Plural Ring Chalcogens In The Bicyclo Ring System Patents (Class 544/377)
  • Patent number: 5378713
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 3, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5356891
    Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: October 18, 1994
    Inventors: Donald T. Witiak, Ineke van Wijngaarden, Raghunathan V. Nair, Josephus H. M. Lange, Jacobus A. J. den Hartog
  • Patent number: 5352678
    Abstract: Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: October 4, 1994
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5340812
    Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl, and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, inter alia, for the treatment of CNS disorders, such as anxiety.
    Type: Grant
    Filed: January 7, 1993
    Date of Patent: August 23, 1994
    Assignee: John Wyeth & Brother, Limited
    Inventor: Ian A. Cliffe
  • Patent number: 5332743
    Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: July 26, 1994
    Assignee: McNeilab, Inc.
    Inventors: Ellen W. Baxter, Allen B. Reitz
  • Patent number: 5326783
    Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: July 5, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
  • Patent number: 5281595
    Abstract: The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B ##STR1## wherein R.sub.1 +R.sub.2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 1-3 C-atoms and the remaining R and Z variables are defined as disclosed herein, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: January 25, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Josephus H. M. Lange, Gerrit P. Toorop, Ineke v. Wijngaarden, Jacobus A. J. den Hartog
  • Patent number: 5260453
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: November 9, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffrey B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5246935
    Abstract: Piperazinyl derivatives of the general formula I ##STR1## wherein R.sup.1 represents substituted phenyl, 1- or 2-diazanaphthyl, azadiazanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is --O-- or ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-6 -alkyl or C.sub.3-8 -cycloalkyl; Y is .dbd.O or .dbd.S or .dbd.NZ wherein Z is hydrogen, C.sub.1-6 -alkyl or --CN and R.sup.3 is selected from a group consisting of various structures have been found to exhibit high affinity for various receptor subtypes including the 5-HT.sub.2 receptor, the 5-HT.sub.1A receptor, the alpha.sub.1 receptor the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: September 21, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Marit Kristiansen, John B. Hansen
  • Patent number: 5242925
    Abstract: Piperazinylbenzodioxane derivatives of formula I ##STR1## wherein B is an indol-3-yl or benzimidazol-1-yl radical which is unsubstituted or monosubstituted by CN, CO--R.sup.1, C.sub.n H.sub.2n --R.sup.1, Hal, OH, OA, O--C.sub.n H.sub.2n --CO--R.sup.1, or NHR.sup.2, and Q is C.sub.n H.sub.2n, or a physiologically acceptable salt thereof. The derivatives are active in the central nervous system, especially as serotonin agonists and antagonists.
    Type: Grant
    Filed: August 24, 1992
    Date of Patent: September 7, 1993
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Henning Boettcher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk
  • Patent number: 5236935
    Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.
