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    • 6. 发明申请
    • PYRROLOTHIAZINE AND PYRROLOTHIAZEPINE COMPOUNDS HAVING SEROTONIN-2 RECEPTOR ANTAGONISTIC AND ALPHA1-BLOCKING ACTION
    • 具有SEROTONIN-2受体拮抗剂和ALPHA1阻断作用的吡罗昔康和吡咯烷酮化合物
    • WO9933840A2
    • 1999-07-08
    • PCT/JP9805954
    • 1998-12-25
    • SUNTORY LTDMIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • MIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • A61K31/54A61K31/55A61P9/00A61P9/02A61P9/06A61P9/08A61P9/10A61P9/12A61P43/00C07D207/36C07D513/04
    • C07D513/04C07D207/36
    • A pyrrolesulfonamide derivative having formula (I) wherein the ring P represented by alpha is a pyrrole ring having structure beta or psi wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group delta in which W represents CH, C= or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C=; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
    • 具有式(I)的吡咯磺酰胺衍生物,其中由α表示的环P是具有β或psi结构的吡咯环,其中R表示烷基,环烷基,环烷基 - 烷基或芳烷基; 虚线表示存在或不存在键; 当存在键时,Z 2不存在,Z1表示H,但当不存在键时,Z1表示H,Z2表示OH或Z1,Z2组合在一起表示O或NOR1基团,其中R1表示 H或烷基,芳烷基或芳基; 代表0或1; A表示亚烷基,亚烯基或亚炔基; 并且Y表示其中W表示CH,C =或N的组δ; 当W为CH或N时,m代表0或1,当W为C =时,m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基。 化合物(I)具有强的5-羟色胺-2受体拮抗作用,毒性低,副作用小,作为循环系统疾病如缺血性心脏病,脑血管障碍和周围循环障碍的治疗有用。
    • 7. 发明申请
    • PYRROLOTHIAZINE AND PYRROLOTHIAZEPINE COMPOUNDS HAVING SEROTONIN-2 RECEPTOR ANTAGONISTIC AND ALPHA-1-BLOCKING ACTION
    • 具有SEROTONIN-2受体拮抗剂和ALPHA-1阻断作用的吡咯烷酮和吡咯烷酮化合物
    • WO9933841B1
    • 2001-05-25
    • PCT/JP9805955
    • 1998-12-25
    • SUNTORY LTDMIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • MIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • A61K31/54A61K31/55A61P9/00A61P9/06A61P9/08A61P9/10A61P9/12A61P43/00C07D207/36C07D513/04
    • C07D513/04C07D207/36
    • A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by ( alpha ) is a pyrrole ring having structure ( beta ) or ( psi ) wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group ( delta ) in which W represents CH, C= or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C=; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with alpha 1-blocking action and serotonin-2 receptor antagonistic action in combination.
    • 具有式(I)的吡咯磺酰胺化合物,其中由(α)表示的环P是具有结构(β)或(psi)的吡咯环,其中A表示亚烷基,亚烯基或亚炔基; Y表示W表示CH,C =或N的基团(delta); 当W为CH或N时,m代表0或1,当W为C =时,m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基; 代表0或1; 虚线表示存在或不存在键; 当存在键时,Z 2不存在,Z1表示H,但当不存在键时,Z1表示H,Z2表示OH或Z1,Z2组合在一起表示O或NOR5基团,其中R5表示 H或烷基,芳烷基或芳基; R代表H,烷基,环烷基,环烷基 - 烷基或芳烷基。 化合物(1)对迄今为止报道的具有α1-阻断作用和5-羟色胺-2受体拮抗作用的药物的效力,对5-羟色胺2受体以外的受体的选择性,毒性,副作用等改善。 结合。
    • 8. 发明申请
    • PYRROLOTHIAZINE AND PYRROLOTHIAZEPINE COMPOUNDS HAVING SEROTONIN-2 RECEPTOR ANTAGONISTIC AND ALPHA-1-BLOCKING ACTION
    • 具有SERONON-2受体拮抗剂和ALPHA-1阻断作用的吡罗昔康和吡咯烷酮化合物
    • WO9933841A2
    • 1999-07-08
    • PCT/JP9805955
    • 1998-12-25
    • SUNTORY LTDMIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • MIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • A61K31/54A61K31/55A61P9/00A61P9/06A61P9/08A61P9/10A61P9/12A61P43/00C07D207/36C07D513/04
    • C07D513/04C07D207/36
    • A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by ( alpha ) is a pyrrole ring having structure ( beta ) or ( psi ) wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group ( delta ) in which W represents CH, C= or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C=; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with alpha 1-blocking action and serotonin-2 receptor antagonistic action in combination.
    • 具有式(I)的吡咯磺酰胺化合物,其中由(α)表示的环P是具有结构(β)或(psi)的吡咯环,其中A表示亚烷基,亚烯基或亚炔基; Y表示W(CH),C =或N的基团(delta); 当W为CH或N时,m代表0或1,当W为C =时,m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基; 代表0或1; 虚线表示存在或不存在键; 当存在键时,Z 2不存在,Z1表示H,但当不存在键时,Z1表示H,Z2表示OH或Z1,Z2组合在一起表示O或NOR5基团,其中R5表示 H或烷基,芳烷基或芳基; 且R代表H,烷基,环烷基,环烷基 - 烷基或芳烷基。 化合物(1)对迄今为止报道的具有α1-阻断作用和5-羟色胺-2受体拮抗作用的药物的效力,对5-羟色胺2受体以外的受体的选择性,毒性,副作用等改善 结合。