Abstract: A process for preparing 1-alkyl-6-oxodecahydroquinolines in 5 steps--a quaternization, hydrogenation, two organometallic reductions and hydrolysis of the thus formed enol ether--from 6-alkyloxyquinoline and intermediates useful therein.
Abstract: 4aR,8aR-5-permissibly substituted-6-oxo-octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines. The compounds are useful as intermediates in preparing dopamine D-2 agonists.
Abstract: Trans-(.+-.)-1-permissibly-substituted-2,6-dioxodecahydroquinoline or enantiomers thereof, intermediates for preparing tautomeric trans-(.+-.)-5-permissibly substituted octahydro-1H(and 2H)pyrazolo[3,4-g]quinolines, 4aR,8aR or 4aS,8aS enantiomers thereof, for preparing trans-(.+-.)-5-permissibly substituted-octahydropyrazolo (or oxazolo)[4,5-g]quinoline, 4aR,8aR or 4aS,8aS enantiomers thereof or for preparing trans-(.+-.)-6-permissibly-substituted octahydropyrimido[4,5-g]quinolines, a 5aR,9aR or 5aS,9aS enantiomer thereof said racemic intermediates being comprised of stereoisomers of the following formulas ##STR1## wherein R is H, alkyl or C.sub.1-3 straight-chain alkyl.
Abstract: There are described compounds of the formula ##STR1## in which either R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 is carboxyl and R.sup.2 is hydrogen, C.sub.3-4 alkenyl or C.sub.1-4 alkyl, and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, nitro, hydroxyl, carboxyl, carboxyC.sub.1-2 alkoxy, C.sub.3-4 alkenyl, C.sub.1-4 alkyl, C.sub.3-4 alkenyloxy, C.sub.1-4 alkoxy or the group ##STR2## where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; and salts and esters thereof. The compounds are indicated for use in the treatment of immediate sensitivity reactions and inflammatory diseases.
Type:
Grant
Filed:
November 30, 1983
Date of Patent:
July 30, 1985
Assignee:
Lilly Industries Limited
Inventors:
Stephen R. Baker, Terry D. Lindstrom, William B. Jamieson, William J. Ross
Abstract: 4aR,8aS,9R-5-C.sub.1-3 straight-chain alkyl (methyl, ethyl or n-propyl) or allyl-9-hydroxy-octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines useful as hypotensives.
Abstract: 2-Fluoro-17.beta.-estradiol is synthesized by mercurating a 17.beta.-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.
Abstract: Sexual dysfunction in mammals is treated with a trans-(.+-.)- or trans-(-)-2-amino-4-permissibly-substituted-6-loweralkyl or allyl octahydropyrimido[4,5-g]quinoline or a pharmaceutically-acceptable acid addition salt thereof.
Abstract: Trans-(.+-.) or trans-(-)-2,4-permissibly-substituted-6-alkyl or allyl octahydropyrimido[4,5-g]quinolines and related compounds, ultraviolet light absorbers.
Type:
Grant
Filed:
September 26, 1983
Date of Patent:
March 26, 1985
Assignee:
Eli Lilly and Company
Inventors:
Cynthia L. Nichols, Edmund C. Kornfeld, John M. Schaus
Abstract: Trans-(.+-.)-2-Amino or substituted amino-4-permissibly-substituted 6-lower alkyl or allyl-5,5a,-6,7,8,9,9a,10-octahydropyrimido[4,5-g]quinolines, the corresponding trans-(-)-stereoisomers and salts thereof, useful in treating anxiety, Parkinson's Syndrome, sexual dysfunction, depression, hypertension and elevated prolactin levels, and intermediates useful for the synthesis thereof.
Abstract: Compounds of formula (I) ##STR1## in which n is 1 or 2, R.sup.1 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, halo or hydroxy, m is 0, 1 or 2, R.sup.2 is an immunogenic determinant and x is 1 or 2, provided that when n is 1, x is 1 or 2 and there is one diazo moiety at the 3-position or two diazo moieties at the 3- and 5-positions, with respect to the isothiocyanate group, and the hydroxy group is at the 4-position; and provided that when n is 2, x is 1 and the diazo moiety is at the 4-position and the hydroxy groups are at the 3- and 5-positions, are described. The compounds are useful in the preparation of immunoglobulin conjugates for employment in diagnostic techniques.
Abstract: This invention relates to a method of treating neoplasms which comprises administering to a mammal suffering from a vindesinesusceptible neoplasm selected from the group consisting of acute lymphatic leukemia, acute granulocytic leukemia, chronic myeloid leukemia, non-small cell lung cancer, Hodgkin's disease, non-Hodgkin's lymphoma, malignant melanoma carcinoma of the breast, esophageal carcinoma and testicular carcinoma an anti-neoplastically-effective amount of vindesine or a pharmaceutically-acceptable acid addition salt thereof.