EP0413532A2
Expired / Lapsed
EP
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Macrocyclic compounds
Assignee: Fisons Ltd
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Filing: 1990-08-10
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Granted: —
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Expires: 2010-08-10
Abstract
Abstract There are described compounds of formula I, <CHEM> wherein R<1> represents H or OH; R<2> represents H; in addition, R<1> and R<2> may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R<3> represents OH or OCH3; X represents O or (H,OH); and Y represents O or N-OR<4>, in which R<4> represents H or alkyl C1-6; provided that when R<1> is OH, R<2> is H and X is O, then Y does not represent O. Processes for their production and compositions containing them, eg for use as immunosuppressive agents, are also described.
Inventors
- 👤 David Keith Donald
- 👤 David Norman Hardern
- 👤 Martin Edward Cooper
- 👤 Mark Furber
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 13:16
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/26; C07H19/00; C07H19/01; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
78 words
A compound of formula I, wherein R¹ represents H or OH; R² represents H; in addition, R¹ and R² may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R³ represents OH or OCH₃; X represents O or (H,OH); and Y represents O or N-OR⁴, in which R⁴ represents H or alkyl C₁₋₆; provided that when R¹ is OH, R² is H and X is O, then Y does not represent O.
Claim 2
Dependent Claim
78 words
A compound of formula I, wherein R¹ represents H or OH; R² represents H; in addition, R¹ and R² may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R³ represents OH or OCH₃; X represents O or (H,OH); and Y represents O or N-OR⁴, in which R⁴ represents H or alkyl C₁₋₆; provided that when R¹ is OH, R² is H and X is O, then Y does not represent O.
Claim 3
Dependent Claim
16 words
A compound of formula I as defined in claim 1, which is 1,2,14-trihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-17-ethyl-13,19,21,27- tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9 ]octacos-18-ene-3,10,16-trione.
Claim 4
Dependent Claim
16 words
A compound of formula I as defined in claim 1, which is 1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-17-ethyl-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9 ]octacos-18-ene-2,3,10,16-tetraone C16-oxime.
Claim 5
Dependent Claim
15 words
A compound of formula I as defined in claim 1, which is 1-hydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]23,25-dimethoxy-17-ethyl-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9 ]octacosa-14,18-diene-2,3,10,16-tetraone.
Claim 6
Dependent Claim
15 words
A compound of formula I as defined in claim 1, which is 1-hydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-17-ethyl-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9 ]octacos-18-ene-2,3,10,16-tetraone.
Claim 7
Dependent Claim
16 words
The use of a compound of formula I, as defined in claim 1, as a pharmaceutical.
Claim 8
Dependent Claim
24 words
A pharmaceutical composition comprising a compound of formula I, as defined in claim 1, in association with a pharmaceutically acceptable adjuvant, diluent or carrier.
Claim 9
Dependent Claim
25 words
The use of a compound of formula I, as defined in claim 1, in the manufacture of a medicament for use as an immunosuppressive agent.
Claim 10
Dependent Claim
205 words
A process for the production of a compound of formula I as defined in claim 1, which comprises: a) dehydration of a compound of formula I as defined in claim 1 but without proviso, in which R¹ represents OH and R² represents H, to give a corresponding compound of formula I in which R¹ and R² together represent a second carbon-carbon bond between the carbon atoms to which they are attached; b) reduction of a compound of formula I as defined in claim in which R¹ and R² together represent a second carbon-carbon bond between the carbon atoms to which they are attached, to give a corresponding compound of formula I in which R¹ and R² each represent hydrogen; c) reacting a compound of formula NH₂-OR⁴, where R⁴ is as defined in claim 1, or a derivative thereof, with a compound of formula I as defined in claim 1, but without proviso, in which Y represents O, to give a corresponding compound of formula I in which Y represents N-OR⁴; or d) reduction of a compound of formula I as defined in claim 1, but without proviso, in which X represents O, to give a corresponding compound of formula I in which X represents (H,OH).
References Cited (Backward Citations)
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