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).
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Patent number: 4804743Abstract: 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: GrantFiled: January 29, 1987Date of Patent: February 14, 1989Assignee: Warner-Lambert CopmanyInventors: James S. Kaltenbronn, Elizabeth A. Lunney, Ernest D. Nicolaides
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Patent number: 4743585Abstract: 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: GrantFiled: November 21, 1986Date of Patent: May 10, 1988Assignee: Warner-Lambert CompanyInventors: 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
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Patent number: 4596819Abstract: 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: GrantFiled: January 23, 1984Date of Patent: June 24, 1986Assignee: Warner-Lambert CompanyInventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
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Patent number: 4278681Abstract: 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: GrantFiled: January 31, 1980Date of Patent: July 14, 1981Assignee: Warner-Lambert Co.Inventors: Theodore H. Haskell, Marland P. Hutt, Jr., Ernest D. Nicolaides, Peter W. K. Woo, Gin G. Huang
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Patent number: 4267180Abstract: 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: GrantFiled: January 31, 1980Date of Patent: May 12, 1981Assignee: Warner-Lambert CompanyInventors: Theodore H. Haskell, Marland P. Hutt, Jr., Ernest D. Nicolaides
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Patent number: 4128540Abstract: 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: GrantFiled: May 25, 1972Date of Patent: December 5, 1978Assignee: Parke, Davis & CompanyInventors: Mildred C. Rebstock, Ernest D. Nicolaides, Thomas F. Mick, Francis J. Tinney, Eugene L. Wittle
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Patent number: 4124577Abstract: 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: GrantFiled: June 13, 1977Date of Patent: November 7, 1978Assignee: Warner-LambertInventors: Francis J. Tinney, Elizabeth A. Lunney, Ernest D. Nicolaides
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Patent number: 4111923Abstract: 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: GrantFiled: December 27, 1976Date of Patent: September 5, 1978Assignee: Parke, Davis & CompanyInventors: Eugene Leroy Wittle, Mildred Catherine Rebstock, Ernest D. Nicolaides, Alfred Campbell
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Patent number: 4101537Abstract: 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: GrantFiled: April 7, 1977Date of Patent: July 18, 1978Assignee: Parke, Davis & CompanyInventors: Ernest D. Nicolaides, Francis John Tinney
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Patent number: 4087416Abstract: 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: GrantFiled: November 5, 1976Date of Patent: May 2, 1978Assignee: Parke, Davis & CompanyInventors: Francis John Tinney, Ernest D. Nicolaides
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Patent number: 4085096Abstract: 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: GrantFiled: September 15, 1976Date of Patent: April 18, 1978Assignee: Parke, Davis & CompanyInventors: Francis John Tinney, Ernest D. Nicolaides
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Patent number: 4075192Abstract: 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: GrantFiled: June 13, 1977Date of Patent: February 21, 1978Assignee: Parke, Davis & CompanyInventor: Ernest D. Nicolaides
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Patent number: 4043993Abstract: 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: GrantFiled: June 23, 1976Date of Patent: August 23, 1977Assignee: Parke, Davis & CompanyInventors: Francis John Tinney, Ernest D. Nicolaides, Alfred Campbell
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Patent number: 4043994Abstract: 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: GrantFiled: June 23, 1976Date of Patent: August 23, 1977Assignee: Parke, Davis & CompanyInventors: Eugene Leroy Wittle, Ernest D. Nicolaides, Marland Paul Hutt
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Patent number: 4035348Abstract: 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: GrantFiled: March 1, 1976Date of Patent: July 12, 1977Assignee: Parke, Davis & CompanyInventors: Francis John Tinney, Ernest D. Nicolaides
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Patent number: 4031069Abstract: 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: GrantFiled: March 1, 1976Date of Patent: June 21, 1977Assignee: Parke, Davis & CompanyInventors: Ernest D. Nicolaides, Francis John Tinney, James Clark French
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Patent number: 4031071Abstract: 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: GrantFiled: March 1, 1976Date of Patent: June 21, 1977Assignee: Parke, Davis & CompanyInventors: Eugene Leroy Wittle, Ernest D. Nicolaides
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Patent number: 4022761Abstract: 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: GrantFiled: January 19, 1976Date of Patent: May 10, 1977Assignee: Parke, Davis & CompanyInventors: Francis John Tinney, Ernest D. Nicolaides, Marland Paul Hutt, Thomas Frederick Mich