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：US20110319414A1

公开(公告)日：2011-12-29

申请号：US13201209

申请日：2010-02-10

申请人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tsuyoshi Hasegawa ,  MIho Oohara ,  Yukio Tada ,  Takeshi Endoh

发明人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tsuyoshi Hasegawa ,  MIho Oohara ,  Yukio Tada ,  Takeshi Endoh

IPC分类号： A61K31/53 ,  C07D251/46 ,  C07D403/06 ,  A61P7/00 ,  C07D413/12 ,  A61K31/5377 ,  A61P29/00 ,  A61P25/00 ,  C07D251/38 ,  C07D251/52

CPC分类号： C07D251/46 ,  C07D251/16 ,  C07D251/44 ,  C07D251/52 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12

摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I); wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ═Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ═Z is ═O, etc.; and n is an integer of 0 to 4.

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Ra，Rb和Rc为（a）Ra和Rb一起为= Z; Rc为由R1c表示的基团; 或（b）Rb和Rc一起形成键; 并且R a是由-Y-R 1a表示的基团; R1a和R1c各自独立地为氢，取代或未取代的烷基等; R2和R3各自独立地是取代或未取代的芳基等; R4a和R4b各自独立地为氢，取代或未取代的烷基等; X是-N（R 5） - 等; R5是氢，取代或未取代的低级烷基等; -Y-是-O-等; ═Z是═O等; n为0〜4的整数。

公开(公告)号：US09150546B2

公开(公告)日：2015-10-06

申请号：US13201209

申请日：2010-02-10

申请人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tsuyoshi Hasegawa ,  Miho Oohara ,  Yukio Tada ,  Takeshi Endoh

发明人： Hiroyuki Kai ,  Takayuki Kameyama ,  Tsuyoshi Hasegawa ,  Miho Oohara ,  Yukio Tada ,  Takeshi Endoh

IPC分类号： A61K31/535 ,  A61K31/53 ,  C07D403/06 ,  C07D251/46 ,  C07D251/52 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12

CPC分类号： C07D251/46 ,  C07D251/16 ,  C07D251/44 ,  C07D251/52 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12

摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I): wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ═Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ═Z is ═O, etc.; and n is an integer of 0 to 4.

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Ra，Rb和Rc为（a）Ra和Rb一起为= Z; Rc为由R1c表示的基团; 或（b）Rb和Rc一起形成键; 并且R a是由-Y-R 1a表示的基团; R1a和R1c各自独立地为氢，取代或未取代的烷基等; R2和R3各自独立地是取代或未取代的芳基等; R4a和R4b各自独立地为氢，取代或未取代的烷基等; X是-N（R 5） - 等; R5是氢，取代或未取代的低级烷基等; -Y-是-O-等; ═Z是═O等; n为0〜4的整数。