Abstract: Octahydro-2H-pyrrolo[3,4-g]quinolines, useful as dopamine agonists, particularly as inhibitors of prolactin secretion and in treatment of Parkinsonism.
Abstract: This invention relates to a novel process for inhibiting the growth of malignant tumor cells in mammals, particularly the growth of multiple myeloma in humans, employing the alkaloid acronycine as the inhibiting agent.
Abstract: Vincristine is prepared from VLB sulfate or free base by oxidation with an acidic ferrous perchloratehydrogen peroxide oxidation reagent at about -30.degree. C.
Abstract: Novel hydantoin compounds are described of the formula (I): ##STR1## wherein Ar is phenyl optionally substituted by up to three radicals selected from the group comprising C.sub.1-6 alkoxy, halogen, 1,3-dioxol-2-yl, hydroxy C.sub.1-4 alkoxy C.sub.1-4 alkyl, phenyl, hydroxyl, nitrile, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl, C.sub.2-4 alkenyloxy, C.sub.1-4 alkoxycarbonyl or phenoxy optionally substituted by C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or halogen;or is thiophene optionally substituted by phenyl or by one or two C.sub.1-4 alkyl groups;R.sup.1 and R.sup.2 are independently hydrogen or taken together represent a chemical bond;R.sup.3 is hydrogen, C.sub.1-6 alkyl or C.sub.2-4 alkenyl; andR.sup.4 is C.sub.1-6 alkyl, C.sub.2-4 alkenyl, phenyl or benzyl;provided that R.sup.3 cannot be hydrogen when Ar is unsubstituted phenyl and R.sup.4 is n-butyl. The compounds are useful in the treatment of immediate hypersensitivity diseases including asthma.
Type:
Grant
Filed:
May 12, 1980
Date of Patent:
October 6, 1981
Assignee:
Lilly Industries Limited
Inventors:
William B. Jamieson, William J. Ross, Robin G. Simmonds, John P. Verge
Abstract: Novel oxiodinium and thiaiodinium compounds having a superior inhibitory effect against micro-organisms coupled with outstanding stability and low toxicity are described.
Abstract: Octahydro-2H-pyrrolo[3,4-g]quinolines, useful as dopamine agonists, particularly as inhibitors of prolactin secretion and in treatment of Parkinsonism.
Abstract: Compounds of formula I ##STR1## wherein either R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 and R.sup.2, taken together, represent a group of formula (a): ##STR2## in which R.sup.5 is hydrogen, halogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen or a group of formula (b): ##STR3## in which R.sup.6 is hydrogen or C.sub.1-4 alkyl, and R.sup.4 is hydrogen or a group of formula --CHR.sup.7 COOH, where R.sup.7 is hydrogen or C.sub.1-4 alkyl,provided that:(i) when R.sup.3 is a group of formula (b), then R.sup.1, R.sup.2 and R.sup.4 are all hydrogen,(ii) when R.sup.3 is hydrogen, then R.sub.4 is --CHR.sup.7 COOH, and(iii) when R.sup.1 and R.sup.2, together, represent a group of formula (a), then R.sub.3 is hydrogen;possess pharmacological activity, in particular anti-inflammatory activity and are particularly useful in treatment of rheumatoid arthritis.
Abstract: Stable polymorphic crystalline form of trans-dl-1-hydroxy-3-(1',1'-dimethylheptyl)-6,6-dimethyl-6,6a,7,8,-10,10a- hexahydro-9H-dibenzo[b,d]pyran-9-one, capable of producing significant blood levels in mammals for long periods of time after oral administration of the drug.
Abstract: Isoquinoline compounds of the following formula are described: ##STR1## wherein the moiety A-B represents a group of formula;--CH.sub.2 --NR.sup.3 -- or --NR.sup.3 --CH.sub.2 --;wherein R.sup.3 represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-4 alkyl, optionally substituted benzyl, C.sub.3-6 alkenyl or C.sub.1-4 alkanoyl;wherein R represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or optionally substituted benzyl;wherein R.sup.1 and R.sup.2 each represent hydrogen or taken together represent a chemical bond; and wherein X is hydrogen or halogen; or an acid-addition salt thereof.The compounds are pharmaceuticals and especially useful in the treatment of disorders of the central nervous system.
Abstract: 4a-Arylhexahydro-1H-2-pyrindines and 4a-aryloctahydroquinolines analgesic agonists and antagonists are prepared doubly alkylating a 4-aryltetrahydropyridine with an .alpha.,.omega.-dihaloalkane.
Abstract: Amino-substituted-4,5,6,7-tetrahydro-1H (or 2H)-indazoles, useful as prolactin inhibitors and in treatment of Parkinson's Syndrome. Intermediate 6-keto(or 6-alkoxy or benzyloxy)-4,5,6,7-tetrahydro-1H (or 2H)-indazoles are also disclosed.
Abstract: Introduction of a pharmaceutically acceptable non-toxic cation salt of a straight-chain or branched chain alkyl sulfonate having from 11 to 16 carbon atoms into the uterine lumen or vaginal cavity prevents conception. Sodium tetradecyl sulfonate is preferred.
Type:
Grant
Filed:
April 8, 1980
Date of Patent:
April 28, 1981
Assignee:
Eli Lilly and Company
Inventors:
Ronald E. Zimmerman, Philip J. Burck, C. David Jones, Arvind L. Thakkar
Abstract: Introduction of a pharmaceutically acceptable non-toxic cation salt of a sterol sulfate into the uterine lumen or vaginal cavity prevents conception. Potassium or pyridinium .beta.-sitosteryl sulfate is preferred.
Type:
Grant
Filed:
April 8, 1980
Date of Patent:
April 28, 1981
Assignee:
Eli Lilly and Company
Inventors:
Philip J. Burck, Ronald E. Zimmerman, Arvind L. Thakkar