Sulfur In The Chain Patents (Class 558/396)
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Publication number: 20150045358Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.Type: ApplicationFiled: May 21, 2013Publication date: February 12, 2015Inventors: Yung-hsi KAO, Ya-chu Tang, Hsin-huei Chang, Hui-chen Ku
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Publication number: 20140120106Abstract: Compositions and method for stimulating and controlling arteriogenesis and lymphatic vasculature by preventing and/or reducing the cellular interaction between RAF1 and AKT have been developed. The compositions include molecules that increase the bioavailability of non-phosphorylated RAF1, for example, the RAF1 Ser259 to Ala259 mutant in (RAF1 S259A), and AKT1 inhibitory molecules. Defects, disorders or diseases of insufficient blood or lymphatic vasculature are treated by administering to a patient in need thereof, a pharmaceutical composition comprising a molecule specifically blocking RAF1-AKT crosstalk in a pharmaceutically acceptable carrier or excipient in an amount effective to enhance the growth of blood or lymphatic vasculature in the patient.Type: ApplicationFiled: July 6, 2012Publication date: May 1, 2014Inventors: Michael Simons, Yong Deng
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Publication number: 20140065550Abstract: A polymer comprises the polymerized product of unsaturated monomers comprising an acid-deprotectable monomer, a base-soluble monomer, a lactone-containing monomer, a photoacid-generating monomer, or a combination comprising at least one of the foregoing monomers, with a chain transfer agent of Formula (I); wherein in Formula (I), Z is a y valent C1-20 organic group, L is a heteroatom or a single bond, A1 and A2 are each independently ester containing or non-ester containing and are fluorinated or non-fluorinated, and are independently C1-40 alkylene, C3-40 cycloalkylene, C6-40 arylene, or C7-40 aralkylene, and A1 contains a nitrile, ester, or aryl substituent group alpha to the point of attachment with sulfur, X1 is a single bond, —O—, —S—, —C(?O)—O—, —O—C(?O)—, —O—C(?O)—O—, —C(?O)—NR—, —NR—C(?O)—, —NR—C(?O)—NR—, —S(?O)2—O—, —O—S(?O)2—O—, —NR—S(?O)2—, or —S(?O)2—NR, wherein R is H, C1-10 alkyl, C3-10 cycloalkyl or C6-10 aryl, Y? is an anionic group, G+ is a metallic or non-metallic cation, and y is an intType: ApplicationFiled: August 28, 2013Publication date: March 6, 2014Applicant: DOW GLOBAL TECHNOLOGIES LLCInventors: John W. Kramer, Daniel J. Arriola
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Patent number: 8242173Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: September 1, 2010Date of Patent: August 14, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Alan DeAngelis, Keith T Demarest, Gee-Hong Kuo, Patricia Pelton, Aihua Wang, Rui Zhang
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Publication number: 20120095048Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.Type: ApplicationFiled: February 19, 2010Publication date: April 19, 2012Applicants: REGION MIDT JYLLAND, AARHUS UNIVERSITETInventors: Henrik Amtoft Neubauer, Ove Kjaer Wiborg, Henrik Helligsø Jensen
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Publication number: 20120083608Abstract: The present invention is a process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine as set forth in formula (I) and new intermediates of the preparation process.Type: ApplicationFiled: October 27, 2011Publication date: April 5, 2012Applicant: SANOFIInventors: Janos FAZEKAS, Peter MISKOLCZI, Annamaria MOLNAR, Bela AGAI, Zsolt PARKANYI
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Publication number: 20110144170Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Publication number: 20100331406Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: ApplicationFiled: September 1, 2010Publication date: December 30, 2010Inventors: Alan DEANGELIS, Keith T. Demarest, Gee-Hong Kuo, Patricia Pelton, Aihua Wang, Rui Zhang
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Publication number: 20100204504Abstract: The invention relates to methods of using certain compounds of formula (I), (II) and (III) in the synthesis of an insecticide intermediate of formula (IV), wherein the substituents are as defined in claim 1, to processes for preparing these compounds, to processes which use these compounds to prepare insecticide intermediates, and to certain novel compounds of formula (II?) and (III?).Type: ApplicationFiled: September 2, 2008Publication date: August 12, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Denis Stoller, Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Peter Maienfisch, Werner Zambach
