Abstract: A 1-substituted-3-permissibly-substituted-6 (or 7)-oxodecahydroquinoline is converted to the corresponding 7 (or 6)-formyl derivative. The 6-oxo-7-formyl compound, upon treatment with hydrazine, is cyclized to a tautomeric mixture of 5-substituted-7-permissibly-substituted-4,4a,5,6,7,8,8a,9-octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines.
Abstract: A 4-acyl-o-phenylenediamine is selectively sulfonated on the amino group meta to the acyl group to provide an important intermediate for benzimidazole pharmaceuticals. Some of the intermediates are new to organic chemistry.
Abstract: This invention provides certain 4-acylamino benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
Abstract: N-Aryl benzamides wherein the aryl group is a nitrogen containing heterocycle are useful as selective herbicidal agents. Compositions containing the novel benzamides and a herbicidal method of selective weed control are disclosed.
Abstract: A process is provided which produces 3-sulfonylamino-4-aminobenzophenone intermediates useful in the regiospecific synthesis of benzimidazole antiviral agents.
Abstract: 3-Aryloxy-3-phenylpropylamines and acid addition salts thereof are useful in blocking uptake of monoamines by brain neurons, and are thus effective in treating disorders of sleep, sexual performance, appetite, muscular function, and pituitary function.
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: Novel oxiodinium and thiaiodinium compounds having a superior inhibitory effect against micro-organisms coupled with outstanding stability and low toxicity are described.
Abstract: 2,4-Difluoro-.beta.-estradiol, 2-fluoro-.beta.-estradiol, and related fluoro estrogens used to treat estrogen-deficiency states in human females with genetic predisposition to cancer of estrogen-sensitive tissues.
Abstract: Crystalline cephalexin hydrochloride ethanol solvate converts to crystalline cephalexin hydrochloride monohydrate upon being exposed to moisture.
Type:
Grant
Filed:
December 1, 1983
Date of Patent:
July 15, 1986
Assignee:
Eli Lilly and Company
Inventors:
Gary L. Engel, Joseph M. Indelicato, Harry A. Rose
Abstract: There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.
Type:
Grant
Filed:
October 19, 1983
Date of Patent:
June 17, 1986
Assignee:
Lilly Industries Limited
Inventors:
John Goldsworthy, Winston S. Marshall, John P. Verge
Abstract: Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.
Type:
Grant
Filed:
May 19, 1982
Date of Patent:
July 1, 1986
Assignee:
Lilly Industries Limited
Inventors:
Stephen R. Baker, William B. Jamieson, William J. Ross