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US 2009/0023917 A1Published application
Selective Estrogen Receptor Modulators for the Treatment of Vasomotor Symptoms
AssigneeEli Lilly and Company
InventorsRobert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
Life of this patent
Estimating the term…
Abstract
The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
Claims29
A compound of formula I:
- wherein:
- m is 0, 1 or 2;
- n is 1, 2, 3 or 4;
- R is H or methyl provided that if m is 1 or 2, then R must be H and that if m is 0, then R must be methyl;
- R1 is H, SO2(n-C4-C6 alkyl) or COR2;
- X is O or NR3;
- Y is O, S, SO or NR4;
- R2 is C1-C6 alkyl;
- C1-C6 alkoxy;
- NR5R5a;
- phenoxy;
- or phenyl optionally substituted with halo;
- R3 and R4 are independently H or C1-C6 alkyl;
- and
- R5 and R5a are independently H, C1-C6 alkyl or phenyl;
- or a pharmaceutical acid addition salt thereof.
13 more elements
(canceled)
(canceled)
(canceled)
(canceled)
A compound of formula II:
- wherein:
- m is 0, 1 or 2;
- n is 1, 2, 3 or 4;
- R is H or methyl provided that if m is 1 or 2, then R must be H and that if m is 0, then R must be methyl;
- R1a is H, SO2CH3, SO2(n-C4-C6 alkyl), COR2, C1-C6 alkyl or benzyl;
- X2 is O or NR7;
- Y is O, S, SO or NR4;
- R2 is C1-C6 alkyl;
- C1-C6 alkoxy;
- NR5R5a;
- phenoxy;
- or phenyl optionally substituted with halo;
- R4 is H or C1-C6 alkyl;
- R5 and R5a are independently H, C1-C6 alkyl or phenyl;
- R7 is H, C1-C6 alkyl or CO2(C1-C6 alkyl);
- provided that if R1a is H, SO2(n-C4-C6 alkyl) or COR2, then X2 is NR7 and R7 is CO2(C1-C6 alkyl);
- or an acid addition salt thereof.
14 more elements
29-36. (canceled)
Dependencies are inferred from the claim text.