EP0077550A2
Expired / Lapsed
EP
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1.4-Naphthoquinones, methods for their preparation and veterinary formulations thereof
Assignee: Wellcome Foundation Ltd
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Filing: 1982-10-15
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Granted: —
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Expires: 2002-10-15
Abstract
Abstract 1,4-Naphthoquinones of formula (I), methods for their preparation veterinary formulations thereof, and the use thereof in animal therapy are disclosed.Particularly preferred compounds of formula (I) are, 2-[trans-(4-t-butylcyclohexyl)methyl]-3-hydroxy-1,4-naphthoquinone, and 2-[trans-(4-t-pentyl cyclohexyl)-methyl]-3-hydroxy-1,4-naphthoquinone. The compounds are of value as anti-protozoal agents, in particular as anti-theilerial agents.
Inventors
- 👤 Alan Thomas Hudson
- 👤 Anthony Winchester Randall
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 08:23
CPC Classifications
C; C07; C07C; C07C50/00; C07C50/10; C07C50/12; C07C61/00; C07C61/16; C07C61/22; C07C50/26; C07C50/32; C07C51/00; C07C51/08; C07C51/347; C07C51/36; C07C51/42; C07C51/487; C07C53/00; C07C53/132; C07C53/134; C07C61/08; C07C61/15
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
19 words
A compound of the formula (I) wherein R is a C 1-10 alkyl group, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
19 words
A compound of the formula (I) wherein R is a C 1-10 alkyl group, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
15 words
A compound as claimed in claim 1, wherein R is a straight chain alkyl group.
Claim 4
Dependent Claim
20 words
A compound as claimed in claim 1 or claim 2, wherein R is a straight chain C 1-4 alkyl group.
Claim 5
Dependent Claim
15 words
A compound as claimed in any of claims 1 to 3 wherein R is methyl.
Claim 6
Dependent Claim
15 words
A compound as claimed in any of claims 1 to 3 wherein R is ethyl.
Claim 7
Dependent Claim
17 words
A compound as claimed in any of claims 1 to 5 in the-form of a cis/trans mixture.
Claim 8
Dependent Claim
14 words
A compound as claimed in claim 6 wherein the isomer ratio is approximately 1:1.
Claim 9
Dependent Claim
21 words
A compound as claimed in any one of claims 1 to 5, essentially in the form of the pure trans isomer.
Claim 10
Dependent Claim
21 words
A compound as claimed in any one of claims 1 to 5 essentially in the form of the pure cis isomer.
Claim 11
Dependent Claim
25 words
A compound of formula (I) as defined in any of claims 1 to 9 for use in the treatment of the animal body by therapy.
Claim 12
Dependent Claim
18 words
A compound as claimed in claim 10 for use in the treatment or prophylaxis of a protozoal infection.
Claim 13
Dependent Claim
18 words
A compound as claimed in claim 10 for use in the treatment or prophylaxis of a Theilerial infection.
Claim 14
Dependent Claim
22 words
A compound as claimed in claim 12 for use in the treatment or prophylaxis of an infection with T.annulata or T.parva (parva).
Claim 15
Dependent Claim
16 words
A veterinary formulation comprising a compound of formula (I) together with a veterinarily acceptable carrier therefor.
Claim 16
Dependent Claim
16 words
A veterinary formulation comprising a compound of formula (I) together with a veterinarily acceptable carrier therefor.
Claim 17
Independent Claim
178 words
A method for the preparation of a compound of formula (I), which method comprises:- (a) conversion of a compound of formula (II) wherein R is as defined in formula (I), (b) hydrolysis of a compound of formula (III), wherein R is as defined in formula in formula (I), and X is a halogeno group; (c) conversion of a compound of formula (IV), wherein R is as defined in formula (I); (d) hydrolysis of a compound of formula (V), wherein R is as defined in formula (I); (e) oxidation of a compound of formula (VIb), wherein R is as defined in formula (I), and R 1 is hydrogen; (f) reaction of a compound of formula (VII), wherein R is halogeno, hydroxy, acetoxy or alkoxy, with a cyclohexyl methyl donor containing the moiety, where R is as defined in formula (I), and where desired, converting the group R 1 into a hydroxy group. (g) conversion of a compound of formula (VIII) wherein R is as defined in formula (I), and R 1 is as defined in formula (VII) or benzyloxy.
Claim 18
Independent Claim
178 words
A method for the preparation of a compound of formula (I), which method comprises:- (a) conversion of a compound of formula (II) wherein R is as defined in formula (I), (b) hydrolysis of a compound of formula (III), wherein R is as defined in formula in formula (I), and X is a halogeno group; (c) conversion of a compound of formula (IV), wherein R is as defined in formula (I); (d) hydrolysis of a compound of formula (V), wherein R is as defined in formula (I); (e) oxidation of a compound of formula (VIb), wherein R is as defined in formula (I), and R 1 is hydrogen; (f) reaction of a compound of formula (VII), wherein R is halogeno, hydroxy, acetoxy or alkoxy, with a cyclohexyl methyl donor containing the moiety, where R is as defined in formula (I), and where desired, converting the group R 1 into a hydroxy group. (g) conversion of a compound of formula (VIII) wherein R is as defined in formula (I), and R 1 is as defined in formula (VII) or benzyloxy.
Claim 19
Dependent Claim
21 words
A method as defined in claim 16 (c) wherein the cyclohexylmethyl donor is a substituted cyclohexyl acetic acid containing the moiety.
Claim 20
Dependent Claim
32 words
A compound of formula (VIII) wherein R is as defined in any of claims 1 to 9, and R 1 is a halogeno, acetoxy, benzyloxy or C 1 to 4 alkoxy group.
References Cited (Backward Citations)
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