Patents Represented by Attorney Robert A. Conrad
  • Patent number: 5136079
    Abstract: This invention provides a process for preparing 3-substituted-3-hydroxypropanenitriles.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: August 4, 1992
    Assignee: Eli Lilly and Company
    Inventor: David Mitchell
  • Patent number: 5116874
    Abstract: This invention provides certain N-[(phenyl)amino]carbonyl-bicyclicsulfonamide sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: May 26, 1992
    Assignee: Eli Lilly and Company
    Inventor: Gerald A. Poore
  • Patent number: 5114948
    Abstract: Pharmaceutical compositions containing pergolide or a salt thereof stabilized to oxidation by incorporation therewith of a stabilizing agent selected from methionine, cysteine, and cysteine hydrochloride.
    Type: Grant
    Filed: October 19, 1989
    Date of Patent: May 19, 1992
    Assignee: Eli Lilly and Company
    Inventors: James W. Conine, Denis L. Sparks, Julian L. Stowers
  • Patent number: 5110830
    Abstract: This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: May 5, 1992
    Assignee: Eli Lilly and Company
    Inventors: Richard W. Harper, Gerald A. Poore, Brent J. Rieder
  • Patent number: 5105017
    Abstract: This invention provides novel benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: July 18, 1983
    Date of Patent: April 14, 1992
    Assignee: Eli Lilly and Company
    Inventor: Robert D. Dillard
  • Patent number: 5098613
    Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: March 24, 1992
    Assignee: Eli Lilly and Company
    Inventors: Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
  • Patent number: 5073566
    Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: November 30, 1989
    Date of Patent: December 17, 1991
    Assignee: Eli Lilly and Company
    Inventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
  • Patent number: 5043341
    Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: August 27, 1991
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 5041461
    Abstract: A pharmaceutically-active compound of the formula ##STR1## in which R.sup.1 is C.sub.1-4 alkythio, C.sub.1-4 alkylsulphinyl or C.sub.1-4 alkylsulphonyl, R.sup.2 is C.sub.1-4 alkyl, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: August 20, 1991
    Assignee: Lilly Industries Limited
    Inventors: Maria I. Fernandez Fernandez, Terrence M. Hotten, David E. Tupper
  • Patent number: 5023269
    Abstract: The present invention provides 3-aryloxy-3-substituted propanamines capable of inhibiting the uptake of serotonin and norepinephrine.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: June 11, 1991
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong, Joseph H. Krushinski, Jr.
  • Patent number: 5021441
    Abstract: There are disclosed pharmaceutical compounds of the formula: ##STR1## in which R.sup.1 is halo-substituted alkyl;X is alkenylene; and R.sup.1 --X-- contains 6 to 34 carbon atoms;R.sup.2 is C.sub.1-5 alkyl substituted by(i) optionally protected carboxyl, nitrile, optionally protected tetrazolyl or --CONR'R", in which R' and R" are each hydrogen or C.sub.1-4 alkyl, ##STR2## (ii) in which R' and R" are each hydrogen or C.sub.1-4 alkyl, or ##STR3## (iii) in which R', R" and R'" are each hydrogen or C.sub.1-4 alkyl, or R.sup.2 is a group of the formula ##STR4## in which R' is hydrogen or an optionally protected amino acid residue, and R" is --OH or an optionally protected amino acid residue; andR.sup.3, R.sup.4 and R.sup.5 are each hydrogen, optionally protected carboxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro or --CONR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl; and salts thereof.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: June 4, 1991
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, Alec Todd
  • Patent number: 5021449
    Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is --CHO, CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.2 is C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.3 is C.sub.1-4 alkyl and X is pyrrolidinyl or pyrrolidinylmethyl; and salts and esters thereof.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: June 4, 1991
    Assignees: Lilly S.A., Lilly Industries Limited
    Inventors: Maria I. Fernandez Fernandez, Terrence M. Hotten, David E. Tupper
  • Patent number: 5015656
    Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: May 14, 1991
    Assignees: Lilly S.A., Lilly Industries Limited
    Inventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
  • Patent number: 5013761
    Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Novel aryloxypropanolamines are also claimed.
    Type: Grant
    Filed: November 8, 1989
    Date of Patent: May 7, 1991
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson, David T. Wong
  • Patent number: 4997956
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: January 24, 1990
    Date of Patent: March 5, 1991
    Assignee: Eli Lilly and Company
    Inventor: William B. Lacefield
  • Patent number: 4996230
    Abstract: This invention provides tricyclic derivatives which are leukotriene B.sub.4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: February 26, 1991
    Assignee: Eli Lilly and Company
    Inventor: D. Mark Gapinski
  • Patent number: 4992576
    Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: February 12, 1991
    Assignee: Eli Lilly and Company
    Inventor: D. Mark Gapinski
  • Patent number: 4983619
    Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R'(HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N-- where R' and R" are each hydrogen or C.sub.1-4 alkyl or R'"CONH-- where R'" is C.sub.1-4 alkyl, or a group of the formula --CR.sup.7 R.sup.8 R.sup.9 in which R.sup.7, R.sup.8 and R.sup.9 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.7 and R.sup.8, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.7, R.sup.8 and R.sup.
    Type: Grant
    Filed: January 11, 1990
    Date of Patent: January 8, 1991
    Assignee: Lilly Industries Limited
    Inventors: Peter T. Gallagher, Terence A. Hicks
  • Patent number: 4981866
    Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: January 1, 1991
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson
  • Patent number: 4973597
    Abstract: This invention provides certain pyridinecarboxamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: November 27, 1990
    Assignee: Eli Lilly and Company
    Inventor: David W. Robertson