The Compound Is Acyclic Patents (Class 564/197)
  • Patent number: 5010108
    Abstract: New N-(2-cycloalkylamino)ethyl-substituted benzamides having a powerful stimulating activity on gastric motility and with a low central anti-dopaminergic activity are described. The synthesis and the pharmaceutical preparation for therapeutical use are also described.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: April 23, 1991
    Assignee: Poli Industria Chimica S.p.A.
    Inventors: Stefano Poli, Germano Coppi, Lucio Del Corona
  • Patent number: 4981987
    Abstract: An adhesion-improver which comprises a reaction product of an amino compound having a primary and/or secondary amino group in the molecule or a modified amino compound obtained by modifying the amino compound with a compound having an epoxy group, and a carbonyl compound, particularly a dicarbonyl compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each an alkyl having 1 to 16 carbon atoms, an aryl having 6 to 12 carbon atoms or an alkoxy having 1 to 4 carbon atoms, R.sup.3 is a hydrocarbon group having one or more carbon atoms, and n is 0 or 1, which is useful for improving adhesion of curable compositions such as adhesives, sealing agents, paints and pourable compounds, and a curable composition comprising a conventional main component and the adhesion-improver as set forth above which has excellent adhesion and curing characteristics.
    Type: Grant
    Filed: March 5, 1986
    Date of Patent: January 1, 1991
    Assignee: Sunstar Giken Kabushiki Kaisha
    Inventors: Masaru Sugimori, Tadao Kunishige, Koichiro Sanji
  • Patent number: 4939266
    Abstract: Nitrosamine-free 3-isothiazolone biocidal compositions suitable for applications where substantial human or animal contact is anticipated, their method of use and process of preparation are disclosed.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: July 3, 1990
    Assignee: Rohm and Haas Company
    Inventors: Horst O. Bayer, Barry C. Lange, Ramesh B. Petigara
  • Patent number: 4931591
    Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: June 5, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Buhlmayer, Vittorio Rasetti, Walter Fuhrer, James L. Stanton, Richard Goschl
  • Patent number: 4906659
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: March 6, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Setsuo Harada, Hideo Ono, Hirotomo Masuya, Hideaki Natsugari
  • Patent number: 4898977
    Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.
    Type: Grant
    Filed: August 13, 1987
    Date of Patent: February 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Herold, Christof Angst
  • Patent number: 4876343
    Abstract: An improved process for the preparation of statine, the phenyl analog of statine, the cyclohexyl analog of statine and derivatives thereof is described, as well as other valuable intermediates used in the process.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: October 24, 1989
    Assignee: Warner-Lambert Company
    Inventors: John C. Hodges, Sylvester Klutchko
  • Patent number: 4871773
    Abstract: N-alkylamide of D(+)-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 D(+)-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: January 11, 1989
    Date of Patent: October 3, 1989
    Assignee: Avantgarde S.p.A.
    Inventors: Paolo Cavazza, Giulio Fiorentini
  • Patent number: 4863926
    Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: September 5, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
  • Patent number: 4827004
    Abstract: Novel Isoprene Derivatives which have mucosa-protective and gastric acid secretion-inhibiting properties and are useful for combatting ulcers both by treating and as a prophylaxis against gastric and/or duodenal ulcers.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Albert Fischli, Max Schmid, Rudolf Schmid
  • Patent number: 4824996
    Abstract: There are disclosed compounds of the formulaR.sup.1 -XwhereinR.sup.1 is alkyl of 8-22 carbon atoms;X is ##STR1## R.sup.2 is --(CH.sub.2).sub.n NR.sup.4 R.sup.5 ; R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or lower alkyl;R.sup.5 is hydrogen or lower alkyl; andn is 0-7, with the proviso that when X is ##STR2## n is 6-7; and their use in the prevention and/or treatment of conditions such as allergic rhinitis, allergic bronchial asthma and other naso-bronchial obstructive air-passageway conditions, other immediate hypersensitivity reactions such as allergic conjunctivitis and various inflammatory conditions.
