Richard Hutchings - Ann Arbor MI, US Haripada Khatuya - San Diego CA, US Xiaobing Li - San Diego CA, US William Murray - Belle Mead NJ, US Catherine Prouty - Doylestown PA, US Frank Villani - Perkasie PA, US Nelson Yim - Ambler PA, US Cynthia Maryanoff - Forest Grove PA, US
This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the -1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.
2- or 3-. beta. -Indolylalanyl and. beta. -indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
James F. Callahan - Philadelphia PA Michael L. Moore - Media PA Nelson C. Yim - Ambler PA
Assignee:
SmithKline Beckman Corporation - Philadelphia PA
International Classification:
A61K 3700 C07C10352
US Classification:
514 11
Abstract:
Certain cyclic vasopressin-like peptides, which have an. omega. -amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have vasopressin antagonist activity. A species of this series of new compounds is [1-(. beta. -mercapto-. beta. ,. beta. -cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-(1,5-diaminopentane)-8-desarginine -9-desglycinamide]-vasopressin.
.Beta.-Indolylalanyl Or .Beta.-Indolylglycinyl Vasopressin Antagonists
2- or 3-. beta. -Indolylalanyl and. beta. -indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
Substituted 1-Thienyl And Furyl-2,3,4,5-Tetrahydro-1H-3-Benzazepine Compounds
Kenneth George Holden - Haddonfield NJ Nelson Chi-Fai Yim - Philadelphia PA
Assignee:
SmithKline Corporation - Philadelphia PA
International Classification:
C07D33324 C07D33316 A01N 900
US Classification:
2603322C
Abstract:
A group of 7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepines with structures containing a thienyl or furyl ring at position 1 which have dopaminergic activity. Particular species of this group include 7,8-dihydroxy-1-(5'-methyl-2'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether derivative, 7,8-dihydroxy-1-(2'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether as well as 7,8-dihydroxy-1-(3'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether.
Method For Preparing Lower Alkyl .Beta.-(S-Benzylmercapto)-.Beta.,.Beta.-Pentamethylenepropionates
William F. Huffman - Malvern PA Nelson C. Yim - Ambler PA
Assignee:
SmithKline Corporation - Philadelphia PA
International Classification:
C07C14940
US Classification:
560 9
Abstract:
Lower alkyl. beta. -(S-benzylmercapto)-. beta. ,. beta. -pentamethylenepropionates are prepared in improved yields by reacting lower alkyl cyclohexylideneacetates with benzylmercaptan in the presence of an alkali metal mercaptide.
James F. Callahan - Philadelphia PA William F. Huffman - Malvern PA Michael L. Moore - Media PA Nelson C. Yim - Ambler PA
Assignee:
SmithKline Beckman Corporation - Philadelphia PA
International Classification:
C07K 716 A61K 3734
US Classification:
514 11
Abstract:
Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an. omega. -amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V. sub. 1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
James F. Callahan - Philadelphia PA William F. Huffman - Malvern PA Michael L. Moore - Media PA Nelson C. Yim - Ambler PA
Assignee:
SmithKline Beckman Corporation - Philadelphia PA
International Classification:
C07K 706 C07K 716
US Classification:
530329
Abstract:
Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an. omega. -amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V. sub. 1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.