Additional Polycyclo Heterocyclic Ring System Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/454)
  • Patent number: 5310932
    Abstract: Novel compounds are disclosed having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: May 10, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, George C. Rovnyak
  • Patent number: 5308850
    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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: May 3, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John W. Gillard, John H. Hutchinson, Richard Frenette, Michel Therien
  • Patent number: 5300651
    Abstract: A derivative of tryptophan is provided wherein the NH-group of the tryptophan indole nucleus is protected with tert.-butyloxycarbonyl (BOC) and the .alpha.-amino group is protected by 9-fluorenyl-methyloxy-carbonyl (FMOC). The carboxylic acid group of the tryptophan derivative may comprise a free COOH group, may be modified with a protecting or activating group, or may comprise an acyl group bonded to another chemical moiety, such as a polymer, another amino acid, a dipeptide, a polypeptide, or a protein. The tryptophan derivative is useful in the preparation of dipeptides, polypeptides or proteins containing at least one tryptophan-derived amino acid residue.
    Type: Grant
    Filed: May 27, 1992
    Date of Patent: April 5, 1994
    Assignee: Calbiochem-Novabiochem AG
    Inventor: Peter D. White
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5284857
    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: December 21, 1990
    Date of Patent: February 8, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5281617
    Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: January 25, 1994
    Assignee: Cortech, Inc.
    Inventors: Gary P. Kirschenheuter, John C. Cheronis
  • Patent number: 5280039
    Abstract: A compound of the formula ##STR1## wherein R is defined herein is useful as an anti-inflammatory agent.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: January 18, 1994
    Assignee: Pfizer Inc.
    Inventor: James F. Eggler
  • Patent number: 5273994
    Abstract: The invention relates to the derivatives of general formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,1.ltoreq.n.ltoreq.6,R.sub.3 represents a nitrile group, an optionally substituted amino group or any one of the groups described in the description, andmedicinal products containing the same.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: December 28, 1993
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Beatrice Guardiola
  • Patent number: 5266707
    Abstract: 4-hydroxytetrahydropyran-2-one and 3,5-Dihydroxyheptanoic acid derivatives of formula (I) and formula (II) have an inhibition effect on HMG-CoA reductase, a cholesterol value reduction effect, and an antioxidation function, thus serving as cholesterol reducing agent or lipid reducing agents: ##STR1## wherein R.sup.1 represents hydrogen, a nitro group, or -N(R.sup.4)R.sup.5 in which R.sup.4 and R.sup.5 each represent an alkyl group, an alkenyl group, an aryl group, an aralkyl group; an acyl group, an aroyl group, a carbamoyl group, or a thiocarbamoyl group, and R.sup.4 and R.sup.5 may be combined to form a cyclic amino group; and R.sup.2 and R.sup.3 each represent hydrogen or an alkyl group; and R.sup.6 represents hydrogen, an alkyl group, an alkali metal, or an alkaline earth metal.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: November 30, 1993
    Assignee: Fujirebio Inc.
    Inventors: Masakatsu Matsumoto, Nobuko Watanabe, Eiko Mori, Tetsuaki Yamaura, Misao Aoyama
  • Patent number: 5262549
    Abstract: 4-[3-(benz[b]pyran-4-ylidene)prop-1-enyl]benz[b]pyrylium, 4-[5-(4H-benz[b]pyran-4-ylidene)penta-1,3-dienyl]benz[b]pyrylium and 4-[7-(4H-benz[b]pyran-4-ylidene)hepta-1,3,5-trienyl]benz[b]pyrylium dyes, wherein at least one of the benzpyrylium nuclei carries at its 2-position a substituent in which a non-aromatic carbon atom is bonded directly to the benzpyrylium nucleus, subject to the proviso that if the or each 2-substituent contains an aromatic nucleus, this aromatic nucleus is not conjugated with the benzpyrylium nucleus, are useful as visible and near infra-red absorbers, having high extinction coefficients and a reduced tendency to develop absorptions at shorter wavelengths when dispersed in polymeric media.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: November 16, 1993
    Assignee: Polaroid Corporation
    Inventors: Stephen J. Telfer, Socorro M. Ramos, Michael J. Zuraw
  • Patent number: 5258401
    Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: November 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick
  • Patent number: 5254578
    Abstract: Compounds of the formula: ##STR1## in which: R.sup.1 is a trifluoromethyl or a pentafluoroethyl;R.sup.2 is ##STR2## in which R.sup.4 is hydrogen; .alpha.-.beta. is a carbon-carbon single bond;and pharmaceutically acceptable salts thereof, have antihypertensive activity and can thus be used for the treatment and prophylaxis of cardiovascular diseases.
    Type: Grant
    Filed: November 9, 1992
    Date of Patent: October 19, 1993
    Assignee: Sankyo Company, Limited
    Inventors: Toshihiko Hashimoto, Hidekazu Masuko, Hiroyuki Koike, Toshio Sada
  • Patent number: 5252597
    Abstract: Disclosed herein are novel benzopyrans represented by formula (I) ##STR1## wherein R.sup.1 is trifluoromethoxy or .beta.,.beta.,.beta.-trifluoroethoxy; R.sup.2, and R.sup.3 are independently selected from the group consisting of hydrogen, lower alkyl containing 1 to 5 carbon atoms, cyclo lower alkyl containing 5 to 8 carbon atoms, ##STR2## or R.sup.2 and R.sup.3 are joined to form (--CH.sub.2 --).sub.n wherein n is 4 to 7; or R.sup.2 and R.sup.3 are joined together to form (--CH.sub.2 --).sub.m CO-- wherein m is 3 to 6; or R.sup.2 and R.sup.3 are joined together to form ##STR3## wherein R.sup.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: October 12, 1993
    Assignee: American Home Products Corporation
    Inventor: Dominick A. Quagliato
  • Patent number: 5234900
    Abstract: The present invention relates to novel oxabicyclo ether derivative compounds, compositions containing these ether derivative compounds, and methods of using these compounds or compositions to control the growth of undesired vegetation. More particularly, the present invention relates to a variety of compounds, compositions, and methods of using them which are herbicidally active on a wide variety of weed species and exhibit safety to rice, cereals or broadleaf crops.
    Type: Grant
    Filed: March 11, 1992
    Date of Patent: August 10, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: James E. Powell, Jr., Wendy S. Taylor
  • Patent number: 5227498
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a cycloaliphatic or aromatic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: July 13, 1993
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5227499
    Abstract: Squarylium compounds of the formula: ##STR1## in which: Q.sup.1 and Q.sup.2 are each a Chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens;R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group; andR.sup.3, R.sup.4 and R.sup.5 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or an electron-withdrawing group able to lower the electron density at the carbon atom to which it is attached, subject to the provisoes that:two of R.sup.3, R.sup.4 and R.sup.5 may form a divalent group of which a single atom is double bonded to the carbon atom to which the two groups are attached, or all three of R.sup.3, R.sup.4 and R.sup.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: July 13, 1993
    Assignee: Polaroid Corporation
    Inventors: Donald A. McGowan, Mark R. Mischke, Stephen J. Telfer
  • Patent number: 5227488
    Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; X represents oxygen or sulfur; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: July 13, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen
  • Patent number: 5225419
    Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O--or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl,andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereofand their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.
    Type: Grant
    Filed: September 16, 1991
    Date of Patent: July 6, 1993
    Assignee: John Wyeth & Brother, Limited
    Inventors: Terence J. Ward, Janet C. White
  • Patent number: 5225427
    Abstract: 10-substituted ether derivatives of 3.alpha., 12.alpha.-Epoxy-3,4,5 5a.alpha., 6,7,8,8a.alpha.,9,10,12.beta., 12a-dodecahydro-10-hydroxy-3.beta.,6.alpha.,9.beta.-trimethylpyano-(4,3-j) (1,2) benzodioxepin, also known as Dihydroartemisinin or Dihydroquinghaosu (DHQ), pharmaceutically acceptable salts thereof, processes for their preparation and their use as chemotherapeutics against protozoal infections are provided.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: July 6, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Bansi Lal, Dipak K. Chatterjee, Subramani N. Iver, Richard H. Rupp
  • Patent number: 5182348
    Abstract: Compounds of the formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 have the meanings given in the description, and the other radicals have the following meanings:X, Y and Z denote identical or different divalent radicals --O--, --S--, --N(R.sup.9)-- or --C(R.sup.10).dbd.C(R.sup.11)--, with the proviso that at least one of the radicals, X, Y and Z is not a radical of the formula --C(R.sup.10).dbd.C(R.sup.11)--, and whereinR.sup.9 is a hydrogen atom, a branched or unbranched C.sub.1 - to C.sub.8 -alkyl radical or an optionally substituted phenyl radical, andR.sup.10 and R.sup.11 are, in each case, identical or different radicals which have one of the meanings of R.sup.1,R.sup.7 and R.sup.8 denote identical or different radicals, that is to say hydrogen atoms or C.sub.1 - to C.sub.6 -alkyl or phenyl radicals, andn, m and o denote identical or different integers with a value of from 1 to 10.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: January 26, 1993
    Assignee: Wacker-Chemie GmbH
    Inventors: Hermann Braeunling, Richard Becker, Georg Bloechl
  • Patent number: 5162362
    Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: November 10, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
  • Patent number: 5134240
    Abstract: Novel 4-substituted-4,8-dimethyl-2,3-dioxabicyclo[3.3.1] nonan-7-ones which have a pronounced activity against the causative organism of malaria and can be used for the prevention and control of malaria.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: July 28, 1992
    Assignee: Hoffmann-LaRoche, Inc.
    Inventors: Werner Hofheinz, Gerard Schmid, Harro Stohler
  • Patent number: 5128346
    Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: July 7, 1992
    Assignee: Abbott Laboratories
    Inventors: Alex M. Nadzan, James F. Kerwin, Chun W. Lin
  • Patent number: 5120858
    Abstract: This invention relates to a process for preparing trimethine dyestuffs of the formula ##STR1## wherein R.sup.1 is lower alkyl; R.sup.2 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, cycloalkoxy, aryloxy, aralkoxy, fluorinated alkyl, alkanoyl, aroyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkanoylamino, aroylamino, alkylaminocarbonyl, arylaminocarbonyl, alkoxycarbonylamino, alkylsulfonyl, arylsulfonyl, halogen, cyano, nitro, carbamoyl, or sulfonamido, or two R.sup.2 together form a fused benzene ring; n is an integer of from 1 to 4; and A.sup.- is an anion, by reacting a mixture of(a) an indoline compound of the formula ##STR2## (b) 1.25 to 1.8 parts by moles, based on the indoline compound, of acetic anhydride; and (c) 0.5 to 0.75 parts by moles, based on the indoline compound, of formic acid to form the dyestuff.
    Type: Grant
    Filed: March 25, 1991
    Date of Patent: June 9, 1992
    Assignee: Miles Inc.
    Inventors: Charles W. Sandefur, Brian L. Thompson, James J. Good
  • Patent number: 5116986
    Abstract: The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: May 26, 1992
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Andreas Bomhard, Joachim Heider, Manfred Psiorz, Norbert Hauel, Berthold Narr, Klaus Noll, Christian Lillie, Walter Kobinger, Willi Diederen
  • Patent number: 5116978
    Abstract: A process for producing a bis-(indolyl)ethylene of the formula ##STR1## is described, wherein A, B, a, b, R, Z, R.sup.5', R.sup.6 and R.sup.6' are as defined in the specification, said method comprising reacting an indole of the formula ##STR2## with an acylindole of the formula in the presence of a Vilsmeier reagent selected from the group consisting of phosphoryl chloride, phosgene, oxalyl chloride, benzoyl chloride, thionyl chloride, alkanesulfonyl chloride, arene-sulfonyl chloride, alkylchoroformate, and arylchloroformate, together with a Lewis Acid selected from the group consisting of zinc chloride, boron trifluoride and aluminum chloride.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: May 26, 1992
    Assignee: Appleton Papers Inc.
    Inventor: Ponnampalam Mathiaparanam
  • Patent number: 5112987
    Abstract: A process for the preparation of an indigo compound which comprises reacting a corresponding indole compound having no substituent at the 2- and 3-positions with a percarboxylic acid in the presence of an alcohol solvent, or with heating over 60.degree. C. in the presence of an aprotic solvent.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: May 12, 1992
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Yoshihiro Yamamoto, Usaji Takaki, Shinobu Aoki, Isao Hara
  • Patent number: 5112989
    Abstract: A process for producing an unsaturated dicarboxylic acid imide compound of formula (I): ##STR1## wherein D represents a divalent organic group having at least one carbon/carbon double bond; R.sup.1 represents an n-valent organic group having at least one carbon atom; and n is an integer of 1 or above, which comprises reacting an unsaturated amide acid compound of formula (II): ##STR2## wherein D, R.sup.1, and n are as defined above, with an orthoester of formula (III): ##STR3## wherein R.sup.2 and R.sup.3, which may be the same or different, each represents a monovalent organic group having at least one carbon atom, to form an unsaturated dicarboxylic acid amide acid ester compound of formula (IV): ##STR4## wherein D, R.sup.1, R.sup.3, and n are as defined above, and then imidating the compound of formula (IV).
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: May 12, 1992
    Assignee: Matsushita Electric Works Ltd.
    Inventors: Tatsuo Yonemoto, Eiichiro Saito, Masahiro Matsumura
  • Patent number: 5099031
    Abstract: Di- and trialkyl-4'-phthalimidomethyl-furocoumarins are prepared by reacting di- or trialkyl-furocoumarins in the presence of an acid and, if appropriate, of a polar solvent with a compound of the formula (I) ##STR1## in which R" represents hydrogen, a second phthalimidomethyl group, C.sub.1 - to C.sub.4 -alkyl or C.sub.1 - to C.sub.6 -acyl,where, when using trialkyl-furocoumarins, R" does not represent hydrogen.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: March 24, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gamal Mikhail, Hans-Josef Buysch
  • Patent number: 5096901
    Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O-- or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl, andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereof and their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: March 17, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: Terence J. Ward, Janet C. White
  • Patent number: 5097034
    Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5095120
    Abstract: A process for preparing photochromic spiropyran compounds having a halogen atom or atoms and a hydrophobic alkyl group wherein a starting photochromic spiropyran compound having the hydrophobic alkyl group is reacted directly with a halogenating agent in a solvent. This reaction efficiently proceeds with the product being obtained in high yield.
    Type: Grant
    Filed: August 21, 1990
    Date of Patent: March 10, 1992
    Assignee: Matsushita Electric Industrial Co., Ltd.
    Inventors: Junichi Hibino, Eiji Ando
  • Patent number: 5086186
    Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with trichloracetyl isocyanate to produce novel N-trichloroacetyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as analgesic and antiinflammatory agents and/or intermediates for such agents.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: February 4, 1992
    Assignee: Pfizer Inc.
    Inventor: Sarah E. Kelly
  • Patent number: 5086171
    Abstract: Bis-(indolyl)ethylenes of the following general formula are prepared: ##STR1## wherein a is 1 or 2, wherein b is 1 or 2,wherein each A is independently selected from a dialkylamino, dialkoxyalkylamino, diaroxyalkylamino, diarylamino, alkylarylamino, dicyloalkylamino, alkylcycloalkylamino, arylcycloalkylamino, pyrrolidino, piperidino, or morpholino radical,wherein each B is independently selected from A or an alkoxy, alkoxyalkyl or aroxy radical,wherein each R is independently selected from hydrogen, halogen, alkyl, or alkoxy,wherein each of R.sup.5, R.sup.5', R.sup.6, and R.sup.6' are each independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), alkoxyalkyl, aroxyalkyl, halogen, phenyl, or phenyl substituted by alkyl or alkoxy,the alkyl moieties referred to herein being of one to eight carbons, the cycloalkyl moieties referred to herein being of three to six carbons.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: February 4, 1992
    Assignee: Appleton Papers Inc.
    Inventor: Ponnampalam Mathiaparanam
  • Patent number: 5053071
    Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: October 1, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Joseph E. Semple
  • Patent number: 5047552
    Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: September 10, 1991
    Assignee: American Home Products Corporation
    Inventors: Dominick A. Quagliato, Leslie G. Humber
  • Patent number: 5019587
    Abstract: The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, benzyl or C.sub.3 -C.sub.7 -cycloalkyl radical, B is hydrogen, R.sub.1 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl radical, R.sub.2 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.3 -C.sub.7 -cycloalkyl ring, n is 0, X is a valency bond or a C.sub.1 -C.sub.6 -alkylene radical, R.sub.3 is a carbocyclic aromatic ring, which may be substituted; and the tautomers, optically-active forms and physiologically acceptable salts thereof with organic and inorganic acids.
    Type: Grant
    Filed: June 5, 1989
    Date of Patent: May 28, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang V. Von Der Saal, Alfred Mertens, Erwin Boehm
  • Patent number: 5015661
    Abstract: Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.
    Type: Grant
    Filed: June 16, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4975455
    Abstract: Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: December 4, 1990
    Assignee: Adir et Cie
    Inventors: Jean-Daniel Brion, Guillaume Le Baut, Patrick Ducrey, Sylvie Piessard-Robert, Claude Cudennec, Genevieve Seurre
  • Patent number: 4970309
    Abstract: This invention relates to a novel method of synthesizing di- and triarylmethane dye precursor compounds possessing a thiolactone ring-closing moiety, from the corresponding lactones.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: November 13, 1990
    Assignee: Polaroid Corporation
    Inventor: Patrick F. King
  • Patent number: 4966973
    Abstract: The present invention relates to a compound of the formula ##STR1## wherein R.sup.1 stands for hydrogen or a lower alkyl; n denotes an integer of 1 to 6; X stands for an optionally oxidized sulphur atom, oxygen atom or an optionally substituted imino; R.sup.2 stands for methyl or an organic residual group bonded through methylene, methine a quaternary carbon; R.sup.3 stands for a lower alkyl; R.sup.4 stands for hydrogen or acyl; R.sup.5 and R.sup.6 each stand for a lower alkoxy or a lower alkyl, or R.sup.5 and R.sup.6 combinedly stand for butadienylene, and salts thereof.The compound (I) of the present invention has a strong 5-lipoxygenase inhibiting action, is of high safety and is useful as, among others, an agent for ameliorating dysfunction of circulatory system, an anti-allergic agent and a pharmaceutical agent for central nervous system.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: October 30, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Shigenori Ohkawa, Naohisa Fukuda
  • Patent number: 4952598
    Abstract: Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indollinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: August 28, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Lerch, Henning Rainer, Joachim Kaiser
  • Patent number: 4945168
    Abstract: Aryl-(1-phthalimido)-alkyl ketones of the general formula ##STR1## are prepared by reacting a suitable aromatic compound with ##STR2## at least one hydrogen atom on the aromatic nucleus in an inert solvent and in the presence of iron-(III)-chloride with an N-phthaloyl-2-amino carboxylic acid chloride of the general formula ##STR3## They can be converted into corresponding 2-phenethanolamines or 2-phenethylamines by reduction of the keto group.
