Bone anabolic compounds and methods of use
OwnerStavros C. Manolagas, John A. Katzenellenbogeninventors
Life of this patent
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Abstract
A variety of bone anabolic compounds are useful for maintaining and/or increasing bone mass, density, and/or strength in mammals. Preferred compounds enhance bone anabolic activity while minimizing or eliminating undesirable feminizing or masculinizing effects.
Claims84
A method comprising administering an ANGELS compound to a subject by a dosage regimen that is effective to increase or maintain a bone property selected from the group consisting of bone mass, bone density and bone strength.
A method comprising administering an ANGELS compound to a subject by a dosage regimen that is effective to provide a treatment selected from the group consisting of increase libido, control vasomotor disturbance, promote vasodilation, reduce bone loss, reduce mood swings, lower cholesterol, decrease low density lipoproteins (LDL), increase high density lipoproteins (HDL), slow atherosclerosis, slow progression of cancer, slow progression of cardiovascular disease, slow age-related neurodegeneration, slow progression of neurodegenerative disease, reduce risk of cancer, reduce risk of cardiovascular disease, reduce risk of stroke, and reduce risk of neurodegenerative disease.
A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 46
- wherein R1, R3 and R6 are each individually hydrogen or methyl;
- wherein m and n are each individually integers in the range of 1 to 3;
- and
- wherein R2 and R5 are each individually selected from the group consisting of hydrogen, halogen, mercapto, hydroxyl, cyano, amino, ethenyl, ethynyl, aryl, C1-C5 heteroaryl, C1-C5 alkyl, C1-C5 cycloalkyl, C1-C5 haloalkyl, C1-C5 alkylthio, C1-C5 ester, C1-C5 alkoxy, C1-C5 acyl, C1-C5 alkylamine, and C1-C5 acyloxy;
- and
- wherein R4 is selected from the group consisting of hydrogen, ethenyl, ethynyl, aryl, C1-C5 heteroaryl, C1-C5 alkyl, C1-C5 cycloalkyl, C1-C5 haloalkyl, C1-C5 ester, and C1-C5 acyl.
A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 55
- wherein R1, R3 and R6 are each individually hydrogen or methyl;
- wherein R2 and R5 are each individually selected from the group consisting of hydrogen, halogen, mercapto, hydroxyl, cyano, amino, ethenyl, ethynyl, aryl, C1-C5 heteroaryl, C1-C5 alkyl, C1-C5 cycloalkyl, C1-C5 haloalkyl, C1-C5 alkylthio, C1-C5 ester, C1-C5 alkoxy, C1-C5 acyl, C1-C5 alkylamine, and C1-C5 acyloxy;
- and
- wherein R4 is selected from the group consisting of hydrogen, ethenyl, ethynyl, aryl, C1-C5 heteroaryl, C1-C5 alkyl, C1-C5 cycloalkyl, C1-C5 haloalkyl, C1-C5 ester, and C1-C5 acyl.
A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 59
- wherein R13, R14, and R15 are each individually selected from the group consisting of hydrogen, ethenyl, ethynyl, C1-C5 alkyl, cycloalkyl and phenyl;
- and wherein R16 is selected from the group consisting of hydrogen, hydroxyl, and C1-C5 hydroxyalkyl.
A pharmaceutical composition comprising a compound represented by a formula selected from the group consisting of
- 63
- in which m and n are each individually integers in the range of 1 to 4;
- R3 and R5 are each individually selected from the group consisting of hydroxy, hydrogen, C1 to C5 alkyl, C1 to C5 hydroxyalkyl, C1 to C5 alkoxy, C1 to C5 thioalkoxy, phenyl, and C1 to C5 alkyl-substituted phenyl;
- and in which R6 is selected from the group consisting of hydrogen and C1-C5 alkyl.
Dependencies are inferred from the claim text.