公开(公告)号：EP0893432A4

公开(公告)日：2002-01-02

申请号：EP97914598

申请日：1997-04-04

申请人： KISSEI PHARMACEUTICAL

发明人： KITAZAWA MAKIO ,  OKAZAKI KOSUKE ,  TAMAI TETSURO ,  SAITO MASARU ,  TANAKA NOBUYUKI ,  KOBAYASHI HIROAKI ,  KIKUCHI KEN ,  MURANAKA HIDEYUKI

IPC分类号： A61K31/165 ,  A61K31/445 ,  A61K31/535 ,  C07C235/06 ,  C07D295/16 ,  C07D295/185 ,  A61K31/495 ,  C07D295/18

CPC分类号： C07D295/185 ,  C07C235/06 ,  C07C2602/10

摘要： Phenylethanolaminotetralincarboxamide derivative represented by general formula (I) and pharmacologically acceptable salts thereof, wherein A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino which may bear oxygen on the ring; the asterisked carbon atom represents a carbon atom with an R- or S-configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective β2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

摘要翻译： 由通式（I）表示的苯乙醇氨基四氢吡喃甲酰胺衍生物及其药理学上可接受的盐，其中A代表低级亚烷基; B表示氨基，二（低级烷基）氨基或在环上可以带有氧的3-7元脂环族氨基; 带星号的碳原子表示具有R-或S-构型的碳原子或这些原子的混合物; 并且用（S）标记的碳原子表示具有S-构型的碳原子。 这些化合物具有选择性β2 - 肾上腺素能受体刺激作用，同时减轻心脏负担，例如心动过速，并且可用作预先堕胎和早产的预防剂，支气管扩张剂和用于缓解泌尿系结石的药物。

公开(公告)号：EP1331221A4

公开(公告)日：2005-11-23

申请号：EP01972648

申请日：2001-10-02

申请人： KISSEI PHARMACEUTICAL

发明人： OKAZAKI KOSUKE ,  UCHIDA MASAHIKO ,  MUKAIYAMA HARUNOBU ,  KOBAYASHI HIROAKI ,  KAI YUICHIRO ,  TAKEUCHI HIDEKI ,  YOKOYAMA KENJI ,  TERAO YOSHIHIRO ,  HOYANO YUJI ,  SHIOHARA HIROAKI ,  KIKUCHI NORIHIKO

IPC分类号： A61P7/02 ,  A61P9/10 ,  C07C311/29 ,  C07C311/37 ,  C07C317/32 ,  C07D277/28 ,  A61K31/216 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/5375 ,  C07D271/10 ,  C07D295/18

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： 5-Amidino-2-hydroxybenzenesulfonamide derivatives of the general formula [I] or their pharmacologically acceptable salts, exhibiting potent and selective inhibitory activity against activated blood coagulation factor X and being useful as preventive or therapeutic drugs for diseases whose onset is related to activated blood coagulation factor X; pharmaceutical compositions containing the same; their use in medicines; and intermediates for their preparation: [I] wherein R is hydrogen or optionally substituted lower alkyl; R is di(lower alkyl)amino, lower alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heterocycloalkyl, or an optionally substituted aromatic heterocyclic group; T is oxygen, sulfur, sulfonyl, or the like; Q is hydrogen or optionally substituted lower alkyl; and Z is hydrogen, hydroxyl, or the like.

摘要翻译： 本发明涉及一种由通式表示的5-脒基-2-羟基苯磺酰胺衍生物： worin - [R <1>是一个氢原子或在OPTIONALLY substituiertem低级烷基; [R <2>是二（低级烷基）氨基，低级烷基，环烷基，在OPTIONALLY substituiertem芳基，在任选取代的杂环基团，或在任选被取代的芳香族杂环基。 T为氧原子，硫原子，磺酰基等; Q处于OPTIONALLY substituiertem氢原子或低级烷基; 且Z为氢原子，羟基基团等，或它们的药学上可接受的盐，其施加一个有效的和选择性的活化血液凝固因子X抑制活性，是作为用于疾病的与在相关联的预防或治疗剂是有用 活化血液凝固第X因子，药物组合物包含相同的，它们并涉及其中间体的药物的用途。

公开(公告)号：EP0894787A4

公开(公告)日：2000-09-20

申请号：EP97914541

申请日：1997-03-26

申请人： KISSEI PHARMACEUTICAL

发明人： KITAZAWA MAKIO ,  OKAZAKI KOSUKE ,  TAMAI TETSURO ,  SAITO MASARU ,  TANAKA NOBUYUKI ,  KOBAYASHI HIROAKI ,  KIKUCHI KEN ,  MURANAKA HIDEYUKI

IPC分类号： C07C217/74 ,  C07C229/46 ,  C07C229/50 ,  A61K31/195 ,  A61K31/215

CPC分类号： C07C229/50 ,  C07C217/74 ,  C07C2602/10 ,  Y02P20/55

摘要： 3,4-Disubstituted phenylethanolaminotetralincarboxylate derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, wherein Q represents vinylene or a group represented by the general formula -A-(CH2)m- (wherein A represents oxygen or methylene, and m represents an integer of 1 to 6); R represents hydrogen or lower alkyl; n represents an integer of 1 or 2; the asterisked carbon atom represents a carbon atom with an R- or S- configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective beta 2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

摘要翻译： 3,4-二取代的通式（I）及其药理学上可接受的盐，其中Q代表亚乙烯基或亚由通式-A-（CH 2）间 - 表示的基团表示phenylethanolaminotetralincarboxylate衍生物（其中A代表氧或亚甲基，且m 表示1至6的整数）; R代表氢或低级烷基; n表示1或2的整数; 带星号的碳原子表示具有R-或S-构型的碳原子或这些原子的混合物; 并且用（S）标记的碳原子表示具有S-构型的碳原子。 这些化合物具有选择性β2肾上腺素能受体刺激作用，同时减少对心脏的负担如心动过速，并可用作预防剂用于先兆流产和早产，支气管扩张药，和剂缓解和排石尿结石是有用的。

公开(公告)号：EP1415983A4

公开(公告)日：2006-01-18

申请号：EP02762759

申请日：2002-08-08

申请人： KISSEI PHARMACEUTICAL

发明人： OKAZAKI KOSUKE ,  UCHIDA MASAHIKO ,  KOBAYASHI HIROAKI ,  KAI YUICHIRO ,  TAKEUCHI HIDEKI ,  YOKOYAMA KENJI ,  TERAO YOSHIHIRO ,  SUZUKI RITSU

IPC分类号： A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P25/28 ,  A61P31/16 ,  A61P37/06 ,  A61P43/00 ,  C07C311/29 ,  C07C311/27 ,  A61K31/18 ,  A61K31/198 ,  A61K31/216 ,  A61K31/223 ,  A61K31/275 ,  A61K31/41 ,  C07D257/04

CPC分类号： C07C311/29

摘要： A 5−amidino−N−(2−aminophenethyl)−2−hydroxybenzenesulfonamide derivative represented by the general formula [I] (wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen, optionally substituted lower alkyl, etc.; R 3 is di(lower alkyl)amino, lower alkyl, cycloalkyl, etc.; Q is hydrogen or optionally substituted lower alkyl; and Z is hydrogen, hydroxy, etc.) or a pharmacologically acceptable salt of the derivative, which have strong and selective inhibitory activity against activated blood coagulation factor X and are useful as a preventive or remedy for diseases in which the activated blood coagulation factor X participates; a medicinal composition containing the compound; a medicinal use of the compound; and an intermediate for the compound.

公开(公告)号：EP0882704A4

公开(公告)日：2000-06-14

申请号：EP97902714

申请日：1997-02-18

申请人： KISSEI PHARMACEUTICAL

发明人： KITAZAWA MAKIO ,  OKAZAKI KOSUKE ,  TAMAI TETSURO ,  SAITO MASARU ,  TANAKA NOBUYUKI ,  KOBAYASHI HIROAKI ,  KIKUCHI KEN ,  MURANAKA HIDEYUKI

IPC分类号： C07C235/06 ,  C07D295/185 ,  A61K31/165 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  C07D295/18

CPC分类号： C07D295/185 ,  C07C235/06 ,  C07C2602/10

摘要： 3,4-Disubstituted phenylethanolaminotetralincarboxamide derivatives represented by general formula (I) and their pharmacologically acceptable salts having a selective β2-adrenergic receptor stimulating effect with a relieved burden on the heart such as frequent pulse. In said formula, A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino optionally containing oxygen in the ring; n is an integer of 1 or 2; the carbon atom marked with '*' means a carbon atom or the R- or S- configuration or a mixture thereof; and the carbon atom marked with '(S)' means a carbon atom of the S-configuration. These compounds are useful as a preventive for threatened abortion/premature birth, a bronchodilator and a pain-relieving and lithagogue agent in ureterolithiasis.

摘要翻译： 由通式（1）表示的3,4-二取代苯乙醇氨基四氢化萘甲酰胺衍生物及其具有选择性β2-肾上腺素能受体刺激作用的药理学上可接受的盐，其具有缓解的心脏负担，例如频繁脉冲。 在所述式中，A表示低级亚烷基; B代表环中任选含有氧的氨基，二（低级烷基）氨基或3-至7-元脂环族氨基; n为1或2的整数; 标有“*”的碳原子是指碳原子或R-或S-构型或其混合物; 标有“（S）”的碳原子是指S-构型的碳原子。 这些化合物可用作威胁性流产/早产的预防剂，支气管扩张剂和输尿管结石症中的止痛和止痛剂。