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Publication number: 20100152248Abstract: The invention relates to the use of at least on inhibitor selected from the group consisting of raf-, protein kinase C(PKC)-, MEK1/2-, or ERK1/2-inhibitors, for the manufacturing of a medicament to be administrated from 1 up to 12 hours after initiation of an ischemic disease.Type: ApplicationFiled: March 25, 2008Publication date: June 17, 2010Applicant: Pronas Pharma ABInventors: Lars Edvinsson, Saema Ansar
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Patent number: 7662986Abstract: This invention concerns a free radical polymerization process, selected chain transfer agents employed in the process and polymers made thereby, in which the process comprises preparing polymer of general Formula (A) and Formula (B) comprising contacting: (i) a monomer selected from the group consisting of vinyl monomers (of structure CH2?CUV), maleic anhydride, N-alkylmaleimide, N-arylmaleimide, dialkyl fumarate and cyclopolymerizable monomers; (ii) a thiocarbonylthio compound selected from Formula (C) and Formula (D) having a chain transfer constant greater than about 0.1; and (iii) free radicals produced from a free radical source; the polymer of Formula (A) being made by contacting (i), (ii) C and (iii) and that of Formula (B) by contacting (i), (ii) D, and (iii); and (iv) controlling the polydispersity of the polymer being formed by varying the ratio of the number of molecules of (ii) to the number of molecules of (iii); wherein Q, R, U, V, Z, Z?, m, p and q are as defined in the text.Type: GrantFiled: May 25, 2007Date of Patent: February 16, 2010Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Tam Phuong Le, Graeme Moad, Ezio Rizzardo, San Hoa Thang
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Patent number: 7138108Abstract: Novel (phenylsulfonyl)acrylonitrile siloxanes/silanes, and cosmetic/dermatological sunscreen compositions comprised thereof, are well suited for UV-A photoprotecting the skin and/or the hair against the damaging effects of solar radiation.Type: GrantFiled: June 13, 2003Date of Patent: November 21, 2006Assignee: L'OrealInventors: Hervé Richard, Philippe Breton
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Publication number: 20040087583Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1Type: ApplicationFiled: October 30, 2003Publication date: May 6, 2004Inventor: Frank Worden Hobbs
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Publication number: 20040059122Abstract: A thioacetamide compound represented by the formula (1) which is useful as an intermediate for an acrylonitrile derivative serving as an active ingredient for medicines and agricultural chemicals, especially insecticides/acaricides; a process for producing the compound; and a process for producing a 3-oxo-2-(2-thiazolyl)propanenitrile compound, characterized by reacting the compound represented by the formula (1) with a phenacyl halide.Type: ApplicationFiled: July 22, 2003Publication date: March 25, 2004Inventors: Tomio Yagihara, Tetsushi Ookuchi
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Publication number: 20030229228Abstract: The invention relates to novel pesticidally active &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1-R9 have the meanings given in the specification R10 is either hydrogen, (a), (b), (c), (d) or (e) wherein R13, R14, R16, R17 and R19 are each independently hydrogen or C1-C4 alkyl, R15 is C4-C12 alkyl; C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R18 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR20R21— or —NR22—, wherein R20, R21 and R22 independently of each other are hydrogen of C1-C4 alkyl; provided that when R8 is hydrogen, R9 is not C1-C6-alkoxy, C3-C6 alkenyloxy or C3-C6-alkynyloxy in position 3 of the phenyl ring carrying these radicals.Type: ApplicationFiled: February 20, 2003Publication date: December 11, 2003Inventors: Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
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Patent number: 6541422Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.Type: GrantFiled: May 28, 1999Date of Patent: April 1, 2003Assignee: Syngenta LimitedInventors: Herbert B. Scher, Jinling Chen
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Publication number: 20020091259Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: February 24, 2002Publication date: July 11, 2002Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6242634Abstract: Novel pyrimidin-4-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is hydrogen or alkyl; R2 is alkyl optionally substituted with halogen; R3 is alkyl optionally substituted with halogen, alkenyl, or alkynyl; and Q is substituted phenyl. Also provided are intermediates for their production and processes for producing these intermediates.Type: GrantFiled: May 31, 2000Date of Patent: June 5, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Masayuki Enomoto, Hisayuki Hoshi, Yuzuru Sanemitsu
