Plural Carbocyclic Rings Containing Patents (Class 546/239)
  • Patent number: 5512584
    Abstract: Compounds of the formula ##STR1## where A-B-D, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: April 30, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Liliane Unger, Hans P. Hofmann, Hans-Juergen Teschendorf, Berthold Behl, Rudolf Binder
  • Patent number: 5489599
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: February 6, 1996
    Assignee: Shell Research Limited
    Inventors: Paul A. Carter, Steven J. Tapp, Nicholas J. Daniels
  • Patent number: 5434171
    Abstract: This invention relates to a process for preparing certain 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates, intermediates, and congeners. Finally, the invention provides new 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates with formulations and methods for using the compounds.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: July 18, 1995
    Assignee: Eli Lilly and Company
    Inventors: Scott A. Frank, Douglas E. Prather, Jeffrey A. Ward, John A. Werner
  • Patent number: 5328917
    Abstract: The present invention relates to piperidine derivatives of the formula: ##STR1## wherein, R, R.sup.1, R.sup.3, X, and n are defined in the specification, pharmaceutical compositions thereof and methods of treating anoxia, traumatic injury, ischemia, migraine and epilepsy.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: July 12, 1994
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Anders Kanstrup, Jane M. Lundbeck
  • Patent number: 5317024
    Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.
    Type: Grant
    Filed: August 3, 1993
    Date of Patent: May 31, 1994
    Assignee: DuPont Merck Pharmaceutical Co.
    Inventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
  • Patent number: 5294623
    Abstract: Compounds of formula (I): ##STR1## in which: R.sup.1 and R.sup.2 are independently alkyl, alkoxy, trifluoromethyl, nitro or halogen; A is an aliphatic hydrocarbon group having from 2 to 8 carbon atoms whose chain contains at least 2 carbon atoms in a linear chain between the piperidine group and --COOH, said group optionally being unsaturated; and m and n are independently 0, 1, 2 or 3; and pharmaceutically acceptable salts and esters thereof have been found to have valuable anti-histamine properties without the usual side effects of anti-histamines. Methods of preparing the compounds are also provided.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: March 15, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Yoshio Iizuka, Takeshi Yamaguchi
  • Patent number: 5290756
    Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: March 1, 1994
    Assignee: Rohm and Haas Company
    Inventors: Colin Swithenbank, Ted Fujimoto
  • Patent number: 5281720
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Yves Girard, John W. Gillard, Laird A. Trimble, John Scheigetz, James A. Yergey, Yves Ducharme, Deborah A. Nicoll-Griffith, John H. Hutchinson
  • Patent number: 5252586
    Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: October 12, 1993
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
  • Patent number: 5246945
    Abstract: Disclosed are compounds of formula (I) ##STR1## in which A is ##STR2## The compounds are selective antagonists of 5HT at 5-HT.sub.3 receptors and useful in the treatment of psychotic disorders, neurotic diseases, gastric stasis symptoms, gastrointestinal disorders, nausea and vomiting.
    Type: Grant
    Filed: February 4, 1992
    Date of Patent: September 21, 1993
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Haruhiko Kikuchi, Hiroaki Satoh, Toshio Suguro, Koichiro Hagihara, Toru Hayakawa, Setsuko Mino
  • Patent number: 5164503
    Abstract: A process is described for the preparation of compounds of the formula ##STR1## in which W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH-- or --CH.sub.2 Ch.sub.2 --Y is a saturated heterocyclic amino group, andR.sup.2 is substituted or unsubstituted phenyl-, thienyl- or naphthyl-alkyl, or cinnamyl,and their salts and solvates.The process comprises hydrolysing a corresponding ester, amide, nitrile or ortho-ester. The starting materials are preferably prepared by reducing the corresponding cyclopentanone and hydrolysis can take place simultaneously with reduction.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: November 17, 1992
    Assignee: Glaxo Group Limited
    Inventors: Ian Waterhouse, David R. Marshall, Eric W. Collington, Christopher J. Wallis, Peter Hallett
  • Patent number: 5162537
    Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: November 10, 1992
    Assignee: Monsanto Company
    Inventors: Lawrence H Brannigan, Ronald J. Brinker, Robert J. Kaufman, Suzanne Metz
  • Patent number: 5158961
    Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meaning as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compound are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: October 27, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Jorgen Drejer
  • Patent number: 5089251
    Abstract: The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.
    Type: Grant
    Filed: January 24, 1990
    Date of Patent: February 18, 1992
    Assignee: Sanofi
    Inventors: Madeleine Mosse, Vincenzo Proietto
  • Patent number: 5063235
    Abstract: Novel compounds of the formula: ##STR1## are disclosed wherein Ar and Ar.sup.1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C.sub.1 -C.sub.12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarbonyl, or aminocarbonyl where the amino is unsubstituted or substituted by one or two groups selected from loweralkyl or aryl. The compounds of this invention are useful in the treatment of allergic disorders.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: November 5, 1991
    Assignee: A. H. Robins Company, Inc.
