EP0241145A1
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EP
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Macrolide compounds
Assignee: Wyeth Holdings LLC
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Filing: 1987-03-11
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Granted: —
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Expires: 2007-03-11
Abstract
Abstract Compounds are described offormula (I) and salts thereof, wherein R 1 represents a methyl, ethyl or isopropyl group; R 2 is alkyl; alkyl substituted by carboxyoralkoxycar- bonyl; alkenyl; phenyl or phenalkyl; R 3 is-OH; OR 4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms. These compounds may be used for controlling insect, acarine, nematode or other pests.
Inventors
- 👤 Derek R. Sutherland
- 👤 Hazel M Noble
- 👤 Michael V J Ramsay
- 👤 Richard A. Fletton
- 👤 John B. Ward
- 👤 David Noble
- 👤 Neil Porter
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 09:00
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/01; A; A61; A61P; A61P33/00; A61P33/10
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
84 words
Compounds of formula (I) and salts thereof, wherein R 1 is a methyl, ethyl or isopropyl group; R 2 is a C 1-4 alkyl group-[optionally substituted by a group CO 2 R 5 (where R 5 is a hydrogen atom or a C 1-4 alkyl g rou p )], a C 2-6 alkenyl group, phenyl or phenyl C 1-3 alkyl group; R 3 is a hydroxyl group; and O R 4 is a hydroxyl or substituted hydroxyl group having up to 25 carbon atoms.
Claim 2
Dependent Claim
84 words
Compounds of formula (I) and salts thereof, wherein R 1 is a methyl, ethyl or isopropyl group; R 2 is a C 1-4 alkyl group-[optionally substituted by a group CO 2 R 5 (where R 5 is a hydrogen atom or a C 1-4 alkyl g rou p )], a C 2-6 alkenyl group, phenyl or phenyl C 1-3 alkyl group; R 3 is a hydroxyl group; and O R 4 is a hydroxyl or substituted hydroxyl group having up to 25 carbon atoms.
Claim 3
Dependent Claim
192 words
Compounds according to claim 1 in which OR 4 is a hydroxyl group; a group -OCOR 7 , -OCO 2 R 7 or -OCSOR 7 (where R 7 is C 1-8 alkyl; C 1-8 alkyl substituted by one or more halogen atoms or a carboxy, C 1-4 alkoxy, phenoxy or silyloxy group; C 2-8 alkenyl; C 2-8 alkynyl; C 3-12 cycloalkyl; aralkyl in which the alkyl portion has 1-6 carbon atoms and the aryl group contains 4-15 carbon atoms; or C 4-15 aryl); a form y lox y group; a group OR 8 (where R 8 is defined above for R 7 ); a group -OSO 2 R 9 ( where R 9 is a C 1-4 alkyl or C 6-10 aryl group); a silyloxy group; a (C 5-7 ) cyclic or acylic acetaloxy group; a group -OCO(CH 2 ) n CO 2 R 10 (where R 10 is a hydrogen atom or a group as defined above for R and n is zero, 1 or 2) or a group OCONR 11 R 12 (where R 11 and R 12 each independently represent a hydrogen atom or a C 1-4 alkyl group).
Claim 4
Dependent Claim
18 words
Compounds according to claim 1 in which O R 4 is a hydroxyl, methoxy, acetoxy or methoxycarbonyloxy group.
Claim 5
Dependent Claim
14 words
Compounds according to any preceding claim in which R 1 is an isopropyl group.
Claim 6
Dependent Claim
18 words
Compounds according to any preceding claim in which R 2 is a methyl, ethyl, vinyl or allyl group.
Claim 7
Dependent Claim
40 words
Compounds according to claim 1 in which R 1 is an isopropyl group; R 2 is a methyl, ethyl, vinyl or allyl group; R 3 is a hydroxyl group; and -O R 4 is a hydroxyl, methoxy or acetoxy group.
Claim 8
Dependent Claim
28 words
A composition for use in human medicine containing an effective amount of at least one compound according to claim 1 together with one or more carriers and/or excipients.
Claim 9
Dependent Claim
28 words
A composition for use in veterinary medicine containing an effective amount of at least one compound according to claim 1 together with one or more carriers and/or excipients.
Claim 10
Dependent Claim
25 words
A pest control composition containing an effective amount of at least one compound according to claim 1 together with one or more carriers and/or excipients.
Claim 11
Dependent Claim
151 words
A process for the preparation of a compound according to claim 1 which comprises: (a) reacting a ketone of formula (II) with a reagent serving to introduce the group R 2 , (b) in the preparation of a compound in which R 2 represents methyl substituted by CO 2 R 5 (where R 5 is as defined above), reacting a ketone of formula (II) with an organolithium reagent R 5 OC=CLi, followed by hydrolysis; (c) in the preparation of a compound in which OR 4 is a hydroxy group, removal of the group R 4 from a corresponding compound of formula (I) in which R 2 is a substituted hydroxyl group; or (d) in the preparation of a compound in which OR 4 is a substituted hydroxyl group, modifying a corresponding compound of formula (I) in which O R 4 is a hydroxyl group to introduce the desired R 4 group.
Claim 12
Dependent Claim
52 words
A method for combatting pests in agriculture, horticulture or forestry, or in stores, buildings or ther public places or locations of the pests, which comprises applying to plants or other vegetation or to the pests themselves or a location thereof an effective amount of one or more compounds according to claim 1.
Claim 13
Dependent Claim
17 words
A method as claimed in claim 11 in which said pests are insect, acarine or nematode pests.
References Cited (Backward Citations)
FR2570390A1
Cited
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