公开(公告)号：US20130172317A1

公开(公告)日：2013-07-04

申请号：US13814346

申请日：2011-08-09

申请人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tohru Horiguchi ,  Kentaro Asahi ,  Takeshi Endoh ,  Yasuhiko Fujii ,  Takuya Shintani ,  Ken'ichiroh Nakamura ,  Sae Jikihara ,  Tsuyoshi Hasegawa ,  Miho Oohara ,  Yukio Tada ,  Toshikatsu Maki ,  Akira Iida

发明人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tohru Horiguchi ,  Kentaro Asahi ,  Takeshi Endoh ,  Yasuhiko Fujii ,  Takuya Shintani ,  Ken'ichiroh Nakamura ,  Sae Jikihara ,  Tsuyoshi Hasegawa ,  Miho Oohara ,  Yukio Tada ,  Toshikatsu Maki ,  Akira Iida

IPC分类号： C07D251/46 ,  C07D417/12 ,  C07D413/12 ,  C07D405/06 ,  C07D401/14 ,  C07D251/52 ,  C07D405/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D413/14

CPC分类号： C07D251/46 ,  C07D251/52 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Rj are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstituted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供具有P2X3和/或P2X2 / 3受体拮抗作用的新化合物。 一种具有止痛作用或排尿障碍改善作用的药物组合物，其包含式（I）化合物：其中Rh和Rj一起形成键; Ra和Rb和/或Rd和Re一起形成氧代等; Rc是氢，取代或未取代的烷基等; Rf是 - （CR4aR4b）n-R2; R4a和R4b是氢，取代或未取代的烷基等; R2是取代或未取代的环烷基等; n为1〜4的整数， -Rg为-X-R3; -X-是-O-，-S-等; R3是取代或未取代的环烷基等，或其药学上可接受的盐或溶剂合物。

公开(公告)号：US20130225596A1

公开(公告)日：2013-08-29

申请号：US13816085

申请日：2011-08-09

申请人： Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

发明人： Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

IPC分类号： C07C233/75 ,  C07D239/84 ,  C07D213/74 ,  C07C217/84 ,  C07D211/72 ,  C07D405/06 ,  C07C217/80 ,  C07D413/12 ,  C07D409/12 ,  C07D409/06 ,  C07D277/28 ,  C07D401/14 ,  C07D237/04

CPC分类号： C07D239/545 ,  C07C217/80 ,  C07C217/84 ,  C07C217/92 ,  C07C233/25 ,  C07C233/75 ,  C07C2601/14 ,  C07D211/72 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D213/82 ,  C07D215/22 ,  C07D215/56 ,  C07D217/22 ,  C07D217/24 ,  C07D231/38 ,  C07D233/88 ,  C07D233/96 ,  C07D235/30 ,  C07D237/04 ,  C07D237/20 ,  C07D237/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/54 ,  C07D239/557 ,  C07D239/78 ,  C07D239/84 ,  C07D239/95 ,  C07D239/96 ,  C07D241/20 ,  C07D255/02 ,  C07D261/12 ,  C07D263/32 ,  C07D263/34 ,  C07D263/48 ,  C07D265/06 ,  C07D265/10 ,  C07D265/26 ,  C07D265/36 ,  C07D277/20 ,  C07D277/28 ,  C07D277/34 ,  C07D277/38 ,  C07D277/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供具有P2X3和/或P2X2 / 3受体拮抗作用的新化合物。 一种具有P2X3和/或P2X2 / 3受体拮抗作用的药物组合物，其包含式（I）化合物：其中环A是取代或未取代的5至7元环烷烃，取代或未取代的5至7元环烯烃或 喜欢; C是碳原子; -X-是-N（R 16） - 等; R 16是氢，取代或未取代的烷基等; R 7是取代或未取代的5元或6元杂芳基，取代或未取代的6至10元芳基; Q1和Q2各自独立地为碳原子或氮原子; -L-是-O-，-S-等; R6是取代或未取代的环烷基，取代或未取代的环烯基等; R2是氢，羟基等，或其药学上可接受的盐或其溶剂合物。

公开(公告)号：US20110183939A1

公开(公告)日：2011-07-28

申请号：US13121072

申请日：2009-09-24

申请人： Hiroyuki Kai ,  Yoshiyuki Taoda ,  Takeshi Endoh ,  Tohru Horiguchi ,  Kentaro Asahi ,  Hiroyuki Tobinaga

发明人： Hiroyuki Kai ,  Yoshiyuki Taoda ,  Takeshi Endoh ,  Tohru Horiguchi ,  Kentaro Asahi ,  Hiroyuki Tobinaga

IPC分类号： A61K31/695 ,  A61K31/4439 ,  C07D487/04 ,  A61K31/422 ,  A61K31/4162 ,  A61K31/444 ,  C07F7/02 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/5377

CPC分类号： C07D487/04 ,  C07D207/38 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D405/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04

摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(═O)—, etc.; Z3a and Z3b are taken together ═O or ═S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.

摘要翻译： 本发明提供了一种新型的P2X3和/或P2X2 / 3受体拮抗剂。 由式（I）表示的化合物; 其中Z1是任选保护的羟基等; Z2是-C（= O） - 等; Z3a和Z3b合在一起= = 0或= t为0〜4的整数; R4a和R4b各自独立地为氢或取代或未取代的低级烷基等; m和n各自独立地为0〜2的整数。 k是0或1的整数; 环A是芳族碳环或杂环等; B是芳族碳环环 - 二基或杂环环二基等; R1a和R1b各自独立地为卤素，羟基，取代或未取代的低级烷基等; R2是取代或未取代的烷基等; R3是取代或未取代的烷基，取代或未取代的芳基或取代或未取代的杂环基等; 或其药学上可接受的盐或其溶剂合物。

公开(公告)号：US09718790B2

公开(公告)日：2017-08-01

申请号：US13814346

申请日：2011-08-09

申请人： Hiroyuki Kai ,  Tohru Horiguchi ,  Kentaro Asahi ,  Yasuhiko Fujii

发明人： Hiroyuki Kai ,  Tohru Horiguchi ,  Kentaro Asahi ,  Yasuhiko Fujii

IPC分类号： C07D251/46 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  A61P25/02 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D251/52 ,  C07D403/04 ,  C07D405/14

CPC分类号： C07D251/46 ,  C07D251/52 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Ri are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstjtuted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.

公开(公告)号：US08575197B2

公开(公告)日：2013-11-05

申请号：US13121072

申请日：2009-09-24

申请人： Hiroyuki Kai ,  Yoshiyuki Taoda ,  Takeshi Endoh ,  Kentaro Asahi ,  Hiroyuki Tobinaga

发明人： Hiroyuki Kai ,  Yoshiyuki Taoda ,  Takeshi Endoh ,  Kentaro Asahi ,  Hiroyuki Tobinaga

IPC分类号： A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/402 ,  A61K31/4025 ,  C07D207/38 ,  C07D271/06 ,  C07D261/08 ,  C07D409/10 ,  C07D403/14 ,  C07D413/14 ,  C07D401/04

CPC分类号： C07D487/04 ,  C07D207/38 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D405/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04

摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(═O)—, etc.; Z3a and Z3b are taken together ═O or ═S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.

摘要翻译： 本发明提供了一种新型的P2X3和/或P2X2 / 3受体拮抗剂。 由式（I）表示的化合物：其中Z 1任选被保护的羟基等; Z2是-C（= O） - 等; Z3a和Z3b在一起= O或= S; t为0〜4的整数; R4a和R4b各自独立地为氢或取代或未取代的低级烷基等; m和n各自独立地为0〜2的整数。 k是0或1的整数; 环A是芳族碳环或杂环等; B是芳族碳环环 - 二基或杂环环二基等; R1a和R1b各自独立地为卤素，羟基，取代或未取代的低级烷基等; R2是取代或未取代的烷基等; R3是取代或未取代的烷基，取代或未取代的芳基或取代或未取代的杂环基等; 或其药学上可接受的盐或其溶剂合物。