    Type: Grant
    Filed: May 21, 1992
    Date of Patent: August 17, 1993
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
  • Patent number: 5194437
    Abstract: The compounds are 1,4-disubstituted piperazines useful for the treatment of disorders of central nervous system and neuroendocrine disorders.A compound disclosed is (R,S)-4-(benzodioxan-5-yl)-1-[(benzocyclobutan-1-yl)methyl]piperazine.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: March 16, 1993
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Mark Millan, Jean-Michel Rivet
  • Patent number: 5182284
    Abstract: Disclosed are a piperazine compound of the formula below or a pharmaceutically acceptable salt thereof, medical uses thereof, and processes for preparing the same: ##STR1## wherein each of R and R' is --OH, a lower alkoxy, a halo, H, a di(lower alkyl) hydrogenphosphate residue or a group --OR" (R" is an aralkyl group, etc.), etc., Y is --CH.dbd.CH-- or --(CH.sub.2).sub.m -- (m is 0, 1 or 2), and Y.sub.1 is a group of the formula ##STR2## (wherein A is --NH-- or --O--, A.sub.1 is a methylene or a carbonyl, n is 6-20, X is --OH, H or a lower alkoxycarbonyl, and X.sub.1 is an optionally halo-substituted phenyl or H) or a group of the formula ##STR3## (wherein X and n are as defined above), provided that when Y.sub.1 is the group of the formula (3), each of R and R' is an --OH group.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: January 26, 1993
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masahiro Suzuki, Kenji Nozaki, Makoto Kajitani, Mitsugi Yasumoto, Naohiko Ono, Takashi Shindo
  • Patent number: 5153198
    Abstract: A compound of the formula [II] or pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 is hydrogen or fluorine;R.sup.2 is hydrogen or fluorine;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkylenedioxy;A is straight or branched lower alkylene having 1 to 6 carbon atoms; and n is 0 or 1,provided that at least one of R.sup.1 or R.sup.2 is fluorine. Such compound is useful for treatment of disorders of the cerebro-neural transmission system.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: October 6, 1992
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Takakazu Morita, Tadashi Iso, Hideyasu Yamauchi
  • Patent number: 5120737
    Abstract: A hexitol derivative represented by formula (I) ##STR1## wherein R represents hydrogen, unsubstituted or lower alkyl-substituted cycloalkyl, lower alkenyl, lower alkoxy, lower alkanoyl, piperidyl or ##STR2## wherein each of m and n independently represents an integer of 0 to 3; each of X, Y and Z independently represents hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxyl, halogen or nitro or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 24, 1991
    Date of Patent: June 9, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Fumio Suzuki, Hiroaki Hayashi, Kazuhiro Kubo, Junichi Ikeda
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5084569
    Abstract: A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substitutents have the meanings given in the description. The described process leads to the formation of a single enantiomer.
    Type: Grant
    Filed: March 15, 1990
    Date of Patent: January 28, 1992
    Assignee: Zambon SpA
    Inventors: Marco Villa, Claudio Giordano, Graziano Castaldi, Silvia Cavicchioli
  • Patent number: 5037825
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: August 6, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 4997836
    Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: March 5, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa
  • Patent number: 4977166
    Abstract: New benzopyran derivatives of formula: ##STR1## in which R.sub.1 is hydrogen, halogen, hydroxy, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl) amino or acylamino,X is nitrogen or a >CH-radicalR is a radical of formula: ##STR2## in which A denotes a single bond or methylene or, when X is nitrogen, A may denote carbonyl, and R.sub.2 and R.sub.3, which are identical or different, are hydrogen, halogen, hydroxy, alkyl, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano, or, when they are adjacent, together form a methylenedioxy or ethylenedioxy radical, or elseR is pyridyl or 2(2H)-benzimidazolonyl if X denotes >CH--, andR' and R" are identical and are hydrogen or alkyl, their isomeric forms and mixtures thereof, and their acid addition salts, can be used as antiarrhythmic and antifibrillation agents.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: December 11, 1990
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Hardy, Christian Renault
  • 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: 4948796
    Abstract: A piperazine derivative represented by the following formula or a salt thereof: ##STR1## which is useful for curing cerebro-vascular disease and post-cerebro-vascular disease.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: August 14, 1990
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Toru Hiraiwa, Kenji Takeda, Joji Nakano, Mineichi Sudani, Kunikazu Furuhata, Makoto Takata, Hiroyo Kawafuchi, Isao Watanabe
  • Patent number: 4940793
    Abstract: New piperazino derivatives of formula ##STR1## in which R is a phenyl radical substituted with at least one sulphonamido group or a substituted nitrogenated heterocyclic ring, and A is CO, CH.sub.2, SO.sub.2, possessing inhibiting activity towards carbonic anhydrase.The new products are prepared from compounds of formula R-A-X in which X is OH, SH, halogen, OR"" or SR"" in which R"" is methyl, ethyl, phenyl, carbomethoxy, carboethoxy, and from a piperazino derivative of formula ##STR2## The R' group can also be introduced on termination of the reaction, by removing and substituting a protective group present at the nitrogen.