    Inventor: David A. Walsh
  • Patent number: 5057524
    Abstract: Novel compounds useful in the treatment of allergic disorders and having the formula: ##STR1## where Ar and Ar.sup.1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O.sup..crclbar. M.sup..sym. m,--O--loweralkyl, --O--Aryl, or NR.sup.1 R.sup.2 (R.sup.1, R.sup.2 .dbd.H, loweralkyl, aryl) are herein disclosed.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: October 15, 1991
    Assignee: A. H. Robins Company Incorporated
    Inventor: David A. Walsh
  • Patent number: 5053504
    Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.
    Type: Grant
    Filed: November 29, 1989
    Date of Patent: October 1, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
  • Patent number: 5039673
    Abstract: Compounds are described of the formula (1) ##STR1## where: R.sup.1 is a hydrogen atom or a methyl group;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, m is 2, 3 or 4 and n is 1; or X is trans --CH.dbd.CH--, m is zero and n is 3;Y is a saturated heterocyclic amino group;Alk is a C.sub.1-5 alkyl chain;l is zero or 1;p is zero, 1, 2, 3 or 4;R.sup.2 is a hydroxyl group or a group selected from --OCOR.sup.3, --CO.sub.2 R.sup.3, CONR.sup.3 R.sup.4, --SO.sub.2 NR.sup.3 R.sup.4, --NHCOR.sup.3, --NHSO.sub.2 R.sup.5, --SO.sub.2 R.sup.5, --SR.sup.5, --NR.sup.3 R.sup.4, --COR.sup.5, --NHCONR.sup.3 R.sup.4 and --NHCSNH.sub.2 ; and their physiologically acceptable salts, solvates and cyclodextrin complexes.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formulated for use as antithrombotic agents.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: August 13, 1991
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Harry Finch, Roger Hayes, Keith Mills, David F. Woodings
  • Patent number: 5036098
    Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: July 30, 1991
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Kiyoshi Kimura, Masahiro Kise, Iwao Morita
  • Patent number: 4983770
    Abstract: Substituted hydroxylamine ester stabilizers corresponding to the formula ##STR1## wherein n is 0-2, X is a direct bond, --S-- or --CH.sub.2 S--, R.sub.1 and R.sub.2 are independently hydrogen, alkyl, cycloalkyl, aralkyl, R.sub.3 and R.sub.4 are independently alkyl, cycloalkyl or aralkyl, and R.sub.5 is hydrogen or the group ##STR2## are effective in stabilizing organic materials against oxidative, thermal and actinic degradation.
    Type: Grant
    Filed: October 12, 1989
    Date of Patent: January 8, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Ramanathan Ravichandran, Stephen D. Pastor
  • Patent number: 4983614
    Abstract: The invention relates to benzhydryloxyethylpiperidine derivatives corresponding to one of the formulae below: ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different, represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an aryloxy group or the trifluoromethyl group,R represents hydrogen, a cation, an alkyl group, an aryl group or an arylalkyl group, andn is equal to 0 or 1, and their pharmaceutically acceptable salts, useful in the treatment of spasmodic states and allergies.
    Type: Grant
    Filed: December 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Les Laboratoires Meram
    Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
  • Patent number: 4977163
    Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;W is C.sub.1-7 alkylene;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;n is 1 or 2;Y is a saturated heterocyclic amino group having 5-8 ring members;R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) substituted or unsubstituted cinnamyl; and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.
    Type: Grant
    Filed: April 11, 1988
    Date of Patent: December 11, 1990
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Alan Wadsworth, Norman F. Hayes
  • Patent number: 4972009
    Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran
  • Patent number: 4950602
    Abstract: The present invention relates to inhibitors of lactate dehydrogenase that can cross the blood brain barrier and there is described herein the preparation of several analogues of nicotinamide-adenine-dinucleotide (NAD.sup.+) pyruvate adduct, of which 3(-4-(reduced 3-pyridine aldehyde-adenine dinucleotide))-pyruvate (RAP) and similar compounds appear to have a very high affinity for lactate dehydrogenase; one of which (RAP) was shown to strongly inhibit lactate production in rat brain extracts.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: August 21, 1990
    Assignee: Cornell Research Foundation, Inc.
