Following is a CAS database record representing a highly cited patent family.
|
CAS indexed 90 chemical substances from this document.
CAS subject entries for this document include: Neoplasm inhibitors; Estrogens. | |
CAPLUS COPYRIGHT 2006 ACS on STN
| TITLE:
| Substituted fused imidazole compounds as aromatase inhibitors |
| INVENTOR(S):
| Browne, Leslie J. |
| PATENT ASSIGNEE(S):
| Ciba-Geigy A.-G. , Switz. |
| SOURCE:
| Eur. Pat. Appl., 105 pp. CODEN: EPXXDW |
| LANGUAGE:
| German |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
EP 165904 A2 19851227 EP 1985-810279 19850617
EP 165904 A3 19870909
EP 165904 B1 19910410
R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE
US 4617307 A 19861014 US 1984-622421 19840620
FI 8502399 A 19851221 FI 1985-2399 19850617
FI 80694 B 19900330
FI 80694 C 19900710
AT 62415 E 19910415 AT 1985-810279 19850617
IL 75546 A1 19900118 IL 1985-75546 19850618
CS 268672 B2 19900411 CS 1985-4449 19850618
CA 1276633 A1 19901120 CA 1985-484263 19850618
DK 8502776 A 19851221 DK 1985-2776 19850619
DK 170302 B1 19950731
NO 8502474 A 19851223 NO 1985-2474 19850619
NO 162467 B 19890925
NO 162467 C 19900110
AU 8543857 A1 19860102 AU 1985-43857 19850619
AU 589565 B2 19891019
ZA 8504615 A 19860226 ZA 1985-4615 19850619
HU 37936 A2 19860328 HU 1985-2417 19850619
HU 202529 B 19910328
ES 544344 A1 19870101 ES 1985-544344 19850619
RO 92583 B3 19871130 RO 1985-119210 19850619
SU 1433413 A3 19881023 SU 1985-3917403 19850619
JP 61012688 A2 19860121 JP 1985-133167 19850620
JP 04007746 B4 19920212
DD 237510 A5 19860716 DD 1985-277587 19850620
PL 145087 B1 19880831 PL 1985-254099 19850620
PL 145103 B1 19880831 PL 1985-259303 19850620
PL 145104 B1 19880831 PL 1985-259306 19850620
PL 145105 B1 19880831 PL 1985-259307 19850620
PL 145348 B1 19880930 PL 1985-259304 19850620
PL 145814 B1 19881130 PL 1985-259305 19850620
US 4728645 A 19880301 US 1986-825830 19860204
ES 555541 A1 19871116 ES 1986-555541 19860530
ES 555540 A1 19871216 ES 1986-555540 19860530
ES 555538 A1 19880316 ES 1986-555538 19860530
ES 555542 A1 19880316 ES 1986-555542 19860530
ES 555539 A1 19880401 ES 1986-555539 19860530
SU 1436878 A3 19881107 SU 1986-4027754 19860702
SU 1436879 A3 19881107 SU 1986-4027755 19860702
SU 1436880 A3 19881107 SU 1986-4027757 19860702
SU 1443802 A3 19881207 SU 1986-4027758 19860702
SU 1482530 A3 19890523 SU 1986-4027756 19860702
CS 268684 B2 19900411 CS 1986-8018 19861105
CS 268685 B2 19900411 CS 1986-8019 19861105
CS 268686 B2 19900411 CS 1986-8020 19861105
CS 268687 B2 19900411 CS 1986-8021 19861105
CS 268688 B2 19900411 CS 1986-8022 19861105
US 4889861 A 19891226 US 1987-120283 19871113
FI 8802863 A 19880615 FI 1988-2863 19880615
FI 83079 B 19910215
FI 83079 C 19910527
US 5428160 A 19950627 US 1990-632584 19901221
ABSTRACT:
Aromatase-inhibiting imidazo[1,5-a]pyridines I [R1 = H, (un)substituted alkyl, NO2, halogen, OH, SH, (un)substituted NH2, SO3H, CHO, C2-20 acyl, CO2H, etc.; R2 = H, (un)substituted alkyl, halogen, OH, SH, CO2H, acyl, etc.], their 7,8-dihydro derivs.; and fused imidazoles II (R1 and R2 as before; n = 0-4), their stereoisomers, or salts, useful in treating aromatase-related diseases such as gynecomastia and breast cancer, were prepd. The compds. inhibit the metabolic conversion of androgens to estrogens by prohibiting the cleavage of the cholesterol side chain. Thus, 5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine (III) was prepd. by reaction of 5-(p-carboxyphenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine in C2H4Cl2 and concd. H2SO4, followed by addn. of HN3. A tablet was formulated contg. III 10, lactose 253.5, corn starch 12.5, PEG 6000 15, Mg stearate 4 mg and water q.s.
Updated 5/3/2007 2:18:25 PM