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Patent number: 6077866Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.Type: GrantFiled: May 10, 1996Date of Patent: June 20, 2000Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
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Patent number: 5856490Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: January 5, 1999Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5674811Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.Type: GrantFiled: October 6, 1994Date of Patent: October 7, 1997Assignee: Tokuyama CorporationInventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
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Patent number: 5629265Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.Type: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Patent number: 5470994Abstract: Sulfonium and oxysulfonium salts, useful as photoinitiators, have directly attached to the sulfur atom thereof:at least one aromatic or heterocyclic aromatic substituent containing at least 14 aromatic atoms and having a removable positive hydrogen ion, said substituent exhibiting a higher energy occupied molecular orbital than at least one other substituent directly attached to said sulfur atom;and at least one substituent comprising an electron withdrawing group and exhibiting a lower energy unoccupied molecular orbital than at least one other substituent directly attached to said sulfur atom;said salt being capable, upon exposure to visible radiation, of undergoing irreversible intramolecular rearrangement to form a Bronsted acid comprising the anion of said salt and said removable positive hydrogen ion.Type: GrantFiled: April 5, 1990Date of Patent: November 28, 1995Assignee: Eastman Kodak CompanyInventors: Franklin D. Saeva, David T. Breslin
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Patent number: 5389619Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.Type: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5354777Abstract: New cyanoalkene derivatives of the formula (I) ##STR1## are described, in which R and R.sup.1 have the meaning given in the description, and a process for their preparation.The new cyanoalkene derivatives are used for combating microorganisms for the protection of industrial materials.Type: GrantFiled: February 23, 1993Date of Patent: October 11, 1994Assignee: Bayer AktiengesellschaftInventors: Peter Wachtler, Wilfried Paulus, Georg-Wilhelm Ludwig
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Patent number: 5317102Abstract: This invention relates to 3,6-diamino-2,5-pyrazinedicarbonitrile which is a red crystal and yellowish green fluorenscent substance and the methods of preparation from compounds represented by formula [I], ##STR1## (wherein R are aryl, alkyl, aralkyl or alkenyl or may be substituted), as a starting material, under acidic condition in the presence of oxygen.Type: GrantFiled: August 7, 1992Date of Patent: May 31, 1994Assignee: Nippon Soda Co., Ltd.Inventors: Seiji Tazaki, Tomio Yagihara, Nobuo Matsui, Atsushi Yanagisawa, Takakazu Kojima
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Patent number: 5300633Abstract: Azo compounds of the formula D.sup.o --N.dbd.N--K.sup.o, in which D.sup.o is a radical of the formula (2), (2a) or (2b) ##STR1## in which Y is a substituent which can be eliminated by alkali to form the vinyl group, X is chlorine or bromine and R is hydrogen, lower alkyl, phenyl or halogen, and K.sup.o is the radical of a coupling component or another radical which contains azo groups, K.sup.o containing a group of the formula --N(R.sup.o)--Z, in which R.sup.o is hydrogen or lower alkyl and Z is a radical of the formula ##STR2## in which A is halogen or cyanoamido, R.sup.20 is hydrogen or lower alkyl, and R.sup.21 has one of the meanings given for R.sup.20, or is an optionally methyl-substituted cycloalkylene radical, or is a phenyl radical, or in which R.sup.20 and R.sup.21, together with the nitrogen atom and if appropriate one or two further hetero groups, can form a 5- or 6-membered heterocyclic radical.Type: GrantFiled: May 8, 1992Date of Patent: April 5, 1994Assignee: Hoechst AktiengesellschaftInventors: Jorg Dannheim, Werner H. Russ
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Patent number: 5294711Abstract: This invention relates to 3,6-diamino-2,5-pyrazinedicarbonitrile which is a red crystal and yellowish green fluorescent substance and the methods of preparation from compounds represented by formula [I], ##STR1## (wherein R are aryl, alkyl, aralkyl or alkenyl or may be substituted), as a starting material, under acidic condition in the presence of oxygen.Type: GrantFiled: April 29, 1991Date of Patent: March 15, 1994Assignee: Nippon Soda Co., Ltd.Inventors: Seiji Tazaki, Tomio Yagihara, Nobuo Matsui, Atsushi Yanagisawa, Takakazu Kojima