    Inventor: Arthur J. L. Cooper
  • Patent number: 4943310
    Abstract: The invention relates to new 4-benzoyl-3-hydroxy-5-oxo-3-cyclohexenecarboxylic acid derivatives of general formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.2 and R.sup.3 have the meanings given in the description, and their use as plant growth regulants.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: July 24, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Alfred Angermann, Helga Franke, Gerhard Johann
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4933461
    Abstract: A process is described for the preparation of a compound of formula (1) ##STR1## or a salt thereof, which comprises reacting a compound of formula (2) ##STR2## (where A is a displaceable atom or group and R is a hydrogen atom or a C.sub.1-6 alkyl or C.sub.7-20 aralkyl protecting group) or a salt thereof, to replace the moiety A with a phenyl group, followed where necessary by removal of a C.sub.1-6 alkyl or C.sub.7-20 aralkyl protecting group and/or by salt formation. The replacement of A in formula (2) by a phenyl group may be effected with a compound PhX (3) wherein Ph represents a phenyl and X is an atom or group as defined for A in formula (2) or X is a metal atom or metal-containing group or a group SiR'.sub.3 (where R' is an alkyl or aryl group) provided that when A is --B(OH).sub.2 X can only represent a conventional leaving group.
    Type: Grant
    Filed: June 21, 1988
    Date of Patent: June 12, 1990
    Assignee: Glaxo Group Limited
    Inventor: Keith Mills
  • Patent number: 4918082
    Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula ##STR1## where R.sub.2 is a radical selected from the group consisting of ##STR2## where m is an integer from 0 to 3.
    Type: Grant
    Filed: September 2, 1988
    Date of Patent: April 17, 1990
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4888444
    Abstract: Substituted hydroxylamine ester stabilizers corresponding to the formula ##STR1## wherein n is 0-2, X is a direct bond, --S-- or --CH.sub.2 S--, R.sub.1 and R.sub.2 are independently hydrogen, alkyl, cycloalkyl, aralkyl, R.sub.3 and R.sub.4 are independently alkyl, cycloalkyl or aralkyl, and R.sub.5 is hydrogen or the group ##STR2## are effective in stabilizing organic materials against oxidative, thermal and actinic degradation.
    Type: Grant
    Filed: October 26, 1987
    Date of Patent: December 19, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Ramanathan Ravichandran, Stephen D. Pastor
  • Patent number: 4876279
    Abstract: Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ta J. Lee, William F. Hoffman, Clarence S. Rooney
  • Patent number: 4871748
    Abstract: Compounds of the formula: ##STR1## wherein R represents hydroxymethyl, alkoxymethyl of 2 to 6 carbon atoms, optionally substituted phenoxymethyl, alkanoyloxymethyl of 3 to 10 carbon atoms, optionally substituted benzoyloxymethyl, alkylsulphonyloxymethyl of 2 to 9 carbon atoms, optionally substituted phenylsulphonyloxymethyl, formyl, aminomethyl optionally substituted by 1 or 2 alkyl groups of 1 to 4 carbon atoms, or hydroxyiminomethyl, and acid addition salts thereof, are useful as rodenticides.
    Type: Grant
    Filed: January 23, 1985
    Date of Patent: October 3, 1989
    Assignee: May & Baker Limited
    Inventor: Leslie R. Hatton
  • Patent number: 4870083
    Abstract: The present invention relates to 1,4-disubstituted-piperidinyl compounds and their use as analgesic agents and as muscle relaxants.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: September 26, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, Thaddeus R. Nieduzak, Francis P. Miller, Stephen M. Sorensen
  • Patent number: 4845095
    Abstract: Piperidine compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, (C.sub.1-6 -alkoxyaryl)alkyl, diphenylmethozy-C.sub.1-6 -alkyl, C.sub.1-8 -alkyl, C.sub.4-10 -cycloalkylalkyl, phenoxy-C.sub.1-8 -alkyl, or C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl; andR is ##STR2## or CH.dbd.NOR' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, aryl-C.sub.0-6 -alkyl, which may optionally be substituted with one or more halogen and (.sub.1-5 -alkoxy, thienyl, or C.sub.4-7 -cycloalkylalkyl.The novel compounds are useful for the treatment of pain conditions and as neuroleptics.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: July 4, 1989
    Assignee: A/S Ferrosan
    Inventor: Frank Watjen
  • Patent number: 4835278
    Abstract: A process is described for the preparation of a compound of formula (2) ##STR1## (wherein R is a C.sub.1-6 alkyl or a C.sub.7-20 aralkyl group) and the salts thereof, which comprises reducing a compound of formula (3) ##STR2## (or a salt thereof), using a reducing system comprising borohydride ions and metal ions selected from lanthanide ions, alkaline earth metal ions or yttrium ions in solution. The reduction system may be provided by a borohydride (e.g. NaBH.sub.4) and a metal salt (e.g. CeCl.sub.3).The ester (2) may then if desired be hydrolyzed to give the parent acid.
