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：US20060111446A1

公开(公告)日：2006-05-25

申请号：US11246641

申请日：2005-10-11

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Ritsu Suzuki

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Ritsu Suzuki

IPC分类号： A61K31/18 ,  C07C311/45

CPC分类号： C07C311/29

摘要： The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts 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-N-（2-氨基苯乙基）-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或低级烷基; R 2表示氢原子，任选取代的低级烷基等; R 3是二（低级烷基）氨基，低级烷基，环烷基等; Q是氢原子或任意取代的低级烷基; Z是氢原子或羟基等，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发生相关疾病的药剂 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：US07022689B2

公开(公告)日：2006-04-04

申请号：US10486137

申请日：2002-08-08

申请人： Kosuke Okazaki ,  Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Ritsu Suzuki

发明人： Kosuke Okazaki ,  Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Hideki Takeuchi ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Ritsu Suzuki

IPC分类号： A01N43/00 ,  A61K31/33

CPC分类号： C07C311/29

摘要： The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, etc.; R3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts 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-N-（2-氨基苯乙基）-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或低级烷基; R 2表示氢原子，任选取代的低级烷基等; R 3是二（低级烷基）氨基，低级烷基，环烷基等; Q是氢原子或任意取代的低级烷基; Z是氢原子或羟基等，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发生相关疾病的药剂 活化凝血因子X，包含其的药物组合物，其药物用途和其中间体。

公开(公告)号：US20050014787A1

公开(公告)日：2005-01-20

申请号：US10495063

申请日：2002-10-29

申请人： Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Hideyuki Muranaka

发明人： Masahiko Uchida ,  Hiroaki Kobayashi ,  Yuichiro Kai ,  Kenji Yokoyama ,  Yoshihiro Terao ,  Hideyuki Muranaka

IPC分类号： A61K31/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P25/28 ,  A61P31/16 ,  C07C311/29 ,  C07D207/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/273 ,  C07D211/42 ,  C07D211/60 ,  C07D213/42 ,  C07D213/82 ,  C07D231/12 ,  C07D233/02 ,  C07D261/08 ,  C07D263/38 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D277/44 ,  C07D277/46 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D317/62 ,  C07D333/20 ,  A61K31/445 ,  A61K31/195 ,  A61K31/40

CPC分类号： C07D207/273 ,  A61K31/18 ,  C07C311/29 ,  C07D207/00 ,  C07D207/16 ,  C07D211/42 ,  C07D211/60 ,  C07D213/42 ,  C07D213/82 ,  C07D231/12 ,  C07D233/02 ,  C07D261/08 ,  C07D263/38 ,  C07D271/113 ,  C07D277/28 ,  C07D277/46 ,  C07D295/088 ,  C07D295/13 ,  C07D295/185 ,  C07D295/192 ,  C07D317/62 ,  C07D333/20

摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or 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 and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

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为任选取代的低级烷基，任选取代的低级烷氧基，任意取代的低级烯基，环烷基 或低级酰基等。 Q是氢原子或任意取代的低级烷基; 和Z是氢原子或羟基等，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试剂， 活化凝血因子X，包含其的药物组合物和其中间体。 这些化合物可用作各种疾病如脑梗塞，脑血栓形成，脑栓塞，TIA，脑血管紧张，阿尔茨海默氏病，心肌梗塞，心脏病发作，心力衰竭，血栓形成，肺梗死和肺栓塞等疾病的预防措施或治疗方法。

公开(公告)号：US6133266A

公开(公告)日：2000-10-17

申请号：US125429

申请日：1999-02-10

申请人： Makio Kitazawa ,  Kosuke Okazaki ,  Tetsuro Tamai ,  Masaru Saito ,  Nobuyuki Tanaka ,  Hiroaki Kobayashi ,  Ken Kikuchi ,  Hideyuki Muranaka

发明人： Makio Kitazawa ,  Kosuke Okazaki ,  Tetsuro Tamai ,  Masaru Saito ,  Nobuyuki Tanaka ,  Hiroaki Kobayashi ,  Ken Kikuchi ,  Hideyuki Muranaka

IPC分类号： C07C235/06 ,  C07D295/185 ,  A61K31/165 ,  A61K31/535 ,  C07D295/192

CPC分类号： C07D295/185 ,  C07C235/06 ,  C07C2102/10

摘要： The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.

摘要翻译： PCT No.PCT / JP97 / 00424 Sec。 371日期1999年2月10日 102（e）1999年2月10日PCT PCT 1997年2月18日PCT公布。 第WO97 / 30023号公报 日期：1997年8月21日本发明涉及由以下通式表示的3,4-二取代苯基乙酰胺基四氢化萘甲酰胺衍生物：其中A表示低级亚烷基; B表示氨基，二（低级烷基）氨基或3- 在环中可以含有氧原子的7元脂环族氨基; n为1或2的整数; *表示的碳原子为R构型，S构型或其混合物中的碳原子，碳原子 标记为（S）表示S构型的碳原子）及其药学上可接受的盐，其具有选择性β2-肾上腺素能受体刺激作用，并且在心脏上缓解负担，例如心动过速，并且可用作预防受威胁的药剂 流产和早产，支气管扩张剂和尿路结石症中的疼痛缓解和除石剂。