Chalcogen Attached Indirectly To The Bicyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/509)
  • Patent number: 4824961
    Abstract: Process for the production of substituted 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acids having useful analgesic and anti-inflammatory activity.
    Type: Grant
    Filed: August 27, 1987
    Date of Patent: April 25, 1989
    Assignee: American Home Products Corporation
    Inventors: Chia-Cheng Shaw, Karel Pelz
  • Patent number: 4758586
    Abstract: Indolyl dieneoic acids and esters are disclosed possessing valuable pharmaceutical activity, particularly as lipoxygenase inhibitors with anti-inflammatory and anti-allergic properties.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: July 19, 1988
    Assignee: USV Pharmaceutical Corp.
    Inventors: Wan-kit Chan, Thomas D. Lee, Fu-chih Huang
  • Patent number: 4742077
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## whereby R.sub.4 and R.sub.5 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and X represents oxygen, sulfur, imino, lower alkylimino, --(CH.sub.2)--, --(S.CH.sub.2)-- or --(O.CH.sub.2)--,R.sub.2 represents hydrogen or lower alkyl,R.sub.3 represents a group of formula ##STR3## whereby R.sub.6, R.sub.7 and R.sub.8 are the same or different and represent hydrogen or alkyl or R.sub.6 together with R.sub.7 or R.sub.7 together with R.sub.8 represent --(CH.sub.2).sub.m -- wherein m is 3 to 6,R.sub.9 represents alkyl, alkenyl, trialkylsilyl or alkyl substituted by hydroxy, lower alkoxy, lower halogenalkyl or aryl andn stands for 1, 2 or 3,which possess pharmaceutical in particular antimycotic activity as well as activity against phytopathogenic fungi.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: May 3, 1988
    Assignee: Sandoz Ltd.
    Inventor: Anton Stutz
  • Patent number: 4740519
    Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: April 26, 1988
    Assignee: Centre International de Recherches Dermatologiques C.I.R.D.
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 4680307
    Abstract: A compound of the formula: ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group, Y.sup.1 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or C.sub.1 -C.sub.4 alkyl group), ##STR4## (R.sup.6 is as defined above), ##STR5## R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a shingle linkage to from a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.
    Type: Grant
    Filed: January 26, 1984
    Date of Patent: July 14, 1987
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masami Muraoka, Toshio Nakamura, Akihiko Sugie, Keiichi Ono, Michihiro Yamamoto
  • Patent number: 4675405
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is --O--, --S--, ##STR3## when n=0, or W is ##STR4## when n=1, and the dotted line represents an optional double bond; Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR5## n is 0-1; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is loweralkyl, perfluoroloweralkyl or perfluorophenyl, with the proviso that when X=N, W=O or S and n=0, R.sup.3 is other than loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.
    Type: Grant
    Filed: January 27, 1986
    Date of Patent: June 23, 1987
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III
  • Patent number: 4661511
    Abstract: Pharmaceutical compositions are provided containing a 2-(hydroxyphenyl)-indole or a 2-(C.sub.2 -C.sub.6 -alkanoxyloxyphenyl) indole and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 27, 1984
    Date of Patent: April 28, 1987
    Assignee: Degussa Aktiengesellschaft
    Inventors: Erwin von Angerer, Helmut Schonenberger
  • Patent number: 4656182
    Abstract: Substituted trans-1,2-diaminocyclohexyl amide compounds demonstrating selective opioid receptor binding possess utility as analgesic, diuretic, and psychotherapeutic agents. A method of preparing the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain employing the compounds are also disclosed.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: April 7, 1987
    Assignee: Warner-Lambert Company
    Inventor: David Horwell
  • Patent number: 4581457
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is ##STR3## Y is ##STR4## n is 0-8; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.
    Type: Grant
    Filed: September 21, 1984
    Date of Patent: April 8, 1986
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak
  • Patent number: 4537903
    Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophilic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.
    Type: Grant
    Filed: October 12, 1983
    Date of Patent: August 27, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Milton L. Hammond, Norman P. Jensen, John McDonald, Robert A. Zambias
  • Patent number: 4496742
    Abstract: Novel structural analogues of 5,6-dihydro PGI.sub.2 of the formula: ##STR1## and the corresponding 10,11-didehydro-11-deoxy derivatives are useful as antiallergy agents.
    Type: Grant
    Filed: October 4, 1982
    Date of Patent: January 29, 1985
    Assignee: The Upjohn Company
    Inventor: Herman W. Smith
  • Patent number: 4485242
    Abstract: 3-[(Alkoxy)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with alcohols in the presence of a base.
    Type: Grant
    Filed: July 30, 1981
    Date of Patent: November 27, 1984
    Assignee: Sterling Drug Inc.
    Inventors: Paul J. Schmidt, William M. Hung
  • Patent number: 4476310
    Abstract: A process for the preparation of indoles which comprises reacting aniline or a derivative thereof with a 1,2-glycol in the presence of a catalyst comprising silver supported on a carrier having a specific surface area of not less than 10 m.sup.2 /g.
    Type: Grant
    Filed: June 9, 1982
    Date of Patent: October 9, 1984
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Tadatoshi Honda, Fujio Matsuda, Tadamitsu Kiyoura, Kazuhiro Terada
  • Patent number: 4424365
    Abstract: Novel antibacterially active compound, 1,2,8,8a-cyclopropa?c!benzo?1,2-b:-4,3-b'!dipyrrol-4(5H)-one, prepared by a novel chemical process. This compound, as well as antibacterially-active intermediates, can be used to eradicate or control susceptible bacteria, for example B. subtilis, K. pneumonia, S. lutea, S. aureus, and M. avium.
    Type: Grant
    Filed: June 22, 1982
    Date of Patent: January 3, 1984
    Assignee: The Upjohn Company
    Inventor: Wendell Wierenga
  • Patent number: 4424231
    Abstract: There are described compounds of formula I, ##STR1## in which Ra, Rb, Rc, Rd, Re, Rf and Rg, which may be the same or different, each represent hydrogen, amino, hydroxy, alkoxy, alkenyloxy, halogen, acyl, alkenyl, alkyl, or alkoxy substituted by phenyl,Rh is hydrogen, alkyl or --COOH.X is a hydrocarbon chain containing from 2 to 10 carbon atoms and optionally substituted by a hydroxy group,A has no significance or represents Y, OY, or SY and Y represents a C 1 to 4 hydrocarbon chain which is optionally substituted by alkyl C 1 to 4,E and G, which may be the same or different, each represent --O--, --S-- or --CH.sub.2 --, provided that at least one of E and G is --O-- or --S--,L, together with the carbon atoms to which it is attached, forms a benzene, furan, thiophene, pyrrole, or pyran-2-one ring,and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: March 19, 1982
    Date of Patent: January 3, 1984
    Assignee: Fisons Limited
    Inventors: John R. Bantick, John Fuher, David N. Hardern, Thomas B. Lee
  • Patent number: 4423229
    Abstract: Novel antibacterially-active compound, 1,2,8,8a-cyclopropa[ c]-benzo[1,2-b:-4,3-b']dipyrol-4(5H)-one, prepared by a novel chemical process. This compound, as well as antibacterially-active intermediates, can be used to eradicate or control susceptible bacteria, for example, B. subtilis, K. pneumonia, S. lutea, S. aureus, and M. avium.
    Type: Grant
    Filed: February 8, 1982
    Date of Patent: December 27, 1983
    Assignee: The Upjohn Company
    Inventor: Wendell Wierenga