The Compound Is Acyclic Patents (Class 564/197)
  • Patent number: 5750733
    Abstract: The present invention relates to novel hydroxy-containing alkyl glycamide surfactants and detergent composition comprising said surfactants. Since they surprisingly provide low foam, these surfactants can be used as cleansing surfactants in applications where low foaming is desirable.
    Type: Grant
    Filed: August 6, 1996
    Date of Patent: May 12, 1998
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Robert Vermeer, Bijan Harichian
  • Patent number: 5739167
    Abstract: A salt of formula (I) where X denotes a group of formula (II), Y denotes a group of formula (III) and R denotes the residue of an aliphatic or cycloaliphatic sulphonic acid having at least 3 carbon atoms after removal of an --SO.sub.3 H group therefrom.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: April 14, 1998
    Assignee: Novartis Corporation
    Inventors: Nicholas Lowther, Ian Francis Hassan, Ian Timothy William Matthews
  • Patent number: 5733935
    Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: March 31, 1998
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
  • Patent number: 5705602
    Abstract: A star-like or comb-like branched aliphatic polyamino compound for use as a basic catalyst or a curing agent, as an effective thixotropic agent or viscosity adjusting agent for an aqueous medium, as a component for any one of a coating-forming agent, a sealing agent, a molding material and an adhesive resin, or as a substantially solvent-free coating composition, molding material or adhesive resin. The process for the production of the above compound comprises (a) forming an adduct of ammonia or an aliphatic amino compound having an amino group (compound A) with methyl acrylate, adding an alkylenediamine having 2 to 12 carbon atoms to the adduct to carry out an ester-amide exchange reaction (b), thereby obtaining a polyamino compound (B) having a total of 2 to 100 aliphatic primary amino and secondary amino groups per molecule and having a number average molecular weight of 170 to 10,000, and forming an adduct of the polyamino compound (B) with an acrylic acid ester (C) of the formula (1),CH.sub.2 =CHCOO--R.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: January 6, 1998
    Assignee: Toyo Ink Manufacturing Co., Ltd.
    Inventors: Miki Kawashima, Takeo Yamaguchi, Toru Kurihashi, Norifumi Watanabe
  • Patent number: 5705689
    Abstract: A family of aza-ether based compounds including linear, multi-branched and aza-crown ethers is provided. When added to non-aqueous battery electrolytes, the family of aza-ether based compounds acts as neutral receptors to complex the anion moiety of the electrolyte salt thereby increasing the conductivity and the transference number of Li.sup.+ ion in alkali metal batteries.
    Type: Grant
    Filed: June 19, 1995
    Date of Patent: January 6, 1998
    Assignee: Associated Universities, Inc.
    Inventors: Hung Sui Lee, Xiao-Qing Yang, James McBreen
  • Patent number: 5700934
    Abstract: A process for the preparation of .epsilon.-caprolactam and .epsilon.-caprolactam precursors, starting from the corresponding 5-formylvalerate ester, ammonia and hydrogen in the presence of a hydrogenation catalyst is disclosed, wherein in a step (a) 5-formylvalerate ester is reacted with ammonia under non-hydrogenating conditions, and in a step (b) the reaction product obtained in step (a) is converted to .epsilon.-caprolactam and the .epsilon.-caprolactam precursor(s) under hydrogenating conditions, in the presence of ammonia.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: December 23, 1997
    Assignees: DSM N.V., E. I. DuPont de Nemours & Company
    Inventors: Henricus F. W. Wolters, Samuel L. Lane, Wim Buijs, Nicolaas F. Haasen, Frank E. Herkes
  • Patent number: 5696071
    Abstract: Described are a tris(3-aminopropyl)amine derivative represented by the following formula (1): ##STR1## wherein R represents a C.sub.1-24 alkyl or alkenyl group which may have --OH, A represents a C.sub.1-6 alkylene or alkenylene group which may have --OH, --COOH or --SO.sub.3 H, Y.sup.1 represents --COOH, --SO.sub.3 H or --OSO.sub.3 H , Y.sup.2 represents --OH, --OSO.sub.3 H or --OCO--A--COOH and n stands for 0 or 1, or a salt or quaternized product thereof; and a detergent composition containing the same. The compound according to the present invention has low skin or hair irritation, has excellent foaming power and imparts favorable touch feeling to the skin or the like.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: December 9, 1997
    Assignee: Kao Corporation
    Inventors: Akiko Okutsu, Tomohito Kitsuki, Katsumi Kita
  • Patent number: 5691366
    Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
    Type: Grant
    Filed: October 31, 1995
    Date of Patent: November 25, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
  • Patent number: 5631389
    Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: May 20, 1997
    Assignee: Lever Brothers Company, Division of Conopco, Inc.
    Inventors: Robert Vermeer, Van Au, Bijan Harichian
  • Patent number: 5627284
    Abstract: The present invention relates to a process for producing (E)-alkoxyiminoacetamide compounds useful as agricultural fungicides and a process for producing (E)-hydroxyiminoacetamide compounds useful as intermediates for producing them. The present invention also relates to an industrial process for producing (E)-methoxyiminoacetamide compounds useful as agricultural fungicides. This process is advantageous in terms of the cost, safety and the like.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: May 6, 1997
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Takase, Hiroyuki Kai, Moriyasu Masui, Kuniyoshi Nishida
  • Patent number: 5618966
    Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: April 8, 1997
    Assignee: Pharm-Eco Laboratories, Incorporated
    Inventors: Biman Pal, Siya Ram, Bing Cai, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard Gabriel
  • Patent number: 5618842
    Abstract: N-acyl derivatives of aminoalcohols with bicarboxylic or tricarboxylic acids able to modulate the degranulation process consequent to the mast cells activation in inflammatory processes caused by supramaximal stimuli of neurogenic and immunogenic origin.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: April 8, 1997
    Assignee: Lifegroup S.p.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
  • Patent number: 5616745
    Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 1, 1997
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Paul Behr, Jean-Philippe Loeffler
  • Patent number: 5587514
    Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: December 24, 1996
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Bharat R. Lagu
  • Patent number: 5532259
    Abstract: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 2, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
  • Patent number: 5527962
    Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: June 18, 1996
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Andre A. Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
  • Patent number: 5510380
    Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and methods of treating diseased or pathological conditions using the pharmaceutical compositions.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: April 23, 1996
    Assignee: Sterling Winthrop, Inc.
    Inventors: Peter R. Seoane, Joseph M. Salvino, Brent D. Douty, Mohamed M. A. Awad, Roland E. Dolle, David G. Sawutz, David M. Faunce, Wayne T. Houck
  • Patent number: 5506356
    Abstract: An N-acylamino acid derivative of the formula: ##STR1##
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: April 9, 1996
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5504115
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5494911
    Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: February 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
  • Patent number: 5495023
    Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
    Type: Grant
    Filed: May 3, 1994
    Date of Patent: February 27, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
  • Patent number: 5481036
    Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: January 2, 1996
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5470878
    Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: November 28, 1995
    Assignee: Cell Therapeutics, Inc.
    Inventors: John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
  • Patent number: 5470949
    Abstract: A compound of the formula ##STR1## is disclosed. X is selected from the group consisting of aryl, alkyl, imidate ester, imino ester, amidine, azide, isocyanate, and dithiocarbonate. R' is a group selected from the group consisting of groups containing a hydroxyl moiety, groups containing a protected hydroxyl moiety, and groups containing an O-linked sugar. G is a carbon chain of 0-10 carbons and R is not a methyl group and is a group capable of removal under conditions compatible with glycopeptide synthesis. In a preferred form the compound, R is selected from the group consisting of benzylic or allyl groups and X is CPh.sub.2. A method of forming a glycocide from the compound is also disclosed.
    Type: Grant
    Filed: December 15, 1992
    Date of Patent: November 28, 1995
    Assignee: The Arizona Board of Regents on Behalf of the University of Arizona
    Inventor: Robin L. Polt
  • Patent number: 5468901
    Abstract: The invention relates to a process for preparing optically active methionine amide in high ee purities in which a mixture of D- and L-methionine amide or the Schiff bases thereof is at least partly converted, optionally in the presence of 0.5-4 equivalents of an aldehyde, relative to the amount of methionine amide, and water, in the presence of an organic solvent, using less than 1.2 equivalents of L- or D-mandelic acid, respectively, relative to the amount of D- or L-methionine amide, respectively, or the Schiff bases thereof, present in the mixture of D- and L-methionine amide or the Schiff bases thereof, into a salt of methionine amide and mandelic acid, a portion consisting substantially of one of the diastereoisomers of the salt is separated from the reaction mixture obtained, and the salt is converted into the optically active methionine. A high degree of optical purity is obtained.
    Type: Grant
    Filed: July 9, 1993
    Date of Patent: November 21, 1995
    Assignee: DSM N.V.
    Inventors: Wilhelmus H. J. Boesten, Quirinus B. Broxterman
  • Patent number: 5466878
    Abstract: A cosmetic composition for the first stage of a permanent deformation of the hair contains, in a cosmetically acceptable vehicle, as a reducing agent, an amino mercaptoalkylamide having the formula ##STR1## wherein A represents the divalent radical, --(CH.sub.2).sub.n -- wherein n is a whole number ranging from 2 to 5, or the divalent radical --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, m is 0 or a whole number ranging from 1 to 4, and (i) when m is 0, R.sub.1 represents hydrogen, methyl, ethyl, isopropyl, isobutyl, 2-methyl butyl, benzyl, 4-amino butyl, 3-guanidino propyl, 2-methylthio ethyl, carboxymethyl or 2-carboxyethyl, and (ii) when m is a whole number from 1 to 4, R.sub.1 represents hydrogen or lower alkyl having 1-5 carbon atoms, and the salts of the compound of formula I.
    Type: Grant
    Filed: October 18, 1991
    Date of Patent: November 14, 1995
    Assignee: L'Oreal
    Inventors: Alex Junino, Gerard Malle
  • Patent number: 5432202
    Abstract: Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-based moiety (or a guanidine moiety) coupled to a straight chain polyamine.These polyamines as well as a method for regulating NMDA through a spermidine-like effect on NMDA receptors by exposing a cell membrane to selected polyamines are also provided.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: July 11, 1995
    Assignee: New York University
    Inventors: Bruce D. Cherksey, Rodolfo R. Llinas, Mutsuyuki Sugimori
  • Patent number: 5399590
    Abstract: The invention relates to the field of organic chemistry and more particularly to that of therapeutic chemistry.More particularly it relates to new quaternary ammonium salts of general formula (I): ##STR1## in which Hal is a halogen atom other than fluorine R and R.sub.1, identical or different, are lower alkyl radicals, n is an integer varying from 2 to 16, Z is an alkenyl radical having up to 3 carbon atoms, a carboxyl, or the OR.sub.2 group in which R.sub.2 is a hydrogen, a lower alkyl radical, an acyl remainder, a tocol radical, a sterol radical or a carboxamide chain and A is a hydroxyl or an anion of a mineral or organic acid.The compounds according to the invention are the active ingredients of pharmaceutical compositions with an anti-tumorous and/or immuno-suppressive action.
    Type: Grant
    Filed: January 14, 1993
    Date of Patent: March 21, 1995
    Inventor: Jean M. Gastaud
  • Patent number: 5369108
    Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.
    Type: Grant
    Filed: October 4, 1991
    Date of Patent: November 29, 1994
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
  • Patent number: 5352705
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5334377
    Abstract: Alkylamino-mercaptoalkylamides have the formula ##STR1## where in A represents the divalent radical --(CH.sub.2).sub.n --, wherein n is a whole number ranging from 2 to 5, or the divalent radical --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --,m is 0, 1 or 2,R.sub.1 represents hydrogen or linear or branched lower alkyl having 1-5 carbon atoms,R.sub.2 and R.sub.3, each independently, represent hydrogen or a linear or branched lower alkyl having 1-4 carbon atoms with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously and the salts of the compound of formula I as well as the corresponding disulfides with the exclusion of the disulfide in which A.dbd.--(CH.sub.2).sub.2 --, m.dbd.0, R.sub.1 and R.sub.2 .dbd.H and R.sub.3 .dbd.--C.sub.2 H.sub.5. The compound of formula I is used as a reducing agent in a cosmetic composition for the permanent deformation of hair.
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: August 2, 1994
    Assignee: L'Oreal
    Inventors: Alex Junino, Gerard Malle, Bernadette Luppi
  • Patent number: 5334761
    Abstract: The present invention discloses cationic lipids useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Also disclosed are lipids useful both for the delivery of macromolecules and also useful as intermediates for making other such lipids.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: August 2, 1994
    Assignee: Life Technologies, Inc.
    Inventors: Gulilat Gebeyehu, Joel A. Jessee, Valentina C. Ciccarone, Pamela Hawley-Nelson, Anna Chytil
  • Patent number: 5332407
    Abstract: A diesel fuel composition comprising a major portion of a middle distillate fuel oil and a minor portion, effective to clean deposits from diesel fuel injectors, of a diesel fuel detergent comprising the reaction product of:(a) a 4-alkyl-2-morpholinone represented by the formula: ##STR1## in which R represents a monovalent aliphatic radical having from 1 to 10 carbon atoms, and(b) an alkylphenoxypolyoxyalkylene amine represented by the formula: ##STR2## in which R' represents a hydrocarbyl radical having from 4 to 30 carbon atoms, x has a value from 5 to 50, and R" represents a methyl radical or a mixture of hydrogen and methyl radicals.A method of cleaning diesel fuel injectors is also provided.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: July 26, 1994
    Assignee: Texaco Inc.
    Inventor: Sheldon Herbstman
  • Patent number: 5310905
    Abstract: Waste nylon 6 and/or nylon 6,6 are treated with aliphatic monocarboxylic acid to depolymerize the polymer to desirable monomer.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: May 10, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Edward F. Moran, Jr.
  • Patent number: 5278148
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: January 11, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
  • Patent number: 5274167
    Abstract: An optically active N-(meth)acryloyl amino acid amide of the formula ##STR1## in which R is hydrogen or methyl,R.sub.1 represents an optionally substituted alkyl, cycloalkyl, aralkyl, aryl or heteroaryl radical,R.sub.3 represents hydrogen or denotes together with R.sub.1 a tri- or tetramethylene group;X denotes oxygen or a NR.sub.4 -group wherein R.sub.4 represents hydrogen or alkyl or denotes together with R.sub.2 and the nitrogen atom a 5- to 7-membered ring which ring is optionally substituted by the group COO-alkyl (1-6 carbon atoms) or by one or two alkyl radicals (1-4 carbon atoms) andR.sub.2 denotes a strongly space-filling hydrocarbon radical.The amide is polymerized and optionally bound to a support such as silica, and can then be used for the chromatographic separation of racemic mixtures of pharmacologically active compounds.
    Type: Grant
    Filed: February 13, 1992
    Date of Patent: December 28, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Lange, Bruno Bomer, Rolf Grosser, Dieter Arlt
  • Patent number: 5258552
    Abstract: N-alkylamide or D(+)-carnitrine having general formula ##STR1## wherein X.sup.- is OH.sup.- or the anion of a pharmacologically acceptable acid (preferably Cl.sup.-), andR is a straight C.sub.10 -C.sub.16 alkyl radical are prepared via transamination by reacting (D(+)-carnitinamide halogenide with an amine or formula NH.sub.2 R wherein R has the above-identified meaning in an acid environment (e.g. H.sub.3 PO.sub.4) in the presence of a high-boiling solvent (e.g. ethylene glycol).N-alkylamides (I) are endowed with potent anti-bacterial activity and are suitable for preparing pharmaceutical and cosmetic compositions.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: November 2, 1993
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Paolo Cavazza, Giulio Fiorentini
  • Patent number: 5242947
    Abstract: Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-based moiety (or a guanidine moiety) coupled to a straight chain polyamine.These polyamines as well as a method for regulating NMDA through a spermidine-like effect on NMDA receptors by exposing a cell membrane to selected polyamines are also provided.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: September 7, 1993
    Assignee: New York University
    Inventors: Bruce D. Cherksey, Rodolfo R. Llinas, Mutsuyuki Sugimori
  • Patent number: 5223644
    Abstract: Bicarbonates and/or carbonates are used in greater than catalytic amounts to inhibit the formation of nitrosamines during the preparation, storage and/or use of amine oxides.
    Type: Grant
    Filed: February 3, 1992
    Date of Patent: June 29, 1993
    Assignee: Albright & Wilson Limited
    Inventors: Michael Blezard, Glyn R. Jones
  • Patent number: 5208375
    Abstract: Methods and compositions for enhancing magnetic resonance imaging in at least a portion of a warm-blooded animal.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: May 4, 1993
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: Dennis A. Moore, Rebecca A. Wallace
  • Patent number: 5196582
    Abstract: Quaternary ammonium halides are prepared in solid form by reacting an alkyl or aralkyl halide with ammonia or an amine in a liquefied gas as the solvent.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: March 23, 1993
    Assignee: Ethyl Corporation
    Inventors: Kim R. Smith, James E. Borland, Jeffrey W. Perine, Joe D. Sauer
  • Patent number: 5175343
    Abstract: Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.