    Type: Grant
    Filed: November 6, 1986
    Date of Patent: April 25, 1989
    Assignee: American Home Products Corporation
    Inventors: William H. McGregor, Joseph Y. Chang
  • Patent number: 4814505
    Abstract: N-Vinylformamide is purified by fractional distillation in the presence of formamide in a column under from 0.5 to 30 mbar by a method in which the distillation is controlled so that N-vinylformamide containing from 0.1 to 15% by weight of formamide is obtained as the distillate. Homopolymers having particularly high molecular weights can be prepared from the N-vinylformamide purified in this manner.
    Type: Grant
    Filed: January 29, 1987
    Date of Patent: March 21, 1989
    Assignee: Basf Aktiengesellschaft
    Inventors: Michael Kroener, Willi Schmidt, Alfred Oftring, Theo Proll, Heinrich Hartmann
  • Patent number: 4812263
    Abstract: Described are bis-quaternary ammonium compounds of 2-hydroxypropylene, e.g., 2-hydroxy propylene-1,3-bis(dimethyl stearyl ammonium chloride).
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: March 14, 1989
    Assignee: PPG Industries, Inc.
    Inventor: Robert B. Login
  • Patent number: 4804782
    Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.
    Type: Grant
    Filed: November 8, 1985
    Date of Patent: February 14, 1989
    Assignee: Pfizer, Inc.
    Inventors: Thomas M. Brennan, Michael E. Hendrick
  • Patent number: 4778804
    Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.
    Type: Grant
    Filed: October 11, 1985
    Date of Patent: October 18, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
  • Patent number: 4767768
    Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.
    Type: Grant
    Filed: December 8, 1983
    Date of Patent: August 30, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
  • Patent number: 4764306
    Abstract: A method of preparing certain bis-quaternary ammonium compounds and mixtures is disclosed. The method involves contacting a tertiary amine with a suitable amount of neutralizing acid, e.g. HCl, and subsequently contacting the resulting mixture with a suitable epoxide, e.g. epichlorohydrin, at an elevated temperature and in an amount that e.g. 2-hydroypropylene-bis-1,3-(dimethyl stearyl ammonium chloride) is obtained in almost stoichiometric yields. The resulting bis-quaternary ammonium compounds can be incorporated into a hair conditioner whereby a softer feel and better control of hair is obtained.The general structure for the resulting bis-quaternary ammonium compounds is as follows: ##STR1## wherein the R's are selected from the group consisting of alkyl, alkylamidoalkyl, aryalkyl, aryl, alkoxy, alkenyl, hydroxyalkyl, and carboxyalkyl and X is a negative radical from the epoxide used, e.g. epichlorohydrin.
    Type: Grant
    Filed: August 22, 1986
    Date of Patent: August 16, 1988
    Assignee: PPG Industries, Inc.
    Inventor: Robert B. Login
  • Patent number: 4760179
    Abstract: Substituted aminoxy propionamide derivatives corrsponding to the formula ##STR1## said derivatives being useful as color improvers and stabilizers in various polymeric substrates.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: July 26, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Ramanathan Ravichandran
  • Patent number: 4743595
    Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.
    Type: Grant
    Filed: June 12, 1985
    Date of Patent: May 10, 1988
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
  • Patent number: 4739059
    Abstract: A novel amine amide of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are useful as thickening agents, disoxidation catalysts and monomers.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: April 19, 1988
    Assignee: Daikin Industries Ltd.
    Inventors: Yohnosuke Ohsaka, Yoshio Amimoto, Yoshio Negishi
  • Patent number: 4736055
    Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 5, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
  • Patent number: 4730075
    Abstract: A process for the production of (1) an ether or (2) a second amine comprises reacting an activated olefin with respectively an alcohol or first amine in the presence of a catalyst which is either (a) an amidine or (b) a Lewis base and epoxide. The same catalyst may also be used to carry out the reverse reaction in which an activated olefin and an alcohol or first amine are produced from the appropriate ether or second amine.
    Type: Grant
    Filed: June 20, 1986
    Date of Patent: March 8, 1988
    Assignee: BP Chemicals Limited
    Inventor: Michael J. Green
  • Patent number: 4719288
    Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
    Type: Grant
    Filed: June 2, 1986
    Date of Patent: January 12, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fuhrer, Peter Buhlmayer, Vittorio Rasetti, Bernhard Riniker
  • Patent number: 4713470
    Abstract: There is disclosed a process for the racemization of amino acids and derivatives thereof. The racemization process of the present invention uses an aromatic aldehyde-containing polymer made from the reaction of a hydroxy-aromatic aldehyde with a chloromethylated vinylbenzene polymer under reaction conditions to form an aromatic aldehyde-containing polymer wherein the aldehydic moiety is linked to the polymer through an ether linkage. There is also disclosed a process for the production of the racemization catalyst. Another embodiment of the invention comprises a process for the promotion of the racemization reaction wherein a tertiary amine-containing resin is used as a promoting agent.
    Type: Grant
    Filed: May 22, 1985
    Date of Patent: December 15, 1987
    Assignee: Stauffer Chemical Company
    Inventor: Stanley B. Mirviss
  • Patent number: 4661510
    Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: April 28, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Arlindo L. Castelhano
  • 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: 4649218
    Abstract: The present inveniton relates to novel lithium ionophores, to a process for producing such lithium ionophores and to their uses as pharmaceutical compositions, electrodes and as components of batteries.
    Type: Grant
    Filed: January 14, 1981
    Date of Patent: March 10, 1987
    Assignee: Yeda Research and Development Company Ltd.
    Inventors: Abraham Shanzer, David Samuel
  • Patent number: 4639468
    Abstract: A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.
    Type: Grant
    Filed: August 23, 1985
    Date of Patent: January 27, 1987
    Assignee: Continental Pharma Inc.
    Inventors: Romeo Roncucci, Claude L. Gillet, Alexis H. Cordi, Mark A. Martens, Joseph L. Roba, Paul J. Niebes, Georges E. Lambelin, William R. Van Dorsser
  • Patent number: 4619944
    Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.
    Type: Grant
    Filed: February 19, 1985
    Date of Patent: October 28, 1986
    Assignee: USV Pharmaceutical Corporation
    Inventors: Raymond D. Youssefyeh, Howard Jones
  • Patent number: 4600794
    Abstract: Gamma dimethylamino L-beta hydroxy butyric acid (L-norcarnitine) is prepared by reacting gamma-iodo beta hydroxy butyric acid octyl ester with dimethylamine in a lower alkanol, e.g. ethanol, thereby obtaining a mixture of the hydroiodides of the gamma-dimethylamino L-beta hydroxy butyric acid ethyl ester and dimethylamide (in a molar ratio of about 60:40). The mixture is eluted on a weakly basic ion exchange resin activated in the OH.sup.- form in order to remove the iodide ions. Upon subsequent alkaline hydrolysis the desired compound is obtained.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: July 15, 1986
    Assignee: Sigma Tau Industrie Farmaceutiche Riunite S.P.A.
    Inventor: Maria O. Tinti
  • Patent number: 4560795
    Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; 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 ##STR3## 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.
    Type: Grant
    Filed: February 6, 1984
    Date of Patent: December 24, 1985
    Assignee: Merrell Dow France et Cie.
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4517379
    Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is CH.sub.2 OH or CH.sub.2 OCH.sub.3 ; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, F.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.
    Type: Grant
    Filed: April 1, 1983
    Date of Patent: May 14, 1985
    Assignee: Pfizer Inc.
