Patents Represented by Attorney Robert A. Conrad
  • Patent number: 4968711
    Abstract: There is disclosed a pharmaceutical compound of the formula ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl, or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl, R.sup.2 is --CN, --COOR.sup.3 or ##STR2## wherein R.sup.3 is hydrogen or a protecting group, X is alkylene containing 1 to 6 carbon atoms and Y is a nitrogen-containing group selected from ##STR3## where each R.sup.4 independently is hydrogen or C.sub.1-4 alkyl; and salts thereof.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: November 6, 1990
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, John Goldsworthy, William J. Ross
  • Patent number: 4963558
    Abstract: Pharmaceutical 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 optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, C.sub.3-9 cycloalkyl, optionally substituted phenyl, or --SR.sup.4 where R.sup.4 is C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, or C.sub.3-9 cycloalkyl, R.sup.3 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, c.sub.3-9 cycloalkyl, or optionally phenyl, and either X and Y are both hydrogen or together are .dbd.O; and acid addition salts thereof. These compounds show useful effects on the central nervous system.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: October 16, 1990
    Assignee: Lilly Industries Limited
    Inventors: Terrence M. Hotten, Graham H. Timms, David E. Tupper
  • Patent number: 4963578
    Abstract: There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: October 16, 1990
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, William B. Jamieson, deceased, Alec Todd
  • Patent number: 4956388
    Abstract: The present invention provides 3-aryloxy-3-substituted propanamines capable of inhibiting the uptake of serotonin and norepinephrine.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: September 11, 1990
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong, Joseph H. Krushinski, Jr.
  • Patent number: 4945099
    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: June 5, 1989
    Date of Patent: July 31, 1990
    Assignee: Eli Lilly and Company
    Inventors: Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
  • Patent number: 4939163
    Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: July 3, 1990
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson
  • Patent number: 4931447
    Abstract: This invention provides (8.beta.)-N-cycloalkyl-1-alkyl-6-(substituted) ergoline-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 hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.
    Type: Grant
    Filed: August 14, 1989
    Date of Patent: June 5, 1990
    Assignee: Eli Lilly and Company
    Inventors: Mark M. Foreman, William L. Garbrecht, Gifford P. Marzoni, Kathleen R. Whitten
  • Patent number: 4931470
    Abstract: This invention provides a method of treating or preventing cardiac arrhythmias employing certain 4-amino-N-2,6-(dimethylphenyl)benzamide derivatives.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: June 5, 1990
    Assignee: Eli Lilly and Company
    Inventors: Donald R. Holland, David W. Robertson
  • Patent number: 4921982
    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: June 14, 1989
    Date of Patent: May 1, 1990
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 4904785
    Abstract: This invention provides for certain 2-phenylimidazo[4,5-c]pyridines, their pharmaceutical formulations, and their use as positive inotropic agents, bronchodilators, vasodilators, and anticoagulants.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: February 27, 1990
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, J. Scott Hayes
  • Patent number: 4902695
    Abstract: The present invention provides novel bicyclic derivatives useful as excitatory amino acid receptor antagonists and in treating a variety of associated nervous system disorders.
    Type: Grant
    Filed: February 13, 1989
    Date of Patent: February 20, 1990
    Assignee: Eli Lilly and Company
    Inventor: Paul L. Ornstein
  • Patent number: 4902691
    Abstract: This invention provides (8.beta.)-N-heteroalkyl-1-alkyl-6-(substituted)ergoline-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: December 19, 1988
    Date of Patent: February 20, 1990
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 4902687
    Abstract: The present invention provides novel piperazine derivatives useful as excitatory amino acid receptor antagonists and in treating a variety of associated nervous system disorders.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: February 20, 1990
    Assignee: Eli Lilly and Company
    Inventor: Paul L. Ornstein
  • Patent number: 4892963
    Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R.sup.1 (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 and R.sup.5 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 R'"CONH-- where R'" is C.sub.1-4 alkyl, R.sup.6, R.sup.7 and R.sup.8 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.6 and R.sup.7, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.6, R.sup.7 and R.sup.
    Type: Grant
    Filed: August 7, 1987
    Date of Patent: January 9, 1990
    Assignee: Lilly Industries Limited
    Inventors: Peter T. Gallagher, Terence A. Hicks, Graham W. Mullier
  • Patent number: 4886885
    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl and the alkenyl and alkynyl groups containing 1 to 3 unsaturated bonds, R.sup.2 is (i) optionally substituted phenyl, (ii) C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.4 where R.sup.4 is C.sub.1-14 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.5 where each R.sup.5 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.6 where R.sup.6 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.7 where R.sup.7 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.8 is hydrogen or C.sub.
    Type: Grant
    Filed: October 26, 1988
    Date of Patent: December 12, 1989
    Assignee: Lilly Industries Limited
    Inventors: Stephen R. Baker, Alec Todd
  • Patent number: 4876282
    Abstract: The present invention provides 1-phenyl-(naphthalenyl)alkylamines which are selective inhibitors of serotonin uptake.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: October 24, 1989
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong
  • Patent number: 4874777
    Abstract: This invention provides benzene derivatives which are leukotriene 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: April 10, 1987
    Date of Patent: October 17, 1989
    Assignee: Eli Lilly and Company
    Inventors: F. Patrick Carr, Robert D. Dillard, Doris E. McCullough
  • Patent number: 4863923
    Abstract: A method of inhibiting superoxide release and reducing tissue damage following an inflammatory or ischemic event employing benzothiophenes, benzofurans, and naphthalenes is disclosed.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: September 5, 1989
    Assignee: Eli Lilly and Company
    Inventors: Peter P. K. Ho, Jill A. Panetta
  • Patent number: 4853398
    Abstract: This invention provides benzene derivatives which are leukotriene 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: April 13, 1987
    Date of Patent: August 1, 1989
    Assignee: Eli Lilly and Company
    Inventors: F. P. Carr, Robert D. Dillard, Doris E. McCullough
  • Patent number: RE33300
    Abstract: There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: August 14, 1990
    Assignee: Eli Lilly and Company
    Inventors: Stephen R. Baker, William B. Jamieson, Alec Todd