    Type: Grant
    Filed: January 28, 1987
    Date of Patent: May 30, 1989
    Assignee: Glaxo Group Limited
    Inventors: Roger Barrett, Clive A. Meerholz, Brian D. Judkins
  • Patent number: 4797489
    Abstract: The compounds ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 9-fluorenyl or 1-fluorenyl;n is 0 or 1;m is 1, 2, 3, 4 or 5; andX is ##STR2## where R.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl, ##STR3## where R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or nitro;or pharmaceutically acceptable salts thereof are useful antidepressant and/or anxiolytic agents.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: January 10, 1989
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack, John P. Yardley
  • 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: 4760146
    Abstract: Novel compounds and processes for making and using them. The compounds include ethyl 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxylate, 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxyamide, and N,N-dimethyl-1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxam ide.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: July 26, 1988
    Assignee: Pennwalt Corporation
    Inventor: Bruce H. Toder
  • Patent number: 4736064
    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## and pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: April 5, 1988
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman
  • Patent number: 4721783
    Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;R.sub.2 is hydrogen or hydroxyl; andR.sub.
    Type: Grant
    Filed: January 9, 1986
    Date of Patent: January 26, 1988
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4721722
    Abstract: A new class of anti-spasmodic compounds having two branch chains and containing quaternary nitrogen is provided. The compounds have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are defined hereinbelow and m is an integer from 0 to 3.
    Type: Grant
    Filed: July 12, 1985
    Date of Patent: January 26, 1988
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4686309
    Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: August 11, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
  • Patent number: 4673683
    Abstract: R.sup.2 and R.sup.3 are hydrogen or alkyl,R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, unsubstituted or substituted aralkyl, COR.sup.5, CO.sub.2 R.sup.6 or CONR.sup.7 R.sup.8,R.sup.5 and R.sup.6 are alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl,R.sup.7 and R.sup.8 are hydrogen, alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl andn is 0, 1, 2 or 3,and its plant-tolerated acid addition salts, excluding the compounds where, simultaneously, R.sup.4 is hydrogen, acetyl or propionyl, n is 0 or 1 and R.sup.1, R.sup.2 and R.sup.3 are hydrogen, and fungicides containing the novel piperidines and salts.
    Type: Grant
    Filed: September 5, 1985
    Date of Patent: June 16, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Buschmann, Ludwig Schuster, Norbert Goetz, Ernst-Heinrich Pommer, Eberhard Ammermann
  • Patent number: 4652649
    Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.
    Type: Grant
    Filed: February 20, 1985
    Date of Patent: March 24, 1987
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4650874
    Abstract: The invention relates to compounds of the formula: ##STR1## which are useful cardiovascular agents.
    Type: Grant
    Filed: November 26, 1984
    Date of Patent: March 17, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Kurt J. Rorig, Chi-Dean Liang, Robert W. Hamilton
  • Patent number: 4628095
    Abstract: The invention relates to compounds of the formula: ##STR1## which are useful cardiovascular agents.
    Type: Grant
    Filed: June 5, 1985
    Date of Patent: December 9, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Kurt J. Rorig, Stevan W. Djuric, Kerry W. Fowler, Chi-Dean Liang
  • Patent number: 4613597
    Abstract: Compounds are described of the formulae (1a) and 1b) ##STR1## in which: R.sup.1 is -H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl,W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH--,Y is a saturated heterocyclic amino group having 5-8 ring members,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) cinnamyl, and Z is --CH.sub.2 OH, --CHO or --CONHR.sup.4 where R.sup.4 is --H or methyl,and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction, and may be formulated for use as antithrombotic and antiasthmatic agents.
    Type: Grant
    Filed: September 5, 1984
    Date of Patent: September 23, 1986
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes
  • Patent number: 4599419
    Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.
    Type: Grant
    Filed: July 9, 1984
    Date of Patent: July 8, 1986
    Assignee: Mitsubishi Chemical Industries, Inc.
    Inventors: Ryoji Kikumoto, Harukazu Fukami, Hiroto Hara, Kunihiro Ninomiya, Mamoru Sugano
  • Patent number: 4595759
    Abstract: The 2-aryl-1-aminoalkylcyclohexane nitrile, carboxylic acid or amide and derivatives thereof and methods of preparing same.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: June 17, 1986
    Assignee: Pennwalt Corporation
    Inventors: Thomas A. Davidson, Telfer L. Thomas
  • Patent number: 4564685
    Abstract: This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects.
    Type: Grant
    Filed: March 10, 1983
    Date of Patent: January 14, 1986
    Inventors: John W. A. Findlay, Geoffrey G. Coker
  • Patent number: RE33907
    Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: =n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;=R.sub.2 is hydrogen or hydroxyl; andR.sub.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: April 28, 1992
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis