Abstract: This invention provides certain benzamide derivatives of the formula: ##STR1## wherein Z is bond, --CH.sub.2 --, or CHCH.sub.3 ; A is --CH.sub.2 --, or CH.sub.2 CH.sub.2 --; and represents a single or double bond; and their pharmaceutical formulations and their use as anticonvulsant agents.
Abstract: This specification describes a process for separating impurities from an impure mixture containing proinsulin-like material with substantially complete recovery of said proinsulin-like material, which comprises:(1) applying said mixture to a reverse phase macroporous acrylate ester copolymer resin support at a pH of from about 7 to about 10; and(2) eluting said proinsulin-like material from said support with an aqueous eluant having a pH of from about 8 to about 11 and containing from about 10% to about 30% by volume of an organic diluent selected from the group consisting of acetone, acetonitrile, and a combination of acetone and acetonitrile.
Abstract: 6,7-Dichloromelatonin and related compounds are ovulation inhibitors of the formula ##STR1## wherein R and R.sup.1 are individually F or Cl, R.sup.2 is C.sub.1-3 alkyl, including methyl, ethyl, n-propyl and isopropyl, and R.sup.3 is H or methyl.
Abstract: Macrolides PTL-448 A and B, which can be prepared by aerobic cultivation of Streptomyces ambofaciens ATCC 15154 in the presence of a macrolide intermediate selected from protylonlide, 5-O-mycaminosylprotylonolide, 20-hydroxy-5-O-mycaminosylprotylonolide and 20-oxo-5-O-mycaminosylprotylonodide, and macrolides PTL-448 C and D, which can be prepared by acidic hydrolysis of PTL-448 A and B are useful antibiotics.
Abstract: This invention provides a method of inhibiting aromatase and treating estrogen-dependent diseases in mammals by administering certain azole derivatives. Certain azole derivatives and their pharmaceutical formulations are also provided.
Type:
Grant
Filed:
June 18, 1984
Date of Patent:
July 22, 1986
Assignee:
Eli Lilly and Company
Inventors:
Kenneth S. Hirsch, Charles D. Jones, Harold M. Taylor
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: 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: The present invention relates to a new class of alkylsulfonamidophenylalkylamines which are potent antiarrhythmic agents having good oral bioavailability properties.
Abstract: Tautomeric mixtures of trans-(.+-.)-3,5-dialkyloctahydropyrazolo[3,4-g]quinoline, of trans-(.+-.)-6-alkyloctahydropyrazolo[4,3-f]quinoline, and of trans-(.+-.)-1,6-dialkyloctahydropyrazolo[4,3-f]quinoline, individual enantiomer thereof, pharmaceutically-acceptable acid addition salts thereof, and intermediates useful in the preparation thereof, useful as hypotensive agents.
Type:
Grant
Filed:
April 3, 1985
Date of Patent:
June 24, 1986
Assignee:
Eli Lilly and Company
Inventors:
John M. Schaus, Diane L. Huser, Richard N. Booher
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: N-Mono or N-disubstituted methyl-2-azetidinones are provided via cyclization of .beta.-hydroxy or .beta.-halo substituted acid sec-amides wherein the amide nitrogen is substituted with a mono- or di-substituted methyl group having activating substituents. Cyclization of .beta.-hydroxy acid amides is mediated by triphenylphosphine-dialkylazodicarboxylate while cyclization of .beta.-halo acid amides is mediated by strong bases e.g. lithium dialkylamides. E.g. Diethyl amino-protected L-serylaminomalonate is cyclized with 200 mole % TPP-diisopropylazodicarboxylate to N-(diethoxycarbonylmethyl)-3-protected-amino-2-azetidinone. The 2-azetidinones provided are useful intermediates.
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