Oxy Patents (Class 562/444)
  • Patent number: 4975444
    Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.
    Type: Grant
    Filed: August 25, 1989
    Date of Patent: December 4, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
  • Patent number: 4971987
    Abstract: The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.
    Type: Grant
    Filed: March 7, 1988
    Date of Patent: November 20, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher, Ulrich Klar
  • Patent number: 4966985
    Abstract: A carboalkylated amino alcohol having each of the below shown formulae is novel and optically active. A separating agent comprising the alcohol and a support is effectively useful to separate a variety of racemates for example with chromatography. The alcohol may be chemically or physically combined with the support. ##STR1## [wherein Ph represents a phenyl group, R represents a hydrogen atom, an alkyl group having the carbon number of 1 to 10, or an aryl group having the carbon number of 6 to 10, X represents an --0-- group or a --S-- group, and Z represents a hydrogen atom, an alkyl group having the carbon number of 1 to 10 or a metal element].
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: October 30, 1990
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Masaki Hasegawa, Kazuhiko Saigo, Yoichi Yuki, Kouzou Tachibana
  • Patent number: 4962224
    Abstract: Disclosed herein are N-naphthoylglycines and methods of their preparation. The N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: October 9, 1990
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4960792
    Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: October 2, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James
  • Patent number: 4946987
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating, diabetic complications.
    Type: Grant
    Filed: June 20, 1988
    Date of Patent: August 7, 1990
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4943591
    Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: July 24, 1990
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
  • Patent number: 4940727
    Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as anti-hypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##
    Type: Grant
    Filed: October 6, 1988
    Date of Patent: July 10, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta J. Lee, Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker
  • Patent number: 4939261
    Abstract: Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.
    Type: Grant
    Filed: September 17, 1987
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Gary M. Ksander
  • Patent number: 4925978
    Abstract: A new process of synthesis of optically active .alpha.-amino acids is described through nitrosation in a non-aqueous, aprotic system, of the corresponding N-carbamyl derivatives followed by decomposition of the thus obtained N-nitroso derivatives in aqueous acidic medium. The process, which is of a general applicability, leads to a remarkable increase in the reaction yields, due to the suppression of the main side reaction leading to the corresponding .alpha.-hydroxy-acid. Some N-nitroso intermediates, which can be recovered from the process of the invention, are also described.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: May 15, 1990
    Assignee: Eniricerche S.p.A.
    Inventors: Sandro Di Gioacchino, Antonio Paolinelli, Luciano Re
  • Patent number: 4923888
    Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 acylamino group;R.sub.1 means hydrogen or a carboxyl-protective group; andR.sub.2 represents a --(CH.sub.2).sub.n --CO.sub.2 R.sub.5 group, whereinn is 1, 2, 3 or 4; andR.sub.5 stands for hydrogen or a carboxyl-protective group; orR.sub.2 means a --(CH.sub.2).sub.n --NH.sub.2 group, whereinn is 1, 2, 3 or 4of E and/or Z configurtion as well as their salts.The compounds according to the invention show a cytoprotective effect and promote the healing of the stomach ulcer. Their toxicity is low.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: May 8, 1990
    Assignee: Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Tamas Fodor, Laaszlo Dobay, Jaanos Fischer, Bela Stefkoo, Elemeer Ezer, Judit Matuz, Katalin Saghy, Laaszlo Szporny
  • Patent number: 4914232
    Abstract: An essentially single stage reaction has been discovered in which a disubstituted ethanolamine, that is, a 2,2'-substituted-2-aminoethanol, may be reacted with a haloform and a carbonyl containing compound selected from the group consisting of monoketones and benzaldehyde, in the presence of an alkali metal hydroxide, and optionally in the presence of a phase transfer catalyst, to produce an alkali metal hydroxyethylaminoacetate ("HEAA") which has N-adjacent C atoms on which there are a total of at least three substituents (hence "polysubstituted"), and one or both pairs of substituents on each N-adjacent C atom may be cyclized. The HEAA may be cyclized by the action of a mineral acid to produce a 2-morpholone hydrochloride which is characterized by having a total of at least three substituents on the N-adjacent C atoms of the ring. The 2-morpholone so produced may be reduced to a polysubstituted aminodiol.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: April 3, 1990
    Assignee: The B. F. Goodrich Company
    Inventor: John Ta-Yuan Lai
  • 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: 4889947
    Abstract: Sunscreen compositions are described which contain certain substituted naphthalenylidenes which act as UV filters when incorporated in a carrier in amounts ranging from 0.1-50% by weight.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 26, 1989
    Assignee: ICI Americas Inc.
    Inventors: Charalambos J. Phalangas, Thomas P. Cleary
  • Patent number: 4879403
    Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: November 7, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Teetz, Rolf Geiger, Hansjorg Urbach, Reinhard Becker, Bernward Scholkens
  • 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: 4861798
    Abstract: Compounds of the formulae ##STR1## wherein n=6-11, M is hydrogen or a pharmaceutically acceptable cation, R is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by a carboxyl group and X.sub.a, X.sub.b and X.sub.c each independently represent hydrogen or a variety of substituent groups are potent inhibitors of 5-lipoxygenase.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: August 29, 1989
    Assignee: Bristol-Myers Company
    Inventors: Kenneth M. Tramposch, Fred C. Zusi, Suresh A. Marathe
  • Patent number: 4859233
    Abstract: Disclosed are herbicidal compounds of the general formula I; ##STR1## wherein A is O-alkylene of 1 to 5 carbon atoms, O-alkenylene of 3 to 6 carbon atoms in which the unsaturation is non-adjacent the oxygen atom thereof or NH-alkylene in which the alkylene is of 1 to 5 carbon atoms, and --COZR is an acid function or forms certain ester or thioester functions, and the mono- and di-salt forms thereof.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: August 22, 1989
    Assignee: Sandoz Ltd.
    Inventor: John W. Williams
  • Patent number: 4843062
    Abstract: Disclosed herein are N-acyl-N-napthoylglycines and methods of their preparation. The N-acyl-N-napthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: June 27, 1989
    Assignee: American Home Products Corporation
    Inventors: Kazimir Sestanj, Jay E. Wrobel, Joseph M. Kelly
  • Patent number: 4833268
    Abstract: DL- or L-Threo-3-(3,4-dihydroxyphenyl)-N-methyl-serine which may also be termed as DL- or L-threo-adrenalinecarboxylic acid are now provided, which are new compounds useful for therapeutic treatment of Parkinson's disease and mental depression disease.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: May 23, 1989
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Toshiharu Nagatsu, Hirotaro Narabayashi, Tomio Takeuchi, Shuichi Iwadare, Ikuo Matsumoto, Junji Yoshizawa, Hajime Morishima, Koji Tomimoto
  • Patent number: 4833169
    Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R-- (Ia), R--alk.sub.1 -- (Ib) or R'.dbd.alk.sub.2 -- (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or subsituted in the .alpha.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: May 23, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
  • Patent number: 4814485
    Abstract: The invention relates to new (4S)-4-aminobutanoic acid derivatives of general formula: ##STR1## in which: R represents an N-protective group,R.sub.1 represents hydrogen, an alkali metal atom such as lithium, sodium or potassium or a liabile group,R.sub.2 represents a group of formula: ##STR2## in which W represents hydrogen, a hydroxy group or an alkyl radical containing from 1 to 4 carbon atoms or an alkoxy radical containing from 1 to 4 carbon atoms, and to a process for the preparation of the said derivatives.The 4-aminobutanoic acid derivatives according to the invention are useful as synthesis intermediates for the preparation of peptides derived from statin analogues.
    Type: Grant
    Filed: December 2, 1986
    Date of Patent: March 21, 1989
    Assignee: Sanofi
    Inventors: Marcel Descamps, Dino Nisato, Walter Verstraeten
  • Patent number: 4783537
    Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.
    Type: Grant
    Filed: November 13, 1985
    Date of Patent: November 8, 1988
    Assignee: Pennwalt Corporation
    Inventor: Robert J. Murray
  • Patent number: 4783476
    Abstract: This invention relates to compounds presented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each), R.sup.
    Type: Grant
    Filed: December 16, 1986
    Date of Patent: November 8, 1988
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 4783480
    Abstract: A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.
