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公开(公告)号：US4510307A
公开(公告)日：1985-04-09
申请号：US293192
申请日：1981-08-17
申请人： Hiroyoshi Hidaka , Takanori Sone , Yasuharu Sasaki , Taisuke Sugihara , Seiji Takagi , Kiyohide Sako
发明人： Hiroyoshi Hidaka , Takanori Sone , Yasuharu Sasaki , Taisuke Sugihara , Seiji Takagi , Kiyohide Sako
IPC分类号： C07D239/86 , C07D239/88 , C07D239/94 , C07D265/00 , C07D247/00 , C07D403/00
CPC分类号： C07D239/94 , C07D239/86 , C07D239/88 , Y10S514/929
摘要： A 6-quinazolinesulfonyl derivative of Formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1-12 alkyl group:R.sub.2 is a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.4-10 cycloalkyl group, an aryl group or an aralkyl group; andR.sub.1 and R.sub.2 may be linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring together with the adjacent nitrogen atom; andR.sub.3 is a ##STR2## group wherein R.sub.4 is a C.sub.1-8 alkyl group; a --HN(CH.sub.2).sub.n NH.sub.2 group wherein n is an integer of 2 to 10; or a ##STR3## group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
摘要翻译： 式（I）的6-喹唑啉磺酰基衍生物：其中R1是氢原子或C1-12烷基：R2是氢原子，C1-12烷基，C4-10环烷基 ，芳基或芳烷基; R1和R2可以直接或通过氧原子连接，与相邻的氮原子一起形成5-至7-元杂环; 并且R 3是一个
基团，其中R 4是C 1-8烷基; 其中n为2〜10的整数的-HN（CH 2）n NH 2基; 或 组 及其药学上可接受的盐; 及其制备方法。 本发明的化合物对于血管平滑肌具有松弛作用，并且可用作血管扩张剂和低血压。 -
公开(公告)号：US4751302A
公开(公告)日：1988-06-14
申请号：US739061
申请日：1985-05-29
IPC分类号： C07D231/56 , C07D295/067 , C07D295/092 , C07D401/06 , C07D403/04 , A61K31/415 , C07C87/00
CPC分类号： C07D231/56 , C07D295/067 , C07D295/088 , C07D401/06 , C07D403/04
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent;Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group;Z.sub.2 is a hydrogen atom or an amino group;when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups;when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR4## in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom;when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group;when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions;and the physiologically acceptable acid addition salt thereof.
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公开(公告)号：US4560755A
公开(公告)日：1985-12-24
申请号：US572419
申请日：1984-01-20
IPC分类号： C07D217/02 , C07D401/12 , A61K31/495
CPC分类号： C07D217/02
摘要： A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least one;R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR3## wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
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公开(公告)号：US4533731A
公开(公告)日：1985-08-06
申请号：US475945
申请日：1983-03-16
IPC分类号： C07D231/56 , C07D295/067 , C07D295/092 , C07D401/06 , C07D403/04 , C07D413/06
CPC分类号： C07D231/56 , C07D295/067 , C07D295/088 , C07D401/06 , C07D403/04
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## group wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## group in ##STR4## group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent;Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group;Z.sub.2 is a hydrogen atom or an amino group;when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups;when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR5## group in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom;when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group;when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof which compounds have pharmaceutical utility, e.g.: treating inflammation.
摘要翻译： 式（I）的化合物：其中W1和W2各自独立地是氢原子或其中Y是n-C1-6亚烷基或n-C1-6亚烷基的基团 具有C 1-6烷基取代基的基团; 并且R 1和R 2各自独立地为氢原子或C 1-6烷基，并且
基团中的 基团可以形成选自吗啉代，吡咯烷子基，哌啶子基，高哌啶基和哌嗪基的饱和杂环 除了吗啉代基以外的饱和杂环可以具有至少一个C 1-4烷基，羟基或卤素原子作为取代基; Z1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C1-3烷基或甲氧基; Z2是氢原子或氨基; 当W1和W2都是氢原子时，Z1是羟基或碘原子，Z2是氢原子，或Z1和Z2都是氨基; 当Z1和Z2都是氢原子时，W1或W2中的“IMAGE”基团是吗啉基; 当Z1是氯原子，羟基，碘原子，甲基或甲氧基时，Z2是氢原子; 当Z 1为氨基时，Z 2为氢原子或氨基; 当Z1是甲基时，甲氧基或氨基，Z1位于5-位; 当Z1为碘原子时，Z1为5-或7-位; 当Z 1和Z 2都是氨基时，Z 1和Z 2在5-和7-位; 和其生理上可接受的酸加成盐，其化合物具有药用效用，例如：治疗炎症。 -
公开(公告)号：US4525589A
公开(公告)日：1985-06-25
申请号：US572418
申请日：1984-01-20
IPC分类号： C07D217/02 , C07D413/12
CPC分类号： C07D217/02
摘要： A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least oneR.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; orthe ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
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公开(公告)号：US4456757A
公开(公告)日：1984-06-26
申请号：US357770
申请日：1982-03-12
IPC分类号： C07D217/02 , A61K31/47 , C07D401/12 , C07D413/12
CPC分类号： C07D217/02
摘要： A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one;m and n each is an integer of one to nine;m+n is an integer of at least one;R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; orR.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group;R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; orthe ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, and aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.
摘要翻译： 式（I）的5-异喹啉磺酰基衍生物：其中I为0或1; m和n各自为1至9的整数; m + n是至少一个的整数; R1是氢原子，C1-10烷基，C5-6环烷基或芳基; 或R 2和R 3各自为氢原子，C 1-10烷基，C 5-6环烷基，芳基或芳烷基; R2和R3是C1-6亚烷基，直接或通过氧原子与相邻氮原子形成5至7元杂环; 或者
组是一个 基团，其中R4和R5各自为氢原子，C1-10烷基，芳基或芳烷基，R6为氢原子，C1-10烷基， 芳基，芳烷基，苯甲酰基，肉桂基，肉桂酰基，糠酰基或ⅩⅩⅧ基，其中R 7为C 1-8烷基; 及其药学上可接受的盐; 及其制备方法。 本发明的化合物对于血管平滑肌具有松弛作用，并且可用作血管扩张剂和低血压。 -
公开(公告)号：US4474964A
公开(公告)日：1984-10-02
申请号：US569524
申请日：1984-01-09
IPC分类号： C07D231/56 , C07D295/092 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## group wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## group wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## group; and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## group; and the pharmaceutically acceptable acid addition salt thereof having antiinflammatory, analgesic and digestive tract ulcer suppressing activity.
摘要翻译： 式（I）的化合物：其中W1是氢原子或其中Y是C1-6亚烷基或具有C1-6烷基的C1-6亚烷基的基团 取代基; 并且R 1和R 2各自独立地为氢原子或C 1-6烷基，并且R 1和R 2可以与相邻的氮原子一起形成C 4-6杂环或含氮的C 4-6杂环，并且C 4-6 杂环可以具有至少一个C 1-6烷基，羟基或卤素原子; W2是氢原子或其中Z是C1-6亚烷基或具有C1-6烷基取代基的C1-6亚烷基的基团; 并且R 3和R 4各自独立地为氢原子或C 1-6烷基，并且R 3和R 4可以与相邻的氮原子一起形成C 4-6杂环或含氮的C 4-6杂环，且C 4-6 杂环可以具有至少一个C 1-6烷基，羟基或卤素原子; 当W1是氢原子时，W2是
组; 当W2是氢原子时，W1是 组; 和其药学上可接受的酸加成盐具有抗炎，止痛和消化道溃疡抑制活性。 -
公开(公告)号：US4585869A
公开(公告)日：1986-04-29
申请号：US636420
申请日：1984-07-31
IPC分类号： C07D231/56 , C07D295/092 , C07D401/06 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## and the pharmaceutically acceptable acid addition salt thereof having antiinflammatory, analgesic and digestive tract ulcer suppressing activity.
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公开(公告)号：US4549023A
公开(公告)日：1985-10-22
申请号：US636293
申请日：1984-07-31
IPC分类号： C07D231/56 , C07D295/092 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , C07D295/088
摘要： A compound of the formula (I): ##STR1## wherein W.sub.1 is a hydrogen atom or a ##STR2## wherein Y is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.1 and R.sub.2 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;W.sub.2 is a hydrogen atom or a ##STR3## wherein Z is a C.sub.1-6 alkylene group or a C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.3 and R.sub.4 each independently is a hydrogen atom or a C.sub.1-6 alkyl group and R.sub.3 and R.sub.4 may form a C.sub.4-6 heterocyclic ring or a nitrogen-containing C.sub.4-6 heterocyclic ring together with the adjacent nitrogen atom and the C.sub.4-6 heterocyclic rings may have at least one C.sub.1-6 alkyl group, hydroxyl group or halogen atom;when W.sub.1 is a hydrogen atom, W.sub.2 is the ##STR4## and when W.sub.2 is a hydrogen atom, W.sub.1 is the ##STR5## and the pharmaceutically acceptable acid addition salt thereof.
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