Patents by Inventor Jerry W. Skiles

Jerry W. Skiles has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20040235896
    Abstract: Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyarylsufonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.
    Type: Application
    Filed: May 13, 2004
    Publication date: November 25, 2004
    Inventors: Roger Aki Fujimoto, Leslie Wighton McQuire, Lauren G. Monovich, Philippe Nantermet, David Thomas Parker, Leslie Ann Robinson, Jerry W. Skiles, Ruben alberto Tommasi
  • Patent number: 5232928
    Abstract: Tetrahydroisoquinoline amides having the general structure ##STR1## are disclosed, the substituents defined hereinbelow, which amides are useful in inhibiting human leukocyte and neutrophil elastaes.
    Type: Grant
    Filed: November 14, 1991
    Date of Patent: August 3, 1993
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Jerry W. Skiles
  • Patent number: 5221665
    Abstract: N-substituted amides which inhibit hydrolysis of elastin, are described, which compounds are tri-and di- fluoromethyl ketone amide and non-naturally occurring n-substituted amino acids derivatives.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: June 22, 1993
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Jerry W. Skiles
  • Patent number: 5200416
    Abstract: Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.6, and R.sub.7 are independently hydrogen or lower alkyl.R.sub.5 is hydrogen, lower alkyl, rad alkanoyl having 1 to 6 carbon atoms.Y is OH or OM wherein M is a pharmaceutically acceptable cation, andn is an integer from 0 to 1, andX.sub.1 and X.sub.2 are independently (CR.sub.8 R.sub.9).sub.mwherein R.sub.8 and R.sub.9 are independently hydrogen or lower alkyl and m is an integer from 1 to 5 are potent angiotensin converting enzyme inhibitors and possess antihypertensive activity.
    Type: Grant
    Filed: May 12, 1980
    Date of Patent: April 6, 1993
    Assignee: USV Pharmaceutical Corporation
    Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams
  • Patent number: 5166154
    Abstract: Imidazo-[1,2-a]piperazines, inhibitors of human neutrophil elastase, having the following general structure ##STR1## wherein the substituents are defined hereinbelow, are disclosed.
    Type: Grant
    Filed: July 8, 1991
    Date of Patent: November 24, 1992
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jerry W. Skiles, Victor Fuchs
  • Patent number: 4843081
    Abstract: A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.
    Type: Grant
    Filed: June 27, 1988
    Date of Patent: June 27, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
  • Patent number: 4831184
    Abstract: This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure ##STR1## wherein R and R.sub.9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino;R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are independently hydrogen, alkyl, alkenyl or alkynyl containing up to 20 carbon atoms, aryl or aryl-lower alkyl having from 7 to 12 carbon atoms, heterocyclic or heterocyclic-lower alkyl having from 6 to 12 carbon atoms, cycloalkyl or cycloalkyl-alkyl containing up to 20 carbon atoms in the cycloalkyl group, provided that each of R.sub.1 and R.sub.2 and R.sub.4 and R.sub.
    Type: Grant
    Filed: February 14, 1983
    Date of Patent: May 16, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
  • Patent number: 4820729
    Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy or lower alkoxy,R.sub.1 and R.sub.2 are hydrogen or lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hygrogen or lower alkyl,R.sub.6 is cycloalkly having from 3 to 20 carbon atoms, aryl or aryl-lower alkyl, and the aryl group contains from 6 to 10 carbon atoms, and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts possess antihypertensive activity.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: April 11, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
  • Patent number: 4795757
    Abstract: Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.
    Type: Grant
    Filed: November 20, 1986
    Date of Patent: January 3, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
  • Patent number: 4766210
    Abstract: Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, alkynyl having from 2 to 6 carbon atoms, cycloalkyl having from 3 to 16 carbon atoms, phenyl, benzyl, tolyl, naphthyl, phenethyl, indanyl, tetrahydronaphthyl, decahydronaphthyl, pyridyl, quinolyl, pyrrolidyl, pyrrolyl, morpholinyl, thiomorpholinyl, furyl, furfuryl, tetrahydrofurfuryl, benzimidazole, thienyl, imidolyl, or tetrahydroindolyl, and where the R.sub.1 to R.sub.7 groups are alkyl, said groups carrying a substituent selected from hydroxy, alkoxy, amino, carboxy, or carbalkoxy, the alkyl group in alkoxy and carbalkoxy having from 1 to 6 carbon atoms, or R.sub.2 taken together with R.sub.3 and the carbons to which they are attached is tetrahydronapthyl or phenyl, and when phenyl R.sub.1 and R.sub.4 are absent, or R.sub.6 and R.sub.
    Type: Grant
    Filed: July 29, 1981
    Date of Patent: August 23, 1988
    Inventors: John T. Suh, Bruce E. Williams, Jerry W. Skiles, Bernard Loev
  • Patent number: 4749698
    Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
    Type: Grant
    Filed: July 8, 1985
    Date of Patent: June 7, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
  • Patent number: 4746676
    Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: May 24, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, Paul Menard
  • Patent number: 4703037
    Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: October 27, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Fu-chih Huang, John T. Suh, Jerry W. Skiles
  • Patent number: 4686295
    Abstract: This invention relates to new compounds of the formula ##STR1## wherein A is a hydroxy, lower alkoxy, lower alkenoxy, diloweralkylamino lower alkoxy, acylamino lower alkoxy, acyloxy, lower alkoxy, aryloxy, arloweralkyloxy, amino, loweralkylamino, diloweralkylamino, aryloweralkylamino, hydroxyamino, or substituted aryloxy, or substituted arloweralkoxy wherein the substituent is methyl, halo or methoxy;R.sub.1, R.sub.2, and R.sub.
    Type: Grant
    Filed: March 7, 1983
    Date of Patent: August 11, 1987
    Assignee: USV Pharmaceutical Corporation
    Inventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
  • Patent number: 4588734
    Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is heterocyclic or heterocyclic alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or ##STR2## wherein Z is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or the radical ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, M and Y are as described above; and where Y is hydroxy their nontoxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.These compounds possess antihypertensive and angiotensin converting enzyme inhibitory activity.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: May 13, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab
  • Patent number: 4585758
    Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
    Type: Grant
    Filed: January 10, 1985
    Date of Patent: April 29, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: Fu-chih Huang, John T. Suh, Jerry W. Skiles
  • Patent number: 4565825
    Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is heterocyclic or heterocyclic alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or ##STR2## wherein Z is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or the radical ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, M and Y are as described above; and where Y is hydroxy their nontoxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts. The compounds of the invention exhibit antihypertensive and angiotensin converting enzyme inhibitory activity.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: January 21, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab
  • Patent number: 4558038
    Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocycliclower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclicand their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.
    Type: Grant
    Filed: November 15, 1984
    Date of Patent: December 10, 1985
    Assignee: USV Pharmaceutical Corp.
    Inventors: Jerry W. Skiles, Raymond D. Youssefyeh, John T. Suh, Howard Jones
  • Patent number: 4556652
    Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substitutents are defined herein, which exhibit antihypertensive activity.
    Type: Grant
    Filed: March 2, 1984
    Date of Patent: December 3, 1985
    Assignee: USV Pharmaceutical Corp.
    Inventors: John T. Suh, Jerry W. Skiles, John J. Piwinski, Paul Menard, Howard Jones
  • Patent number: 4549992
    Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycyclo-alkyl-alkyl, aryl, aryalkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, dialkylaminoalkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused hetero-aryl-cycloalkyl, or fused heteroaryl-cycloalkyl-alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is a group of the formula ##STR2## wherein X is a branched alkane or cycloalkyl; and where Y is hydroxy their non-toxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.
    Type: Grant
    Filed: March 8, 1982
    Date of Patent: October 29, 1985
    Assignee: USV Pharmaceutical Corp.
    Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab