公开(公告)号：US20070232586A1

公开(公告)日：2007-10-04

申请号：US11587309

申请日：2005-04-20

申请人： Kazuyuki Ohmoto ,  Akira Hatayama ,  Katsuya Hisaichi ,  Makoto Tanaka ,  Hiroyuki Yamada

发明人： Kazuyuki Ohmoto ,  Akira Hatayama ,  Katsuya Hisaichi ,  Makoto Tanaka ,  Hiroyuki Yamada

IPC分类号： A61K31/421 ,  A61K31/426 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  C07D239/48 ,  C07D263/48 ,  C07D277/20

CPC分类号： C07D487/04 ,  A61K31/421 ,  A61K31/426 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07D239/42 ,  C07D239/48 ,  C07D239/70 ,  C07D491/048 ,  Y02A50/411

摘要： A compound having an inhibitory activity against cysteine protease, represented by formula (I): (wherein ring X is a heterocyclic group which may contain 1 to 4 hetero atoms selected from an nitrogen atom(s), a oxygen atom(s) and a sulfur atom(s) which may be oxidized, in addition to said nitrogen atom in the ring; J is a bond or a spacer having from 1 to 8 atoms; R, R1, R2 and R3 is each independently hydrogen atom or a substituent; n is 0 or an integer of 1 to 10), a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof; and an agent for prevention and/or treatment for a cysteine protease-related disease, such as osteoporosis, comprising it as an active ingredient are provided.

摘要翻译： 由式（I）表示的具有对半胱氨酸蛋白酶的抑制活性的化合物：其中，环X是可以含有1〜4个选自氮原子，氧原子和 除了环中的所述氮原子之外，可以被氧化的硫原子; J是具有1至8个原子的键或间隔基; R 1，R 1，R 2， 2和R 3各自独立地为氢原子或取代基; n为0或1〜10的整数），其盐，其溶剂合物或其N-氧化物 ，或其前药; 并提供了包含其作为活性成分的半胱氨酸蛋白酶相关疾病如骨质疏松症的预防和/或治疗药剂。

公开(公告)号：US20070197510A1

公开(公告)日：2007-08-23

申请号：US10592117

申请日：2005-03-09

申请人： Kazuyuki Ohmoto ,  Katsuya Hisaichi ,  Motohiro Okuma ,  Makoto Tanaka ,  Naoki Kawada

发明人： Kazuyuki Ohmoto ,  Katsuya Hisaichi ,  Motohiro Okuma ,  Makoto Tanaka ,  Naoki Kawada

IPC分类号： A61K31/5513 ,  A61K31/5383 ,  A61K31/52 ,  A61K31/519 ,  A61K31/53 ,  C07D491/02 ,  C07D487/02 ,  C07D473/02 ,  A61K31/428 ,  A61K31/423

CPC分类号： C07D487/04

摘要： The present invention relates to a compound of formula (I) wherein Y and Z each is independently N or C; ring A is a carbocyclic group or a heterocyclic group; ring B is a heterocyclic group containing at least one nitrogen atom; R is a hydrogen atom, a substitutent, etc.; n is 0, or an integer of from 1 to 10, a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof. The compound of formula (I), a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof has an inhibitory activity against cysteine protease, and it is useful for the prophylaxis and/or treatment of a cysteine protease-related disease such as osteoporosis, etc.

摘要翻译： 本发明涉及式（I）化合物，其中Y和Z各自独立地为N或C; 环A是碳环基或杂环基; 环B是含有至少一个氮原子的杂环基; R是氢原子，取代基等; n为0或1〜10的整数，其盐，其溶剂化物或其N-氧化物，或其前药。 式（I）化合物，其盐，其溶剂合物或其N-氧化物或其前药对半胱氨酸蛋白酶具有抑制活性，可用于预防和/或治疗半胱氨酸蛋白酶 相关疾病如骨质疏松症等