Farmos-yhtyma Oy

Orion-yhtyma Oy

Arja L Karjalainen

Arto J Karjalainen

Raimo E Virtanen

Risto A Lammintausta

Kauko O Kurkela

Arja Marketta Kalapudas

Reino O Pelkonen

Jarmo Sakari Salonen

Marja-Liisa Sodervall

Maire M Eloranta

Antti S Haapalinna

Hannu T Sipila

Matti A Lahde

4(5) substituted imidazoles and their preparation and use

Novel 4(5)-imidazole derivatives of specified formula and their non-toxic salts possess selective aromatase inhibiting properties, which are valuable in the treatment of estrogen dependent diseases e.g. breast cancer.

Aromatase inhibiting 4(5)-imidazoles

Compounds of the formula: ##STR1## wherein X is --CH.sub.2 -- or ##STR2## R.sub.1 is H, C.sub.1-5 -alkyl or benzyl, which can be substituted or unsubstituted

Substituted imidazole derivatives and their preparation and use

The invention provides 4(5)-substituted imidazole derivatives of formula ##STR1## and their acid addition salts, in which either X is --CH.sub.2 -- and R.sub.1 is --CN, --COOH, COO(lower alkyl), --CHO, --CO(lower alkyl), lower alkyl of 3 or 4 carbon atoms, lower alkenyl, or lower (hydroxy alkyl) or X is ##STR2## --C(:CH--R)-- or --CH(CH.sub.2 R)--, where R is hydrogen or lower alkyl, and R.sub.1 is lower alkyl, and R.sub.3 and R.sub.4 are each hydrogen, methyl, ethyl, methoxy, or halogen, and novel intermediates and processes for their preparation. These compounds, in particular when R.sub.1 is lower alkyl, lower alkenyl, or lower (hydroxy alkyl), possess valuable pharmacological properties and are useful especially as selective .alpha..sub.2 -receptor antagonists.

Indenyl imidazoles

The invention provides 4(5)-substituted imidazole derivatives of formula ##STR1## and their acid addition salts, in which either X is --CH.sub.2 -- and R.sub.1 is --CN, --COOH, COO(lower alkyl), --CHO, --CO(lower alkyl), lower alkyl or 3 or 5 carbon atoms, lower alkenyl, or lower (hydroxy alkyl) or X is ##STR2## --C(:CH--R)-- or --CH(CH.sub.2 R)--, where R is hydrogen or lower alkyl, and R.sub.1 is lower alkyl, and R.sub.3 and R.sub.4 are each hydrogen, methyl, ethyl, methoxy, or halogen, and novel intermediates and processes for their preparation. These compounds, in particular when R.sub.1 is lower alkyl, lower alkenyl, or lower (hydroxy alkyl), possess valuable pharmacological properties and are useful especially as selective .alpha..sub.2 -receptor antagonists.

4(5)-substituted imidazole derivatives as .alpha..sub.2 -adrenergic

A process for the preparation of a substituted imidazole of the formula ##STR1## wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --O-- R.sub.1 is H, lower alkyl or lower alkenyl, OCH.sub.3 or OCH.sub.2 CH.sub.3, R.sub.2 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or OH, R.sub.3 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or Hal, R.sub.4 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or Hal, and Hal is halogen and their non-toxic acid addition salts exhibit valuable pharmacological activity and are useful especially as selective .alpha..sub.2 -receptor antagonists.

4-dihydroinden-2-yl-, 4-tetrahydronaphth-2-yl-, and

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Oulu, Finland

Arja L Karjalainen