公开(公告)号：US06346532B1

公开(公告)日：2002-02-12

申请号：US09529096

申请日：2000-04-07

申请人： Tatsuya Maruyama ,  Takayuki Suzuki ,  Kenichi Onda ,  Masahiko Hayakawa ,  Hiroyuki Moritomo ,  Tetsuya Kimizuka ,  Tetsuo Matsui

发明人： Tatsuya Maruyama ,  Takayuki Suzuki ,  Kenichi Onda ,  Masahiko Hayakawa ,  Hiroyuki Moritomo ,  Tetsuya Kimizuka ,  Tetsuo Matsui

IPC分类号： A61K31495

CPC分类号： C07D231/12 ,  C07D213/30 ,  C07D213/56 ,  C07D213/81 ,  C07D215/48 ,  C07D233/26 ,  C07D235/16 ,  C07D235/30 ,  C07D239/26 ,  C07D241/12 ,  C07D257/04 ,  C07D277/36 ,  C07D277/82 ,  C07D401/04 ,  C07D513/04

摘要： Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—. The compounds are useful as a diabetes remedy which not only functions to both accelerate the secretion of insulin and enhance insulin sensitivity but has an antiobestic action and an antihyperlipemic action based on its selective stimulative action on a &bgr;3 receptor.

摘要翻译： 由通式（I）表示的酰胺衍生物或其盐，其中每个符号具有以下含义：环B：任选地与苯环稠合的任选取代的杂芳基; X：任选被羟基或低级烷基取代的低级亚烷基或低级亚烯基，羰基或由-NH-表示的基团（当X为任选被低级烷基取代的低级烷基时，该低级烷基可以键合到与 环B的构成碳原子形成低级亚烷基，从而形成环）; A：低级亚烷基或由 - （低级亚烷基）-O-表示的基团。 R1a和R1b：相同或不同，各个氢或低级烷基; R2：氢或卤素; 和Z：氮或由= CH-表示的基团。 该化合物可用作糖尿病药物，其不仅可以加速胰岛素的分泌并增强胰岛素敏感性，而且具有基于其对β3受体的选择性刺激作用的抗胆碱作用和抗高脂血症作用。

公开(公告)号：US5498635A

公开(公告)日：1996-03-12

申请号：US314057

申请日：1994-09-28

申请人： Hiromu Hara ,  Tatsuya Maruyama ,  Munetoshi Saito ,  Toshiyasu Mase

发明人： Hiromu Hara ,  Tatsuya Maruyama ,  Munetoshi Saito ,  Toshiyasu Mase

IPC分类号： A61K31/165 ,  A61K31/17 ,  A61K31/275 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/54 ,  C07C237/06 ,  C07C237/20 ,  C07C255/43 ,  C07C275/34 ,  C07C275/40 ,  C07D295/13 ,  C07D295/14 ,  C07D295/145

CPC分类号： C07D295/13 ,  C07C237/20 ,  C07C275/34 ,  C07D295/145

摘要： This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.

摘要翻译： 本发明涉及通式（I）的三（低级烷氧基）苯衍生物或其盐，旋光异构体或溶剂化物，其中：R1，R2和R3相同或不同，并且各自表示 低级烷基; A：通式“IMAGE”和R 4和R 5的基团相同或不同，各自表示低级烷基，芳烷基或芳基，条件是R 4和R 5可以与相邻的氮原子一起形成 吡咯烷基，哌啶子基，吗啉代基，硫代吗啉代基或任选被4-位的低级烷基取代的哌嗪基; 包含其的药物组合物及其生产方法。 本发明的化合物可用作肺表面活性剂分泌促进剂的价值。

公开(公告)号：US5162318A

公开(公告)日：1992-11-10

申请号：US684866

申请日：1991-04-15

申请人： Hiromu Hara ,  Tatsuya Maruyama ,  Munetoshi Saito ,  Makoto Takeuchi ,  Toshiyasu Mase

发明人： Hiromu Hara ,  Tatsuya Maruyama ,  Munetoshi Saito ,  Makoto Takeuchi ,  Toshiyasu Mase

IPC分类号： C07D235/26 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/26 ,  C07D249/08

摘要： Benzimidazolinone derivatives of the general formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch; R.sup.4 and R.sup.5, which may be the same or different, each is a lower alkyl group or R.sup.4 and R.sup.5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when ##STR2## is a piperidino or diethylamino group, at least one of R.sup.1, R.sup.2 and R.sup.3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity.