The Polycyclo Ring System Is Bicyclo-carbocyclic Patents (Class 546/205)
  • Patent number: 5015678
    Abstract: The Michael addition products of N-hydroxy hindered amines with alpha,beta-unsaturated carbonyl compounds including derivatives of esters, amids, imides and anhydrides are effective stabilizers for protecting organic polymers from the deleterious effects of actinic light.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: May 14, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Raymond Seltzer, James P. Galbo, Ramanathan Ravichandran
  • Patent number: 5000777
    Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.
    Type: Grant
    Filed: November 21, 1989
    Date of Patent: March 19, 1991
    Assignees: Ciba-Geigy Corporation, Janssen Pharmaceutica
    Inventors: Henry Szczepanski, Lourens Wals
  • Patent number: 4999352
    Abstract: 1-(1-Aryl-2-hydroxyethyl)-imidazoles and salts thereof, processes for the preparation thereof, medicaments containing these compounds, and the use thereof.The invention relates to 1-(1-aryl-2-hydroxyethyl)-imidazoles of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, Q, W, X and Y have the meanings specified, and also to medicaments based on these compounds, in particular those having an antimycotic and an antidepressive action.
    Type: Grant
    Filed: November 28, 1989
    Date of Patent: March 12, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus-Dieter Kampe, Patricia Usinger, Herbert Siegel, Hans G. Alpermann, Hermann J. Gerhards
  • Patent number: 4996215
    Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: February 26, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
  • Patent number: 4980477
    Abstract: Sterically hindered amino compounds definable by the general formula (I): ##STR1## where R represents a hydrogen atom, a C.sub.1 -C.sub.18 alkyl radical or a C.sub.7 -C.sub.18 alkaryl radical, are useful as organic polymer stabilizers. Processes for preparing these compounds are described.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: December 25, 1990
    Assignees: Eniricerche SpA, Enichem Synthesis SpA
    Inventors: Arnaldo Roggero, Guglielmo Bertolini
  • Patent number: 4976889
    Abstract: 4-Formylaminopiperidine derivatives of the formula (I) ##STR1## where n is 1 or 2, R.sup.1 to R.sup.4 are each alkyl or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 are tetra- or pentamethylene, R.sup.5 is hydrogen or alkyl, R.sup.6 is hydrogen, unsubstituted or substituted alkyl, alkenyl, aralkyl or acyl, and, when n is 1, Y is hydrogen, unsubstituted or substituted alkyl, alkenyl, cycloalkyl, bicycloalkyl, aralkyl, aryl, alkyl containing heterocyclic radicals, or ##STR2## or, when n is 2, Y is alkylene, cycloalkylene, aralkylene or arylene or is alkylene which is interrupted by oxygen, nitrogen, sulfur or a 5-membered or 6-membered heterocyclic structure, and their acid addition salts have very good stabilizing properties in plastics.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: December 11, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
  • Patent number: 4970022
    Abstract: Mustard oils of the formula IR--(A.sup.1 --Z.sup.1).sub.n --A.sup.2 --Z.sup.2 --A.sup.3 --NCSin which A.sup.1, A.sup.2, A.sup.3, R, Z.sup.1, Z.sup.2 and n have the meaning specified in claim 1 can be used as components of liquid-crystalline phases.
    Type: Grant
    Filed: August 19, 1987
    Date of Patent: November 13, 1990
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4968677
    Abstract: 1-Aryl-2-naphthoylamines of formula I are described ##STR1## wherein R.sub.1 is halogen, nitro, cyano, C.sub.1 -C.sub.6 alkyl that is unsubstituted or mono- or poly-substituted by halogen and/or C.sub.1 -C.sub.3 alkoxy, or is C.sub.3 -C.sub.6 cycloalkyl, OR.sub.4, NR.sub.5 R.sub.6, CO2R.sub.5, CONR.sub.5 R.sub.6 or NHCOR.sub.7, or wherein two adjacent positions in the nucleus are bridged by a methylenedioxy or ethylenedioxy group that is unsubstituted or mono- or poly-substituted by fluorine, wherein further R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl that is unsubstituted or substituted by C.sub.1 -C.sub.3 alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.4 alkenyl, 2-propynyl, 3-halo-2-propynyl, ##STR2## or COR.sub.7, each of R.sub.5 and R.sub.6, independently of the other, is H or C.sub.1 -C.sub.4 alkyl, R.sub.7 is C.sub.1 -C.sub.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: November 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Riebli
  • Patent number: 4960890
    Abstract: Methine dyes (I) which conform in one of their tautomeric forms to the general formula ##STR1## where Y.sup.1 is in both or either case an electron-attracting group and the other Y.sup.1 is hydrogen,Y.sup.2 is in each case, independently of the others, hydrogen, --CN, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl, pyridyl or together with a further Y.sup.2 a five- or six-membered ring which may have a fused-on benzene ring,R is hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.7 -C.sub.10 -aralkyl or .beta.
    Type: Grant
    Filed: October 5, 1989
    Date of Patent: October 2, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Ewald Daltrozzo, Werner Sulger
  • Patent number: 4942261
    Abstract: An allyl type amine is prepared by reacting an allyl type alcohol represented by the following formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently stand for a hydrogen atom, an aliphatic hydrocarbon group or alicyclic hydrocarbon having 1 to 8 carbon atoms, or an aromatic hydrocarbon group,with at least one member selected from the group consisting of ammonia, a primary amine and a secondary amine in the presence of a palladium compound and a multidentate phosphorus compound.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: July 17, 1990
    Assignee: Showa Denko Kabushiki Kaisha
    Inventors: Yoshimasa Ishimura, Takami Oe, Yuseki Suyama, Nobuyuki Nagato
  • Patent number: 4940696
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: July 10, 1990
    Assignee: Centre International de Recherches Dermatologioues (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 4939160
    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'=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 substituted in the .alpha.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
  • 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: 4921863
    Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.
    Type: Grant
    Filed: February 17, 1988
    Date of Patent: May 1, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
  • Patent number: 4914227
    Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.
    Type: Grant
    Filed: May 16, 1986
    Date of Patent: April 3, 1990
    Assignee: Banyu Pharmaceutical Company, Ltd.
    Inventors: Tetsuji Miyano, Kunio Suzuki, Ryosuke Ushijima, Susumu Nakagawa
  • Patent number: 4909830
    Abstract: Herbicidal 3-aminopyrazolin-5-ones of the formula ##STR1## in which R.sup.1 stands for alkyl, alkenyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, for optionally substituted aralkyl or for optionally substituted aryl,R.sup.2 stands for hydrogen or alkyl,R.sup.3 stands for hydrogen or alkyl,R.sup.4 stands for hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonylalkyl or alkanoyl, orR.sup.3 and R.sup.4 together stand for an alkylene or alkenylene radical, each of which is divalent,X stands for halogen, alkyl, alkoxy, alkylthio, halogenoalkyl. halogenoalkoxy or halogenoalkylthio, andZ stands for hydrogen, halogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,and acid addition salts thereof. Intermediates of the formula ##STR2## are also disclosed.
    Type: Grant
    Filed: November 10, 1988
    Date of Patent: March 20, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uta Jensen-Korte, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 4898607
    Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: February 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Henry Szczepanski, Lourens Wals
  • Patent number: 4897397
    Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: January 30, 1990
    Assignee: Schering Corporation
    Inventors: Neng Y. Shih, David J. Blythin
  • Patent number: 4895834
    Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension, hyperaldosternoism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
    Type: Grant
    Filed: November 2, 1987
    Date of Patent: January 23, 1990
    Assignee: Warner-Lambert Company
    Inventors: James P. Hudspeth, James S. Kaltenbronn, Joseph T. Repine, William H. Roark, Michael A. Stier
  • Patent number: 4889849
    Abstract: The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.
    Type: Grant
    Filed: January 9, 1989
    Date of Patent: December 26, 1989
    Assignee: Duphar International Research B.V.