    Type: Grant
    Filed: August 22, 1988
    Date of Patent: July 31, 1990
    Assignee: Degussa Aktiengesellschaft
    Inventors: Franz Effenberger, Dieter Steegmuller
  • Patent number: 4931566
    Abstract: Process for the preparation of 1,4-diketopyrrolo[3,4-c]pyrroles of the formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are phenyl, biphenyl or naphthyl radicals or aromatic O-heterocyclic, S-heterocyclic or N-heterocyclic radicals, by reacting 1 mole of a dicyclohexyl succinate, dialkyl succinate, monoalkylmonophenyl or diphenyl succinate, alkyl in the succinic acid ester radical being C.sub.1 -C.sub.18 alkyl and phenyl being phenyl which is unsubstituted or substituted by one or two halogen atoms or one or two C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy groups, with 2 moles of a nitrile of the formula II or III or with 1 mole of a nitrile of the formula II and 1 mole of a nitrile of the formula III ##STR2## in which R.sub.1 and R.sub.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: June 5, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Surber, Abul Iqbal, Christian Stern
  • Patent number: 4925839
    Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.
    Type: Grant
    Filed: June 24, 1988
    Date of Patent: May 15, 1990
    Assignee: American Home Products Corporation
    Inventors: Dominick A. Quagliato, Leslie G. Humber
  • Patent number: 4924004
    Abstract: New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkyl or cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is a alkylene chain which is optionally substituted by hydroxyl.
    Type: Grant
    Filed: October 28, 1988
    Date of Patent: May 8, 1990
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuehl, Gerd Buschmann, Stephen Magda
  • Patent number: 4921982
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: May 1, 1990
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 4908378
    Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: March 13, 1990
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings
  • Patent number: 4892973
    Abstract: Disclosed herein is a novel process for producing 1,1-diphenylalkenes, comprising contacting lead peroxide with 1,1-diphenylalkanes having the structure wherein a nitrogen atom of a tertiary amino group is bonded to the para-position of each of the two benzene rings of the 1,1-diphenylalkane, thereby obtaining the corresponding 1,1-diphenylalkenes.
    Type: Grant
    Filed: August 31, 1988
    Date of Patent: January 9, 1990
    Assignee: Yamada Chemical Co., Ltd.
    Inventors: Kozo Mizuno, Hideaki Fujisaki, Yoshinori Uda, Tadashi Imai, Katsuhiko Tsunemitsu
  • Patent number: 4892899
    Abstract: Composition of matter containing(a) a compound of the formula I ##STR1## in which A is one of the groups of the formulae ##STR2## in which B is --O--, --S--, --SO.sub.2 --, --N.dbd.N--, --CH.sub.2 --, --CH.dbd.CH--, ##STR3## --CONH--, --NHCONH--, or --CONHNHCO--, Q is --O-- or --NH-- and Z is --O-- or --S-- and R and R' are independently of each other hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or phenoxy, and(b) a compound of the formula II ##STR4## in which A' is as defined above for A, D is hydrogen, amino or a group of the formula III ##STR5## E is --O-- or --S--, T.sub.1, T.sub.2 and T.sub.3 independently of one another are chlorine or a group --ET', T' is a group of the formulae ##STR6## X.sup..sym. is H.sup..sym. or a group of the formulae M.sup.n.sym. /n or N.sup..beta. (R.sub.1)(R.sub.2)(R.sub.3)(R.sub.4), Mhu n.sym. is an n-valent metal cation, n is 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently of one another hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: January 9, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Edward E. Jaffe, Jost von der Crone, Bernhard Medinger