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Derivatives of antibiotic substance milbemycin and processes therefor

Assignee: Merck and Co Inc
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Filing: 1977-04-11
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Granted: 1978-06-06
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Expires: 1997-04-11
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Abstract

Abstract Derivatives of the antibiotic substance milbemycin, also identified as B-41 are prepared. Milbemycin is brominated, acetylated and hydrolized in order to prepare the 13-hydroxy derivative thereof. The novel derivatives have antiparasitic activity.

Inventors

  • 👤 Michael H. Fisher

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 23:37
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/01; A; A61; A61P; A61P33/00; A61P33/10

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 29 words
13-Hydroxy milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 2
Dependent Claim 29 words
13-Hydroxy milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 3
Dependent Claim 29 words
13-Bromo milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 4
Dependent Claim 29 words
13-Bromo milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 5
Dependent Claim 29 words
13-Acetoxy milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 6
Dependent Claim 29 words
13-Acetoxy milbemycin A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 .
Claim 7
Dependent Claim 63 words
A process for the preparation of 13-hydroxy milbemycins A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 which comprises: (a) brominating the 13-unsubstituted milbemycins with N-bromosuccinimide; (b) acetylating the 13-bromomilbemycins with an alkali metal acetate; and (c) hydrolizing the 13-acetoxy milbemycins with aqueous alkali metal hydroxide.
Claim 8
Dependent Claim 63 words
A process for the preparation of 13-hydroxy milbemycins A 1 , A 2 , A 3 , A 4 , B 1 , B 2 , B 3 , C 1 or C 2 which comprises: (a) brominating the 13-unsubstituted milbemycins with N-bromosuccinimide; (b) acetylating the 13-bromomilbemycins with an alkali metal acetate; and (c) hydrolizing the 13-acetoxy milbemycins with aqueous alkali metal hydroxide.

References Cited (Backward Citations)

US3950360A Cited
US3984564A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-06-05 1981-12-05 1982-06-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-06-05 1985-12-05 1986-06-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-06-05 1989-12-05 1990-06-06 $7700.00 Window Closed / Lapsed

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