Arylsecocholadiene derivatives
First Claim
Patent Images
1. A compound of formula (I) ##STR26## wherein A is a single or double bond;
- B is CH2 CH2, CH═
CH, or C.tbd.C;
T is CH2 or CH2 CH2 ;
R1 and R3 are H or OH;
C(R,R) is CH2 or C═
CH2 ;
R2 is CH3 and R4 is H, or R2 is H and R4 is CH3 ;
L is phenyl and R5 is OH or C(C1-4 -alkyl)2 OH or L--R5 is 2-furyl which is 5-substituted by C(C1-4 -alkyl)2 OH, with the proviso that when L is phenyl;
A is a single bond;
B is C.tbd.C;
T is CH2 ;
R1 and R3 are OH;
C(R,R) is C═
CH2 ;
R2 is CH3 ;
R4 is H; and
R5 is C(CH3)2 OH;
then R5 is in the ortho or para position.
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Accused Products
Abstract
Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.
5 Citations
31 Claims
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1. A compound of formula (I) ##STR26## wherein A is a single or double bond;
- B is CH2 CH2, CH═
CH, or C.tbd.C;
T is CH2 or CH2 CH2 ;
R1 and R3 are H or OH;
C(R,R) is CH2 or C═
CH2 ;
R2 is CH3 and R4 is H, or R2 is H and R4 is CH3 ;
L is phenyl and R5 is OH or C(C1-4 -alkyl)2 OH or L--R5 is 2-furyl which is 5-substituted by C(C1-4 -alkyl)2 OH, with the proviso that when L is phenyl;
A is a single bond;
B is C.tbd.C;
T is CH2 ;
R1 and R3 are OH;
C(R,R) is C═
CH2 ;
R2 is CH3 ;
R4 is H; and
R5 is C(CH3)2 OH;
then R5 is in the ortho or para position. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30)
- B is CH2 CH2, CH═
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31. A pharmaceutical composition which comprises an amount of the compound of formula I ##STR36## wherein A is a single or double bond;
- B is CH2 CH2, CH.tbd.CH, or T is CH2 or CH2 CH2 ;
CH═
CH R1 and R3 are H or OH;
C(R,R) is CH2 or C═
CH2 ;
R2 is CH3 and R4 is H, or R2 is H and R4 is CH3 ;
L is phenyl and R5 is OH or C(C1-4 -alkyl)2 OH or L--R5 is 2-furyl which is 5-substituted by C(C1-4 -alkyl)2 OH, with the proviso that when L is phenyl;
A is a single bond;
B is C.tbd.C;
T is CH2 ;
R1 and R3 are OH;
C(R,R) is C═
CH2 ;
R2 is CH3 ;
R4 is H; and
R5 is C(CH3)2 OH;
then R5 is in the ortho or para position and a pharmaceutically acceptable carrier.
- B is CH2 CH2, CH.tbd.CH, or T is CH2 or CH2 CH2 ;
Specification