    Type: Grant
    Filed: January 28, 1987
    Date of Patent: November 8, 1988
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hirohisa Wakatsuka, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 4778514
    Abstract: N-halogenophenoxyacetyl amino acid or ester thereof and salt thereof, a process for production thereof comprising acylation of amino acid or derivative thereof, a herbicidal composition comprising the compound, and a method for killing or controlling plants using the compound. The compounds have a selective herbicidal effect.
    Type: Grant
    Filed: June 6, 1986
    Date of Patent: October 18, 1988
    Assignee: Suntory Limited
    Inventors: Takaharu Tanaka, Naoki Higuchi, Masayuki Saito, Masaki Hashimoto
  • Patent number: 4769486
    Abstract: A method for racemizing an optically active amino acid, which comprises heating the optically active amino acid in an aqueous solution under an alkaline condition in the presence of an alkali metal salt.
    Type: Grant
    Filed: August 26, 1987
    Date of Patent: September 6, 1988
    Assignee: Toyo Soda Manufacturing Co., Ltd.
    Inventors: Tsuneo Harada, Kiyotaka Oyama
  • Patent number: 4755614
    Abstract: Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formulaBzx--CH.sub.2 --CO--Y (II)in whichBzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4R.sup.1 and R.sup.2 are H or such that OR.sup.1 and OR.sup.2 are hydrolyzableY is --OM or --NR.sup.3 R.sup.4M is H or is such that COOM is a salt or an esterR.sup.3 and R.sup.4 are H or a hydrocarbon radical, and one of them can be R.sup.5 --SO.sub.2 --, andR.sup.5 is a hydrocarbon radical, substiuted if appropriate. Products obtained by the process and their use as herbicides.
    Type: Grant
    Filed: March 20, 1986
    Date of Patent: July 5, 1988
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Jean-Pierre Corbet
  • Patent number: 4751324
    Abstract: Benzoyl alanines having the formula: ##STR1## in which the symbols R.sup.1 and R.sup.2 (a) both represent hydrogen or(b) both represent a straight-chain or branched chain alkyl residue having from 1 to about 6 carbon atoms, or(c) R.sup.1 represents hydrogen and R.sup.2 represents a straight-chain or branched chain alkyl residue having from 1 to about 6 carbon atoms and in which the symbol R.sup.3 represents a C(CH.sub.3).sub.m (CH.sub.2 OH).sub.3-m moiety wherein the symbol m represents an integer of from 0 to 3and alkali metal and ammonium salts thereof, are disclosed.The compounds are useful as corrosion-inhibitors for metals in aqueous systems.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: June 14, 1988
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Josef Penninger, Karl H. Schmid, Juergen Geke
  • Patent number: 4740615
    Abstract: A process for the recovery in substantially pure form of an amino acid represented by the formula ##STR1## from an aqueous production mixture by a low pressure temperature gradient chromatographic process is described.
    Type: Grant
    Filed: October 29, 1986
    Date of Patent: April 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: James W. McManus, Larry D. Forshey
  • Patent number: 4735959
    Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
    Type: Grant
    Filed: May 14, 1985
    Date of Patent: April 5, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
  • Patent number: 4729781
    Abstract: Disclosed are herbicidal compounds of the general formula I: ##STR1## wherein A is O-alkylene of 1 to 5 carbon atoms, O-alkenylene of 3 to 6 carbon atoms in which the unsaturation is non-adjacent the oxygen atom thereof or NH-alkylene in which the alkylene is of 1 to 5 carbon atoms, and --COZR is an acid function or forms certain ester or thioester functions, and the mono- and di-salt forms thereof.
    Type: Grant
    Filed: August 4, 1986
    Date of Patent: March 8, 1988
    Assignee: Sandoz Ltd.
    Inventor: John W. Williams
  • Patent number: 4724102
    Abstract: A new process for the optical resolution of racemic mixtures of .alpha.-naphthylpropionic acids of formula ##STR1## wherein R.sub.1 is (C.sub.1-6) alkyl and R.sub.2 represents hydrogen or a halogen atom comprises reacting a racemic mixture of a compound of formula II ##STR2## wherein R.sub.1 and R.sub.2 have the above seen meanings and R.sub.3 is a reactive group, with an optically active aminoacid of formula ##STR3## wherein R.sub.4 represents a (C.sub.1-8) alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or carboxy, and m is an integer from 0 to 4, to give a pair of diastereoisomeric amides of formula ##STR4## wherein R.sub.1, R.sub.2, R.sub.4 and m have the above seen meanings, and M is a hydrogen atom or a cation of an alkali metal or a cation of an organic base. Compounds IV are resolved into the single diastereoisomeric amides d,d or 1,d, or d,1 or 1,1. Acid hydrolysis gives the optically active compound I.
    Type: Grant
    Filed: March 27, 1986
    Date of Patent: February 9, 1988
    Assignee: Alfa Chemicals Italiana S.p.A.
    Inventors: Vincenzo Cannata, Giancarlo Tamerlani, Mauro Morotti
  • Patent number: 4718994
    Abstract: A method for perparing hydroxy compounds of the aromatic and heteroaromatic series of the general formula: ##STR1## wherein when R.sub.1 .dbd.--COOH, --CH.sub.2 CH(NH.sub.2)COOH then R.sub.2 .dbd.--OH, --H, --COOH; R.sub.3 .dbd.--H, --OH; R.sub.4, R.sub.5 .dbd.--H with no connecting bond; R.sub.6 .dbd.--OH; and when R.sub.1,R.sub.6,R.sub.3 .dbd.--H, R.sub.2 .dbd.--OH; then R.sub.4 .dbd.>NH; R.sub.5 .dbd.--CR.sub.7 .dbd.CHR.sub.4, where R.sub.7 .dbd.--CH.sub.2 --CH.sub.2 --NH.sub.2, --CH.sub.2 --CH(NH.sub.2)COOH, consists in that aromatic and heteroaromatic compounds of the general formula ##STR2## wherein when R.sub.1 .dbd.--COOH, --CH.sub.2 CH(NH.sub.2)COOH, then R.sub.2 .dbd.--OH, --H, --COOH; R.sub.3 .dbd.--H, --OH; R.sub.4,R.sub.5 .dbd.--H with no connecting bond; and when R.sub.1,R.sub.2,R.sub.3 .dbd.--H, then R.sub.4 .dbd.>NH; R.sub.5 .dbd.--CR.sub.7 .dbd.CHR.sub.4, where R.sub.7 .dbd.--CH.sub.2 --CH.sub.2 --NH.sub.2, --CH.sub.2 --CH(NH.sub.2)COOH.
    Type: Grant
    Filed: June 14, 1985
    Date of Patent: January 12, 1988
    Assignee: Latviisky Gosudarstvenny Universaitet Imeni P. Stuchki
    Inventors: Andrei K. Zhagars, Voldemar Y. Grinshtein, Sniedzite A. Ozola, Andris K. Zitsmanis, Avgust K. Arens
  • Patent number: 4717736
    Abstract: Compounds having the formula: ##STR1##are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents and cytoprotective agents.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: January 5, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joshua Rokach, Robert N. Young
  • Patent number: 4701210
    Abstract: N-substituted glutamic acid derivative and salt thereof, a process for production thereof comprising acylation of glutanic acid or derivative thereof, a herbicidal composition comprising the compound, and a method for killing or controlling plants using the compound. The compounds have a selective herbicidal effect.
    Type: Grant
    Filed: June 17, 1986
    Date of Patent: October 20, 1987
    Assignee: Suntory Limited
    Inventors: Takaharu Tanaka, Naoki Higuchi, Masayuki Saito, Masaki Hashimoto
  • Patent number: 4699926
    Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein R=H or lower alkyl;R'=H, lower alkyl, benzyl, CH.sub.2 OH;A=(CH.sub.2).sub.1 to 5, >C(CH.sub.3).sub.2, >C (CH.sub.2).sub.3 ; andX=0 or 1.The present invention is also directed to a method of treating a person for sickle cell anemia comprising administering to the person a therapeutically effective dosage of the above compounds.In addition the invention includes the novel compound: ##STR2## which is inaccessible by synthetic procedures previously described for this general class of compounds.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: October 13, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Donald J. Abraham, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Patent number: 4692512
    Abstract: alpha-L-Aspartyl-D-phenylglycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: September 8, 1987
    Assignee: The Procter & Gamble Company
    Inventor: John M. Janusz
  • Patent number: 4684639
    Abstract: A compound having the partial structure (I) ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a group --COR.sup.5 or --CO--OR.sup.5 wherein R.sup.5 represents an optionally substituted hydrocarbon group; R.sup.3 is halogen and R.sup.4 is hydrogen, methoxy, hydroxymethyl or formamido.These compounds are suitably bicyclic .beta.-lactam antibiotics.
    Type: Grant
    Filed: July 5, 1984
    Date of Patent: August 4, 1987
    Assignee: Beecham Group
    Inventors: George Burton, Desmond J. Best
  • Patent number: 4683330
    Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: July 28, 1987
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4678806
    Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: September 2, 1986
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
  • Patent number: 4677126
    Abstract: Oxa-fenchyl esters and amides of alpha-L-aspartyl-D-phenylglycine are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.
    Type: Grant
    Filed: September 19, 1986
    Date of Patent: June 30, 1987
    Assignee: The Procter & Gamble Company
    Inventors: John M. Janusz, John M. Gardlik
  • Patent number: 4673690
    Abstract: The acylated enamide compounds are acylated enamides corresponding to the general formula ##STR1## in which Z represents an electron donor group,n is 1, 2 or 3, andR.sup.1 represents hydrogen, a halogen or any organic group,or salts, complexes, alkylated derivatives or acylated derivatives of these compounds.Typical acylated enamide compounds according to the invention correspond to the formula ##STR2## These acylated enamide compounds and the pharmaceutical compositions containing the compounds are useful in the prevention and treatment of cancers.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: June 16, 1987
    Assignee: Biotec
    Inventors: Marcel B. Roberfroid, Heinz G. Viehe, Francoise M. Hervens
  • Patent number: 4668814
    Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: May 26, 1987
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4668703
    Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.
    Type: Grant
    Filed: July 1, 1985
    Date of Patent: May 26, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
  • Patent number: 4668727
    Abstract: Ester substituted benzylhydroxylamine derivatives are effective in stabilizing polyolefin compositions containing a stabilizer or mixture of stabilizers selected from the group consisting of the phenolic antioxidants, the hindered amine light stabilizers, the alkylated hydroxybenzoate light stabilizers, the ultraviolet light absorbers, the organic phosphorus compounds, the alkaline metal salts of fatty acids and the thiosynergists, against degradation upon high temperature extrusion, exposure to the combustion products of natural gas, gamma irradiation or upon storage for extended periods. These ester substituted benzylhydroxylamine derivatives exhibit resistance to loss or extraction during processing and in end-use applications.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: May 26, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Ramanathan Ravichandran, Thomas E. Snead
  • Patent number: 4666963
    Abstract: Substituted aminoxy succinate derivatives of the formula ##STR1## are effective in stabilizing organic materials against oxidative, thermal and actinic degradation, said derivatives being particularly effective as color improvers and process stabilizers in organic materials containing phenolic antioxidants and/or metal salts of fatty acids and/or hindered amine light stabilizers and/or organic phosphorus compounds.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: May 19, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Ramanathan Ravichandran, Thomas E. Snead
  • 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: 4661515
    Abstract: Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which 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, and cycloalkyl, and may be the same or different; 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-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: April 28, 1987
    Assignee: USV Pharmaceutical Corporation
    Inventors: Edward S. Neiss, John T. Suh, John J. Piwinski
  • Patent number: 4652635
    Abstract: A method for converting ether groups such as alkyl or aryl ether groups including hydroquinone ether groups to hydroxyl groups and ester groups such as alkyl or aryl ester groups to carboxylic acid groups which comprises reacting a compound including at least one ether and/or ester group with a 2-halo-1,3,2-benzodioxaborole to form an intermediate and hydrolyzing the intermediate such as by quenching it into water to form the desired final product.
    Type: Grant
    Filed: June 15, 1984
    Date of Patent: March 24, 1987
    Assignee: Polaroid Corporation
    Inventor: Patrick F. King