    Type: Grant
    Filed: June 19, 1987
    Date of Patent: December 29, 1992
    Assignee: NeoRx Corporation
    Inventors: Alan R. Fritzberg, Sudhakar Kasina, Ananthachari Srinivasan, Daniel S. Wilbur
  • Patent number: 5171678
    Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6; R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: December 15, 1992
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Paul Behr, Jean-Philippe Loeffler
  • Patent number: 5154912
    Abstract: The peroxides which include the O.sup.17 isotope, especially the hydrogen peroxides and peroxides and hydroperoxides prepared therefrom, are well adapted as nonradioactive labeled compounds for use in the medicinal and biological arts.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: October 13, 1992
    Assignee: Atochem
    Inventors: Jean-Pierre Schirmann, Jean-Jacques Barieux
  • Patent number: 5136093
    Abstract: Quaternized panthenol compounds of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are alkyl and R.sub.3 is alkylene, each independently, straight or branched chain of 1-24 carbon atoms, and X is a halogen.
    Type: Grant
    Filed: February 6, 1991
    Date of Patent: August 4, 1992
    Inventor: Ronald J. Smith
  • Patent number: 5122523
    Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined or a salt thereof, which is useful as hypotensive drugs.
    Type: Grant
    Filed: September 6, 1988
    Date of Patent: June 16, 1992
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5089043
    Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: February 18, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
  • Patent number: 5051525
    Abstract: N-acyl-2-amino acid amides containing phosphinic esters, process for their preparation, and N-acyl-2-amino acid nitriles as precursorsPhosphorus-containing N-acyl-2-amino acid amides of the general formula (I) ##STR1## where R.sup.1 is alkyl, optionally substituted by halogen or alkoxy, or is benzyl or phenyl, each of which is optionally substituted by alkyl, alkoxy, halogen, nitro or CF.sub.3, or is cycloalkyl, andR.sup.2 is H, or alkyl, optionally substituted by halogen or alkoxy, or is (CH.sub.2).sub.n -phenyl, optionally substituted in the phenyl ring by alkyl, alkoxy, halogen, nitro or CF.sub.3, where n=0, 1, 2 or 3,are valuable intermediates for the preparation of L-phosphinothricin by enzymatic cleavage, and can be obtained from the corresponding N-acyl-2-amino acid nitrile by selective acid hydrolysis.
    Type: Grant
    Filed: February 2, 1990
    Date of Patent: September 24, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Lothar Willms
  • Patent number: 5045306
    Abstract: N-alkylamide of DL and L(-)-carnitine having general formula (I) ##STR1## wherein: x.sup.- is OH.sup.- or the anion of a pharmacologically acceptable acid (preferably Cl.sup.-`), andR is a straight C.sub.10 -C.sub.16 alkyl radicalare prepared via transamination by reacting DL or L(-)-carnitinamide halogenide with an amine of formula NH.sub.2 R wherein R has the above-identified meaning in an acid environment (e.g. H.sub.3 PO.sub.4) in the presence of a high-boiling solvent (e.g. ethylene glycol).N-alkylamides (I) are endowed with potent antibacterial activity and are suitable for preparing pharmaceutical and cosmetic compositions.
    Type: Grant
    Filed: November 4, 1988
    Date of Patent: September 3, 1991
    Assignee: Avantgarde S.p.A.
    Inventors: Paolo Cavazza, Giulio Fiorentini
  • Patent number: 5015773
    Abstract: An amine is produced by reacting in the presence of hydrogen at elevated temperature a first reactant which is a compound substantially involatile at the elevated temperature employed and having either one, two or more hydroxyl functions, each of which is independently either a primary or secondary hydroxyl function, with a second reactant which is either ammonia or a primary or a secondary amine in the presence of a reductive amination catalyst wherein the reaction is effected in either a continuously or periodically open system.
    Type: Grant
    Filed: August 4, 1989
    Date of Patent: May 14, 1991
    Assignee: BP Chemicals Limited
    Inventor: Ian D. Dobson