Patents by Inventor Ernest D. Nicolaides

Ernest D. Nicolaides 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).

  • Patent number: 4804743
    Abstract: This invention concerns novel renin-inhibitory peptides containing proline which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Intermediates and processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included. Also included is a method of diagnosis of renin-associated hypertension using the compounds of the invention.
    Type: Grant
    Filed: January 29, 1987
    Date of Patent: February 14, 1989
    Assignee: Warner-Lambert Copmany
    Inventors: James S. Kaltenbronn, Elizabeth A. Lunney, Ernest D. Nicolaides
  • Patent number: 4743585
    Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Novel intermediates, processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: May 10, 1988
    Assignee: Warner-Lambert Company
    Inventors: James P. Hudspeth, James S. Kaltenbronn, Elizabeth A. Lunney, Joseph T. Repine, W. Howard Roark, Michael A. Stier, Francis J. Tinney, Peter W. K. Woo, Ernest D. Nicolaides
  • Patent number: 4596819
    Abstract: Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.
    Type: Grant
    Filed: January 23, 1984
    Date of Patent: June 24, 1986
    Assignee: Warner-Lambert Company
    Inventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
  • Patent number: 4278681
    Abstract: Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(acylaminoacylamino or aminoacylamino)-phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(acylaminoacylamino or aminoacylamino) phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
    Type: Grant
    Filed: January 31, 1980
    Date of Patent: July 14, 1981
    Assignee: Warner-Lambert Co.
    Inventors: Theodore H. Haskell, Marland P. Hutt, Jr., Ernest D. Nicolaides, Peter W. K. Woo, Gin G. Huang
  • Patent number: 4267180
    Abstract: Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl] penicillin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid of 6-aminopenicillamic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
    Type: Grant
    Filed: January 31, 1980
    Date of Patent: May 12, 1981
    Assignee: Warner-Lambert Company
    Inventors: Theodore H. Haskell, Marland P. Hutt, Jr., Ernest D. Nicolaides
  • Patent number: 4128540
    Abstract: A new decapeptide having the formula, pGlu-His-Trp-Ser-Tyr-Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2); salts thereof; production thereof by reacting pGlu-His-Trp-Ser-Tyr(N.sub.3) with Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), by reacting pGlu-His-Trp-Ser-Tyr-Gly(N.sub.3) with Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), or by reacting pGlu-His-Trp-Ser-Tyr-Gly-Leu(N.sub.3) with NO.sub.2 Arg-Pro-Gly(NH.sub.2); certain peptide intermediates and their salts used in the production thereof; and the use thereof in the preparation of luteinizing hormone releasing factor.
    Type: Grant
    Filed: May 25, 1972
    Date of Patent: December 5, 1978
    Assignee: Parke, Davis & Company
    Inventors: Mildred C. Rebstock, Ernest D. Nicolaides, Thomas F. Mick, Francis J. Tinney, Eugene L. Wittle
  • Patent number: 4124577
    Abstract: New nonapeptides having the formula R-Trp-Ser(benzyl)-Tyr(benzyl)-D-Phe-Leu-Arg(X)-Pro-Gly-Y wherein X is a protective group, R is pGlu, protected His(benzyl), protected Ser(benzyl) or protected Cys(benzyl), and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: June 13, 1977
    Date of Patent: November 7, 1978
    Assignee: Warner-Lambert
    Inventors: Francis J. Tinney, Elizabeth A. Lunney, Ernest D. Nicolaides
  • Patent number: 4111923
    Abstract: New octapeptides having the formula Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-R.sub.3 ; salts thereof; wherein R is Gln, Gln (bzl), His (bzl), Ser (bzl), Pro, Leu, Tyr (bzl), Ile, Cys (bzl) or Phe, R.sub.2 is D-Phe, D-Ala, D-Leu, D-Trp, D-Tyr, D-Tyr (Me), D-Ser, D-Met, D-Arg, D-Val, D-His, D-Gln, D-Phs, D-Thr, D-Pro, D-Me.sub.5 Phe or D-Asn and R.sub.3 is NH.sub.2, NH(lower alkyl), N-(lower alkyl).sub.2, NH-benzyl, NHCH.sub.2 CH.sub.2 N-(lower alkyl).sub.2 or NH-CH.sub.2 CH.sub.2 SO.sub.2 NH-benzyl; methods for their production; certain peptide intermediates and their salts used in the production thereof; and the use of said octapeptides as luteinizing hormone releasing factor antagonists.
    Type: Grant
    Filed: December 27, 1976
    Date of Patent: September 5, 1978
    Assignee: Parke, Davis & Company
    Inventors: Eugene Leroy Wittle, Mildred Catherine Rebstock, Ernest D. Nicolaides, Alfred Campbell
  • Patent number: 4101537
    Abstract: New octapeptides having the formula X-R.sup.1 -Trp-Ser(benzyl)-Tyr(benzyl)-R.sup.2 -Leu-Arg(R)-Pro-R.sup.3 -Y wherein X is a protective group, R is hydrogen or a protective group, R.sup.1 is a single bond, Gln, D-Leu or D-Val, R.sup.2 is D-Phe or D-Ala, R.sup.3 is a single bond or Gly and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: April 7, 1977
    Date of Patent: July 18, 1978
    Assignee: Parke, Davis & Company
    Inventors: Ernest D. Nicolaides, Francis John Tinney
  • Patent number: 4087416
    Abstract: New heptapeptides having the formula X-R-His(benzyl)-His(benzyl)--R.sup.1 --R.sup.2 --Trp--Ala--Y wherein X is a protective group, R is Pro or Gln; R.sup.1 and R.sup.2 are Ser(benzyl) or Tyr(benzyl) and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)-amino.
    Type: Grant
    Filed: November 5, 1976
    Date of Patent: May 2, 1978
    Assignee: Parke, Davis & Company
    Inventors: Francis John Tinney, Ernest D. Nicolaides
  • Patent number: 4085096
    Abstract: New hexapeptides having the formula X-R-Trp-His(benzyl)-Tyr(benzyl)-Ser(benzyl)-R.sup.1 -Ala-Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single bond, His, His(benzyl) or Gln; R.sup.1 is a single bond or Pro and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino with the proviso that the total number of amino acid units when R and R.sup.1 are combined is one.
    Type: Grant
    Filed: September 15, 1976
    Date of Patent: April 18, 1978
    Assignee: Parke, Davis & Company
    Inventors: Francis John Tinney, Ernest D. Nicolaides
  • Patent number: 4075192
    Abstract: New nonapeptides having the formula pGlu-D-Phe-Trp-Tyr(benzyl)-Ser(benzyl)-D-Ala-Leu-Orn-Pro-Y and Y is amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: June 13, 1977
    Date of Patent: February 21, 1978
    Assignee: Parke, Davis & Company
    Inventor: Ernest D. Nicolaides
  • Patent number: 4043993
    Abstract: New pentapeptides having the formula X-R-Tyr-(benzyl)-Ser(benzyl)-R.sup.1 -Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single amino acid fragment, a dipeptide fragment or tripeptide fragment utilizing amino acids selected from the group consisting of Pro, Aze, His-(benzyl) and Trp; R.sup.1 is a single bond or a single amino acid fragment or a dipeptide fragment utilizing amino acids selected from the group consisting of Ala, Trp and His and Y is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino with the proviso that the total number of amino acid units when R and R.sup.1 are combined is three.
    Type: Grant
    Filed: June 23, 1976
    Date of Patent: August 23, 1977
    Assignee: Parke, Davis & Company
    Inventors: Francis John Tinney, Ernest D. Nicolaides, Alfred Campbell
  • Patent number: 4043994
    Abstract: New pentapeptides having the formula X-R-Ser-(benzyl)-Tyr(benzyl)-R.sup.1 -Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single amino acid fragment or a dipeptide fragment utilizing amino acids selected from the group consisting of Aze, His(benzyl) and Trp; R.sup.1 is a single amino acid fragment or a dipeptide fragment utilizing amino acids selected from the group consisting of Ala, Leu and Pro and Y is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino with the priviso that the total number of amino acid units when R and R.sup.1 are combined is three.
    Type: Grant
    Filed: June 23, 1976
    Date of Patent: August 23, 1977
    Assignee: Parke, Davis & Company
    Inventors: Eugene Leroy Wittle, Ernest D. Nicolaides, Marland Paul Hutt
  • Patent number: 4035348
    Abstract: New tetrapeptides having the formula A-R.sub.1 -Tyr(benzyl)-Ser(benzyl)-D-Ala-R.sub.2 wherein A is t-butoxycarbonyl, cyclohexylcarbonyl, benzyloxycarbonyl and p-nitrobenzyloxycarbonyl; R.sub.1 is L-His(benzyl), D-Pro, or L-Trp; Tyr(benzyl) is D-Tyr-(benzyl) or L-Tyr(benzyl); Ser(benzyl) is D-ser(benzyl) or L-Ser(benzyl) and R.sub.2 is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: March 1, 1976
    Date of Patent: July 12, 1977
    Assignee: Parke, Davis & Company
    Inventors: Francis John Tinney, Ernest D. Nicolaides
  • Patent number: 4031069
    Abstract: New tetrapeptides having the formula A-R.sub.1 -Ser(benzyl)-Tyr(benzyl)-R.sub.2 -R.sub.3 wherein A is t-butoxycarbonyl, cyclohexylcarbonyl, benzyloxycarbonyl and p-nitrobenzyloxycarbonyl; R.sub.1 is L-Trp, L-Thr(benzyl), L-Met or Gly; Ser(benzyl) is D-Ser(benzyl) or L-Ser(benzyl); Tyr(benzyl) is D-Tyr(benzyl) or L-Tyr(benzyl); R.sub.2 is D-Ala, .beta.-Ala, D-Leu or D-Val; and R.sub.3 is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: March 1, 1976
    Date of Patent: June 21, 1977
    Assignee: Parke, Davis & Company
    Inventors: Ernest D. Nicolaides, Francis John Tinney, James Clark French
  • Patent number: 4031071
    Abstract: New tetrapeptides having the formula A-Ser(benzyl)-Try(benzyl)-D-Ala-Leu-R.sub.1 wherein A is t-butoxycarbonyl, cyclohexylcarbonyl, benzyloxycarbonyl and p-nitrobenzyloxycarbonyl; Ser(benzyl) is D-Ser(benzyl) or L-Ser(benzyl); Tyr(benzyl) is D-Tyr(benzyl) or L-Tyr(benzyl); Leu is D-Leu or L-Leu, and R.sub.1 is lower alkoxy, hydrazino, amino, lower alkylamino or di(lower alkyl)amino.
    Type: Grant
    Filed: March 1, 1976
    Date of Patent: June 21, 1977
    Assignee: Parke, Davis & Company
    Inventors: Eugene Leroy Wittle, Ernest D. Nicolaides
  • Patent number: 4022761
    Abstract: New tripeptides having the formula A-R.sub.1 -Ser(benzyl)-Tyr (benzyl)-R.sub.2 wherein A is t-butoxycarbonyl or cyclohexyl carbonyl, R.sub.1 is Trp, His(benzyl), Cys(benzyl) or Pro and R.sub.2 is lower alkoxy, hydrazino, amino, lower alkylamino, di(lower alkyl)amino, benzylamino, allylamino, (diethoxyphosphinyl)methylamino, 2-(diethoxyphosphinyl)ethylamino or 2-[[(phenylmethyl)amino]sulfonyl]ethylamino, methods for their production, and the use of said tripeptides as luteinizing hormone releasing factor antagonists.
    Type: Grant
    Filed: January 19, 1976
    Date of Patent: May 10, 1977
    Assignee: Parke, Davis & Company
    Inventors: Francis John Tinney, Ernest D. Nicolaides, Marland Paul Hutt, Thomas Frederick Mich