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PHARMACEUTICAL PREPARATION FOR BONE MATTER LOSS INHIBITION

机译:药物制剂对骨丢失的抑制作用

摘要

A method of inhibiting bone loss comprising administering to a human in need of treatment an effective amount of a compound having the formula CHEM wherein R is hydrogen; hydroxy; C1-C6 alkoxy; a group of the formula -O-C(O)-Ra, wherein Ra is hydrogen, C1-C6 alkyl optionally substituted with amino, halo, carbonyl, C1-C6 alkoxycarbonyl, C1-C7 alkanoyloxy, carbamoyl and/or aryl; or Ra is C1-C6 alkenyl optionally substituted with aryl; or Ra is a C3-C7 cycloalkyl; or Ra is aryl optionally substituted with hydroxy, C1-C6 alkyl, C1-C6 alkoxy, and/or halo; or Ra is -O-aryl, said aryl optionally substituted with hydroxy C1-C6 alkyl, C1-C6 alkoxy, and/or halo, or R is a group of the formula -O-SO2-Rb wherein Rb may be C1-C6 alkyl or aryl optionally substituted with C1-C6 alkyl; or R is carbamoyloxy wherein the nitrogen may be substituted once or twice with C1-C6 alkyl; or R is a group of the formula -O-C(O)Rc-O-(C1-C6 alkyl) wherein Rc is a bond or C1-C6 alkanediyl; R1 is halo, C1-C6 alkyl, C1-C7 alkyl substituted with C1-C6 alkyl, substituted or unsubstituted C3-C7 cycloalkyl, or substituted or unsubstituted C3-C7 cycloalkenyl; R2 is O or CH2; R3 is CH2 or (CH2)2; R4 is CHEM CH2, or a bond; and R5 is amino, nitrilo optionally substituted once or twice with C1-C6 alkyl; or an N-heterocyclic ring which optionally has another hetero atom selected from N, O, or S in said ring; or a pharmaceutically acceptable salt or solvate thereof.
机译:一种抑制骨质流失的方法,该方法包括向需要治疗的人给药有效量的具有式的化合物,其中R是氢;羟基C1-C6烷氧基;式-OC(O)-R a的基团,其中R a是氢,任选地被氨基,卤素,羰基,C1-C6烷氧基羰基,C1-C7烷酰氧基,氨基甲酰基和/或芳基; R a是任选地被芳基取代的C 1 -C 6烯基;或或R a为C 3 -C 7环烷基;或或R a为任选地被羟基,C 1 -C 6烷基,C 1 -C 6烷氧基和/或卤素取代的芳基;或或R a为-O-芳基,所述芳基任选地被羟基C 1 -C 6烷基,C 1 -C 6烷氧基和/或卤素取代,或R为式-O-SO 2 -R b的基团,其中R b可以是C 1 -C 6烷基或任选地被C 1 -C 6烷基取代的芳基;或R为氨基甲酰氧基,其中氮可被C1-C6烷基取代一次或两次;或R为式-O-C(O)R c -O-(C 1 -C 6烷基)的基团,其中R c为键或C 1 -C 6烷二基; R 1为卤素,C 1 -C 6烷基,被C 1 -C 6烷基取代的C 1 -C 7烷基,取代或未取代的C 3 -C 7环烷基,或取代或未取代的C 3 -C 7环烯基; R 2为O或CH 2; R 3为CH 2或(CH 2)2; R 4为 CH 2或键; R 5是氨基,次氮基任选被C 1 -C 6烷基取代一次或两次; N-杂环,在所述环中任选地具有选自N,O或S的另一个杂原子;或或其药学上可接受的盐或溶剂化物。

著录项

  • 公开/公告号CZ250194A3

    专利类型

  • 公开/公告日1995-05-17

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号CZ19940002501

  • 发明设计人 BRYANT HENRY UHLMAN;GRESE TIMOTHY ALAN;

    申请日1994-10-10

  • 分类号A61K31/38;A61K31/435;A61K31/495;A61K31/535;A61K31/54;

  • 国家 CZ

  • 入库时间 2022-08-22 04:20:15

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