Chalcogen Bonded Directly To The Tricyclo-carbocyclic Ring System Patents (Class 546/204)
  • Patent number: 4310668
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: January 12, 1982
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4310529
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: January 12, 1982
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4275070
    Abstract: The levorotatory enantiomers of 3-methoxy cyproheptadine and a related compound are antipsychotic agents.
    Type: Grant
    Filed: May 19, 1980
    Date of Patent: June 23, 1981
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Patent number: 4237133
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2)is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: December 2, 1980
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4188495
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: November 14, 1977
    Date of Patent: February 12, 1980
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4160031
    Abstract: 10,11-Dihydro-3-carboxycyproheptadine is disclosed to have pharmaceutical utility as an appetite stimulant and as an antihistaminic agent. Also disclosed are processes for the preparation of such compound; pharmaceutical compositions comprising such compound; and methods of treatment comprising administering such compound and compositions.
    Type: Grant
    Filed: November 22, 1976
    Date of Patent: July 3, 1979
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Patent number: 4141992
    Abstract: 2,6 Anthraquinonylene cycloalkylcarboxamidines and halobenzamidines that are effective against cecal and hepatic amebic infestations in warm-blooded animals, methods of treatment therewith and therapeutic compositions thereof.
    Type: Grant
    Filed: July 13, 1977
    Date of Patent: February 27, 1979
    Assignee: American Cyanamid Company
    Inventors: Stanley A. Lang, Jr., Yang-I Lin, Thomas L. Fields, Paul F. Fabio, Keith C. Murdock
  • Patent number: 4137331
    Abstract: This invention provides new compounds of formula I, ##STR1## wherein Het is a radical formed by removing one of the hydrogens from the phenyl ring of 2-indolinone or fluorenone, andR is the group A, B, C or D, ##STR2## wherein N IS THE NUMBER 2 OR 3,n' is the number 1, 2, 3 or 4, andX-x' is ethylene or vinylene,Wherein in group D each of the two C atoms adjacent to the N atom are identically substituted by hydrogen or by one or two alkyl groups of 1 to 4 carbon atoms useful as antiarrhythmic agents.
    Type: Grant
    Filed: December 16, 1976
    Date of Patent: January 30, 1979
    Assignee: Sandoz Ltd.
    Inventors: Richard Berthold, Franz Troxler
  • Patent number: 4132796
    Abstract: Cyproheptadine derivatives substituted with a trifluoromethylsulfinyl group in one of the benzo rings and having an alkyl group, either unsubstituted or substituted with a hydroxy or cycloalkyl group, on the piperidine nitrogen are potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects that are experienced with most major tranquilizers. The novel compounds are generally prepared by treatment of the intermediate 5-carbinol with a dehydrating reagent, or by alkylation of the piperidine nitrogen with the appropriate alkyl or substituted alkyl group.
    Type: Grant
    Filed: December 1, 1977
    Date of Patent: January 2, 1979
    Assignee: Merck & Co., Inc.
    Inventor: David C. Remy
  • Patent number: 4131673
    Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
    Type: Grant
    Filed: June 7, 1977
    Date of Patent: December 26, 1978
    Assignees: Mitsubishi Chemical Industries, Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
  • Patent number: 4130561
    Abstract: Compounds of the formula ##STR1## where R.sub.4 X is a polycyclocoupled group and R.sub.1 and R.sub.2 are H or simple hydrocarbon and R.sub.3 has the same value and additionally simple acyl, can be made by a variety of syntheses. They have hypolipedemic and antiatherosclerotic properties, and are useful in that field.
    Type: Grant
    Filed: May 26, 1977
    Date of Patent: December 19, 1978
    Assignee: The Upjohn Company
    Inventor: Daniel Lednicer
  • Patent number: 4127717
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; R.sub.1 is alkanoyl; and R.sub.2 is a tertiary amino group; have hypotensive activity.
    Type: Grant
    Filed: March 20, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Patent number: 4125604
    Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
    Type: Grant
    Filed: June 7, 1977
    Date of Patent: November 14, 1978
    Assignees: Mitsubishi Chemical Industries Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura