RU93058561A - DERIVATIVES OF AROMATOSIS SELECTIVELY 4 (5) -IMIDAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION ON THEIR BASIS - Google Patents
DERIVATIVES OF AROMATOSIS SELECTIVELY 4 (5) -IMIDAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITION ON THEIR BASISInfo
- Publication number
- RU93058561A RU93058561A RU93058561/04A RU93058561A RU93058561A RU 93058561 A RU93058561 A RU 93058561A RU 93058561/04 A RU93058561/04 A RU 93058561/04A RU 93058561 A RU93058561 A RU 93058561A RU 93058561 A RU93058561 A RU 93058561A
- Authority
- RU
- Russia
- Prior art keywords
- derivatives
- aromatosis
- selectively
- basis
- pharmaceutical composition
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 102000014654 Aromatase Human genes 0.000 claims 1
- 108010078554 Aromatase Proteins 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010020718 Hyperplasia Diseases 0.000 claims 1
- 210000002307 Prostate Anatomy 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000001419 dependent Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000000262 estrogen Substances 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 1
- 230000003000 nontoxic Effects 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (1)
где A -
или
где один из R1 и R2 представляет собой CN, а другой H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2f или галоген, R1 - H или
где R3 - H, CH3 или галоген, R4 - H и R5 - H или R4 и R5 вместе образуют связь, n - 1 или 2, y - 0, 1, 2, их стереоизомеры и их нетоксичные фармацевтически приемлемые соли присоединения кислоты обнаруживают свойства селективного ингибирования ароматазы, сравнимые с их свойствами ингибирования десмолазы. Предложенные соединения полезны при лечении заболеваний, зависящих от эстрогена, например рака молочной железы или гиперплазии предстательной железы (ВРН).Proposed New Derivatives of 4/5 / -imidazole of General Formula
where A is
or
where one of R 1 and R 2 represents CN, and the other H, CH 3 , OCH 3 , NO 2 , NH 2 , CN, CF 3 , CHF 2 , CH 2 f or halogen, R 1 - H or
where R 3 - H, CH 3 or halogen, R 4 - H and R 5 - H or R 4 and R 5 together form a bond, n - 1 or 2, y - 0, 1, 2, their stereoisomers and their non-toxic pharmaceutically acceptable acid addition salts exhibit properties of selective aromatase inhibition comparable to their desmolase inhibition properties. The compounds of the invention are useful in the treatment of estrogen-dependent diseases, for example, breast cancer or prostate hyperplasia (BPH).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB91131425 | 1991-06-18 | ||
GB91259242 | 1991-12-05 |
Publications (1)
Publication Number | Publication Date |
---|---|
RU93058561A true RU93058561A (en) | 1996-12-27 |
Family
ID=
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