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
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
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
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.
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
Abstract: The invention provides tetrahydroquinolinylalkylamino pyrimidones, and ring homologues thereof, of the general formula (1): ##STR1## wherein R.sup.1 is hydrogen or an alkyl, alkoxy, halogen or amino-substituent, m and n are each 2, 3 or 4 and R.sup.2 is hydrogen, alkyl or variously substituted benzyl.The compounds are useful as histamine-H.sub.1 -receptor antagonists.
Abstract: Vasopressin antagonists which have a tripeptide side chain comprised of three basic amino acids, such as arginine, lysine or ornithine, demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-arginine]-va sopression.
Abstract: 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.
Abstract: A DNA fragment from Streptomyces sp. which contains a gene which can code for an excretable protein is isolated, inserted into a plamid vector and used to transform other Streptomycetes.
Type:
Grant
Filed:
December 14, 1984
Date of Patent:
January 5, 1988
Assignee:
SmithKline Beckman Corporation
Inventors:
Mary E. Brawner, Thomas G. Eckhardt, Louis R. Fare
Abstract: Vasopressin antagonists which have a dipeptide side chain comprised of two basic amino acids demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-desglycine]- vasopressin.
Abstract: Disclosed is a temperature - sensitive (ts) mutant of bovine viral diarrhoea (BVD) virus which shows a considerably limited replication ability at the animal body temperature. The mutant is prepared by reacting wild-type BVD with a chemical mutagen such as nitrous acid. The mutant virous is advantageously used in vaccine compositions because it is capable of inducing immunity in bovines without causing serious side effects.
Abstract: Cysteamine is used as an active ingredient in animal feed compositions and in methods for increasing the feed efficiency of immature, monogastric, meat-producing animals. A particularly useful active ingredient of this invention is cysteamine hydrochloride in a quantity selected from the range of 15-1200 ppm.
Abstract: Vasopressin derivatives having unexpected VSP site binding activity whose structures are characterized by a Mpr unit at position 1 and a Pen unit at position 6 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a linear peptide dimercaptan. A representative species is [1-.beta.-mercaptopropionic acid-2-(O-ethyl)-D-tyrosine-4-valine-6-penicillamine-8-arginine]vasopressi n.
Abstract: A novel subspecies of Kibdelosporangium aridum, subsp. largum (SK&F-AAD-609) produces AAD-216 antibiotics and AAD-609 antibiotics, the ADD-609 antibiotics differing from the AAD-216 antibiotics in presence of glucosamine in the glycolipid radical in place of amino glucuronic acid.
Type:
Grant
Filed:
September 30, 1985
Date of Patent:
September 15, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
John J. Dingerdissen, Rajanikant Mehta, Louis J. Nisbet, Marcia C. Shearer, Gail F. Wasserman