Sulfur In Acid Moiety Patents (Class 560/147)
  • Patent number: 5068445
    Abstract: 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: Grant
    Filed: April 3, 1989
    Date of Patent: November 26, 1991
    Assignee: Societe Nationale Elf Aquitaine (Production)
    Inventor: Emmanuel Arretz
  • Patent number: 5041617
    Abstract: 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: Grant
    Filed: February 19, 1988
    Date of Patent: August 20, 1991
    Assignee: Mallinckrodt Specialty Chemicals Company
    Inventors: Neil Dunski, Ali A. Bazzi, Henry J. Buehler
  • Patent number: 5026910
    Abstract: 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: Grant
    Filed: May 22, 1990
    Date of Patent: June 25, 1991
    Assignee: Societe Atochem
    Inventors: Eric Bollens, Francois Szonyi, Aime Cambon
  • Patent number: 5011975
    Abstract: 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: Grant
    Filed: July 17, 1989
    Date of Patent: April 30, 1991
    Assignee: Nippon Miktron Limited
    Inventors: Tokiyuki Hiramitsu, Ken-ichi Sakamoto
  • Patent number: 5010097
    Abstract: 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: Grant
    Filed: December 20, 1988
    Date of Patent: April 23, 1991
    Assignee: Beecham Pharmaceuticals
    Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes, Laramie M. Gaster
  • Patent number: 5010189
    Abstract: 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: Grant
    Filed: October 24, 1989
    Date of Patent: April 23, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Herold, Christof Angst
  • Patent number: 5010103
    Abstract: 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: Grant
    Filed: January 17, 1990
    Date of Patent: April 23, 1991
    Assignee: The Research Foundation of State University of N.Y.
    Inventor: Thomas I. Kalman
  • Patent number: 5010105
    Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 23, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Ta J. Lee
  • Patent number: 5008432
    Abstract: 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: Grant
    Filed: July 11, 1985
    Date of Patent: April 16, 1991
    Assignee: Phillips Petroleum Company
    Inventor: John S. Roberts
  • Patent number: 5002964
    Abstract: 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: Grant
    Filed: June 15, 1988
    Date of Patent: March 26, 1991
    Assignee: Brigham & Women's Hospital
    Inventor: Joseph Loscalzo
  • Patent number: 4994150
    Abstract: 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: Grant
    Filed: August 24, 1989
    Date of Patent: February 19, 1991
    Assignee: Phillips Petroleum Company
    Inventor: James E. Shaw
  • Patent number: 4935510
    Abstract: 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: Grant
    Filed: June 7, 1989
    Date of Patent: June 19, 1990
    Assignee: Ethyl Corporation
    Inventor: Barbara C. Stahly
  • Patent number: 4935514
    Abstract: 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: Grant
    Filed: June 6, 1989
    Date of Patent: June 19, 1990
    Assignee: Ethyl Corporation
    Inventor: Barbara C. Stahly
  • Patent number: 4935513
    Abstract: 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: Grant
    Filed: June 7, 1989
    Date of Patent: June 19, 1990
    Assignee: Ethyl Corporation
    Inventor: Barbara C. Stahly
  • Patent number: 4927966
    Abstract: 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: Grant
    Filed: June 4, 1987
    Date of Patent: May 22, 1990
    Assignee: The Research Foundation of State University of New York
    Inventor: Thomas I. Kalman
  • Patent number: 4927808
    Abstract: .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: Grant
    Filed: March 7, 1988
    Date of Patent: May 22, 1990
    Assignee: Teijin Limited
    Inventors: Shigehisa Kitahara, Akira Ohtsu, Katsuhiko Fujii
  • Patent number: 4919831
    Abstract: Ester-type ashless dispersants containing additional integral sulfur-ester moieties which have been found to possess enhanced thermal oxidative stability are claimed.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: April 24, 1990
    Assignee: Mobil Oil Corporation
    Inventor: Andrew G. Horodysky
  • Patent number: 4916237
    Abstract: 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: Grant
    Filed: August 26, 1988
    Date of Patent: April 10, 1990
    Assignee: American Cyanamid Company
    Inventors: Ving J. Lee, William V. Curran
  • Patent number: 4914223
    Abstract: 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: Grant
    Filed: August 17, 1988
    Date of Patent: April 3, 1990
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Jerald K. Rasmussen, Steven M. Heilmann, Frederick J. Palensky
  • Patent number: 4898977
    Abstract: 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: Grant
    Filed: August 13, 1987
    Date of Patent: February 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Herold, Christof Angst
  • Patent number: 4889950
    Abstract: 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: Grant
    Filed: August 24, 1988
    Date of Patent: December 26, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Kaspar Bott, Horst Hartmann, Josef Guth
  • Patent number: 4882341
    Abstract: The invention relates to amino substituted propenoates and their use against fungi.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: November 21, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Ian T. Kay
  • Patent number: 4879314
    Abstract: 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: Grant
    Filed: January 8, 1986
    Date of Patent: November 7, 1989
    Inventor: Adam C. Hsu
  • Patent number: 4845257
    Abstract: 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: Grant
    Filed: May 18, 1987
    Date of Patent: July 4, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kenzo Naito, Yukio Ishibashi
  • Patent number: 4812478
    Abstract: 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: Grant
    Filed: June 29, 1987
    Date of Patent: March 14, 1989
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Carlo A. Bagolini, Domenico Misiti, Carlo Scolastico
  • Patent number: 4808628
    Abstract: 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: Grant
    Filed: November 12, 1987
    Date of Patent: February 28, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Margaret C. Shephard, Patrick J. Crowley
  • Patent number: 4769325
    Abstract: 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: Grant
    Filed: July 28, 1986
    Date of Patent: September 6, 1988
    Inventors: Jack E. Baldwin, Amit Basak
  • Patent number: 4755528
    Abstract: 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: Grant
    Filed: April 17, 1987
    Date of Patent: July 5, 1988
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark T. DuPriest, Billie M. York, Jr.
  • Patent number: 4742067
    Abstract: 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: Grant
    Filed: July 30, 1986
    Date of Patent: May 3, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4734120
    Abstract: 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: Grant
    Filed: December 12, 1986
    Date of Patent: March 29, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Klaus Bauer, Hermann Bieringer
  • Patent number: 4727199
    Abstract: 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: Grant
    Filed: July 10, 1985
    Date of Patent: February 23, 1988
    Assignee: Union Carbide Corporation
    Inventor: Stephen W. King
  • Patent number: 4701282
    Abstract: 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: Grant
    Filed: August 30, 1985
    Date of Patent: October 20, 1987
    Assignee: Philip Morris Incorporated
    Inventors: W. Geoffrey Chan, Yoram Houminer
  • Patent number: 4699972
    Abstract: 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: Grant
    Filed: August 22, 1986
    Date of Patent: October 13, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Hammer, Herbert Eichenauer, Ernst Roos, Eberhard Jurgens
  • Patent number: 4684644
    Abstract: 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: Grant
    Filed: March 21, 1986
    Date of Patent: August 4, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Bruno Cavalleri
  • Patent number: 4677129
    Abstract: 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: Grant
    Filed: June 20, 1985
    Date of Patent: June 30, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Alder, Jaroslav Stanek, Daniel Bellus
  • Patent number: 4677223
    Abstract: 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: Grant
    Filed: March 21, 1986
    Date of Patent: June 30, 1987
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock
  • Patent number: 4659733
    Abstract: 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: Grant
    Filed: December 6, 1984
    Date of Patent: April 21, 1987
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark T. DuPriest, Billie M. York, Jr.
  • Patent number: 4656308
    Abstract: Ethylenically unsaturated monomers containing activated ester groups are used to make polymers and copolymers which are useful in coatings, adhesives and moldings.
    Type: Grant
    Filed: September 5, 1985
    Date of Patent: April 7, 1987
    Assignee: American Cyanamid Company
    Inventors: Peter J. Schirmann, Werner J. Blank, Girish G. Parekh
  • Patent number: 4652297
    Abstract: 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: Grant
    Filed: February 25, 1982
    Date of Patent: March 24, 1987
    Assignee: Monsanto Company
    Inventors: John E. Franz, Robert J. Kaufman
  • Patent number: 4652670
    Abstract: 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: Grant
    Filed: January 23, 1986
    Date of Patent: March 24, 1987
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock, Kevin P. Miller, Domenick Luccarelli, Jr., Charles Wiener
  • Patent number: 4633014
    Abstract: 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: Grant
    Filed: July 6, 1984
    Date of Patent: December 30, 1986
    Assignee: Institut Organicheskogo Sinteza Akademii Nauk Latviiskoi Ssr
    Inventors: Gunar A. Bremanis, Ivars Y. Kalvinsh, Irene B. Antsena, Edmund Y. Lukevits, Maris M. Veveris, Valeryans Y. Kauss, Peter T. Trapentsier, Edvards E. Liepinsh
  • Patent number: 4624980
    Abstract: 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: Grant
    Filed: March 28, 1985
    Date of Patent: November 25, 1986
    Assignee: Milliken Research Corporation
    Inventors: John W. Rekers, Edward W. Kluger
  • Patent number: 4613510
    Abstract: 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: Grant
    Filed: October 4, 1985
    Date of Patent: September 23, 1986
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock
  • Patent number: 4611002
    Abstract: 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: Grant
    Filed: June 8, 1984
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb and Sons, Inc.
    Inventor: Miguel A. Ondetti
  • Patent number: 4594188
    Abstract: 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: Grant
    Filed: May 20, 1985
    Date of Patent: June 10, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Norma G. Delaney, Eric M. Gordon
  • Patent number: 4593043
    Abstract: 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: Grant
    Filed: March 19, 1982
    Date of Patent: June 3, 1986
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Emma Quaresima, Carlo Bagolini, Paolo DeWitt
  • Patent number: 4587353
    Abstract: 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: Grant
    Filed: August 23, 1983
    Date of Patent: May 6, 1986
    Assignee: Ciba-Geigy Corporation
    Inventor: Hansjakob Fah
  • Patent number: 4576759
    Abstract: 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: Grant
    Filed: June 20, 1984
    Date of Patent: March 18, 1986
    Assignee: SOLVAY & Cie (Societe Anonyme)
    Inventors: Heinz Viehe, Nadine S. Mesmaeker, Robert Merenyi
  • Patent number: 4567200
    Abstract: 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: Grant
    Filed: March 15, 1982
    Date of Patent: January 28, 1986
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Emma Quaresima, Carlo Bagolini, Paolo deWitt
  • Patent number: 4557941
    Abstract: 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: Grant
    Filed: March 25, 1985
    Date of Patent: December 10, 1985
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Alan O. Pittet, Ranya Muralidhara, Manfred H. Vock