    Type: Grant
    Filed: July 18, 1985
    Date of Patent: July 10, 1990
    Assignee: Ravizza S.p.a.
    Inventors: Francesco Botre, Roberto Signorini
  • Patent number: 4898876
    Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: February 6, 1990
    Assignee: Kowa Co., Ltd.
    Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Koichiro Watanabe, Kazuhiro Onogi, Masahiko Nagakura
  • Patent number: 4895847
    Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].
    Type: Grant
    Filed: September 21, 1988
    Date of Patent: January 23, 1990
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 4891373
    Abstract: Novel aminopropanol derivatives of 1,4:3,6-dianhydro-hexitol nitrates of the general formula I ##STR1## in which X has the meaning given in the specification, processes for their preparation and their use in preventing and treating angina pectoris, systemic hypertension and pulmonary hypertension in mammals.
    Type: Grant
    Filed: November 23, 1988
    Date of Patent: January 2, 1990
    Assignee: Pfizer Inc.
    Inventors: Peter Stoss, Matyas Leitold, Rodney Yeates
  • Patent number: 4886799
    Abstract: The invention relates to new acetamides derived from 2,3-dihydro-3-phenyl-2-benzofuranone, of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen or halogen atom,R.sub.2 and R.sub.3, which may be identical or different, each denote a hydrogen atom or a linear or branched alkyl radical containing 1 to 4 carbon atoms, a benzyl radical optionally substituted with a halogen atom, with an alkoxy radical containing 1 to 4 carbon atoms or with an alkyl radical having 1 to 4 carbon atoms, or a 3,4-methylene-dioxybenzyl radical, or form, together with the nitrogen to which they are attached, a 4-morpholinyl radical or a 1-piperazinyl radical.
    Type: Grant
    Filed: September 14, 1988
    Date of Patent: December 12, 1989
    Assignee: Adir Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4885299
    Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: December 5, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4885385
    Abstract: Water-soluble triphendioxazine compounds having fiber-reactive dye properties conforming to the general formula ##STR1## where: B is --O-- or --S-- or --NH-- or (C.sub.1 -C.sub.6)-alkylamino;R* is hydrogen or optionally substituted alkyl or aryl;W and W.sup.1 are each a bivalent, aliphatic or optionally alkyl-substituted cycloaliphatic or aliphatic-cycloaliphatic radical, which aliphatic radicals can be interrupted by --O--, --S--, sulfonyl, carbonyl, 1,4-piperidino, amino, alkylamino and/or alkanoylamino groups, orthe grouping --B--W.sup.1 --N(R*) and/or --N(R*)--W--B-- each represent the bivalent radical of a five- or six-membered saturated heterocycle which contains two nitrogen atoms, orthe grouping --B--W.sup.1 -- and/or --W--B-- each represent the bivalent radical of a five- or six=-membered saturated heterocycle which contains two nitrogen atoms and which is bonded by one of the two nitrogen atoms via an alkylene group of 2 to 4 carbon atoms to the grouping --N(R*)--CO--G.sup.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 5, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hartmut Springer, Walter Helmling, Gunther Schwaiger
  • Patent number: 4883796
    Abstract: Oxime ethers of 2,6-dioxabicyclo[3.3.0]octanones of the formula I ##STR1## have pharmacological activity and are especially applicable as drugs for the prophylaxis and therapy of cardiac and circulatory diseases.
    Type: Grant
    Filed: February 2, 1988
    Date of Patent: November 28, 1989
    Assignee: Heinrich Mack Nachf.
    Inventors: Matyas Leitold, Peter Stoss
  • Patent number: 4876271
    Abstract: Novel substituted thieno[3,2-b]thiophene-2-sulfonamides are prepared by novel synthetic processes. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4859700
    Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: August 22, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4833142
    Abstract: Blood-pressure lowering compounds having a structure as shown in the accompanying formula sheets.