    Inventors: Ineke Van Wijngaarden, Johannes M. A. Zwagemakers, Jan Van Dijk
  • Patent number: 4888433
    Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.
    Type: Grant
    Filed: August 5, 1987
    Date of Patent: December 19, 1989
    Assignee: Zambon, S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4888355
    Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: December 19, 1989
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret, Michel Fortin, Francoise Delevallee
  • Patent number: 4879284
    Abstract: The invention relates to a compound of formula: ##STR1## in which formula: R.sub.1 to R.sub.4 denote, independently, H, OH, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; andA denotes --COR.sub.5, R.sub.5 being H when at least one of the substituents R.sub.1 to R.sub.4 is other than H; C.sub.1 -C.sub.6 alkyl; amino; (C.sub.1 -C.sub.6)alkylamino; di(C.sub.1 -C.sub.6) alkylamino; arylamino; benzylamino; amino drived from a cyclic or heterocyclic amine; (--COR.sub.5 being able, when it is an amide group, to be the amide group of an amino acid or of a glucosamine); or alternatively R.sub.5 denotes --OR.sub.6, R.sub.6 being H or (C.sub.1 -C.sub.6)alkyl; C.sub.1 -C.sub.6 mono- or polyhydroxyalkyl, or aryl or benzyl, both optionally substituted; --OR.sub.6 also being able to be derived from a sugar; and the salts and isomers of this compound. The invention also relates to a process for preparing this compound and medicinal and cosmetic compositions containing them.
    Type: Grant
    Filed: December 5, 1986
    Date of Patent: November 7, 1989
    Assignee: L'Oreal
    Inventors: Gerard Land, Jean Maignan, Serge Restle, Gerard Malle
  • Patent number: 4879410
    Abstract: A process is disclosed for the preparation of aralkyl mono- and diurethanes or ureas by carbamylmethylation, or acid-catalyzed addition at a temperature of 40.degree. C. to about 100.degree. C. of formaldehyde and esters of carbamic acid to aromatic hydrocarbons. Aralkyl carbamates and ureas formed by this process can be cracked directly to produce aralkyl diisocyanates, or hydrogenated and then cracked to produce aliphatic diisocyanates, or reacted directly with polyols to produce polyurethanes by functioning as blocked isocyanates.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: November 7, 1989
    Assignee: American Cyanamid Company
    Inventors: Balwant Singh, Laurence W. Chang, William A. Henderson, Jr.
  • Patent number: 4877799
    Abstract: Novel piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, aryl or heteroaryl which are optionally substituted with one or more C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, C.sub.3-5 -alkylene or aralkoxy,R.sup.1 is straight or branched C.sub.1-8 -alkyl, C.sub.4-8 -alkoxy-C.sub.4-8 -alkyl, C.sub.4-7 -cycloalkyl, aryloxy-C.sub.3-8 -alkyl, C.sub.4-8 -alkenyl, or C.sub.4-8 -cycloalkylalkyl, or R.sup.1 may also be hydrogen or C.sub.1-3 -alkyl, when R.sup.3 is aryl, which is substituted with two or more of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, aralkoxy, or with C.sub.3-5 -alkylene.X is hydrogen or halogen, and whereinY is O or S or a salt thereof with a pharmaceutically-acceptable acid, pharmaceutical compositions thereof, method-of-treating therewith.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.
