Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/427)
  • Patent number: 4618683
    Abstract: Disclosed herein are tetrahydro-benzo[e]isoindolines represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are independently selected from hydrogen, loweralkyl of 1 to 4 carbon atoms, hydroxy, loweralkoxy of 1 to 3 carbon atoms, allyloxy, benzyloxy, benzoyloxy, thiomethyl, halo, ##STR2## wherein t is 0 or 1, n is 0 to 5 and R.sub.11 and R.sub.14 are independently selected from hydrogen, halo, hydroxy, loweralkyl of 1 to 4 carbon atoms, loweralkoxy of 1 to 3 carbon atoms or amino; orR and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen and the proviso that two of R, R.sub.1, or R.sub.2 must be other than methoxy in the 7 and 8 positions when the remaining one of R, R.sub.1 or R.sub.2 is hydrogen; andR.sub.
    Type: Grant
    Filed: November 20, 1984
    Date of Patent: October 21, 1986
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Daniel J. Kerkman, William J. McClellan
  • Patent number: 4614805
    Abstract: The invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR1## in which n denotes 0 or 1, A denotes --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S--, O-- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R.sup.
    Type: Grant
    Filed: September 6, 1985
    Date of Patent: September 30, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hansjorg Urbach, Rainer Henning, Reinhard Becker
  • Patent number: 4599410
    Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.
    Type: Grant
    Filed: February 19, 1985
    Date of Patent: July 8, 1986
    Assignee: Eastman Kodak Company
    Inventor: Wolfgang H. H. Gunther
  • Patent number: 4598156
    Abstract: Indoles of the formula I which are unsubstituted in the 2- and 3-positions: ##STR1## wherein Z is hydrogen or a group --COR, and X and Y have the meanings defined in claim 1, can be produced by a novel, simple and economical process which comprises reacting a compound of the formula II ##STR2## at a temperature of between 0.degree. and 120.degree. C., in the presence of a mercury or palladium catalyst, with benzoic acid vinyl ester, or with the vinyl ester of an aliphatic C.sub.1 -C.sub.4 -monocarboxylic acid; and optionally saponifying compounds of the formula I in which Z is --COR. The compounds of the formula I can be used for example for producing indigo dyes, or they can be used as pharmaceutical or agricultural active substances.
    Type: Grant
    Filed: February 7, 1983
    Date of Patent: July 1, 1986
    Assignee: Ciba Geigy Corporation
    Inventor: Pierre Martin
  • Patent number: 4578470
    Abstract: Phthalimides and the like in which the substituent on the imide nitrogen is a highly electron-deficient group may be prepared by the reaction of the appropriate amine with phthalic anhydride. These imides are useful for the preparation of polyimides by reaction with diamines.
    Type: Grant
    Filed: June 20, 1983
    Date of Patent: March 25, 1986
    Assignee: General Electric Company
    Inventor: Jimmy L. Webb
  • Patent number: 4560688
    Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3, or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optional double bond, R.sup.2 being absent if the double bond is present, and Y is substiuted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.
    Type: Grant
    Filed: February 8, 1984
    Date of Patent: December 24, 1985
    Assignee: Schering Corporation
    Inventor: Frank J. Villani
  • Patent number: 4546107
    Abstract: 1,4-Methano-2,3,4,5-tetrahydro-1H-2-benzazepin-3-one derivatives of the formula: ##STR1## wherein X is halogen, n is 1 or 2, and R is hydrogen, lower alkyl or phenyl-lower alkyl. They are useful as medicaments, e.g. cerebral dysfunction-improving drugs, anti-convulsants, anti-epileptics and anti-anxiety drugs.
    Type: Grant
    Filed: May 7, 1984
    Date of Patent: October 8, 1985
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tetsuya Tahara, Masafumi Arita, Tsuyoshi Kuroda
  • Patent number: 4535085
    Abstract: A perfluorotricyclic amine compound which is usable as an oxygen carrier in an artificial blood, represented by the general formula ##STR1## wherein R denotes a perfluoroalkyl group having 1-4 carbon atoms; the ring A denotes a five- or six-membered ring, the ring B denotes a five-, six- or seven-membered ring, the ring C denotes a five- or six-membered ring any one of the rings A, B and C optionary being substituted by one or more lower perfluoroalkyl group in addition to the above-mentioned substituent R; and further f, g, h, i, j and k denote integers appropriately selected to construct the above-mentioned size of rings A, B, and C; is prepared by reacting the corresponding perhydrotricyclic amine with fluorine.
    Type: Grant
    Filed: March 29, 1983
    Date of Patent: August 13, 1985
    Assignee: The Green Cross Corporation
    Inventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
  • Patent number: 4529736
    Abstract: This disclosure describes 3a-(substituted-phenyl)-2,3,3a,4,7,7a-hexahydro[or 3a-(substituted-phenyl) octahydro]-4,7-alkano-1H-isoindoles which possess activity as antidepressants and as antistress agents in mammals.
    Type: Grant
    Filed: April 6, 1983
    Date of Patent: July 16, 1985
    Assignee: American Cyanamid Company
    Inventors: Thomas C. McKenzie, William J. Fanshawe, Joseph W. Epstein
  • Patent number: 4513142
    Abstract: A method of preparation of cationic dyestuffs having the formula ##STR1## wherein A, B, R, and R.sup.1 are defined in the specification carried out in the substantial absence of solvent and removing water formed in the reaction.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: April 23, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roderich Raue, Volker Huhne, Hans-Peter Kuhlthau
  • Patent number: 4510157
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: April 9, 1985
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4494547
    Abstract: Isoindoledione compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.3 each separately is phenyl, substituted phenyl, alkyl of 1 to 4 carbons, --CHO, --CH.sub.2 OR.sub.6, --CO.sub.2 R.sub.6, --COR.sub.6, hydrogen, or together with R.sub.2 is a divalent alkyl or alkenyl group of 3 to 5 carbons which form a cyclic ring;R.sub.2 is phenyl, substituted phenyl, --CH.sub.2 OR.sub.6, --CH.sub.2 CH.sub.2 OR.sub.6, alkyl of 1 to 4 carbons or with either R.sub.1 or R.sub.3 is a divalent alkyl or alkenyl group of 3 to 5 carbons which form a cyclic ring;R.sub.4 and R.sub.5 which may be the same or different each separately is hydrogen, alkyl of 1 to 4 carbons, --OR.sub.6, --CO.sub.2 R.sub.6, --COR.sub.6, --CHO, --CH.sub.2 OR.sub.6 or together R.sub.4 and R.sub.5 is a butadiene radical which forms a benzene ring;R.sub.6 is hydrogen or alkyl of 1 to 4 carbons; provided that R.sub.1 and R.sub.3 are not both phenyl and that when R.sub.4 and R.sub.5 are both hydrogen, R.sub.1, R.sub.2 and R.sub.3 are not all methyl.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: January 22, 1985
    Assignee: North Carolina Central University
    Inventor: John A. Myers
  • Patent number: 4454150
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: October 19, 1981
    Date of Patent: June 12, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4444981
    Abstract: A compound of formula (II): ##STR1## wherein R is a C.sub.1-4 alkyl group;R.sub.1 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;and pro-drugs thereof; and the pharmaceutically acceptable salts of the compounds of formula (II) and of their pro-drugs; has useful anti-inflammatory and analgesic activity.
    Type: Grant
    Filed: July 25, 1980
    Date of Patent: April 24, 1984
    Assignee: Beecham Group Limited
    Inventor: Alexander C. Goudie
  • Patent number: 4440779
    Abstract: Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.
    Type: Grant
    Filed: June 4, 1982
    Date of Patent: April 3, 1984
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Conrad P. Dorn, Bruce E. Witzel, Debra L. Allison, Tsung-Ying Shen
  • Patent number: 4370341
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: December 11, 1980
    Date of Patent: January 25, 1983
    Assignee: Ayerst, McKenna & Harrison, Ltd.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4359423
    Abstract: A compound of formula (II): ##STR1## wherein R is a C.sub.1-4 alkyl group;R.sub.1 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;and pro-drugs thereof; and the pharmaceutically acceptable salts of the compounds of formula (II) and of their pro-drugs; has useful anti-inflammatory and analgesic activity.
    Type: Grant
    Filed: July 25, 1980
    Date of Patent: November 16, 1982
    Assignee: Beecham Group Limited
    Inventors: Alexander C. Goudie, Robert W. Ward
  • Patent number: 4351842
    Abstract: Compounds of the general formula: ##STR1## in which A is a benzene ring or a carbocyclic aromatic group consisting of two or three fused benzene rings, the group A being linked to the nitrogen containing ring at two adjacent carbon atoms and the benzene ring or each benzene ring optionally carrying one or more substituents which may be the same or different, and may be alkyl, aryl, halo, hydroxy, acyloxy or alkoxy, or two adjacent positions in a ring may be substituted so as to form a methylene dioxy group (--O--CH.sub.2 --O--);R.sub.1 and R.sub.2 which may be the same or different, each represent hydrogen; an alkyl group which contains 1 to 6 carbon atoms and which may be substituted; a hydroxycarbonyl or an alkoxycarbonyl group; andone of R.sub.3 and R.sub.4 represents hydrogen, an alkyl group which contains 1 to 6 carbon atoms and which may be substituted, or a hydroxy, alkoxy, hydroxycarbonyl or alkoxycarbonyl group and the other of R.sub.3 and R.sub.
    Type: Grant
    Filed: July 21, 1980
    Date of Patent: September 28, 1982
    Assignee: Glaxo Laboratories Limited
    Inventor: Richard J. Coles