Abstract: Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a 6-dehydro derivative of a 3-oxo-4,5-dehydro steroid intended for radioimmunoassay, said steroid being saturated in the 1,2-position; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4; and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays. The unlabeled analogs can be coupled with an immunogenic carrier and used to induce antibody formation in animals.
Abstract: Compounds having the formula ##STR1## wherein R.sub.3 and R.sub.5 each is independently hydrogen or alkyl are useful intermediates for the preparation of mercaptoacylamino acids having hypotensive activity.
Abstract: Culturing aerobically Agrobacterium radiobacter no. 31700 in a culture medium containing carbon and nitrogen sources yields the antibiotic substance EM5400, comprising salts of certain azetidinesulfonic acid derivatives.
Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; and R.sub.2 is a tertiary amino group; are intermediates useful in the preparation of compounds having hypotensive activity.
Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or a hydrolyzable acyl protecting group;R.sub.2 is hydrogen, alkyl or trifluoromethyl;R.sub.3 and R.sub.4 each is independently hydrogen, halogen, trifluoromethyl, alkylamino, furylmethylamino, phenylamino, thienylmethylamino, alkoxy, aryloxy, benzylthio, arylthio, benzyl, benzoyl, hydroxy, cyano or arylmethoxy;R.sub.5 is hydrogen, alkyl or arylalkyl; andn is 0, 1 or 2, have hypotensive activity.
Abstract: Angiotensin converting enzyme inhibitory action is shown in mammals by compounds having the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and each is hydrogen, halogen, trifluoromethyl, or aminosulfonyl;R.sub.3 is hydrogen, alkyl, halogen or trifluoromethyl;R.sub.4 is proline or a proline derivative;R.sub.5 is hydrogen, alkyl, phenylalkyl, or a metal ion;R.sub.6 is hydrogen, hydroxy, alkyl, halogen, azido, amino, cycloalkyl, aryl, arylalkyl, carbamoyloxy, N,N-dialkylcarbamoyloxy, or --Y--R.sub.9 ;R.sub.7 and R.sub.7 ' are the same and each is halogen or --Y--R.sub.10, or R.sub.7 and R.sub.7 ' together are .dbd.O, --O--(CH.sub.2).sub.m --O-- or --S--(CH.sub.2).sub.m --S--;R.sub.8 is hydrogen and R.sub.8 ' is phenyl, 2-hydroxyphenyl or 4-hydroxyphenyl or R.sub.8 and R.sub.8 ' together are .dbd.O;R.sub.9 is alkyl, aryl, arylalkyl, 1- or 2-naphthyl, or biphenyl;R.sub.10 is alkyl, aryl or arylalkyl;Y is oxygen or sulfur; andm is 1 or 2.
Abstract: Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.
Type:
Grant
Filed:
November 20, 1980
Date of Patent:
December 29, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward W. Petrillo, Jr., Miguel A. Ondetti
Abstract: 1-Mercaptoacyl proline or pipecolic acid having an azido group in the 4-position inhibits the conversion of angiotensin I to angiotensin II in mammals and is useful for the treatment of hypertension.
Type:
Grant
Filed:
October 29, 1980
Date of Patent:
December 29, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward W. Petrillo, Jr., Frank L. Weisenborn
Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is hydrogen or alkanoyl of 2 to 10 carbon atoms;R.sub.2 is hydroxy, amino, or ##STR2## R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR3## R.sub.4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; andm is 0 or an integer of 1 to 9.
Abstract: 1-Mercaptoacyl proline having an azido group in the 4-position inhibits the conversion of angiotensin I to angiotensin II in mammals and is useful for the treatment of hypertension.
Type:
Grant
Filed:
July 23, 1980
Date of Patent:
October 20, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward W. Petrillo, Jr., Frank L. Weisenborn
Abstract: Peptides having the formula ##STR1## wherein R.sub.1 is hydrogen and R.sub.2 is hydroxyl, alkyl, aryl, arylalkyl, alkoxy, alkylthio, aryloxy, arylthio, halogen or azido, or R.sub.1 and R.sub.2 are the same and each is hydrogen, halogen, alkoxy or alkylthio, or R.sub.1 and R.sub.2 together are oxo, --O--(CH.sub.2).sub.n --O--, or --S--(CH.sub.2).sub.n --S--, wherein n is 1 or 2;R.sub.3 is hydrogen, alkyl or trifluoromethyl;R.sub.4 is hydrogen or an acyl protecting group; andR.sub.5 is hydrogen or alkyl;are inhibitors of angiotensin converting enzyme and can be used for the treatment of hypertension in mammals.
Abstract: Compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl or arylalkyl;R.sub.2 is hydrogen and R.sub.3 is hydrogen, hydroxy, alkoxy or halogen, or together R.sub.2 and R.sub.3 can be .dbd.O or --X--(CH.sub.2).sub.t --X-- wherein X is oxygen or sulfur and t is 2 or 3;R.sub.4 is hydrogen or alkyl;R.sub.5 is hydrogen, alkyl or trifluoromethyl;R.sub.6 is alkyl of 1 to 20 carbon atoms, aryl, arylalkyl or a 5- or 6-membered heterocyclic group having 1 or 2 nitrogen, sulfur or oxygen atoms in the ring;R.sub.7 is aryl;m is 0, 1 or 2; andn is 1 or 2have useful hypotensive activity.
Abstract: Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.
Type:
Grant
Filed:
December 3, 1979
Date of Patent:
August 18, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward W. Petrillo, Jr., Miguel A. Ondetti
Abstract: New substituted derivatives of thiazolidine-, thiazane and related carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Abstract: 5,6,7,8-Tetrahydronaphthalenes having the structure ##STR1## and the pharmaceutically acceptable salts thereof, are useful as blood pressure lowering agents. In the above formula R.sub.1 can be hydrogen or alkyl; R.sub.2 is alkyl; R.sub.3 and R.sub.4 can each be hydrogen, hydroxyl, alkoxy, or arylalkoxy, but both cannot be hydroxyl. Those compounds wherein at least one of R.sub.3 and R.sub.4 is other than hydrogen are novel, and constitute a part of this invention.
Type:
Grant
Filed:
November 14, 1977
Date of Patent:
May 12, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Frederic P. Hauck, Christopher M. Cimarusti, Joseph E. Sundeen
Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R'.sub.3 is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; are intermediates useful in the preparation of substituted amides having antiinflammatory activity.
Abstract: Compounds having the formula ##STR1## and basic salts thereof, wherein R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR2## wherein R.sub.6 is alkyl or aryl; R.sub.2 is hydrogen, alkyl, trifluoromethyl or pentafluoroethyl;R.sub.3 is hydrogen or alkyl;R.sub.4 is hydrogen, alkyl or arylalkyl;R.sub.5 is hydrogen or alkyl; andn is 0, 1 or 2;have hypotensive activity.
Abstract: Steroids having the formula ##STR1## are useful intermediates for the preparation of novel antiinflammatory agents having the formula ##STR2## In the above formulas, X is S, ##STR3## R.sub.1 is alkyl, aryl, arylalkyl or acyloxyalkyl; R.sub.2 is fluoro, chloro, bromo or iodo (all R.sub.2 groups are the same);R.sub.3 is hydrogen, fluoro, chloro, bromo or iodo;R.sub.4 is carbonyl, or .beta.-hydroxymethylene;R.sub.5 is hydrogen, methyl or fluorine; andR.sub.6 is chloro, bromo, alkoxy, aryloxy, alkylthio, or arylthio.
Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; andn is an integer of 1 to 20.