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Patent number: 5279764Abstract: The invention relates to dihalogenobenzene derivatives of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --(Z.sup.2 --A.sup.3).sub.n --R.sup.2wherein R.sup.1, R.sup.2, A.sup.1, A.sup.2, A.sup.3, Z.sup.1, Z.sup.2 and n are as defined in the specification.Type: GrantFiled: November 23, 1992Date of Patent: January 18, 1994Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Volker Reiffenrath, Joachim Krause, Georg Weber, Ulrich Finkenzeller, Andreas Wachtler, Thomas Geelhaar, David Coates, Ian C. Sage, Simon Greenfield
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Patent number: 5234894Abstract: A cyanoketone derivative of the following formula (1) ##STR1## wherein A.sub.1 is a substituted or unsubstituted phenyl or naphthyl group or a substituted or unsubstituted heterocyclic group;each of X.sub.1, X.sub.2 and X.sub.3 is independently an oxygen or sulfur atom;each of B.sub.1, B.sub.2 and B.sub.3 is independently a hydrogen atom or C.sub.1 -C.sub.6 -alkyl group;each of Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 is independently a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.6 -alkyl group; andA.sub.2 is a substituted or unsubstituted group selected from the group consisting of a C.sub.1 -C.sub.6 -alkyl group, a C.sub.2 -C.sub.6 -alkenyl group, a C.sub.2 -C.sub.6 -alkynyl group, a C.sub.1 -C.sub.4 -alkoxy group, a C.sub.1 -C.sub.4 -alkylthio group, a C.sub.1 -C.sub.6 -alkoxycarbonyl group, an unsubstituted benzoyl group, a halogen-substituted benzoyl group, a cyano group or a group as defined in A.sub.1 ;provided that when B.sub.1 is a hydrogen atom and B.sub.Type: GrantFiled: March 27, 1992Date of Patent: August 10, 1993Assignee: Tokuyama Soda Kabushiki KaishaInventors: Masahiko Ishizaki, Seiji Nagata, Tadashi Kobutani
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Patent number: 5216138Abstract: There are described water soluble azo compounds conforming to the formula (1)D--N.dbd.N--K (1)where D is a radical of the formula (2), (2a) or (2b) ##STR1##where Y is a substituent which is eliminable by alkali to form a vinyl group, Y.sup.2 has one of the meanings of Y or is hydroxyl, X is chlorine or bromine, and R is hydrogen, lower alkyl, phenyl or halogen, and K is a radical of a singly couplable coupling component which may additionally contain an azo group, or the radical of a doubly couplable coupling component.The compounds of the formula (1) have fiber-reactive properties and are very highly suitable for use as dyes for dyeing hydroxy- and/or carboxamido-containing material, in particular fiber material, for example cellulose-fiber materials, wool and synthetic polyamide fibers, in strong, fast shades.There are also described novel starting compounds of the formulae (7), (7a) and (7b) ##STR2##where Y.sup.2, X and R are each as defined above, x is zero or 2 and W is nitro or amino.Type: GrantFiled: November 27, 1991Date of Patent: June 1, 1993Assignee: Hoechst AktiengesellschaftInventor: Jorg Dannheim
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Patent number: 5185460Abstract: Aminoacetonitrile derivatives, where the 2-position of aminoacetonitrile is optionally substituted by alkylthio groups, arylthio groups and heterocyclicthio groups. The process for making such compounds comprises reacting hydrogen cyanide with the desired corresponding R-S-H and recovering the crystallized salt thereof. The aminoacetonitrile derivatives are useful as starting materials to produce pharmaceutical and agricultural intermediates such as benzomide derivatives with fungicidal and herbicidal activities.Type: GrantFiled: April 22, 1992Date of Patent: February 9, 1993Assignee: Nippon Soda Co., Ltd.Inventors: Seiji Tazaki, Nobuhiro Umeda, Nobuo Matsui, Tomio Yagihara, Katsunori Mikuma
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Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
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Patent number: 5126349Abstract: Substituted 3-thio-2-propynenitriles are prepared which correspond to the formula:R--S--C.tbd.C--C.tbd.Nwherein R is an alkyl, cyclic alkyl, aryl, or heterocyclo group.These compounds have been found to exhibit a high degree of antimicrobial activity in industrial and commercial applications and compositions containing these compounds are so employed.Type: GrantFiled: December 26, 1990Date of Patent: June 30, 1992Assignee: The Dow Chemical CompanyInventors: Connie I. Deford, Charles D. Gartner, Kalakota S. Reddy, John K. Swayze, David E. Wallick, Warren L. Treptow, George A. Paul, Billy R. Hardas
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Patent number: 5066822Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted in the 4 position by an alkoxy or benzyloxy group or a benzylthio group, which alkoxy or benzyloxy group is directly substituted by a tetrazole ring, and which benzylthio group is directly substituted by carboxy or tetrazolyl are useful as inhibitors of leukotriene biosynthesis and as antiallergic agents. Synthetic intermediates for preparing such compounds are also described.Type: GrantFiled: June 29, 1990Date of Patent: November 19, 1991Assignee: Riker Laboratories, IncInventor: Mark A. Rustad
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Patent number: 5039702Abstract: Userful as antimicrobial agents in aqeuous systems are .alpha.-halo.beta.-(substituted)thioacrylonitriles of the formula ##STR1## wherein X represents Cl, Br or I and R represents a lower alkyl, aryl, aralkyl, heterocyclo, or a thiocarbonyl group. The configuration about the double bond may be E or Z or a mixture thereof. These compounds provide effective control of microbial growth. The derivatives of formula I are economically prepared from acrylonitrile via a three-step process involving (a) halogenation, (b) dehydrohalogenation and (c) nucleophilic-type displacement. Except for those compounds wherein X is bromo and R is methyl or phenyl, the compounds of formula I are not mentioned in the prior art.Type: GrantFiled: April 14, 1989Date of Patent: August 13, 1991Assignee: Givaudan CorporationInventors: Alyce Brandman, Milton Manowitz, Albert I. Rachlin
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Patent number: 5034537Abstract: This invention relates to (R)-.alpha.-methyl-4-halobenzenemethanamine salts of epimers of acids of the formula ##STR1## and the use of these salts to separate these epimers. These acids are leukotriene antagonists.Type: GrantFiled: February 8, 1990Date of Patent: July 23, 1991Assignee: SmithKline Beecham CorporationInventor: James S. Frazee
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Patent number: 5008430Abstract: The invention relates to mercaptopyrenes of the formula ##STR1## in which n denotes a whole number from 3 to 10 andR stands for a substitute or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or aryl radicalto a process for its preparation, its use for the preparation of CT complexes and to the CT complexes obtained.Type: GrantFiled: April 10, 1989Date of Patent: April 16, 1991Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Friedrich Jonas
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Patent number: 5006158Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or ##STR2## wherein R.sup.a is C.sub.1 -C.sub.4 alkyl; R.sup.1 and R.sup.2 together are alkylene having 3 to 6 carbon atoms; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.7 is hydrogen or 3-C.sub.1 -C.sub.4 alkoxy; and R.sup.8 is (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) OCF.sub.3 ; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)-- wherein R.sup.e is C.sub.1 -C.sub.Type: GrantFiled: February 23, 1988Date of Patent: April 9, 1991Assignee: ICI Americas Inc.Inventors: Charles G. Carter, David L. Lee, William J. Michaely, Gary W. Kraatz
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Patent number: 4997940Abstract: Novel compounds, e.g. 3-cyano-5,7-dimethyl-N-(2,6-dichlorophenyl)pyrazolo[1,5-a]pyrimidine-2-sul fonamide and their use as herbicides and/or for the suppression of nitrification of ammonium nitrogen in soil.Type: GrantFiled: July 27, 1988Date of Patent: March 5, 1991Assignee: The Dow Chemical CompanyInventors: Anna P. Vinogradoff, William A. Kleschick
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Patent number: 4994495Abstract: Fungicidal compounds having the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted C.sub.2-10 alkenyl, optionally substituted C.sub.5-6 cycloalkenyl, optionally substituted C.sub.2-10 alkynyl, or C.sub.1-10 alkyl substituted with --CN, --NC, --COR.sup.2, --CO.sub.2 R.sup.2, --NO.sub.2 or --SCN; X is O, S(O)n or NR.sup.2 and is attached to the 3- or the 4-position of the phenyl ring; Y and Z, which may be the same or different, are H, halogen, --CH.sub.3, --C.sub.2 H.sub.5, or --OCH.sub.3 ; R.sup.2 is H, C.sub.1-4 alkyl, C.sub.1-4 alkenyl, or, when R.sup.2 is C.sub.1-4 alkyl in the group --COR.sup.2, it joins with the alkyl group to which --COR.sup.2 is attached to form a 5- or 6-membered aliphatic ring; and n is 0, 1 or 2.Type: GrantFiled: May 11, 1989Date of Patent: February 19, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Michael G. Hutchings, Ian Ferguson
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Patent number: 4992091Abstract: Novel compounds, e.g. 3-cyano-5,7-dimethyl-N-(2,6-dichlorophenyl)pyrazolo]1,5-a]pyrimidine-2-sul fonamide and their use as herbicides and/or for the suppression of nitrification of ammonium nitrogen in soil.Type: GrantFiled: July 11, 1986Date of Patent: February 12, 1991Assignee: The Dow Chemical CompanyInventors: Anna P. Vinogradoff, William A. Kleschick
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Patent number: 4992576Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: March 27, 1990Date of Patent: February 12, 1991Assignee: Eli Lilly and CompanyInventor: D. Mark Gapinski
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Patent number: 4971959Abstract: Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure.Type: GrantFiled: December 30, 1988Date of Patent: November 20, 1990Assignee: Warner-Lambert CompanyInventor: Lynn D. Hawkins
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Patent number: 4954514Abstract: (Di-tert-butylhydroxyphenyl)thio derivatives of the formula: ##STR1## wherein R is cyano, carbamoyl, or 5-tetrazolyl; n is an integer of 2 to 6; provided that when R is cyano, n is not 2; or a pharmaceutically acceptable salt thereof; useful in treating arterioschlerosis, ulcer, inflammation, allergy, or the like.Type: GrantFiled: December 18, 1989Date of Patent: September 4, 1990Assignee: Shionogi & Co, LtdInventors: Toru Kita, Shuh Narumiya, Masayuki Narisada, Fumrhio Watanabe, Masami Doteuchi, Takuji Mizui
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Patent number: 4933377Abstract: Sulfonium and oxysulfonium salts, useful as photoinitiators, have directly attached to the sulfur atom thereof:at least one aromatic or heterocyclic aromatic substituent containing at least 14 aromatic atoms and having a removable positive hydrogen ion, said substituent exhibiting a higher energy occupied molecular orbital than at least one other substituent directly attached to said sulfur atom;and at least one substituent comprising an electron withdrawing group and exhibiting a lower energy unoccupied molecular orbital than at least one other substituent directly attached to said sulfur atom;said salt being capable, upon exposure to visible radiation, of undergoing irreversible intramolecular rearrangement to form a Bronsted acid comprising the anion of said salt and said removable positive hydrogen ion.Type: GrantFiled: February 29, 1988Date of Patent: June 12, 1990Inventors: Franklin D. Saeva, David T. Breslin
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Patent number: 4874792Abstract: This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.Type: GrantFiled: March 25, 1988Date of Patent: October 17, 1989Assignee: Smithkline Beckman CorporationInventors: John G. Gleason, Ralph F. Hall, Thomas W. Ku, Carl D. Perchonock
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Patent number: 4869748Abstract: Herbicidal compounds of the formula ##STR1## wherein R is halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; trifluoromethoxy; difluoromethoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; R.sup.a SO.sub.n - wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl, trifluoromethyl or difluoromethyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; andR.sup.5 and R.sup.6 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n - wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)- wherein R.sup.Type: GrantFiled: December 2, 1988Date of Patent: September 26, 1989Assignee: ICI Americas Inc.Inventor: Christopher G. Knudsen
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Patent number: 4845119Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent of each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substitutent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl;wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --; andwherein R.sup.9 is alkyl or up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: February 18, 1986Date of Patent: July 4, 1989Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, Howard Tucker
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Patent number: 4845110Abstract: There are provided anti-allergic pharmaceutical compounds of formula: ##STR1## in which n is 0, 1 or 2; R.sup.1 is a hydrocarbyl group containing 6 to 30 carbon atoms and optionally substituted with an optionally substituted phenyl group; R.sup.2 is (i) optionally optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.10 is hydrogen or C.sub.1-4 alkyl; and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.Type: GrantFiled: December 4, 1986Date of Patent: July 4, 1989Assignee: Lilly Industries LimitedInventors: Stephen R. Baker, Alec Todd