Z Radical Contains Sulfur Or Halogen Patents (Class 514/550)
  • Patent number: 5145611
    Abstract: Carboxylic acid derivatives of the formula ##STR1## R.sub.1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R.sub.2 is optionally substituted aryl or, when B is alkylene also a hydrogen atom. A is a straight-chained or branched, saturated or unsaturated alkylene containing 3 to 10 carbon atoms which is optionally interrupted by a heteratom attached to a saturated carbon and has a chain length of at least 3 atoms. Y is S(O).sub.n group or oxygen, n being 0, 1 or 2. B is a valency bond or a straight-chained or branched, saturated or unsaturated alkylene containing 1 to 18 carbon atoms. Physiologically acceptable salts, esters and amides thereof are also included. The compounds are useful in the treatment of metabolic diseases.
    Type: Grant
    Filed: January 12, 1988
    Date of Patent: September 8, 1992
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuehnle
  • Patent number: 5140044
    Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: August 18, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
  • Patent number: 5120759
    Abstract: Novel compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkylthio-lower-alkyl or furyl, R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylenedioxy or ethylenoxy and n is an integer from 1 to 3, have a pronounced activity in counteracting cerebral insufficiency or improving cognitive functions and also reduce the multiple-resistance towards cytostatics in the treatment of tumors or of chloroquine resistance in the treatment of malaria. They can accordingly be used as medicaments, especially for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions. The novel compounds of formula I can be manufactured by O-acylating a likewise novel compound of the formula ##STR2## wherein R.sup.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: June 9, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urs Hengartner, Henri Ramuz
  • Patent number: 5116861
    Abstract: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: May 26, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Shigenori Ohkawa, Shoji Fukumoto
  • Patent number: 5109000
    Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine; CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 --AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12) O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.5 is hydrogen; alkyl; or --CH(R.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: April 28, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
  • Patent number: 5096700
    Abstract: The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy, aryloxy, or an amino acid residue bonded at the amino nitrogen; --R" is hydrogen or an amino acid residue bonded at the carbonyl carbon; --X is halogen; and --Y is hydrogen or halogen.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: March 17, 1992
    Assignee: The Procter & Gamble Company
    Inventors: William L. Seibel, Joseph H. Gardner
  • Patent number: 5093365
    Abstract: A method is provided for the treatment of hypolipaemic conditions and for reducing the concentration of cholesterol and triglycerides in the blood of mammals. The method comprises administering to a mammal an effective amount of non-.beta.-oxidizable fatty acid analogue of the formula Alkyl-X-CH.sub.2 COOR where the alkyl group is a saturated or unsaturated hydrocarbon chain of 8 to 22 carbon atoms, where X represents an oxygen atom, a sulfur atom, a sulfoxide (SO) or sulfone (SO.sub.2) group and where R is a hydrogen atom or an alkyl group of 1 to 4 carbon atoms. Pharmaceutical compositions are also provided.
    Type: Grant
    Filed: June 2, 1989
    Date of Patent: March 3, 1992
    Assignee: Norsk Hydro A.S.
    Inventors: Rolf K. Berge, Jon Bremer
  • Patent number: 5091558
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.
    Type: Grant
    Filed: March 6, 1987
    Date of Patent: February 25, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
  • Patent number: 5089657
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein:R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are selected from the group consisting of hydrogen, R.sup.4 and -C(O)W, whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.
    Type: Grant
    Filed: March 11, 1987
    Date of Patent: February 18, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 5084482
    Abstract: This invention concerns novel methods employing compositions containing as an active antioxidant or antiinflammatory agent the amino acid methionine, and/or one or more related compounds including certain metabolic precursor compounds, for treating or inhibiting inflammatory ischemic, thrombotic and cholesterolemic disease response in a subject. The compounds include the methionine hydroxy analogs, as well as compounds having the structural formula I: ##STR1## and pharmaceutically acceptable N-(mono- and di-carboxylic acid) acyl derivatives and alkyl esters thereof, where n is an integer from 1 to 3.