    Type: Grant
    Filed: November 9, 1987
    Date of Patent: May 23, 1989
    Assignee: Duphar International Research B.V.
    Inventors: Jan Hartog, Wouter Wouters, Lneke van Wijngaarden
  • Patent number: 4826844
    Abstract: Compounds of the formula: ##STR1## in which m is one of the integers 1, 2 or 3; n is one of the integers 0, 1 or 2; o is one of the integers 0, 1 or 2; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R.sub.3 is alkyl, ##STR2## where R.sub.4 and R.sub.5 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R.sub.6 is hydrogen or halo; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: May 2, 1989
    Assignee: American Home Products Corporation
    Inventors: G. E. M. Husbands, Gary P. Stack
  • Patent number: 4824968
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: April 25, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Ponticello, J. Mark Wiggins
  • Patent number: 4816457
    Abstract: Heterocyclic aminoethanols of the formula:Het--CHOH--CH.sub.2 --NH-aralkylwhere Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: March 28, 1989
    Inventors: John J. Baldwin, Joseph Atkinson, David E. McClure
  • Patent number: 4812469
    Abstract: The invention relates to new acetamides derived from 2,3-dihydro-3-phenyl-2-benzofuranone, of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen or halogen atom,R.sub.2 and R.sub.3, which may be identical or different, each denote a hydrogen atom or a linear or branched alkyl radical containing 1 to 4 carbon atoms, a benzyl radical optionally substituted with a halogen atom, with an alkoxy radical containing 1 to 4 carbon atoms or with an alkyl radical having 1 to 4 carbon atoms, or a 3,4-methylenedioxybenzyl radical, or form, together with the nitrogen to which they are attached, a 4-morpholinyl radical or a 1-piperazinyl radical.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: March 14, 1989
    Assignee: Adir Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4797413
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Patent number: 4788184
    Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: November 29, 1988
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4788290
    Abstract: The compounds ##STR1## in which X and Y are, independently, --O-- or --S--;R.sup.1 and R.sup.2 are, independently, halo, trifluoromethyl, cyano, hydroxy, amino, alkylamino, dialkylamino, alkoxy, alkyl or alkanoylamino; andn is 1 to 4;or a pharmaceutically acceptable salt thereof, are selective serotonergic agents useful in the treatment of depression and/or anxiety, as well as related sexual dysfunctions and appetite disorders.
    Type: Grant
    Filed: December 11, 1987
    Date of Patent: November 29, 1988
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 4782061
    Abstract: The invention relates to a group of new bicyclic heteroarylpiperazine derivatives of formula 1. It was found that these compounds have interesting psychotropic in particular anti-psychotic properties.The compounds can be prepared according to methods known for the synthesis of analogous compounds.
    Type: Grant
    Filed: December 18, 1985
    Date of Patent: November 1, 1988
    Assignee: Duphar International Research B.V.
    Inventors: Cornelis G. Kruse, Johannes A. M. van der Heyden, Ineke van Wijngaarden, Jan Hartog, Berend Olivier
  • Patent number: 4772604
    Abstract: The invention relates to new aryl-substituted (N-piperidinyl)methyl- and (N-piperazinyl)methylazoles having interesting pharmacological, notably antipsychotic, properties.The compounds may be prepared in a manner known for the synthesis of analogous compounds and be processed to compositions according to known methods.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: September 20, 1988
    Assignee: Duphar International Research B.V.
    Inventors: Ineke van Wijngaarden, Cornelis G. Kruse, Johannes A. M. van der Heyden, Martinus T. M. Tulp
  • Patent number: 4767757
    Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: August 30, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Daum, Gerd Hanssler
  • Patent number: 4743595
    Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.
