Patents Represented by Attorney, Agent or Law Firm Steven A. Fontana
  • Patent number: 5451403
    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
  • Patent number: 5446071
    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.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: August 29, 1995
    Assignee: Eli Lilly and Company
    Inventor: Timothy A. Grese
  • Patent number: 5426123
    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.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventor: Steven A. Fontana
  • Patent number: 5426187
    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
  • Patent number: 5426110
    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.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventors: Lynn S. Gossett, Chuan Shih
  • Patent number: 5416211
    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.
    Type: Grant
    Filed: May 24, 1993
    Date of Patent: May 16, 1995
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Patent number: 5407955
    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.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: April 18, 1995
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Jeffrey A. Dodge
  • Patent number: 5391492
    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.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: February 21, 1995
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Raymond C. Yao
  • Patent number: 5389670
    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.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: February 14, 1995
    Assignee: Eli Lilly Company
    Inventor: Steven A. Fontana
  • Patent number: 5384332
    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.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: January 24, 1995
    Assignee: Eli Lilly and Company
    Inventor: Steven A. Fontana
  • Patent number: 5382668
    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.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: January 17, 1995
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Patent number: 5378725
    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
  • Patent number: 5366890
    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
  • Patent number: 5350579
    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
  • Patent number: 5321150
    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.
    Type: Grant
    Filed: July 7, 1992
    Date of Patent: June 14, 1994
    Assignee: Eli Lilly and Company
    Inventors: Homer L. Pearce, Mark A. Winter
  • Patent number: 5314875
    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.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: May 24, 1994
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Raymond C. Yao
  • Patent number: 5302722
    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.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: April 12, 1994
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Patent number: 5292647
    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
  • Patent number: 5292650
    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
  • Patent number: 5286631
    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