    Type: Grant
    Filed: October 8, 1987
    Date of Patent: October 31, 1989
    Assignee: A/S Ferrosan
    Inventors: Jorgen Drejer, Palle Jakobsen
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4873241
    Abstract: 2-Amino-N-(2-phenylindan-2-yl)acetamides of the following formula are provided ##STR1## wherein, a=0 to 3,R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen and methyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl, cyclopropyl and (aminomethyl)carbonyl, orR.sub.4 and R.sub.5 taken together with the nitrogen atom to which they are attached from a heterocyclic ring selected from pyrrolidinyl, piperidinyl and morpholinyl, orR.sub.3 and R.sub.4 taken together with the carbon atom and nitrogen atom to which they are respectively attached form a heterocyclic ring selected from pyrrolidinyl and piperidinyl, andR.sub.6 is selected from hydrogen, halogen, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl and combinations thereof.The compounds have antiepileptic or antihypoxia activity.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: October 10, 1989
    Assignee: Fisons Corporation
    Inventors: James J. Napier, Ronald C. Griffith
  • Patent number: 4857524
    Abstract: In one embodiment this invention provides novel thiazolidine compounds, such as 3-[R-(-)-3-benzyloxycarbonylthiazolidine-4-carbonyl]thiazolidine corresponding to the formula: ##STR1## An invention thiazolidine compound exhibits prolyl endopeplidase inhibitory activity, and has utility as a therapeutic agent for the treatment of dementia and amnesia disorders.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: August 15, 1989
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Sunao Furukawa, Tadashi Yoshimoto, Yukiyoshi Ajisawa, Seiichi Ikeguchi, Yukihiko Kinoshita
  • Patent number: 4855464
    Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.
    Type: Grant
    Filed: December 17, 1987
    Date of Patent: August 8, 1989
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4855316
    Abstract: Certain 1,2-diamino-4,5-dimethoxycyclohexane amide derivatives have analgesic activity, and bind selectively to the kappa opioid receptor site. Pharmaceutical compositions containing these compounds, and a method of alleviating pain in mammals are also disclosed.
    Type: Grant
    Filed: February 18, 1988
    Date of Patent: August 8, 1989
    Assignee: Warner-Lambert Company
    Inventors: David C. Horwell, Stephen J. Johnson
  • Patent number: 4838931
    Abstract: 1,2-Disubstituted piperidines of the general formula I ##STR1## in which X denotes oxygen or sulfur; R denotes alkyl, R.sup.1 and R.sup.2 denote hydrogen, alkyl or benzyl, R.sup.3 denotes hydrogen, (substituted) alkyl, (substituted) benzyl or a radical of the formulae ##STR2## Y and X denote S or O; Z denotes S, O or NR.sup.1 ; R.sup.4 denotes hydrogen, (substituted) alkyl, (substituted) phenyl, (substituted) naphthyl or (substituted) pyridyl, A denotes (substituted) phenyl or (substituted) naphthyl and m denotes 0, 1 or 2, possess advantageous herbicidal properties.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: June 13, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Liebl, Michael Frey, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer
  • Patent number: 4835164
    Abstract: Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl;R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl;R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ;the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: May 30, 1989
    Assignee: A. H. Robins Company, Incorporated
    Inventors: James R. Shanklin, Jr., Christopher P. Johnson, III
  • 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: 4818431
    Abstract: New tetrahydropyran derivatives of the formula I ##STR1## in which G is H.sub.2 or .dbd.O, R.sup.1 and R.sup.2 are each an alkyl group having 1-10 C atoms, it also being possible for one or two CH.sub.2 groups to be replaced by O atoms, or are F, Cl, Br or CN, R.sup.2 is also H, A.sup.1 and A.sup.2 are each 1,4-phenylene, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo[2.2.2]octylene or pyrimidine-2,5-diyl groups which are unsubstituted or substituted by 1-4 F atoms, Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, or a single bond, m and n are each 0, 1, 2 or 3, but (m+n) is at least 1 and at most 3, it being possible, when m is 2 or 3, for the group A.sup.1 and, when n is 2 or 3, for the groups A.sup.2 each to be identical or different from one another, and the acid addition salts of those among these compounds which are basic, are suitable for use as components in liquid-crystal dielectrics.
