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US 5,998,362 AGranted
Conjugates useful in the treatment of prostate cancer
AssigneeMerck & Co., Inc.
InventorsDong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Jenny M. Wai
Life of this patent
Estimating the term…
Abstract
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
Claims10
A conjugate which is selected from:
- ##STR33## or an optical isomer or pharmaceutically acceptable salt thereof.
A conjugate which is selected from:
- 2-hydroxyacetyl-hArgSerSerTyrGln-SerNle-DOX (3') (SEQ.ID.NO.:
- 64)
- 2-hydroxyacetyl-hArgSerSerChgGln-SerNle-DOX (3') (SEQ.ID.NO.:
- 65)
- 2-hydroxyacetyl-SerhArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 66)
- 2-hydroxyacetyl-hArgSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 67)
- 2-hydroxyacetyl-hArgAlaSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 68)
- (d) 2,3-dihydroxypropionyl-SerhArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 69)
- (l) 2,3-dihydroxypropionyl-SerhArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 70)
- PEG(2)-SerhArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 71)
- PEG(2)-hArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 72)
- (2R,3S) 2,3,4-trihydroxybutanoyl-hArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 73)
- PEG(2)-SerhArgTyrGln-SerLeu-DOX(3') (SEQ.ID.NO.:
- 74)
- PEG(2)-hArgTyrGln-SerSerSerLeu-DOX (3') (SEQ.ID.NO.:
- 75)
- PEG(2)-LysTyrGln-SerSerSerLeu-DOX (3') (SEQ.ID.NO.:
- 76)
- 2-hydroxyacetyl-hArgSerSerTyrGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 77)
- (l)(2,3-dihydroxypropionyl)hArgSerSerChgGlnSerLeu-DOX (3') (SEQ.ID.NO.:
- 78)
- PEG(2)-hArgSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 79)
- 2-hydroxyacetyl-SerTyrGln-SerSerSerLeu-DOX (3') (SEQ.ID.NO.:
- 80)
- PEG(16)-SerhArgTyrGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 81)
- (2R,3S) 2,3,4-trihydroxybutanoyl-SerhArgChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 82)
- PEG(2)-SerhArgTyrGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 83)
- (d)(2,3-dihydroxypropionyl)-hArgSerSerChgGln-SerLeu-DOX(3') (SEQ.ID.NO.:
- 84)
- (l)(2,3-dihydroxypropionyl)SerSerSerChgGln-Ser(dLeu)-DOX (3') (SEQ.ID.NO.:
- 85)
- (d)(2,3-dihydroxypropionyl)SerSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 86)
- (l)(2,3-dihydroxypropionyl)SerSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 87)
- (l)(2,3-dihydroxypropionyl)SerSerChgGln-Ser(dLeu)-DOX (3') (SEQ.ID.NO.:
- 88)
- (d)(2,3-dihydroxypropionyl)SerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 89)
- PEG(2)SerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 91)
- (d)(2,3-dihydroxypropionyl)-3PAL-SerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 94)
- (l)(2,3-dihydroxypropionyl)-SerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 95)
- (2,3-dihydroxypropionyl)-hSerSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 96)
- PEG(2)-AlaSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 97)
- PEG(6)-SerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 98)
- PEG(6)-SerSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 99)
- PEG(6)-AlaSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 100)
- PEG(4)-3PALSerSerChgGln-SerLeu-DOX (3') (SEQ.ID.NO.:
- 101)
- or an optical isomer or pharmaceutically acceptable salt thereof.
68 more elements
A conjugate which is:
- ##STR34## or a pharmaceutically acceptable salt or optical isomer thereof.
A conjugate which is:
- ##STR35## or a pharmaceutically acceptable salt or optical isomer thereof.
Dependencies are inferred from the claim text.