公开(公告)号：US07928264B2

公开(公告)日：2011-04-19

申请号：US11547847

申请日：2005-09-20

Applicant: Kouji Hattori ,  Susumu Toda ,  Kenichi Washizuka ,  Shinji Ito ,  Daisuke Tanabe ,  Takanobu Araki ,  Minoru Sakurai

Inventor： Kouji Hattori ,  Susumu Toda ,  Kenichi Washizuka ,  Shinji Ito ,  Daisuke Tanabe ,  Takanobu Araki ,  Minoru Sakurai

IPC: C07C213/00

CPC classification number: C07D213/70 ,  C07C311/51 ,  C07C323/63 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/42 ,  C07D213/38 ,  Y02P20/55

Abstract: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, —Z—R9 or (b), in which —Z— is —0—, —S—, R9 —SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.

Abstract translation: 本发明涉及式[I]的化合物：其中（a）其中-Y-，R4，R5和R6各自如说明书中所定义的R 5等，R 1是氢，卤素，低级烷基 ，羟基等，R2是氢，低级烷基或羟基（低级）烷基，R3是氢或氨基保护基，20R7是氢，低级烷基，环（低级）烷基，低级R9链烯基，-Z-R9或 （b）中，-Z-是-O - ， - S - ，R 9 -SO-或-SO 2 - ，各R 9独立地是氢，低级烷基，环（低级）烷基等， DE-R10，其中-D-是-CONHSO2-或-SO 2 NHCO-，E是键或低级亚烷基，R 10是卤素，氰基，羧基等，或其前药或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于溃疡，膀胱过度活动症等的预防和/或治疗性治疗。

公开(公告)号：US20050137236A1

公开(公告)日：2005-06-23

申请号：US11016886

申请日：2004-12-21

Applicant: Kouji Hattori ,  Susumu Toda ,  Masashi Imanishi ,  Shinji Ito ,  Kenichi Washizuka ,  Takanobu Araki ,  Minoru Sakurai ,  Daisuke Tanabe

Inventor： Kouji Hattori ,  Susumu Toda ,  Masashi Imanishi ,  Shinji Ito ,  Kenichi Washizuka ,  Takanobu Araki ,  Minoru Sakurai ,  Daisuke Tanabe

IPC: C07C229/38 ,  C07C229/56 ,  C07C271/16 ,  C07C311/51 ,  C07C323/63 ,  C07D213/38 ,  C07D213/61 ,  A61K31/44 ,  A61K31/195

CPC classification number: C07C229/56 ,  C07C229/38 ,  C07C271/16 ,  C07C311/51 ,  C07C323/63 ,  Y02P20/55

Abstract: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract translation: 本发明涉及化合物式[I]：其中X是键，-CH 2 - ， - O-或-NH-，R 1和R 2 > 12个各自独立地为氢，卤素，低级烷基等，R 2为氢或任选取代的低级烷基，R 3为氢或氨基 保护基，R 4，R 5和R 6各自独立地为氢或任选取代的低级烷基，R 7 O 其中Z为键，等等，R 13为羧基，低级烷氧基羰基，（低级烷基磺酰基）氨基甲酰基或低级烷酰基氨磺酰基，R 0为 其中Y为键，-CH 2 - ， - O - ， - S-等，其中R为 - 低级烷基，环（低级）烷基等，R 11是氢，低级烷基，低级烷氧基等，或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

公开(公告)号：US20100256048A1

公开(公告)日：2010-10-07

申请号：US12740129

申请日：2008-10-28

Applicant: Masaki Tomishima ,  Hiroshi Morikawa ,  Takuya Makino ,  Masashi Imanishi ,  Natsuko Kayakiri ,  Toru Asano ,  Takanobu Araki ,  Toshiya Nakagawa

Inventor： Masaki Tomishima ,  Hiroshi Morikawa ,  Takuya Makino ,  Masashi Imanishi ,  Natsuko Kayakiri ,  Toru Asano ,  Takanobu Araki ,  Toshiya Nakagawa

IPC: A61K38/12 ,  C07K7/54 ,  A61P31/10

CPC classification number: C07K7/56 ,  A61K38/00

Abstract: [Problems] To provide an antibacterial agent, particularly a novel polypeptide compound having an antifungal action. [Means for Solution] As a result of an extensive study on a novel antifungal agent, the inventors have found that an excellent anti-deep-fungal activity is exhibited by introducing a cyclohexylmethylamino group or a piperidylmethylamino group as a partial structure of a natural polypeptide compound, and completed the present invention. The compound of the present invention has an excellent antibacterial activity and is therefore useful as an agent for preventing or treating various fungal infections.

Abstract translation: [问题]提供抗菌剂，特别是具有抗真菌作用的新型多肽化合物。 [解决方案]作为对新型抗真菌剂的广泛研究的结果，本发明人发现通过引入环己基甲基氨基或哌啶基甲基氨基作为天然多肽的部分结构，显示出优异的抗深度真菌活性 化合物，完成了本发明。 本发明的化合物具有优异的抗菌活性，因此可用作预防或治疗各种真菌感染的药剂。

公开(公告)号：US07417060B2

公开(公告)日：2008-08-26

申请号：US11016886

申请日：2004-12-21

Applicant: Kouji Hattori ,  Susumu Toda ,  Masashi Imanishi ,  Shinji Ito ,  Kenichi Washizuka ,  Takanobu Araki ,  Minoru Sakurai ,  Daisuke Tanabe

Inventor： Kouji Hattori ,  Susumu Toda ,  Masashi Imanishi ,  Shinji Ito ,  Kenichi Washizuka ,  Takanobu Araki ,  Minoru Sakurai ,  Daisuke Tanabe

IPC: A61K31/44 ,  A61K31/195

CPC classification number: C07C229/56 ,  C07C229/38 ,  C07C271/16 ,  C07C311/51 ,  C07C323/63 ,  Y02P20/55

Abstract: The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract translation: 本发明涉及化合物式[I]：其中X是键，-CH 2 - ， - O-或-NH-，R 1和R 2 > 12个各自独立地为氢，卤素，低级烷基等，R 2为氢或任选取代的低级烷基，R 3为氢或氨基 保护基，R 4，R 5和R 6各自独立地为氢或任选取代的低级烷基，R 7 O 其中Z为键，等等，R 13为羧基，低级烷氧基羰基，（低级烷基磺酰基）氨基甲酰基或低级烷酰基氨磺酰基，R 0为 其中Y为键，-CH 2 - ， - O - ， - S-等，其中R为 - 低级烷基，环（低级）烷基等，R 11是氢，低级烷基，低级烷氧基等，或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。

公开(公告)号：US20080039506A1

公开(公告)日：2008-02-14

申请号：US11547847

申请日：2005-09-20

Applicant: Kouji Hattori ,  Susumu Toda ,  Kenichi Washizuka ,  Shinji Ito ,  Daisuke Tanabe ,  Takanobu Araki ,  Minoru Sakurai

Inventor： Kouji Hattori ,  Susumu Toda ,  Kenichi Washizuka ,  Shinji Ito ,  Daisuke Tanabe ,  Takanobu Araki ,  Minoru Sakurai

IPC: A61K31/44 ,  A61K31/164 ,  A61K31/265 ,  A61P1/04 ,  C07C233/00 ,  C07D213/02 ,  C07C271/00 ,  A61P13/10 ,  A61K31/35 ,  A61K31/404

CPC classification number: C07D213/70 ,  C07C311/51 ,  C07C323/63 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/42 ,  C07D213/38 ,  Y02P20/55

Abstract: The present invention relates to a compound of the formula [I]: wherein (a), in which —Y—, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, -Z-R9 or (b), in which -Z- is -0-, —S—, R9—SO— or —SO2—, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R , in which -D- is —CONHSO2— or —S02NHCO—, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.

Abstract translation: 本发明涉及式[I]化合物：其中（a），其中-Y-，R 4，R 5和R 6 每一个如说明书中所定义的，其中R 1是氢，卤素，低级烷基，羟基 等等，R 2是氢，低级烷基或羟基（低级）烷基，R 3是氢或氨基保护基，R 20，R 20， 其中-Z-是-O - ， - S - ， - S（O） - ， - （R） 9个-SO-或-SO 2 - ，每个R 9独立地是氢，低级烷基，环（低级）烷基等，R 其中D是-CONHSO 2 - 或-SO 2 NHCO-，其中D是 - E是键或低级亚烷基，R 10是卤素，氰基，羧基等，或其前药或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于溃疡，膀胱过度活动症等的预防和/或治疗性治疗。