Maytansinoids

• US 4,331,598 A
• Filed: 09/17/1980
• Issued: 05/25/1982
• Est. Priority Date: 09/19/1979
• Status: Expired due to Term

• Current Assignee: Takeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
• Original Assignee: Takeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
• Inventors: Hasegawa, Toru, Tanida, Seiichi, Izawa, Motowo
• Primary Examiner(s): Bond, Robert T.
• Application Number:
  US06/188,242
• Time in Patent Office: 615 Days
• Field of Search: 260/239.3 P, 260/239.3 T
• US Class Current: 540/462
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07D 498/18 Bridged systems
• CPC Class Codes: C12N 1/205 Bacterial isolates
• CPC Class Codes: C12P 17/188 Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms ergot-alcaloids C12P17/183
• CPC Class Codes: C12R 2001/365 Nocardia
• CPC Class Codes: Y10S 435/872 Nocardia

Abstract

Novel antibiotic C-15003 PHM, which is produced by cultivating a microorganism belonging to the genus Nocardia and being capable of producing antibiotic C-15003 PHM, and novel C-15003 PHM acylate, which is produced by subjecting C-15003 PHM thus obtained to acylation reaction with an acylating agent, have antiprotozoan and antitumor activities.

Claims

1. A compound of the formula:

##STR10## wherein R is --COCH₃, --COCH₂ CH₃, ##STR11## and R₁ is hydrogen or R₂ CO-- in which R₂ is phenyl or alkyl of 1 to 5 carbon atoms, the alkyl being optionally substituted by phenyl.

2. A compound as claimed in claim 1, wherein R is ##STR12##

3. A compound as claimed in claim 1, wherein R₁ is R₂ CO-- in which R₂ is alkyl of 1 to 5 carbon atoms.

4. A compound as claimed in claim 1, wherein R₁ is acetyl.

5. A compound as claimed in claim 1, wherein R is ##STR13## and R₁ is acetyl.

6. A compound as claimed in claim 1, wherein R is ##STR14## and R₁ is isovaleryl.

7. A compound as claimed in claim 1, wherein R is ##STR15## and R₁ is n-butyryl.

8. A compound as claimed in claim 1, wherein R is ##STR16## and R₁ is benzoyl.