    Type: Grant
    Filed: November 24, 1986
    Date of Patent: April 4, 1989
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Eidenschink, Joachim Krause, Peter Fuss
  • Patent number: 4810791
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definintion of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: March 7, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4788187
    Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: February 26, 1988
    Date of Patent: November 29, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4785006
    Abstract: The invention provides fungicidal compositions comprising as an active ingredient a compound having the general formula (I): ##STR1## or a stereoisomer thereof wherein X and Y are hydrogen, alkyl, or alkoxy, provided that when one of X and Y is hydrogen the other is not --C(CH.sub.3).sub.2 R, where R is hydrogen, methyl or ethyl; Z is carbonyl, or a derivative thereof, or is --CR.sup.3 R.sup.4 -- or --CR.sup.3 OR.sup.4 -- in which R.sup.3 and R.sup.4 are hydrogen or C.sub.1-4 alkyl; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the adjacent N-atom constitute an optionally substituted heterocyclic ring; and n is 0 or 1.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: November 15, 1988
    Inventors: Paul A. Worthington, Brian K. Snell, Paul DeFraine, Vivienne M. Anthony
  • Patent number: 4783458
    Abstract: The invention provides fungicidal compositions comprising as an active ingredient a compound having the general formula (I): ##STR1## or a stereoisomer thereof, wherein one of X and Y is hydrogen and the other is ##STR2## where R is H, methyl or ethyl; Z is carbonyl, or a derivative thereof, or is --CR.sup.3 R.sup.4 -- or --CR.sup.3 OR.sup.4 in which R.sup.3 and R.sup.4 are hydrogen or alkyl groups; R.sup.1 and R.sup.2, which may be the same or different, are alkyl groups containing from 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom constitute an optionally substituted heterocyclic ring; and n is 0 or 1.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: November 8, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul A. Worthington, Brian K. Snell, Paul De Fraine, Vivienne M. Anthony
  • Patent number: 4777176
    Abstract: This invention provides fungicidal compositions comprising as an active ingredient a compound having the general formula (I): ##STR1## or a stereoisomer thereof, wherein one of X and Y represents hydrogen and the other represents the group ##STR2## in which R is hydrogen, methyl or ethyl; Z represents hydrogen or an alkyl group containing from one to four carbon atoms; R.sup.1 and R.sup.2, which may be the same or different, represent hydrogen or an alkyl group containing one to four carbon atoms, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom represent an optionally-substituted heterocyclic ring; and n is 0 or 1.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: October 11, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul A. Worthington, Brian K. Snell, Paul DeFraine, Vivienne M. Anthony
  • Patent number: 4764618
    Abstract: Novel arginine derivatives represented by the general formula ##STR1## wherein R.sup.1 stands for a naphthalenesulfonyl, a naphthalenecarbonyl, a 1,2,3,4-tetrahydronaphthalenesulfonyl, a 1,2,3,4-tetrahydronaphthalenecarbonyl, a dioxa b-6,7-naphthalenesulfonyl, a dioxa b-6,7-naphthalenecarbonyl, a 1,2,3,4-tetrahydro-8-quinolinesulfonyl, a 1,2,3,4-tetrahydro-8-quinolinecarbonyl, a dibenzofuransulfonyl, a dibenzofurancarbonyl, a fluorenesulfonyl, a fluorenecarbonyl, a dibenzothiophenesulfonyl or a dibenzothiophene, and R.sup.2 stands for a piperidino or a piperazino are disclosed. These arginine derivatives and their pharmaceutically acceptable salts have trypsin-inhibiting activity and useful as a pancreatitis remedy.
    Type: Grant
    Filed: June 19, 1987
    Date of Patent: August 16, 1988
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Ryoji Kikumoto, Yoshikuni Tamao, Shinji Tonomura, Akira Maruyama, Shosuke Okamoto, Akiko Okunomiya
  • Patent number: 4757079
    Abstract: Novel compounds of the formula: ##STR1## are described wherein Z is a bicyclic aryl group containing between 9 and 10 ring atoms, up to two of which may be nitrogen and up to one of which may be oxygen or sulfur; A is an ethenyl group which may be lower-alkyl-substituted; and R and R' each represent H or an aliphatic group of 1-4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: July 12, 1988
    Assignee: Dynamac Corporaton
    Inventor: Allan P. Gray
  • Patent number: 4734507
    Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.
