Patents Represented by Attorney Alan D. Lourie
  • Patent number: 4761415
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: August 28, 1986
    Date of Patent: August 2, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
  • Patent number: 4760089
    Abstract: Potent, irreversible dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors or 2-cyano-2-phenethylamine, and methods of using these inhibitors or 2-cyano-2-phenethylamine to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: September 9, 1985
    Date of Patent: July 26, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Pamela A. Chambers, James S. Frazee, Carl Kaiser, Lawrence I. Kruse
  • Patent number: 4758576
    Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylallyl group. The compounds have histamine H.sub.2 -antagonist activity.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: July 19, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • Patent number: 4758589
    Abstract: Tetraphosphine-coordinated gold (I) compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method of treating tumor cells sensitive to such a compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
    Type: Grant
    Filed: February 2, 1987
    Date of Patent: July 19, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: David T. Hill, Randall K. Johnson
  • Patent number: 4757142
    Abstract: A novel process for preparing 6-amino-3-hydrazinopyridazine derivatives comprising reacting a 3-amino-6-chloropyridazine derivative with ethyl carbazate under aqueous conditions.
    Type: Grant
    Filed: May 13, 1986
    Date of Patent: July 12, 1988
    Assignee: ISF Societa per Azioni
    Inventors: Mario Pinza, Riccardo Monguzzi, Riccardo Colombo
  • Patent number: 4755611
    Abstract: Heterocyclic phosphine compounds, pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a compound which comprises adminstering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: July 5, 1988
    Assignee: SmithKline Beckman Corporation
    Inventor: David T. Hill
  • Patent number: 4755511
    Abstract: This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is 7-carboxamido-4,4a-dihydro-4a-methyl-[5H]-indeno[1,2-c]-pyridazin-3[2H]-on e.
    Type: Grant
    Filed: September 22, 1987
    Date of Patent: July 5, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Brian H. Warrington
  • Patent number: 4755507
    Abstract: Method of producing symptomatic relief in benign prostatic hypertrophy by administering 3-alkyl-6-halo-2,3,4,5-tetrahydro-1H-3-benzazepines.
    Type: Grant
    Filed: October 27, 1987
    Date of Patent: July 5, 1988
    Assignee: SmithKline Beckman Corporation
    Inventor: Jacob P. Hieble
  • Patent number: 4749782
    Abstract: Certain vasopressin-like compounds whose structures have a .beta.,.beta.-diethyl-.beta.-mercaptopropionic acid at position 1 have unexpectedly potent V.sub.2 -antagonist activity. A species of the group is [1-.beta.,.beta.-diethyl-.beta.-mercaptopropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: March 19, 1987
    Date of Patent: June 7, 1988
    Assignee: Smithkline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore, Nelson C. Yim
  • Patent number: 4749717
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: January 8, 1987
    Date of Patent: June 7, 1988
    Assignee: SmithKline Beckman Corporation
    Inventor: Lawrence I. Kruse
  • Patent number: 4743588
    Abstract: Compositions and methods useful for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering to human or animal skin or other membranes the resulting compositions.
    Type: Grant
    Filed: June 13, 1984
    Date of Patent: May 10, 1988
    Assignee: Allergan Pharmaceuticals, Inc.
    Inventors: Dorla Mirejovsky, Harun Takruri
  • Patent number: 4743613
    Abstract: Compounds having the formula: ##STR1## which are ester prodrugs of potent dopamine-.beta.-hydroxylase inhibitors and thus are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmeceutical compositions including these compounds, and methods of using these compounds to inhibit dopamine-.beta.-hydroxylase activity in mammals.
    Type: Grant
    Filed: April 8, 1986
    Date of Patent: May 10, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: James S. Frazee, Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
  • Patent number: 4742154
    Abstract: Peptides whose structures resemble those of vasopressin antagonists but have both a carboxamido amino acid unit and a basic amino acid unit in the side chain have good antagonist activity. A species of the invention is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-glutamine-9-desglycine]-vasopressi n.
    Type: Grant
    Filed: October 23, 1985
    Date of Patent: May 3, 1988
    Assignee: Smithkline Beckman Corporation
    Inventors: William M. Bryan, William F. Huffman, Michael L. Moore
  • Patent number: 4742045
    Abstract: Novel glycopeptide antibiotics of the CWI-785 complex are produced by the Actinomycete SKF-CWI-785.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: May 3, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Ashok K. Verma, Anil K. Goel, V. Arjuna Rao, Akella Venkateswarlu, Robert D. Sitrin
  • Patent number: 4738969
    Abstract: This invention relates to 2-substituted aminopyridone compounds which have histamine H.sub.2 -antagonist activity.
    Type: Grant
    Filed: June 19, 1986
    Date of Patent: April 19, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Patent number: 4739077
    Abstract: Process for preparing N-cyano-N'-methyl-1-aziridinoamidine by reacting aziridine with a N-cyano-N'-methyl-O-arylisourea.
    Type: Grant
    Filed: January 28, 1986
    Date of Patent: April 19, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George R. White
  • Patent number: 4732980
    Abstract: This invention relates to intermediates of Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular final product of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: March 22, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Peter Blurton
  • Patent number: 4730005
    Abstract: The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.
    Type: Grant
    Filed: May 16, 1986
    Date of Patent: March 8, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: John G. Gleason, Carl D. Perchonock
  • Patent number: 4728741
    Abstract: 1-substituted-2-mercapto(or aminomethyl)benzimidazole compounds of the formula ##STR1## inhibit dopamine-.beta.-hydroxylase activity. Intermediates are also disclosed.
    Type: Grant
    Filed: January 8, 1985
    Date of Patent: March 1, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Patent number: 4728648
    Abstract: New 3,4-diamino-1,2,5-thiadiazole oxide derivatives which are histamine H.sub.1 -antagonists. A specific compound of this invention is 3-[3-[N-(4-fluorobenzyl)-N-pyrid-2-yl-amino]propylamino]-4-[pyrimidin-4-yl -methylamino]-1,2,5-thiadiazole-1-oxide.
    Type: Grant
    Filed: February 4, 1986
    Date of Patent: March 1, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Andrew D. Gribble, Robert J. Ife