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US 2004/0072737 A1Published application
Echinocandin derivatives, their method of preparation and their application as anti-fungal agents
AssigneeAventis Pharma S.A.
InventorsOlivier Courtin, Patrick Fauveau, Astrid Markus, Dominique Melon Manguer, Jean-Marc Michel, Laurent Schio
Life of this patent
Estimating the term…
Abstract
Novel compounds of the formula 1 wherein the substituents are defined in the specification which are useful intermediates in the process to obtain compounds of Formula I which are useful as anti-fungal agents.
Claims27
1) The compounds of formula (I) in all the possible isomer forms as well as their compounds:
- 18
- in which
- either R1 and R2 identical or different from one another, represent a hydrogen atom, a hydroxyl radical, an alkyl radical containing up to 8 atoms of linear, branched or cyclic carbon atoms, optionally interrupted by an oxygen atom optionally substituted by a hydrogen atom, an OH radical, an
- 19
- radical, a and b identical or different from one another,
- representing a hydrogen atom or an alkyl radical containing up to 8 carbon atoms, a and b able optionally to form a heterocycle with the nitrogen atom optionally containing one or several additional heteroatoms,
- or else R1 forms a double bond with the endocyclic carbon atom carrying the radical
- 20
- or else R2 represents an XRa radical,
- X representing an oxygen atom or an NH or N-alkyl radical containing up to 8 carbon atoms and Ra represents a hydrogen atom, a linear, branched or cyclic alkyl radical containing up to 8 carbon atoms optionally substituted by one or several hydrogen atoms, by one or several OH, CO2H, CO2alc radicals,
- an
- 21
- radical, a′ and b′ representing a hydrogen atom, an alkyl radical containing up to 8 carbon atoms, a′ and b′ able to form a heterocycle optionally containing one or several additional heteroatoms and/or by a heterocycle containing one or several heteroatoms where R2 represents a
- 22
- radical in which d, e, f and g represent a hydrogen atom or an alkyl radical containing up to 8 carbon atoms, f and g able moreover to represent an acyl radical containing up to 8 carbon atoms, e and f equally able to form a ring optionally containing one or several heteroatoms,
- R3 represents a hydrogen atom, a methyl or hydroxyl radical
- R4 represents a hydrogen atom or a hydroxyl radical
- R represents a linear, branched or cyclic chain containing up to 30 carbon atoms, optionally containing one or several heteroatoms, one or several heterocycles or a linear, branched or cyclic acyl radical containing up to 30 carbon atoms optionally containing one or several heteroatoms and/or one or several heterocycles,
- T represents a hydrogen atom, a methyl radical, a CH2CONH2, CH2C═N radical, a (CH2)2NH2 or (CH2)2Nalc+X− radical,
- X being a halogen atom and alc an alkyl radical containing up to 8 carbon atoms,
- Y represents a hydrogen atom, a hydroxyl radical or a halogen atom or an OSO3H radical or one of the salts of this radical,
- W represents a hydrogen atom or an OH radical,
- Z represents a hydrogen atom or a methyl radical,
- as well as the addition salts with the acids of the products of formula (I).
21 more elements
15). The compounds of formula (I) described in one of claims 1 to 10, in which R2 represents a radical
- (CH2)pNY″
- in which Y″ represents a hydrogen atom or an alkyl radical containing up to 8 carbon atoms and p represents an integer varying from 1 to 8.
17) The compounds of formula (I) described in claim 15, in which p represents the number 2.
Dependencies are inferred from the claim text.