    Inventors: Thomas M. Brennan, Michael E. Hendrick
  • Patent number: 4500662
    Abstract: Polysubstituted .alpha.-aminoacetamides of the formula ##STR1## wherein R.sup.1 is tert-alkyl; R.sup.4 is alkyl, phenyl, substituted phenyl, cycloalkyl, piperidinyl, tetraalkylpiperidinyl or an alkylene (.alpha.-aminoacetamide). These compounds are prepared by first reacting an .alpha.-haloacetamide with a base to form an .alpha.-lactam intermediate which in turn is reacted with a primary amine. The compounds are useful as stabilizers of polymeric materials against ultraviolet light degradation.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: February 19, 1985
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4473694
    Abstract: Process for the synthesis of hindered polysubstituted .alpha.-amino acetamides which comprises first reacting an .alpha.-haloacetamide with a base to form an intermediate .alpha.-lactam which in turn is reacted with a primary or secondary amine. The product thus obtained can comprise a multifunctional compound having one or more hindered amino moieties. These compounds are highly effective as UV stabilizers in a variety of plastics, especially the alpha monoolefins.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: September 25, 1984
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4466915
    Abstract: A known base-induced catalytic ketoform synthesis can now be carried out without sacrificing the directivity of the prior art process, but non-catalytically, that is, in the absence of the phase transfer catalyst heretofore required, provided the ketone/araldehyde is present in large excess from about 2 to about 25 times the calculated molar amount necessary to yield the reaction product. This synthesis obviates the problems of separating and recovering a phase transfer catalyst used in the prior art process.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: August 21, 1984
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4443627
    Abstract: Process for the production of carnitine amide in the form of a chloride. The carnitine ethyl ester is obtained by reaction of 4-chloroacetoacetic acid ethyl ester with trimethyl amine and the subsequent hydrogenation is carried out with the help of a Pt/C catalyst. Such carnitine ethyl ester, without isolating it, is reacted with ammonia in an autoclave at -30.degree. to +10.degree. C. Everything is heated to 40.degree. to 80.degree. C. The mixture is stirred at such temperature at an ammoniac pressure of 8 to 24 atu. The product is filtered after cooling it to ambient temperature and counterbalancing the excess pressure. The product is then washed with alcohol and subsequently dried at 30.degree. to 50.degree. C. and at a pressure of 15 to 25 torr.
    Type: Grant
    Filed: January 20, 1982
    Date of Patent: April 17, 1984
    Assignee: Lonza Ltd.
    Inventors: Leander Tenud, Rene Blum
  • Patent number: 4440788
    Abstract: This invention relates to S-alkylcysteines and processes for preparing same. The compounds according to this invention are expected to be applicable as therapeutic agents for hepatic failures.
    Type: Grant
    Filed: December 30, 1981
    Date of Patent: April 3, 1984
    Assignee: Mitsubishi Chemical Industries, Limited
    Inventors: Hiroshi Terayama, Yoshiharu Morita, Kohei Umezu
  • Patent number: 4439619
    Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: March 27, 1984
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Fritz Gerhart, Michel Jung
  • Patent number: 4418077
    Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: November 29, 1983
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Fritz Gerhart, Michel Jung, Daniel Schirlin
  • Patent number: 4394305
    Abstract: Compounds which are carboxylic acids, or their salt, ester or amide derivatives, having an oxyalkylene amine oxide substituent at the alpha-carbon atom are disclosed. The compounds are useful as detergent surfactants which provide outstanding cleaning, particularly of oily soils, under cold water laundering conditions. Detergent compositions containing the compounds also preferably contain other surfactants, builders, and detergent adjunct materials.
    Type: Grant
    Filed: March 17, 1981
    Date of Patent: July 19, 1983
    Assignee: The Procter & Gamble Company
    Inventor: Eugene P. Gosselink
  • Patent number: 4375477
    Abstract: Beta-monofluoromethyl beta-alanine, beta-difluoromethyl beta-alanine and pharmaceutically acceptable esters and amides derived from the acid group, amides derived from the amine group, and salts thereof are novel compounds which inhibit .gamma.-aminobutyric acid transaminase (GABA-T).
    Type: Grant
    Filed: July 21, 1980
    Date of Patent: March 1, 1983
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michael Jung, Fritz Gerhart
  • Patent number: 4370497
    Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.
    Type: Grant
    Filed: August 7, 1980
    Date of Patent: January 25, 1983
    Inventors: Derek H. R. Barton, Steven V. Ley, Clive A. Meerholz
  • Patent number: 4362877
    Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
    Type: Grant
    Filed: April 21, 1980
    Date of Patent: December 7, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Dybas, Bruce E. Witzel, Nathaniel Grier
  • Patent number: 4348536
    Abstract: The instant invention is directed to novel compounds and the use thereof in producing polyurethane resins. The compounds generally correspond to the following formula: ##STR1## wherein n is an integer of from 1 to 5,R is a C.sub.1 -C.sub.5 alkyl groupY is a C.sub.1 -C.sub.5 alkyl group or a ##STR2## and Z is a ##STR3## where n=0 or 1, X is --O-- or ##STR4## and R' is an aliphatic group having from 1 to 15 carbon atoms and may contain ester, ether, or amide groups or tertiary nitrogen and, when m=0, R' may be a hydrogen atom.
