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US 7,459,474 B2Granted
Modulators of the glucocorticoid receptor and method
AssigneeBristol-Myers Squibb Company
InventorsLeslie A. Robinson, Jaimie K. Rueter, Wilna J. Moree
Life of this patent
Estimating the term…
Abstract
Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where A, B, and R1-R6 are defined herein.
Claims16
A compound having formula (I),
- including all stereoisomers thereof, wherein:
- A and B are independently aryl or heteroaryl, each of which is optionally substituted;
- R1 is
- (i) hydrogen, COR9, CO2R9, SO2R9, S(O)R9, or CONR7R8;
- or
- (ii) C1-6alkyl, C1-6haloalkyl, C1-6heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each group of which is optionally substituted;
- R2, R3 and R4 are independently hydrogen, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, aryl, or heteroaryl, each group of which is optionally substituted where valence allows;
- R5 and R6 are independently
- (i) hydrogen, F, Cl, Br, I, NO2, CN, OR7, NR7R8, SR7, COR9, CO2R9, or CONR7R8;
- or
- (ii) C1-6alkyl, C1-6heteroalkyl, C3-8cycloalkyl, C2-6alkenyl, C2-6alkynyl, aryl, heteroaryl, heteroarylalkyl, or arylalkyl, each group of which is optionally substituted;
- R7 and R8 are independently at each occurence
- (i) hydrogen, COR9, SO2R9, or S(O)R9;
- or
- (ii) C1-6alkyl, C1-6heteroalkyl C1-6haloalkyl, aryl, heteroaryl, heteroarylalkyl, or arylalkyl, each group of which is optionally substituted;
- and
- R9 is, at each occurrence hydrogen, C1-6alkyl, heteroalkyl, haloalkyl, aryl, heteroaryl, heteroarylalkyl, or arylalkyl;
- with the following provisos:
- (i) A is not a benz[c,d]indole;
- (ii) R3 or R4 is not
- if the other of R3 or R4 is hydrogen;
- and
- (iii) formula (I) is not
20 more elements
A compound having formula (II),
- including all stereoisomers thereof, wherein:
- B is aryl or heteroaryl, each of which is optionally substituted;
- R1 is
- (i) hydrogen, COR9, CO2R9, SO2R9, S(O)R9, or CONR7R8;
- or
- (ii) C1-6alkyl, C1-6haloalkyl, C1-6heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each group of which is optionally substituted;
- R2, R3 and R4 are independently hydrogen, C1-6alkyl, C1-6heteroalkyl, C1-6arylalkyl, C1-6heteroarylalkyl, C2-6alkenyl, C2-6alkynyl, or allyl, wherein the heteroaryl or aryl component of the C1-6heteroarylalkyl and C1-6arylalkyl groups is optionally substituted,
- R7 and R8 are independently
- (i) hydrogen, COR9, SO2R9, or S(O)R9
- (ii) C1-6alkyl, C1-6heteroalkyl C1-6haloalkyl, aryl, heteroaryl, allyl, or arylalkyl, each group of which is optionally substituted;
- T1 through T5 are independently
- (i) hydrogen, F, Cl, Br, I, NO2, CN, OR9, or SR9;
- or
- (ii) C1-6alkyl or C1-6heteroalkyl, each group of which is optionally substituted;
- and
- R9 is hydrogen, C1-6alkyl, heteroalkyl, haloalkyl, aryl, heteroaryl, or arylalkyl;
- with the following proviso:
- (i) formula (II) is not
15 more elements
A compound having formula (III),
- including all stereoisomers thereof, wherein:
- R3 and R4 are independently hydrogen, C1-6alkyl, C1-6heteroalkyl, C1-6arylalkyl, C1-6heteroarylalkyl C2-6alkenyl, C2-6alkynyl, or allyl, wherein the heteroaryl or aryl component of the C1-6heteroarylalkyl and C1-6arylalkyl groups is optionally substituted;
- T1 through T10 are independently
- (i) hydrogen, F, Cl, Br, I, NO2, CN, OR9, or SR9;
- or
- (ii) C1-6alkyl or C1-6heteroalkyl, each group of which is optionally substituted;
- and
- R9 is hydrogen, C1-6alkyl, heteroalkyl, haloalkyl, aryl, heteroaryl heteroarylalkyl, or arylalkyl;
- with the proviso that if T8 is fluoro and T6, T7, T9 and T10 are all hydrogen then T1 and T3 cannot both be chloro if T2, T4, and T5 are all hydrogen.
6 more elements
A compound selected from:
- (i)
- (ii) or a stereoisomer thereof.
Dependencies are inferred from the claim text.