    Type: Grant
    Filed: April 5, 1985
    Date of Patent: March 29, 1988
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4727072
    Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.
    Type: Grant
    Filed: February 12, 1986
    Date of Patent: February 23, 1988
    Assignee: McNeilab, Inc.
    Inventors: Philip P. Grous, Richard J. Mohrbacher
  • Patent number: 4721786
    Abstract: Fungicidally active novel .beta.-naphthylalkylamines of the formula ##STR1## in which Ar represents optionally substituted .beta.-naphthyl andR.sup.1 and R.sup.2, which can be identical or different, represent alkyl or alkenyl orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can contain further hetero-atoms,or plant-tolerated acid addition salts thereof.
    Type: Grant
    Filed: April 1, 1985
    Date of Patent: January 26, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4705805
    Abstract: Certain 2,2'-dithiobis-N-substituted or unsubstituted benzamides or derivatives thereof are useful as antithrombotic agents because of their ability to suppress aggregation of blood platelets.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: November 10, 1987
    Inventors: Koji Yamada, Tamotsu Hashimoto, Masao Naruse, Yo Murayama, Hideki Ninno
  • Patent number: 4704227
    Abstract: Compounds of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 IwhereinR.sup.1 and R.sup.2 are each H, an alkyl, alkoxy, alkanoyl, alkanoyloxy or alkoxycarbonyl group with in each case 1-10 C atoms, F, Cl, Br, CN or R.sup.3 --A.sup.3 --Z.sup.2 --,A.sup.1 is --A--, --A.sup.4 --A--or --A--A.sup.4 --,A is a 1,3-dioxane-2,5-diyl or a 1,3-dithiane-2,5-diyl group,A.sup.2, A.sup.3 are each a 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl,and A.sup.4 1,3-dithiane-2,5-diyl, piperidine-1,4-diyl or 1,4-bicyclo(2,2,2)octylene group, or a 1,4-phenylene, pyrimidine-2,5-diyl or pyridazine-3,6-diyl group which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups and/or CN groups,Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O or a single bond andR.sup.3 is H, an alkyl, alkoxy, alkanoyl, alkanoyloxy or alkoxycarbonyl group with in each case 1-10 C atoms, F, Cl, Br or CN, with the proviso that(a) at least one group A.sup.2, A.sup.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: November 3, 1987
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Joachim Krause, Andreas Wachtler, Reinhard Hittich, Georg Weber, Bernhard Scheuble
  • Patent number: 4665076
    Abstract: The piperidine derivatives of formula: ##STR1## in which X denotes --CO--, --CHOH-- or --CH(NH.sub.2)-- and Ar denotes ##STR2## in which R denotes hydrogen or alkyl of 1 to 4 carbon atoms, and Y and Z, which may be identical or different, each denote a hydrogen atom or alkoxy of 1 to 3 carbon atoms, and their addition salts with pharmaceutically acceptable inorganic or organic acids are useful for treating and/or preventing disturbances of cardiac rhythm. These compounds are new except when X is --CO-- and Ar is 1-naphthyl or 1-isoquinolyl.
    Type: Grant
    Filed: March 6, 1985
    Date of Patent: May 12, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Michel Mestre, Christian Renault
  • Patent number: 4656269
    Abstract: Novel amino acid derivatives useful as a therapeutic agent are disclosed. These amino acid derivatives and the pharmaceutically acceptable salts thereof have a human renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.
    Type: Grant
    Filed: April 15, 1986
    Date of Patent: April 7, 1987
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, Yoshiaki Kiso
  • Patent number: 4656282
    Abstract: Piperidines substituted in the 3- and/or 4-position are prepared by reacting a glutardialdehyde substituted in the 2- and/or 3-position with ammonia or a primary amine and hydrogen at elevated temperature and under superatmospheric pressure in the presence of a hydrogenation catalyst.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: April 7, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Walter Himmele, Walter-Wielant Wiersdorff, Marco Thyes