    Type: Grant
    Filed: April 10, 1990
    Date of Patent: January 28, 1992
    Assignee: The Lithox Corporation
    Inventors: Gerald P. Hirsch, Robert K. Bayless
  • Patent number: 5073380
    Abstract: A pharmaceutical sustained release tablet or tablet layer is formed by making a wet granulation, using povidone (PVP) in water or alcohol-water as the granulating fluid which is mixed with a pharmaceutical active, hydroxyethyl cellulose, a wicking agent e.g. microcrystalline cellulose, then drying and milling the granulation and blending with dry powdered smoothness enhancer, e.g. povidone, erosion promoter, e.g. pregelatinized starch, additional wicking agent, lubricant e.g. magnesium stearate and glidant e.g. silicon dioxide, and compressing the resultant granulation into a tablet with a smooth outer surface, which tablet provides, upon administration, a slow release of the pharmaceutical active.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: December 17, 1991
    Assignee: McNeil-PPC, Inc.
    Inventors: Suresh R. Babu, Robert Glinecke, John L. Murtha, Galen W. Radebaugh
  • Patent number: 5068250
    Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: November 26, 1991
    Assignee: Trustees of University of Pennsylvania
    Inventors: Trevor M. Penning, Leslie J. Askonas
  • Patent number: 5045366
    Abstract: An effective, environmentally compatible anti-fungal composition for protecting lumber from infestation by wood-staining and wood-rotting fungi comprises, as an active ingredient, an alkyl sulfosuccinate compound. A preferred alkyl sulfosuccinate is dioctyl sodium sulfosuccinate. The anti-fungal composition may further comprise water and an adjuvant such as sodium benzoate or a lower alcohol or diol (e.g., ethanol, isopropanol, ethylene glycol or propylene glycol). The composition may also comprise an oil component such as a paraffinic mineral oil, a triglyceride or a terpenoid based oil. The concentration of active ingredient present in the composition ranges between 0.5 and 10.0% by weight.
    Type: Grant
    Filed: October 3, 1990
    Date of Patent: September 3, 1991
    Assignee: Safer, Inc.
    Inventor: Frederick S. Sedun
  • Patent number: 5035956
    Abstract: An effective, environmentally compatible anti-fungal composition for protecting lumber from infestation by wood-staining and wood-rotting fungi comprises, as an active ingredient, an alkyl sulfosuccinate compound. A preferred alkyl sulfosuccinate is dioctyl sodium sulfosuccinate. The anti-fungal composition may further comprise water and an adjuvant such as sodium benzoate or a lower alcohol or diol (e.g., ethanol, isopropanol, ethylene glycol or propylene glycol). The composition may also comprise an oil component such as a paraffinic mineral oil, a triglyceride or a terpenoid based oil. The concentration of active ingredient present in the composition ranges between 0.5 and 10.0% by weight.
    Type: Grant
    Filed: August 9, 1989
    Date of Patent: July 30, 1991
    Assignee: Safer, Inc.
    Inventor: Frederick S. Sedun
  • Patent number: 5025017
    Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.
    Type: Grant
    Filed: September 28, 1989
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • 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: 4981873
    Abstract: The present invention concerns compounds of the formula: ##STR1## where R.sub.1 is an alkyl or alkenyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3 to 7 carbon atoms, an aralkyl, aralkenyl or aryl radical in which the aryl radical or moiety can be substituted one or more times by halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.12 -dialkylamino, C.sub.1 -C.sub.6 -acylamino, C.sub.1 -C.sub.16 -acyl, C.sub.1 -C.sub.6 -alkylsulphenyl, -sulphinyl or -sulphonyl or by azido, R.sub.2 is hydrogen atom or a C.sub.1 -C.sub.6 -alkyl, aralkyl, aralkenyl or acyl radical, A and B are saturated or unsaturated alkylene chains containing up to 10 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: January 1, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge, Robert A. Slater
  • Patent number: 4952580
    Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.
    Type: Grant
    Filed: November 9, 1988
    Date of Patent: August 28, 1990
    Assignee: FMC Corporation
    Inventors: Anthony J. Martinez, Thomas G. Cullen
  • Patent number: 4940696
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: July 10, 1990
    Assignee: Centre International de Recherches Dermatologioues (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 4937243
    Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 where R.sub.8 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine, CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 -AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12)O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: June 26, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
  • Patent number: 4921696
    Abstract: A method has been discovered for the control of arthropod pests which comprises treating the pest with an effective amount of selected fluorocarbons.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: May 1, 1990
    Assignees: The United States of America as represented by the Secretary of Agriculture, Southern Research Institute, Inc.
    Inventors: Robert K. Vander Meer, Clifford S. Lofgren, David F. Williams
  • Patent number: 4921873
    Abstract: This invention relates to antiviral and antitumor compositions, a process for producing the compositions and a method for inhibiting viruses and tumors utilizing the compositions. More particularly, the compositions are cyclohexadienone derivatives which are derived from red alga Desmia hornemanni.
    Type: Grant
    Filed: June 14, 1985
    Date of Patent: May 1, 1990
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Tatsuo Higa, Kenneth M. Snader
  • Patent number: 4918095
    Abstract: The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described.Such compounds have antibiotic activity and are useful in human and veterinary therapy.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: April 17, 1990
    Assignee: Zambon S.p.A.
    Inventors: Davide Della Bella, Giancarlo Jommi, Mario Fantucci, Dario Chiarino
  • Patent number: 4916156
    Abstract: The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.
    Type: Grant
    Filed: April 6, 1988
    Date of Patent: April 10, 1990
    Assignee: Sanofi
    Inventors: Madeleine Mosse, Vincenzo Proietto
  • Patent number: 4916130
    Abstract: An antithrombotic composition containing an amide derivative which is obtained by binding a sulfur-containing amine to an unsaturated fatty acid having 4 to 13 carbon atoms through an amide bond and which exerts a high platelet agglutination-inhibiting effect.
    Type: Grant
    Filed: September 8, 1988
    Date of Patent: April 10, 1990
    Assignee: Green Cross Corporation
    Inventors: Masakazu Iwai, Chikara Fukaya, Kazumasa Yokoyama
  • 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: 4871769
    Abstract: Tetrachlorobenzoic acid derivative having the formula: ##STR1## (2-trichloroacetoxy-3,4,5,6-tetrachlorobenzoic acid), chemotherapeutically active against cutaneous and subcutaneous benign neoformations, process for its preparations and compositions containing the same.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: October 3, 1989
    Assignees: Wiktor Djaczenko, Maria Strumillo
    Inventors: Gianfranco Fedeli, Giuseppe Diamantini, Wiktor Djaczenko, Maria Strumillo
  • Patent number: 4868211
    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 amino-acid and carnitine protecting groups, thus obtaining the desired compound.
    Type: Grant
    Filed: November 8, 1988
    Date of Patent: September 19, 1989
    Assignee: 501 Sigma Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Carlo A. Bagolini, Domenico Misiti, Carlo Scolastico
  • Patent number: 4855323
    Abstract: Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the indicated meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds, are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: August 8, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hiristo Anagnostopulos
  • Patent number: 4851440
    Abstract: Leukotriene antagonists, processes for the preparation thereof, the use thereof for the treatment of diseases, and precursors.Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the indicated meanings, processes for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds are described. In addition, precursors for the preparation of compounds of the formula I are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: July 25, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Beck, Peter Below, Andreas Bergmann
  • Patent number: 4829087
    Abstract: Utilization of cysteine derivatives or the salts thereof having the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an acetyl radical, R.sub.2 is a hydrogen atom, a methyl radical or an ethyl radical, R.sub.3 is a hydrogen atom or a methyl radical, R.sub.4 is a hydrogen atom or a methyl radical and X is a Proton acid, to enhance the glucose-induced insulin secretion of the Islets of Langerhans of the pancreas.
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: May 9, 1989
    Inventor: Hermann P. T. Ammon
  • 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: 4808572
    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: February 28, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
  • Patent number: 4788061
    Abstract: The healing of a number of skin disorders is effectively enhanced by prolonged continuous occlusion and/or hydration. Treating these disorders, e.g. psoriasis, is significantly facilitated by occluding affected skin areas with a suitable barrier for a prolonged and continuous period of time. Such occlusion is effective by itself, but is materially improved by concurrent topical administration of medicament useful for treating the disorder. In such cases the prolonged, continuous occlusion markedly increases hydration which has the further therapeutic benefit of tremendously facilitating penetration of medicament. The provided barrier is advantageously one with low vapor transmission or one which is water impermeable.
    Type: Grant
    Filed: July 5, 1985
    Date of Patent: November 29, 1988
    Inventor: Ronald N. Shore
  • Patent number: 4767781
    Abstract: 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: Grant
    Filed: December 8, 1986
    Date of Patent: August 30, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada
  • Patent number: 4760061
    Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.
    Type: Grant
    Filed: April 24, 1985
    Date of Patent: July 26, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Philip N. Edwards, Brian S. Tait
  • Patent number: 4745233
    Abstract: Antitumor compounds corresponding to the following formula: ##STR1## in which the substituents R.sub.1 and R.sub.2 may be the same or different and represent hydrogen, an aminocarbonyl group, a C.sub.1 -C.sub.6 alkylaminocarbonyl group, a di-C.sub.1 -C.sub.6 -alkylaminocarbonyl group, the group PO(OH).sub.2, a C.sub.2 -C.sub.8 alkanoyl group, a C.sub.2 -C.sub.8 halogen alkanoyl group or a C.sub.3 -C.sub.8 alkenoyl group, a process for their preparation, and their use in treating oestrogen-receptor-positive-tumors as well as the prostate carcinoma.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: May 17, 1988
    Assignee: Asta-Werke Aktiengesellschaft
    Inventors: Helmut Schonenberger, Rolf W. Hartmann, Martin Schneider, Walter Schwarz, Jurgen Engel
  • Patent number: 4695588
    Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.
    Type: Grant
    Filed: March 16, 1978
    Date of Patent: September 22, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Janos Kollonitsch, Arthur A. Patchett
  • 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: 4675335
    Abstract: Pharmaceutical compounds are described of the formula ##STR1## in which R.sup.1 is (i) R.sup.4 O(CH.sub.2 CH.sub.2 O).sub.n (CH.sub.2).sub.m --, where R.sup.4 is hydrogen or C.sub.1-5 alkyl, n is 0 or 1 to 5 and m is 1 to 7, or (ii) R.sup.5 --X-- where R.sup.5 is a polar group and X is a C.sub.6-20 alkylene or a C.sub.6-20 alkenylene radical containing from 1 to 3 double bonds, R.sup.2 is a group of the formula A--B-- where A is --COOH or ##STR2## where R.sup.6 is hydrogen or a protecting group, and B is C.sub.1-6 alkylene, and R.sup.3 is --COOH or ##STR3## where R.sup.7 is hydrogen or a protecting group; or a salt or ester thereof.
    Type: Grant
    Filed: January 27, 1986
    Date of Patent: June 23, 1987
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, William J. Ross
  • Patent number: 4675330
    Abstract: 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: Grant
    Filed: May 6, 1986
    Date of Patent: June 23, 1987
    Assignee: Sandoz Ltd.
