Abstract: Fermentation product A87689 is produced by a strain of Amycolatopsis mediterranei selected from NRRL 18815 and NRRL 18851, or an A87689-producing mutant thereof. A87689, its C.sub.1-6 -alkyl ether and C.sub.1-6 -alkanoyl ester derivatives and pharmaceutically acceptable salts thereof are phospholipase A.sub.2 inhibitors that are useful as antiinflammatory agents. Fermentation products known as BU-3889V, its components and pharmaceutically acceptable salts thereof, are phospholipase A.sub.2 inhibitors that are also useful as antiinflammatory agents.
Type:
Grant
Filed:
April 28, 1994
Date of Patent:
September 19, 1995
Assignee:
Eli Lilly and Company
Inventors:
Dennis R. Berry, Anne H. Dantzig, Manuel Debono, Robert Hamill, R. Michael Molloy, Raymond C. Yao
Abstract: The present invention provides methods for lowering serum cholesterol comprising administering to a mammal in need of treatment a serum cholesterol lowering amount of a compound of formula I or formula II ##STR1## wherein L is --CON< or --N<; andthe dotted line in the B-ring is an optional bond; or a pharmaceutically acceptable salt thereof; and ##STR2## wherein Q is a moiety having the formula ##STR3## L is --CON< or --N<; B is --O--, --S--, --CH.sub.2 -phenyl-O--, -phenyl-O--, or -benzyl-O--;G is a moiety which together with L forms a substituted or unsubstituted heterocyclic ring having at least one nitrogen atom or is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(lower)alkyl, cyano(lower)alkyl, carboxy(lower)alkyl, (lower)alkoxycarbonyl(lower)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.7 -C.sub.11)aryl akyl, di(lower)alkylamino(lower)alkyl, and fluoro-substituted analogs of the foregoing;Z is --O--, --S--, --CH.sub.
Abstract: The present invention provides a novel method of lowering serum cholesterol in humans comprising ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is a benzyl group, or a pharmaceutically acceptable salt thereof.
Abstract: Processes for preparing 4-hydroxy-5-ethynylpyrrolo[2,3-d]pyrimidine intermediates and N-[4-(2-{4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-glutamic acid derivatives having antineoplastic activity are provided.
Type:
Grant
Filed:
November 30, 1993
Date of Patent:
June 20, 1995
Assignee:
Eli Lilly and Company
Inventors:
Charles J. Barnett, Michael E. Kobierski
Abstract: The present invention provides novel pyrimidinyl-glutamic acid derivatives and intermediates thereto. Further provided are methods for inhibiting dihydrofolate reductase in mammals and for treating susceptible neoplasms in mammals, particularly humans.
Abstract: Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.
Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 allkyl)piperazino, and 4-phenyl-piperazino; or a pharmaceutically acceptable salt thereof.
Abstract: New glycopeptide antibiotic A83850, comprising A83850A, and A83850B, is produced by Amycolatopsis albus strain NRRL 18532. A83850A and A83850B can be reduced to give new biologically active denatures. The A83850 antibiotics have activity against Gram-positive bacteria comparable to that of vancomycin.
Abstract: A method of inhibiting one or more symptom of premenstrual syndrome/late luteal phase dysphoric disorder comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, --CO--(C.sub.1 -C.sub.6 alkyl), or --CO--Ar, in which Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
Abstract: The present invention provides novel methods of inhibiting aortal smooth muscle cell proliferation, particularly restenosis, in humans, comprising administering to a human in need of treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is a benzyl group, or a pharmaceutically acceptable salt thereof.
Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d]pyrimidines which are useful for the treatment of susceptible neoplasms.
Abstract: Wortmannin and certain of its analogs are inhibitors of phosphatidylinositol 3-kinase. The compounds are particularly useful for inhibiting phosphatidylinositol 3-kinase in mammals and for treating phosphatidylinositol 3-kinase-dependent conditions, especially neoplasms, in mammals.
Type:
Grant
Filed:
July 19, 1993
Date of Patent:
January 3, 1995
Assignees:
The Arizona Board of Regents, Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Chris J. Vlahos, Garth Powis
Abstract: New hapalindole-type alkaloids called A89271 A-F and I are antifungal and antitumor agents. Methods for preparing them and for preparing hapalindoles G and H by culturing the blue-green alga Fischerella ambigua ATCC 55210 are provided. Methods for preparing A89271 factors B and F by culturing the blue-green alga Hapalosiphon hibernicus ATCC 55225 and a biologically pure culture of this alga are also provided. Further provided are methods and compositions for the inhibition of fungal growth and the treatment of susceptible neoplasms.
Type:
Grant
Filed:
October 13, 1993
Date of Patent:
November 22, 1994
Assignee:
Eli Lilly and Company
Inventors:
Roseanne Bonjouklian, Richard E. Moore, Gregory M. L. Patterson, Tim A. Smitka
Abstract: Fermentation product A87689 is produced by a strain of Amycolatopsis mediterranei selected from NRRL 18815 and NRRL 18851, or an A87689-producing mutant thereof. A87689, its C.sub.1-6 -alkyl ether and C.sub.1-6 -alkanoyl ester derivatives and pharmaceutically acceptable salts thereof are phospholipase A.sub.2 inhibitors that are useful as antiinflammatory agents. Fermentation products known as BU-3889V, its components and pharmaceutically acceptable salts thereof, are phospholipase A.sub.2 inhibitors that are also useful as antiinflammatory agents.
Type:
Grant
Filed:
August 9, 1993
Date of Patent:
September 27, 1994
Assignee:
Eli Lilly and Company
Inventors:
Dennis R. Berry, Anne H. Dantzig, Manuel Debono, Robert Hamill, R. Michael Molloy, Raymond C. Yao
Abstract: 5-Deaza-10-oxo- and 5-deaza-10-thio-5,6,7,8-tetrahydrofolic acid derivatives are provided as agents useful for treating susceptible neoplasms in mammals. Pharmaceutical formulations and intermediates are also provided.
Abstract: New polyether antibiotic A82810, its acyl and alkyl ester, acyl ester and urethane derivatives, and salts thereof, are useful antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A82810 by culture of Actinomodura fibrosa sp. nov. NRRL 18348 and synergistic compositions of the A82810 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and metichlorpindol are also provided.
Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d] pyrimidines which are useful for the treatment of susceptible neoplasms.
Abstract: A new microorganism, Streptomyces avermitilis subspecies niger NRRL 21005, and processes using the microorganism for producing known avermectins are provided.
Type:
Grant
Filed:
November 30, 1992
Date of Patent:
March 8, 1994
Assignee:
Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Otis W. Godfrey, Tim A. Smitka, Raymond C. Yao
Abstract: New hapalindole-type alkaloids called A89271 A-F and I are antifungal and antitumor agents. Methods for preparing them and for preparing hapalindoles G and H by culturing the blue-green alga Fischerella ambigua ATCC 55210 are provided. Methods for preparing A89271 factors B and F by culturing the blue-green alga Hapalosiphon hibernicus ATCC 55225 and a biologically pure culture of this alga are also provided. Further provided are methods and compositions for the inhibition of fungal growth and the treatment of susceptible neoplasms.
Type:
Grant
Filed:
September 16, 1992
Date of Patent:
March 8, 1994
Assignees:
Eli Lilly and Company, University of Hawaii
Inventors:
Roseanne Bonjouklian, Richard E. Moore, Gregory M. L. Patterson, Tim A. Smitka
Abstract: Newly-discovered antibiotic A10255 factors B, C, E, and F are produced by submerged aerobic fermentation of previously-unknown Streptomyces gardneri strain NRRL 15922, or an A10255-producing variant, mutant or recombinant thereof. The antibiotics are active against a wide variety of pathogenic bacteria, and also enhance feed-utilization efficiency in chickens, weanling pigs and cattle.
Type:
Grant
Filed:
February 28, 1991
Date of Patent:
February 15, 1994
Assignee:
Eli Lilly and Company
Inventors:
LaVerne D. Boeck, Otis W. Godfrey, Jr., Karl H. Michel