Claims
- 1. A compound of formula I having the structure,
- 2. The compound according to claim 1, wherein X is S.
- 3. The compound according to claim 2, wherein R2 is phenyl optionally substituted with 1-4 Y groups and R3 is hydrogen or alkyl of 1-6 carbon atoms.
- 4. The compound according to claim 3, wherein Z is —CHO, —CN, —CH═NOH, or —CH═NOR4.
- 5. The compound according to claim 1, which is
a) 5-(3-hydroxyphenyl)-3-(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; b) 3-(3-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; c) 3-(4-hydroxy-2-methylphenyl)-5-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; d)-3-(5-hydroxy-2-methylphenyl)-5-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; e) 3-(3-fluoro-4-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; f) 3-(3-formyl-4-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; g) 3-(3-chloro-4-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; h) 5-(3-fluoro-4-hydroxyphenyl)-3-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; i) 5-(3-fluoro-4-hydroxyphenyl)-3-(4-hydroxy-2-methylphenyl)-4-methylthiophene-2-carbaldehyde; j) 3-(3-chloro-4-hydroxyphenyl)-5-(3-fluoro-4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; k) 5-(4-hydroxy-2-methylphenyl)-3-(4-hydroxyphenyl)-4-methyl-2-thiophenecarbaldehyde; l) 3-(3-fluoro-4-hydroxyphenyl)-5-(4-hydroxy-2-methylphenyl)-4-methylthiophene-2-carbaldehyde; m) 5-(3-chloro-4-hydroxyphenyl)-3-(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; n) 5-(3-chloro-4-hydroxyphenyl)-3-(3-fluoro-4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; o) 3,5-bis(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde; p) 3-(3-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde oxime; q) 3-(3-hydroxyphenyl)-5-(4-hydroxyphenyl)-4-methylthiophene-2-carbonitrile; r) 3,5-bis(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde oxime; s) 3,5-bis(4-hydroxyphenyl)-4-methylthiophene-2-carbonitrile; t) 3,5-bis(4-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde O-methyloxime; u) 3-(4-hydroxyphenyl)-5-(3-hydroxyphenyl)-4-methylthiophene-2-carbaldehyde oxime; v) 3-(4-hydroxyphenyl)-5-(3-hydroxyphenyl)-4-methylthiophene-2-carbonitrile; w) 3-(3-fluoro-4-hydroxyphenyl)-5-(4-hydroxy-2-methylphenyl)-4-methylthiophene-2-carbaldehyde O-methyloxime or a pharmaceutically acceptable salt thereof.
- 6. A method of treating or inhibiting osteoporosis or inhibiting bone demineralization in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 7. A method of treating or inhibiting inflammatory bowel disease, Crohn's disease, ulcerative proctitis, or colitis in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 8. A method of treating or inhibiting prostatic hypertrophy, uterine leiomyomas, breast cancer, endometriosis, endometrial cancer, polycystic ovary syndrome, endometrial polyps, benign breast disease, adenomyosis, ovarian cancer, melanoma, prostrate cancer, colon cancer, glioma or astioblastomia in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 9. A method of lowering cholesterol, triglycerides, Lp(a), or LDL levels; inhibiting or treating hypercholesteremia; hyperlipidemia; cardiovascular disease; atherosclerosis; peripheral vascular disease; restenosis, or vasospasm; or inhibiting vascular wall damage from cellular events leading toward immune mediated vascular damage in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 10. A method of providing cognition enhancement or neuroprotection; or treating or inhibiting senile dementias, Alzheimer's disease, cognitive decline, stroke, anxiety, or neurodegenerative disorders in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 11. A method of treating or inhibiting free radical induced disease states in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 12. A method of treating or inhibiting vaginal or vulvar atrophy; atrophic vaginitis; vaginal dryness; pruritus; dyspareunia; dysuria; frequent urination; urinary incontinence; urinary tract infections in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 13. A method of treating or inhibiting vasomotor symptoms in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 14. A method of inhibiting conception in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 15. A method of treating or inhibiting arthritis in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 16. The method according to claim 15, wherein the arthritis is rheumatoid arthritis, osteoarthritis, or spondyloarthropathies.
- 17. A method of treating or inhibiting joint swelling or erosion; or treating or inhibiting joint damage secondary to arthroscopic or surgical procedures in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 18. A method of treating or inhibiting infertility in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 19. A method of treating or inhibiting ischemia, reperfusion injury, asthma, pleurisy, multiple sclerosis, systemic lupus erythematosis, uveitis, sepsis, hemmorhagic shock, or type II diabetes in a mammal in need thereof, which comprises providing to said mammal an effective amount of a compound of formula I, having the structure
- 20. A pharmaceutical composition which comprises a compound of formula I, having the structure
Parent Case Info
[0001] This application claims priority from copending provisional application Serial No. 60/348,853, filed Jan. 15, 2002, the entire disclosure of which is hereby incorporated by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60348853 |
Jan 2002 |
US |