3-amino-1,2-benzoisoxazole derivatives, process for preparation, and use thereof
AssigneeDong Wha Pharm. Ind. Co., Ltd.
InventorsHong-Suk Suh, Jae-Ha Ryu, Yong-Nam Han, Sung-June Yoon, Jong-Woo Kim
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Abstract
The present invention relates to a novel 3-amino-1,2-benzoisoxazole derivatives, represented by Formula I, LTB-4[leukotriene-B-4; 5(S),12(R)-dihydroxy-6,14-cis-8,10-trans-eicosatetraenoic acid] receptor antagonist, process for preparation thereof, and use thereof for LTB-4 receptor antagonist or therapeutics for osteoporosis. ##STR1## (in which n is integer of 3-5).
Claims6
3-Amino-1,2-benzoisoxazole derivatives, represented by Formula I, as follows:
- ##STR7## in which n is an integer of 3-5.
LTB-4 receptor antagonist composition containing a 3-amino-1,2-benzoisoxazole derivative, represented by Formula I, in effective amount and a pharmaceutical carrier ##STR8## in which n is an integer of 3-5.
A method of treating osteoporosis by administering to a patient in need thereof an effective amount of a 3-amino-1,2-benzoisoxazole derivative, represented by Formula I ##STR9## in which n is an integer of 3-5.
A process for preparation of a 3-amino-1,2-benzoisoxazole derivative, represented by Scheme I, as follows:
- ##STR10## in which, I is diisopropylamine;
- II is dibromobutane(a), dibromopropane(b) or dibromopentane(c);
- III is sodium iodide (NaI);
- IV is 2-fluoro-4-hydroxybenzonitrile;
- V is acetoneoxime;
- VI is hydrochloric acid;
- and
- VII is potassium carbonate (K.sub.2 CO.sub.3).
Dependencies are inferred from the claim text.