    Inventors: Heinz Berner, Hermann Vyplel
  • 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: 4643994
    Abstract: This invention relates to novel organic trithio oxides of the formula:R.sup.1 --X --R--X.sup.1 --R.sup.1wherein R is selected from --CH.sub.2 CH.dbd.CH--, ##STR1## and (CH.sub.2).sub.3 ; X is selected from ##STR2## X.sup.1 is selected from --S--S, ##STR3## and, each R.sup.1 is independently selected from carboxyalkyl, alkoxy, alkylthio, amino, alkylamino and acyl substituted and unsubstituted lower alkyl, lower alkenyl, lower alkynyl, phenyl and lower alkylphenyl; provided when R is --CH.sub.2 CH.dbd.CH--, X is ##STR4## and X.sup.1 is --S--S--, then R.sup.1 is not in both instances --CH.sub.2 CH.dbd.CH.sub.2.This invention also relates to a method of preparing the above-identified compounds by heating and further oxidizing various oxides of organic disulfides and to antithrombotic uses of the compounds.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: February 17, 1987
    Assignee: The Research Foundation of State University of New York
    Inventors: Eric Block, Saleem Ahmad
  • Patent number: 4609673
    Abstract: 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: Grant
    Filed: December 18, 1984
    Date of Patent: September 2, 1986
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hermann Eggerer, Bernd Hagenbruch, Tran G. Nguyen, Karlheinz Stegmeier, Johannes Pill
  • Patent number: 4596828
    Abstract: [(2-Hydroxy-5-alkoxyphenyl)methylthio]phenylmethanol and derivatives thereof were prepared from an appropriate 2-hydroxy-5-alkoxybenzaldehyde with a hydroxymethylthiophenol. These compounds were found to be potent anti-inflammatory agents.
    Type: Grant
    Filed: March 28, 1985
    Date of Patent: June 24, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, Robert A. Zambias
  • Patent number: 4584318
    Abstract: A method is described for the control of nematodes in agricultural crops which comprises applying to the situs of infestation of a nematicidal composition containing as active ingredient a compound of the formula ##STR1## wherein Q is hydroxy, carbamoyloxy, or acyloxy, R is alkyl, alkenyl, alkynyl, X is halogen or methyl, n is 1 or 2. Preparation of active ingredient compounds is described, and nematicidal utility of compositions is exemplified.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: April 22, 1986
    Assignee: FMC Corporation
    Inventors: Clinton J. Peake, Carmine P. DiSanzo, John F. Engel
  • Patent number: 4552896
    Abstract: The title compound, 1-(3-phenoxy-propyl-2,3-dibromopropionate, ##STR1## is an insect repellent.
    Type: Grant
    Filed: June 6, 1984
    Date of Patent: November 12, 1985
    Assignee: Stauffer Chemical Co.
    Inventor: Nathan S. Bunker
  • Patent number: 4540695
    Abstract: Aminonaphthacene derivatives of the formula: ##STR1## wherein A is either one of the following groups: ##STR2## wherein R.sup.1 is a hydrogen atom or a group of the formula: --COR.sup.7, R.sup.2 and R.sup.3 are each a lower alkoxy group or, when taken together, represent an ethylenedioxy group or an oxo group, R.sup.4 and R.sup.5 are both hydrogen atoms or either one of them is a hydrogen atom and the other is a group of the formula: --COR.sup.7, R.sup.6 is a hydrogen atom, a hydroxyl group or a group of the formula: --OCOR.sup.7 and R.sup.7 is a lower alkyl group, a halo(lower)alkyl group, a phenyl group or a halophenyl group, which are useful as anti-microbial and/or anti-tumor agents, or as intermediates in their production.
    Type: Grant
    Filed: August 11, 1982
    Date of Patent: September 10, 1985
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Kikuo Ishizumi, Naohito Ohashi, Michihisa Muramatsu
  • Patent number: 4524150
    Abstract: Pesticidal mixtures of carbamate insecticides and synthetic pyrethroids can be improved by the addition of stabilizers to prevent racemization of the pyrethroid to a less pesticidally-active isomeric form.
    Type: Grant
    Filed: March 3, 1983
    Date of Patent: June 18, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Orn Adalsteinsson
  • Patent number: 4496588
    Abstract: A novel method of treating psoriasis which comprises administering a halomethyl derivative of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .gamma.-guanidinopropyl or R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4; 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 p-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.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.
    Type: Grant
    Filed: April 28, 1983
    Date of Patent: January 29, 1985
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michel Jung