| 摘要 |
<p>1492175 Indan-5-acetic acid and indan-5- ethanol derivatives HEXACHIMIE 6 Feb 1975 [7 Feb 1974 23 Aug 1974 16 Dec 1974] 5726/74 37220/74 and 54292/74 Heading C2C The invention comprises compounds of formula wherein X is H or halogen; R 1 and R 2 are each H, C 1-5 alkyl or C 3-7 cycloalkyl; provided that at least one of them is other than H; R 3 is H or C 1-5 alkyl; and Y is -CH 2 OH or -COOR 4 in which R 4 is H, 1/v (M) where M is a metal of valency v, or a group of formula wherein n is an integer of 1 to 5 and R 5 and R 6 are each H, C 1-5 alkyl, C 3-7 cycloalkyl, aryl or aralkyl, or NR 5 R 6 forms an N-heterocyclic group with 5 to 7 ring members, which heterocyclic group optionally contains a second heteroatom and/or one or more substituents, or a pharmaceutically acceptable addition salt of compound of formula (I). In examples, the acids are prepared by (a) hydrolysing the nitriles or a thionoacetic acid morpholide; (b) reducing indan- 5-glyoxylic acids (themselves made by hydrolysing the Et sters); or (c) hydrogenating alphaalkylidene-indan-5-acetic acids. The aminoalkyl esters are prepared from either the acid chlorides+R 5 R 6 N(CH 2 ) n OH or the acids as Na salts + R 5 R 6 N(CH 2 ) n Cl. The alcohols (Y = CH 2 OH) are prepared by reducing the acids. Starting materials and intermediates otherwise prepared have the formulae where R is 2-isopropyl-5-indaryl, Z is 1,3- dimethyl-5-indaryl and X is substituted 5- indaryl. Therapeutic compositions having analgesic and antiinflammatory activity comprise compounds of the above formula, and may be administered orally, parenterally or rectally.</p> |
