Tropane And Oxirane In The Tricyclo Ring System Patents (Class 546/91)
  • Patent number: 5258388
    Abstract: Compounds of the formula ##STR1## wherein: pounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
    Type: Grant
    Filed: August 18, 1992
    Date of Patent: November 2, 1993
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 4783534
    Abstract: The invention relates to novel N-alkylnorscopines wherein the alkyl group may have 2 to 10 carbon atoms, which are useful in the preparation of valuable pharmaceutical compositions. These compounds may be prepared from the corresponding N-alkylnorscopolamines by hydrogenolysis with complex hydrides, which reaction is preferably carried out with sodium borohydride in ethanol at ambient temperature.
    Type: Grant
    Filed: March 31, 1987
    Date of Patent: November 8, 1988
    Assignee: Boehringer Ingelheim KG
    Inventor: Rolf Banholzer
  • Patent number: 4755603
    Abstract: Norscopine is prepared from norscopolamine by hydrogenation cleavage with a complex hydride in an inert solvent at room temperature.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: July 5, 1988
    Assignee: Boehringer Ingelheim KG
    Inventor: Rolf Banholzer
  • Patent number: 4608377
    Abstract: The invention herein relates to novel quaternary 6,11-dihydro-dibenzo-[b,e]-thiepine-11-N-alkylnorscopine ethers, the preparation thereof, and their use as spasmolytics or bronchospasmolytics.
    Type: Grant
    Filed: June 25, 1984
    Date of Patent: August 26, 1986
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Rudolf Bauer
  • Patent number: 4558054
    Abstract: The invention relates to new products, namely endo-8,8-dialkyl-8-azoniabicyclo [3.2.1] octane-6,7-exo-epoxy-3-alkylcarboxylates, of formula: ##STR1## in which R.sub.1 and R.sub.2, which can be the same or different, are linear or branched alkyl radicals of 1-5 C atoms or cycloalkyl radicals of 3-6 C atoms;R.sub.3 and R.sub.4, which can be the same or different, are alkyl radicals of 1-6 C atoms;X.sup.- is a halide ion.The new compounds are powerful spasmolytics.
    Type: Grant
    Filed: July 6, 1984
    Date of Patent: December 10, 1985
    Assignee: Valeas S.p.A.
    Inventors: Virgilio Bernareggi, Fausto Bonifacio, Roberto Margutti, Maurizio Fano
  • Patent number: 4379936
    Abstract: 3.alpha.-Benzoylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with benzylamine in the presence of phenol.
    Type: Grant
    Filed: April 19, 1982
    Date of Patent: April 12, 1983
    Assignee: Sterling Drug Inc.
    Inventor: Robert L. G. Clarke
  • Patent number: 4341895
    Abstract: 3.alpha.-Benzylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with enzylamine in the presence of phenol.
    Type: Grant
    Filed: March 3, 1981
    Date of Patent: July 27, 1982
    Assignee: Sterling Drug Inc.
    Inventor: Robert L. Clarke
  • Patent number: 4139534
    Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorpinan has been found to posess potent agonist/antagonist activity as a non-narcotic analgesic. An improved total snythesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline. A preferred feature of the process involves borane reduction of 2-cyclobutylcarbonyl-9,10-dihydroxy-1-(p-methoxybenzyl)perhydroisoquinolin e (Va) to provide the corresponding cyclobutylmethyl derivative complexed with borane which is converted directly to N-cyclobutylmethyl-14.beta.-hydroxy-3-methoxymorphinan (LVa) by treating with acid.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: February 13, 1979
    Assignee: Bristol-Myers Company
    Inventors: Gary Lim, Ivo Monkovic
  • Patent number: 4132710
    Abstract: [2]Benzopyrano[3,4-c]pyridine derivatives characterized by having a 2,3,4,4a,6,10b-hexahydro-1H-[2]benzopyrano[3,4-c]pyridine nucleus bearing a substituent at position 6 are disclosed. The nucleus can be optionally further substituted at positions 2,3,4,6 and on the aromatic ring. The derivatives are useful diuretic, anorexic, antidepressant, anticonvulsant and antihypertensive agents. Methods for their preparation and use also are disclosed.
    Type: Grant
    Filed: December 20, 1976
    Date of Patent: January 2, 1979
    Assignee: Ayerst, McKenna and Harrison, Ltd.
    Inventors: Jean A. Gauthier, Leslie G. Humber, Clara Revesz