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    • 9. 发明授权
    • Thiophene compounds, compositions and use
    • 噻吩化合物,组成和用途
    • US5061704A
    • 1991-10-29
    • US617501
    • 1990-11-23
    • Michel WierzbickiFrederic SauveurJacqueline BonnetMartine BrissetCharles Tordjman
    • Michel WierzbickiFrederic SauveurJacqueline BonnetMartine BrissetCharles Tordjman
    • A61K31/38A61K31/381A61K31/495A61K31/535A61K31/54A61P3/00A61P43/00C07D333/20C07D333/24
    • C07D333/24C07D333/20
    • 1. New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.2. As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: ##STR2## in which: X, n, a, b, c, R.sub.1, R.sub.2, R and R' are as above defined.
    • 1.下式的新噻吩化合物:其中:X表示氢,卤素,C 1 -C 5烷基或烷氧基或二烷基氨基; n表示1或2; a表示2〜6的整数, b表示2或3; c表示1或2,并且b + c = 4; R1和R2表示氢或(C1-C5)烷基,或与它们所键合的碳原子一起形成含有3至6个碳原子的烃环; 并且R和R'表示氢或(C1-C5)烷基,或与它们所键合的氮原子一起形成任选地含有氧原子的五价或六价杂环或本身可被取代的第二氮原子; 及其生理上可耐受的盐。 本发明的产品可以治疗特别用于治疗以组织损失为特征的病理学。 2.作为合成上述化合物I的新中间体产物,下式的酰胺如下:其中:X,n,a,b,c,R1,R2,R和R'如上所述 定义