Patents Represented by Attorney Donald J. Barrack
  • Patent number: 4323511
    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.
    Type: Grant
    Filed: May 22, 1978
    Date of Patent: April 6, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Sam T. Chao
  • Patent number: 4322541
    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.
    Type: Grant
    Filed: August 22, 1980
    Date of Patent: March 30, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Patent number: 4321326
    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.
    Type: Grant
    Filed: February 25, 1981
    Date of Patent: March 23, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard B. Sykes, William L. Parker
  • Patent number: 4317910
    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.
    Type: Grant
    Filed: August 14, 1978
    Date of Patent: March 2, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Patent number: 4312990
    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.
    Type: Grant
    Filed: September 11, 1980
    Date of Patent: January 26, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Rudiger D. Haugwitz
  • Patent number: 4312809
    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.
    Type: Grant
    Filed: October 31, 1980
    Date of Patent: January 26, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Rudiger D. Haugwitz
  • Patent number: 4310461
    Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
    Type: Grant
    Filed: June 23, 1980
    Date of Patent: January 12, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Peter C. Wade
  • Patent number: 4308392
    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
  • Patent number: 4308388
    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
  • Patent number: 4297275
    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.
    Type: Grant
    Filed: February 14, 1980
    Date of Patent: October 27, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Tamara Dejneka
  • Patent number: 4296033
    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
  • Patent number: 4293481
    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.
    Type: Grant
    Filed: July 24, 1980
    Date of Patent: October 6, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Michael E. Condon, Miguel A. Ondetti
  • Patent number: 4288368
    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.
    Type: Grant
    Filed: July 30, 1979
    Date of Patent: September 8, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Rudiger D. Haugwitz
  • Patent number: 4284561
    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
  • Patent number: 4282235
    Abstract: New substituted derivatives of thiazolidine-, thiazane and related carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: September 27, 1979
    Date of Patent: August 4, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Miguel A. Ondetti
  • Patent number: 4267373
    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
  • Patent number: 4267354
    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.
    Type: Grant
    Filed: February 4, 1980
    Date of Patent: May 12, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Chester F. Turk
  • Patent number: 4266065
    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.
    Type: Grant
    Filed: April 14, 1980
    Date of Patent: May 5, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Patent number: 4265815
    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.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: May 5, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Ravi K. Varma
  • Patent number: 4263293
    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.
    Type: Grant
    Filed: May 30, 1980
    Date of Patent: April 21, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Tamara Dejneka