    Type: Grant
    Filed: February 6, 1978
    Date of Patent: September 7, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes Blahak, Hans Hubner, Johannes Koster, Hans J. Meiners, Heinz Thomas
  • Patent number: 4326071
    Abstract: Novel compounds of the following general formula are useful pharmacological agents: ##STR1## wherein Y is FCH.sub.2 - or F.sub.2 CH-; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, -NR.sub.10 R.sub.11 wherein each of R.sub.10 and R.sub.11 is hydrogen or a straight or branched alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.12 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 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 ##STR3## wherein R.sub.8 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and n is the integer 2 or 3; pharmaceutically acceptable salts and individual optical isomers thereof.
    Type: Grant
    Filed: September 28, 1977
    Date of Patent: April 20, 1982
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michel Jung
  • Patent number: 4323704
    Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R 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 straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## 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 ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.
    Type: Grant
    Filed: January 16, 1981
    Date of Patent: April 6, 1982
    Assignee: Merrell Toraude et Compagnie
    Inventors: Brian W. Metcalf, Michel Jung, Charles Danzin
  • Patent number: 4311858
    Abstract: The disclosure herein relates to a new process for the preparation of N-(halomethyl) acylamides by reacting the corresponding N-(alkoxymethyl) acetamide with a hydrogen halide.
    Type: Grant
    Filed: December 1, 1980
    Date of Patent: January 19, 1982
    Assignee: Monsanto Company
    Inventor: John P. Chupp
  • Patent number: 4310472
    Abstract: This invention relates to adducts of salts of polymerizable tertiary amines with acrylic compounds illustrated by acrylamide and acrylonitrile; to polymers and copolymers containing said adducts and to processes for preparing them. This invention also relates to the use of said polymers and copolymers, particularly in the clarification of turbid waters by flocculation or flotation of oil and/or suspended solids. In the preferred embodiment, the quaternary adduct monomer is: ##STR1## where X is an anion, preferably halide such as chloride or carboxylate such as acetate; and polymers and copolymers containing units thereof.
    Type: Grant
    Filed: March 24, 1980
    Date of Patent: January 12, 1982
    Assignee: Petrolite Corporation
    Inventors: Rudolf S. Buriks, Allen R. Fauke, David W. Griffiths
  • Patent number: 4310429
    Abstract: Novel .alpha.-aminoacetamides are powerful stabilizers for organic materials subject to oxygen and heat degradation, and particularly for synthetic natural rubber and synthetic ester lubricants. A wide range of substituents on the amine and amide N atoms, and also on the saturated carbon atom, yields an array of stabilizers having a wide range of compatibility in compositions comprising various synthetic resinous compounds to be stabilized.Novel syntheses are provided utilizing at least one amine nucleophilic agent, a dichlorocarbene ion generating agent, and an alkoxide ion generating agent, which together in the presence of aqueous alkali and an onium salt, yield novel .alpha.-aminoacetamides in which a wide choice of substituents may be introduced. The nucleophilic agent may be a primary or secondary amine, or one of each. The dichlorocarbene ion generating agent is a haloform. The alkoxide ion generating agent may be a ketone, an aldehyde, or a cyanohydrin which reacts with the haloform. An .alpha.
    Type: Grant
    Filed: June 19, 1978
    Date of Patent: January 12, 1982
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4306080
    Abstract: A novel process for the purification of industrial effluents, wherein the effluents are brought into contact with cationically modified, cellulose-containing materials, the cationic constituent of which is bonded to the cellulose part via the grouping of the general formula--O--CH.sub.2 --N<in which the nitrogen belongs to an amide group of the cationic constituent and the oxygen is bonded to the cellulose part.
    Type: Grant
    Filed: February 9, 1979
    Date of Patent: December 15, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Haase, Peter Liechti, Hans Wegmuller, Rudolf F. Wurster, Quentin Bowes