Abstract: Hydantoin compounds are described of the formula (I) : ##STR1## wherein R.sup.1 is phenyl, C.sub.1-4 hydroxyalkyl or carboxy C.sub.1-4 alkyl and wherein R.sub.2 is C.sub.1-6 alkyl. The compounds are useful in the prophylactic treatment of immediate hypersensitivity diseases including asthma.
Type:
Grant
Filed:
May 14, 1979
Date of Patent:
October 28, 1980
Assignee:
Eli Lilly Industries Limited
Inventors:
William B. Jamieson, William J. Ross, Robin G. Simmonds, John P. Verge
Abstract: Crystalline monohydrate (Form III) and anhydrate (Form IV) of N-2-(6-methoxy)benzothiazolyl-N'-phenylurea (frentizole) are stable, have a greater bulk density, are less electrostatic and more freely flowing than previous crystalline forms.
Type:
Grant
Filed:
February 9, 1979
Date of Patent:
September 16, 1980
Assignee:
Eli Lilly and Company
Inventors:
Lewis C. Lappas, Leslie J. Lorenz, James H. Wikel
Abstract: A process for preparing antidepresssant 2-phenylbicyclooctylamines of formula (I): ##STR1## where R.sup.1 and R.sup.2 represent C.sub.1-3 alkyl and Ar represents a phenyl group optionally substituted by up to two halogen atoms, by reduction of a novel enamine intermediate of formula: ##STR2## where R.sup.3 and R.sup.4 are hydrogen or taken together represent a single bond and where X is hydrogen, bromine or chlorine.
Abstract: Vindesine is prepared by converting 4-desacetyl VLB C-3 carboxhydrazide to the corresponding azide with a nitrite such as n-butyl nitrite in THF and then reacting the thus formed azide with triphenylphosphine to yield an intermediate acyl iminophosphorane, which compound is decomposed with acid to yield vindesine of high purity and in good yield.
Abstract: Vinblastine (vincaleucoblastine, VLB) and other anti-mitotic vinca alkaloid is useful in the treatment of rheumatoid arthritis and related diseases, alone or in combination with an anti-inflammatory agent.
Abstract: Benzimidazolyl, benzothiazolyl and benzoxazolyl ureas and thioureas are employed as immune regulatory agents, as agents capable of altering the immune response in mammals.
Abstract: Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids are useful as anti viral and anti-neoplastic agents or as intermediates in the preparation of such agents.
Abstract: 6-n-Propyl (ethyl or allyl)-8.beta.-methoxy-(methylsulfinyl, methylsulfonyl, or methylmercapto) methylergolines, 8-ergolenes or 9-ergolenes, useful as prolactin inhibitors and in the treatment of Parkinsonism.
Abstract: Bridged vinca dimers in which two indole-dihydro-indole C-3 carboxamides are linked through the nitrogen atom of a carboxamide group, useful as oncolytic agents.
Abstract: 4-Desacetoxy-4.alpha.-hydroxyvinblastine, prepared by reduction of 4-desacetoxy-4-oxovinblastine, and derivatives thereof, useful as antimitotic agents.
Abstract: A solution of nabilone and PVP in anhydrous ethanol is used to granulate ethanol-insoluble pharmaceutically-acceptable excipients such as starch.