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Rapamycin dimers

Assignee: Wyeth LLC
•
Filing: 1991-05-29
•
Granted: 1992-06-09
•
Expires: 2011-05-29
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Abstract

Abstract A rapamycin dimer of general formula (1) <IMAGE> (I) <IMAGE> wherein A is -(CH2)n-, -(CH2)n-(CH=CH)-(CH2)m-, -(CH2)n-(-C 3BOND C-)-(CH2)m-, <IMAGE> <IMAGE> substituted alkyl, substituted alkenyl, substituted alkynyl, and substituted aromatic; n=1-10, m=1-10 and n=m or n NOTEQUAL m or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

Inventors

  • 👤 Wenling Kao
  • 👤 Robert L. Vogel
  • 👤 John H. Musser

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 14:36
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/12; C07D498/18; A; A61; A61P; A61P29/00; A61P31/00; A61P31/04; A61P31/10; A61P35/00; A61P37/00; A61P37/02; A61P37/06; C07D519/00

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 43 words
A rapamycin dimer of formula (1) ##STR6## wherein A is --(CH 2 ) n --, --(CH 2 )n--(CH═CH)--(CH 2 ) m --, --(CH 2 )n--(--C.tbd.C--)--(CH 2 ) m -- , ##STR7## n=1-10, m=1-10 and n=m or n≠m or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 43 words
A rapamycin dimer of formula (1) ##STR6## wherein A is --(CH 2 ) n --, --(CH 2 )n--(CH═CH)--(CH 2 ) m --, --(CH 2 )n--(--C.tbd.C--)--(CH 2 ) m -- , ##STR7## n=1-10, m=1-10 and n=m or n≠m or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 19 words
A compound of claim 1 wherein A is -(CH 2 ) 4 - or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim 19 words
A compound of claim 1 wherein A is -(CH 2 ) 5 - or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 19 words
A compound of claim 1 wherein A is -(CH 2 ) 6 - or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim 19 words
A compound of claim 1 wherein A is -(CH 2 ) 7 - or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim 15 words
A compound of claim 1 wherein A is ##STR8## or a pharmaceutically acceptable salt thereof.
Claim 8
Independent Claim 66 words
A method of treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of a compound which is a rapamycin dimer of formula (1) ##STR9## wherein A is --(CH 2 ) n --, --(CH 2 )n--(CH═CH)--(CH 2 ) m --, --(CH 2 )n--(--C.tbd.C--)--(CH 2 ) m -- , ##STR10## n=1-10, m=1-10 and n=m or n≠m.
Claim 9
Independent Claim 66 words
A method of treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of a compound which is a rapamycin dimer of formula (1) ##STR9## wherein A is --(CH 2 ) n --, --(CH 2 )n--(CH═CH)--(CH 2 ) m --, --(CH 2 )n--(--C.tbd.C--)--(CH 2 ) m -- , ##STR10## n=1-10, m=1-10 and n=m or n≠m.
Claim 10
Dependent Claim 42 words
A pharmaceutical composition useful for treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal comprising an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US3929992A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1995-06-09 1995-12-09 1996-06-09 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1999-06-09 1999-12-09 2000-06-09 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2003-06-09 2003-12-09 2004-06-09 $7700.00 Window Closed / Lapsed

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