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AZETIDINE COMPOUNDS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
专利权人:
ANDERS JOHANSSON;JOACHIM PERSSON;ALBIREO AB;ASTRAZENECA AB
发明人:
ANDERS JOHANSSON,JOACHIM PERSSON
申请号:
IL17189405
公开号:
IL171894A
申请日:
2005.11.10
申请国别(地区):
IL
年份:
2012
代理人:
摘要:
The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C<;SUB>;1<;/SUB>;-C<;SUB>;4 <;/SUB>;alkyl, C<;SUB>;3<;/SUB>;-C<;SUB>;4 <;/SUB>;cycloalkyl, C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkenyl or C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkynyl; R2 and R3 is each and independently selected from hydrogen, C<;SUB>;1<;/SUB>;-C<;SUB>;4 <;/SUB>;alkyl, C<;SUB>;3<;/SUB>;-C<;SUB>;4 <;/SUB>;cycloalkyl, C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkenyl, C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkynyl, C<;SUB>;1<;/SUB>;-C<;SUB>;4 <;/SUB>;alkoxy, halogen and cyano, provided that R2 and R3 may not both be hydrogen; R4 is C<;SUB>;1<;/SUB>;-C<;SUB>;4 <;/SUB>;alkyl, C<;SUB>;3<;/SUB>;-C<;SUB>;4 <;/SUB>;cycloalkyl, C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkenyl or C<;SUB>;2<;/SUB>;-C<;SUB>;4 <;/SUB>;alkynyl; Ar is an optionally substituted aromatic ring system selected from pyridinyl; 1-naphthyl; 5,6,7,8-tetrahydro-1-naphthyl; quinolinyl; 2,3-dihydro-1,4-benzodioxinyl; 1,3-benzodioxolyl; 5,6,7,8-tetrahydroquinolinyl; 5,6,7,8-tetrahydroisoquinolinyl; 5,6,7,8-tetrahydroquinazolin-4-yl; 1-benzo[b]thiophen-7-yl; 1-benzo[b]thiophen-4-yl; 1-benzo[b]thiophen-3-yl; isoquinolinyl; quinazolinyl; and indan-4-yl; or Ar is substituted phenyl; or an enantiomer thereof or any salt thereof; to a pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I and to new intermediates used in the preparation thereof.
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