    Type: Grant
    Filed: June 12, 1985
    Date of Patent: May 10, 1988
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
  • Patent number: 4737501
    Abstract: An oxindol compound of the formula (I) ##STR1## wherein A represents a lower alkylene group;R represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a phenoxy-lower alkyl group, a benzoyl-lower alkyl group, a lower alkoxycarbonyl group, a lower alkanoyl group, a benzoyl group which may be substituted with 1 to 3 of a lower alkyl group, a lower alkoxy group and a halogen atom on the benzene ring thereof, or a benzoyl group which is substituted with a lower alkylenedioxy group on the benzene ring thereof; andm and n, which may be the same or different, each represents an integer of 0 or 1, with proviso that when n is an integer of 1, then m is an integer of 1,when A is an ethylene group and m is an integer of 1, then R should not be 3,4,5-trimethoxybenzoyl group, and when A is a group of the formula: --C(R.sup.1)(R.sup.2)--(where R.sup.1 and R.sup.
    Type: Grant
    Filed: July 5, 1985
    Date of Patent: April 12, 1988
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Michiaki Tominago, Hidenori Ogawa, Takafumi Fujioka, Kazuyuki Nakagawa
  • Patent number: 4736031
    Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.
    Type: Grant
    Filed: April 15, 1986
    Date of Patent: April 5, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Minoru Hirata
  • Patent number: 4686222
    Abstract: Heterocyclic aminoethanols of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: August 11, 1987
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
  • Patent number: 4684651
    Abstract: Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.
    Type: Grant
    Filed: February 26, 1982
    Date of Patent: August 4, 1987
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Ryoji Kikumoto, Harukazu Fukami, Kenichiro Nakao, Mamoru Sugano
  • Patent number: 4668681
    Abstract: This invention relates to 2-(4-phenylpiperazinylethyl)anilines, to methods for preparing them and to their uses in medical therapy.These compounds have the following general formula ##STR1## wherein R.sub.1 represents one or more substituents selected from the group consisting of H, CH.sub.3, CF.sub.3, F, Cl, and OCH.sub.3 ; R.sub.2 and R.sub.3, which may be the same or different, and are selected from the group consisting of H and (C.sub.1 -C.sub.4) alkoxy, or R.sub.2 and R.sub.3 taken together can form a chain selected from the group consisting of --O-- (CH.sub.2).sub.n --O--, wherein n=1 or 2 and --O--CH.sub.2 --O--CH.sub.2 with the proviso that R.sub.1 is not meta CF.sub.3 when R.sub.2 =R.sub.3 =H, and pharmaceutically non-toxic salts thereof. The compounds of this invention are useful in the treatment of allergic and anaphylatic conditions and motion sickness.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: May 26, 1987
    Assignee: Societe Cortial, S.A.
    Inventors: Henri Pontagnier, Marie-H/e/ l/e/ ne Creuzet, Claude Feniou, Francoise Guichard, Gis/e/ le Prat
  • Patent number: 4666911
    Abstract: An analgesic compositon containing as active ingredient an allophanoylpiperazine compound represented by the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group or phenyl group; R.sup.2 and R.sup.3 each represents a hydrogen atom or a lower alkyl group; and R.sup.4 represents a phenyl group or a substituted phenyl group having as substituent a halogen atom or methyl, trifluoromethyl, hydroxyl, methoxy, methylenedioxy, nitro, or carboxyl group; pyridyl group, pyrimidyl group, thiazolyl group, benzyl group, cinnamyl group, cyclohexyl group, a lower alkyl group, a substituted lower alkyl group having chlorine atom or hydroxyl group as substituent; or a lower alkenyl group.
    Type: Grant
    Filed: July 8, 1981
    Date of Patent: May 19, 1987
    Assignee: Taiho Pharmaceutical Company Limited
    Inventors: Hajime Fujimura, Yasuzo Hiramatu, Takahiro Yabuuchi, Masakatu Hisaki, Katsuo Takikawa, Takaji Honna, Hidekazu Miyake, Makoto Kajitani