanyInventors: Peter J. Schirmann, Werner J. Blank, Girish G. Parekh
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Patent number: 4652297Abstract: This invention relates to a new class of organic chemical compounds. More particularly, this invention is concerned with amido and hydrazido derivatives of N-phosphinothioylmethylglycine esters. This class of compounds has been found to be useful as herbicides.Type: GrantFiled: February 25, 1982Date of Patent: March 24, 1987Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4652670Abstract: Described are the cycloalkyl esters of mercaptoalkanoic acids defined according to the structure: ##STR1## wherein R.sub.1 represents hydrogen or methyl; R.sub.2 represents mono C.sub.1 -C.sub.4 alkyl substituted or unsubstituted C.sub.5 -C.sub.8 cycloalkyl; R.sub.3 represents hydrogen or methyl; and N represents 0, 1 or 2 and uses thereof in augmenting or enhancing the aroma or taste of foodstuffs.Type: GrantFiled: January 23, 1986Date of Patent: March 24, 1987Assignee: International Flavors & Fragrances Inc.Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock, Kevin P. Miller, Domenick Luccarelli, Jr., Charles Wiener
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Patent number: 4633014Abstract: Substituted 3-hydrazinopropionates comprising compounds of the general fola: ##STR1## wherein R.sup.1, R.sup.2 =H, an alkyl, a substituted alkyl, hydroxycarbonyl, alkoxycarbonyl, an aryl, an aralkyl, an unsaturated alkyl, a substituted aryl or a substituted aralkyl: ##STR2## wherein R.sup.7, R.sup.8 =H, an alkyl, an unsaturated alkyl, an aralkyl, an aryl, a substituted alkyl,R.sup.9 =OH, an alkoxy, an aralkoxy, an alkyl, an unsaturated alkyl, an aryl, a substituted aryl, an aralkyl;R.sup.4 is --C.tbd.N, --COR.sup.10, wherein R.sup.10 =OR.sup.11, NR.sup.12 R.sup.13, where R.sup.11 is H, an alkyl, an aralkyl and an alkali metal, R.sup.11 and R.sup.12 are each H, an alkyl, an aralkyl, an aryl;R.sup.5, R.sup.6 = an alkyl, an aryl, an aralkyl.Type: GrantFiled: July 6, 1984Date of Patent: December 30, 1986Assignee: Institut Organicheskogo Sinteza Akademii Nauk Latviiskoi SsrInventors: Gunar A. Bremanis, Ivars Y. Kalvinsh, Irene B. Antsena, Edmund Y. Lukevits, Maris M. Veveris, Valeryans Y. Kauss, Peter T. Trapentsier, Edvards E. Liepinsh
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Patent number: 4624980Abstract: An N-t-alkyl-N-sec-alkyl secondary amine compound of the formula: ##STR1## wherein X, Y and Z are each independently selected from --H, --OH, or an alkyl group having from 1 to about 15 carbon atoms; and n is an integer of from 3 to about 6.Type: GrantFiled: March 28, 1985Date of Patent: November 25, 1986Assignee: Milliken Research CorporationInventors: John W. Rekers, Edward W. Kluger
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Patent number: 4613510Abstract: Described is the genus of mercapto-C.sub.2 -C.sub.3 -alkanoic acid esters of citronellol, geraniol, homologues thereof and partially saturated derivatives thereof defined according to the structure: ##STR1## wherein N represents 0 or 1; M represents 0, 1 or 2; P represents 0 or 1; and the dashed line represents a carbon-carbon single bond or a carbon-carbon double bond with the proviso that when N is 0 then the dashed line represents a carbon-carbon single bond uses thereof in augmenting or enhancing the aroma or taste of foodstuffs.Type: GrantFiled: October 4, 1985Date of Patent: September 23, 1986Assignee: International Flavors & Fragrances Inc.Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock
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Patent number: 4611002Abstract: New carboxymethyl esters of mercaptopropanoic acids, and salts thereof, have the formula ##STR1## wherein R is hydrogen or lower alkanoyl;R.sub.1 is hydrogen, lower alkyl, phenylalkyl and phenyl;R.sub.2 is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, 4-hydroxyphenyl-lower alkyl or indolyl-lower alkyl.These compounds are useful as enkephalinase inhibitors and hypotensive agents.Type: GrantFiled: June 8, 1984Date of Patent: September 9, 1986Assignee: E. R. Squibb and Sons, Inc.Inventor: Miguel A. Ondetti
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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: 4593043Abstract: A novel class of mercapto acyl-carnitines is disclosed, wherein the mercapto acyl radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These mercapto acyl-carnitines are prepared, e.g., by first preparing the corresponding halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the --SH group for the halogen atom.These mercapto acyl-carnitines are useful therapeutic agents, e.g., for the treatment of intoxications and burns and as mucolytic agents. Dithio diacyl carnitines and hydrochloride salts thereof, which are intermediates, are also disclosed.Type: GrantFiled: March 19, 1982Date of Patent: June 3, 1986Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Maria O. Tinti, Emma Quaresima, Carlo Bagolini, Paolo DeWitt
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Patent number: 4587353Abstract: There is described a process for producing N-chlorosulfenyl compounds of the formula ##STR1## in which R.sub.1 is alkyl, alkoxycarbonyl, alkoxycarbonylalkyl or 2,3-dihydro-2,2-dimethylbenzofuran-7-yloxycarbonyl, and R.sub.2 is alkyl or alkoxycarbonylalkyl, which process is based on the reaction of an amino compound of the formula ##STR2## with sulfur dichloride. The essential feature of the process is that the reaction of the amino compound of the above formula with the sulfur dichloride is performed in excess sulfur dichloride as solvent and in the absence of a base. The formed N-chlorosulfenyl compounds of the above formula are intermediates for insecticidal and acaricidal active substances.Type: GrantFiled: August 23, 1983Date of Patent: May 6, 1986Assignee: Ciba-Geigy CorporationInventor: Hansjakob Fah
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Patent number: 4576759Abstract: The polysubstituted dienes according to the invention correspond to the general formula: ##STR1## in which: X denotes a group chosen from the groups SH, SR.sup.3, OR.sup.3, SeR.sup.3, NHR.sup.3 and N.dbd.R.sup.3 in which R.sup.3 denotes an aliphatic or cyclic, saturated or unsaturated group containing from 1 to 20 carbon atoms,Y denotes a group chosen from the groups C.tbd.N and ##STR2## where R.sup.4 denotes hydrogen or an aliphatic or cyclic, saturated or unsaturated group containing from 1 to 20 carbon atoms, provided that, when X denotes the group SCH.sub.3, Y does not denote the group ##STR3## and, when X denotes an OR.sup.3 group where R.sup.3 is an alkyl group containing at least three carbon atoms, Y does not denote the group C.tbd.N,R.sup.1 denotes hydrogen, halogen or an aliphatic, substituted or unsubstituted group containing from 2 to 8 carbon atoms,R.sup.Type: GrantFiled: June 20, 1984Date of Patent: March 18, 1986Assignee: SOLVAY & Cie (Societe Anonyme)Inventors: Heinz Viehe, Nadine S. Mesmaeker, Robert Merenyi
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Patent number: 4567200Abstract: A novel class of esters of mercapto acyl-carnitines is disclosed, wherein the mercapto acyl radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These esters of mercapto acyl-carnitines are prepared e.g. by first preparing the corresponding ester of halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the --SH group for the halogen atom.These esters of mercapto acyl-carnitines are useful therapeutic agents, e.g. for the treatment of intoxications and burns, and as mucolytic agents.Type: GrantFiled: March 15, 1982Date of Patent: January 28, 1986Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Maria O. Tinti, Emma Quaresima, Carlo Bagolini, Paolo deWitt
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Patent number: 4557941Abstract: Described is the genus of mercapto-C.sub.2 -C.sub.3 -alkanoic acid esters of citronellol, geraniol and melanol defined according to the structure: ##STR1## wherein N represents 0 or 1, M represents 0, 1 or 2; P represents 0 or 1; and the dashed line represents a carbon-carbon single bond or a carbon-carbon double bond with the proviso that when N is 0 then the dashed line represents a carbon-carbon single bond and uses thereof in augmenting or enhancing the aroma or taste of foodstuffs.Type: GrantFiled: March 25, 1985Date of Patent: December 10, 1985Assignee: International Flavors & Fragrances Inc.Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock