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WO1999044628A8 - Conjugates useful in the treatment of prostate cancer - Google Patents

Conjugates useful in the treatment of prostate cancer

Info

Publication number
WO1999044628A8
WO1999044628A8 PCT/US1999/004882 US9904882W WO9944628A8 WO 1999044628 A8 WO1999044628 A8 WO 1999044628A8 US 9904882 W US9904882 W US 9904882W WO 9944628 A8 WO9944628 A8 WO 9944628A8
Authority
WO
WIPO (PCT)
Prior art keywords
conjugates
treatment
prostate cancer
disclosed
cytotoxic agents
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US1999/004882
Other languages
French (fr)
Other versions
WO1999044628A1 (en
Inventor
Dong-Mei Feng
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9815855.3A external-priority patent/GB9815855D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to JP2000534229A priority Critical patent/JP2002505298A/en
Priority to AU29858/99A priority patent/AU749063B2/en
Priority to CA002321171A priority patent/CA2321171A1/en
Priority to EP99911146A priority patent/EP1069906A1/en
Publication of WO1999044628A1 publication Critical patent/WO1999044628A1/en
Publication of WO1999044628A8 publication Critical patent/WO1999044628A8/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by a hydroxylalkylamino linker between the oligopeptide and vinblastine. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH). Also disclosed are novel cytotoxic agents that are derivatives of vinca alkaloid drugs.
PCT/US1999/004882 1998-03-05 1999-03-04 Conjugates useful in the treatment of prostate cancer Ceased WO1999044628A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2000534229A JP2002505298A (en) 1998-03-05 1999-03-04 Conjugates useful for treating prostate cancer
AU29858/99A AU749063B2 (en) 1998-03-05 1999-03-04 Conjugates useful in the treatment of prostrate cancer
CA002321171A CA2321171A1 (en) 1998-03-05 1999-03-04 Conjugates useful in the treatment of prostate cancer
EP99911146A EP1069906A1 (en) 1998-03-05 1999-03-04 Conjugates useful in the treatment of prostrate cancer

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US7686098P 1998-03-05 1998-03-05
US60/076,860 1998-03-05
GBGB9815855.3A GB9815855D0 (en) 1998-07-21 1998-07-21 Conjugates useful in the treatment of prostate cancer
GB9815855.3 1998-07-21

Publications (2)

Publication Number Publication Date
WO1999044628A1 WO1999044628A1 (en) 1999-09-10
WO1999044628A8 true WO1999044628A8 (en) 1999-10-14

Family

ID=26314083

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/004882 Ceased WO1999044628A1 (en) 1998-03-05 1999-03-04 Conjugates useful in the treatment of prostate cancer

Country Status (5)

Country Link
EP (1) EP1069906A1 (en)
JP (1) JP2002505298A (en)
AU (1) AU749063B2 (en)
CA (1) CA2321171A1 (en)
WO (1) WO1999044628A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9924759D0 (en) 1999-10-19 1999-12-22 Merck Sharp & Dohme Process for preparing peptide intermediates

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4203898A (en) * 1977-08-29 1980-05-20 Eli Lilly And Company Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids
US4639456A (en) * 1980-06-10 1987-01-27 Omnichem S.A. Vinblastin-23-oyl amino acid derivatives
US6143864A (en) * 1994-06-28 2000-11-07 Merck & Co., Inc. Peptides
US5599686A (en) * 1994-06-28 1997-02-04 Merck & Co., Inc. Peptides

Also Published As

Publication number Publication date
CA2321171A1 (en) 1999-09-10
AU2985899A (en) 1999-09-20
WO1999044628A1 (en) 1999-09-10
AU749063B2 (en) 2002-06-20
JP2002505298A (en) 2002-02-19
EP1069906A1 (en) 2001-01-24

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Free format text: PAT. BUL. 36/99 UNDER (54) THE TITLE IN ENGLISH SHOULD READ "CONJUGATES USEFUL IN THE TREATMENT OF PROSTATE CANCER"

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