公开(公告)号：US07208524B2

公开(公告)日：2007-04-24

申请号：US10398383

申请日：2001-10-02

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： A61K31/195 ,  A61K31/18 ,  C07C59/52 ,  C07C307/06

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

摘要翻译： 本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病的药剂， 活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

公开(公告)号：US20060116361A1

公开(公告)日：2006-06-01

申请号：US10398383

申请日：2001-10-02

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： A61K31/44 ,  A61K31/40 ,  A61K31/195

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

公开(公告)号：US07589126B2

公开(公告)日：2009-09-15

申请号：US11553573

申请日：2006-10-27

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： A61K31/195 ,  A61K31/18

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

摘要翻译： 本发明涉及由下列通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任意取代的低级烷基; R2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病， 活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

公开(公告)号：US07217832B2

公开(公告)日：2007-05-15

申请号：US11359430

申请日：2006-02-23

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： C07D265/30 ,  C07D271/113 ,  C07D277/30 ,  C07C255/53 ,  C07C255/63

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

公开(公告)号：US20070105829A1

公开(公告)日：2007-05-10

申请号：US11553573

申请日：2006-10-27

申请人： Kosuke OKAZAKI ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke OKAZAKI ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： A61K31/553 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/445 ,  A61K31/421 ,  A61K31/40 ,  A61K31/18

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

摘要翻译： 本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病的药剂， 活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

公开(公告)号：US20060205812A1

公开(公告)日：2006-09-14

申请号：US11359430

申请日：2006-02-23

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Harunobu Mukaiyama ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Yuji Hoyano ,  Hiroaki Shiohara ,  Norihiko Kikuchi

IPC分类号： A61K31/24 ,  A61K31/195 ,  C07C311/47

CPC分类号： A61K31/18 ,  A61K31/40 ,  A61K31/421 ,  A61K31/445 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

摘要翻译： 本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病， 活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

公开(公告)号：US07563822B2

公开(公告)日：2009-07-21

申请号：US10508209

申请日：2003-03-18

申请人： Takashi Koizumi ,  Yuji Hoyano ,  Satoshi Akahane

发明人： Takashi Koizumi ,  Yuji Hoyano ,  Satoshi Akahane

IPC分类号： A61K31/195

CPC分类号： C07D271/113 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/216 ,  A61K31/275 ,  A61K31/4245 ,  A61K31/5375 ,  A61K45/06 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14 ,  C07D271/10 ,  C07D277/28 ,  C07D295/185 ,  A61K2300/00

摘要： The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2- hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.

摘要翻译： 本发明涉及一种用于预防或治疗肾病的药物，其包含作为活性成分的由通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1为氢原子或任选取代的烷基; R2是二烷基氨基，烷基，环烷基，任意取代的芳基等; T是氧原子，硫原子等; Q是氢原子或任选取代的烷基; Z是对肾小球系膜细胞增殖具有抑制作用，对尿中蛋白质排泄作用下降的氢原子，羟基等，或其药学上可接受的盐，可用于预防或治疗各种肾脏疾病 作为IgA肾病，糖尿病性肾病，肾炎综合征等。

公开(公告)号：US20050107354A1

公开(公告)日：2005-05-19

申请号：US10508209

申请日：2003-03-18

申请人： Takashi Koizumi ,  Yuji Hoyano ,  Satoshi Akahane

发明人： Takashi Koizumi ,  Yuji Hoyano ,  Satoshi Akahane

IPC分类号： A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/216 ,  A61K31/275 ,  A61K31/4245 ,  A61K31/5375 ,  A61K45/06 ,  A61P3/10 ,  A61P13/12 ,  A61P37/02 ,  A61P43/00 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D295/185 ,  A61K31/397 ,  A61K31/445 ,  A61K31/55

CPC分类号： C07D271/113 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/216 ,  A61K31/275 ,  A61K31/4245 ,  A61K31/5375 ,  A61K45/06 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/14 ,  C07D271/10 ,  C07D277/28 ,  C07D295/185 ,  A61K2300/00

摘要： The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.

摘要翻译： 本发明涉及一种用于预防或治疗肾脏疾病的药物，其包含作为活性成分的由通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子 或任选取代的烷基; R 2是二烷基氨基，烷基，环烷基，任选取代的芳基等; T是氧原子，硫原子等; Q是氢原子或任选取代的烷基; Z是对肾小球系膜细胞增殖具有抑制作用，对尿中蛋白质排泄作用下降的氢原子，羟基等，或其药学上可接受的盐，可用于预防或治疗各种肾脏疾病 作为IgA肾病，糖尿病性肾病，肾炎综合征等。

公开(公告)号：US20070105825A1

公开(公告)日：2007-05-10

申请号：US10572515

申请日：2004-09-16

申请人： Yuji Hoyano

发明人： Yuji Hoyano

IPC分类号： A61K31/60 ,  A61K31/519 ,  A61K31/24 ,  A61K31/195

CPC分类号： A61K31/24 ,  A61K31/195 ,  A61K31/519 ,  A61K31/60 ,  A61K2300/00

摘要： The present invention provides a combination drug which is useful for the prevention or treatment of thromboembolism. A pharmaceutical agent comprising an antiplatelet agent in combination with a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R represents a hydrogen atom or a lower alkyl group, and Z represents a hydrogen atom or a hydroxy group, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了可用于预防或治疗血栓栓塞的组合药物。 一种药剂，其特征在于，含有与下述通式表示的5-脒基-2-羟基苯磺酰胺衍生物结合的抗血小板剂：其中R表示氢原子或低级烷基，Z表示氢原子或羟基，或 其药学上可接受的盐。