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31 条记录 (耗时 0.021 秒)

    1,5-benzoxathiepin derivatives
    1.
    发明授权
    1,5-benzoxathiepin derivatives 失效
    1,5-苯并氧硫辛啶衍生物

    公开(公告)号：US4751316A

    公开(公告)日：1988-06-14

    申请号：US38787

    申请日：1987-04-15

    申请人： Hirosada Sugihara ,  Minoru Hirata

    发明人： Hirosada Sugihara ,  Minoru Hirata

    IPC分类号： A61K31/385 ,  A61K31/39 ,  A61K31/495 ,  A61P11/00 ,  C07D327/02 ,  C07D411/06 ,  C07D411/12

    CPC分类号： C07D327/02 ,  C07D411/06 ,  C07D411/12

    摘要： Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.2 receptor blocking activity, calcium antagonism, actions to relieve cerebral vasospasm and to improve renal circulation and diuretic and antithrombotic activities, and are of value as a prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

    2-(piperazinylalkyl)-1-benzothiepin, 1-benzoxepin, and 1,5-benzodioxepin derivatives
    2.
    发明授权
    2-(piperazinylalkyl)-1-benzothiepin, 1-benzoxepin, and 1,5-benzodioxepin derivatives 失效
    2-（哌嗪基烷基）-1-苯并硫代苯，1-苯并氧杂庚环和1,5-苯并二氧杂环庚烯衍生物

    公开(公告)号：US4736031A

    公开(公告)日：1988-04-05

    申请号：US852214

    申请日：1986-04-15

    申请人： Hirosada Sugihara ,  Minoru Hirata

    发明人： Hirosada Sugihara ,  Minoru Hirata

    IPC分类号： C07D313/08 ,  C07D321/10 ,  C07D337/08 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D241/04 ,  A61K31/335 ,  A61K31/38 ,  A61K31/495

    CPC分类号： C07D405/06 ,  C07D313/08 ,  C07D321/10 ,  C07D337/08 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

    摘要： Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.2 receptor blocking activity, actions to relieve cerebral vasospasm and antithrombotic activity, and are of value as a prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

    摘要翻译： 新颖的下式结构的七元杂环化合物：其中R 1和R 2独立地是氢，卤素，羟基，低级烷基或低级烷氧基，R 3和R 4独立地是氢，任选取代的低级烷基，任选取代的环烷基或任选取代的 芳烷基或二者共同与相邻氮原子一起形成任选取代的环，X为氢，任选取代的低级烷基，任选取代的芳基或可被酯化或酰胺化的羧基，Y为> C = O或> CH- OR5，其中R5是氢，酰基或任选取代的氨基甲酰基，A是氧原子或硫原子，E是氧原子或亚甲基，G是低级亚烷基，条件是当A是硫原子时，E是亚甲基，其盐表现出 5-羟色胺S2受体阻断活性，减轻脑血管痉挛和抗血栓形成活性的作用，并且作为缺血性心脏病，血栓形成的预防和治疗剂具有价值 sis，高血压和脑循环障碍。

    1,5-benzoxathiepin derivatives, their production and use
    3.
    发明授权
    1,5-benzoxathiepin derivatives, their production and use 失效
    1,5-苯并恶灵衍生物，其生产和使用

    公开(公告)号：US4672064A

    公开(公告)日：1987-06-09

    申请号：US806809

    申请日：1985-12-10

    申请人： Hirosada Sugihara ,  Minoru Hirata

    发明人： Hirosada Sugihara ,  Minoru Hirata

    IPC分类号： A61K31/385 ,  A61K31/39 ,  A61K31/495 ,  A61P11/00 ,  C07D327/02 ,  C07D411/06 ,  C07D411/12

    CPC分类号： C07D327/02 ,  C07D411/06 ,  C07D411/12

    摘要： Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.2 receptor blocking activity, calcium antagonism, actions to relieve cerebral vasospasm and to improve renal circulation and diuretic and antithrombotic activities, and are of value as a prophylactic and therapeutic agent for ischemic cardiopathies, thrombosis, hypertension and cerebral circulatory disorders.

    Intermediates for the preparation of condensed seven-membered ring compounds
    4.
    发明授权
    Intermediates for the preparation of condensed seven-membered ring compounds 失效
    用于制备缩合的七元环化合物的中间体

    公开(公告)号：US4739066A

    公开(公告)日：1988-04-19

    申请号：US900816

    申请日：1986-08-27

    申请人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    发明人： Hirosada Sugihara ,  Kohei Nishikawa ,  Katsumi Ito

    IPC分类号： A61K38/00 ,  C07D209/48 ,  C07D281/10 ,  C07D417/04 ,  C07K5/02 ,  C07D211/44 ,  C07D211/86 ,  C07D211/94

    CPC分类号： C07D209/48 ,  C07D281/10 ,  C07D417/04 ,  C07K5/0222 ,  A61K38/00

    摘要： Novel condensed seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 and R.sup.5 are independently hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or lower alkyl; R.sup.6 is a condensed or non-condensed hetero-alicyclic containing at least one atom of N, O and S as a ring-forming atom which may be substituted; A is an alkylene chain; n is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases, such as hypertension, cardiopathy and cerebral apoploxy.

    摘要翻译： 新颖的具有下式的稠合的七元环化合物：其中R 1和R 2独立地是氢，卤素，三氟甲基，低级烷基或低级烷氧基，或两者共同形成三 - 或四亚甲基; R3和R5独立地是氢，低级烷基或芳烷基; R4是氢或低级烷基; R6是含有至少一个N，O和S原子的缩合或非稠合的杂脂环，其可以被取代成环原子; A是亚烷基链; n为1或2]及其盐。 这些化合物对血管紧张素转换酶等表现出抑制活性，作为诊断，预防和治疗循环系统疾病如高血压，心脏病和脑酰胞磷脂的药物具有价值。

    2-piperazinone compounds and their use
    7.
    发明授权
    2-piperazinone compounds and their use 失效
    2-哌嗪酮化合物及其用途

    公开(公告)号：US5550131A

    公开(公告)日：1996-08-27

    申请号：US262315

    申请日：1994-06-17

    申请人： Hirosada Sugihara ,  Zenichi Terashita ,  Hideto Fukushi

    发明人： Hirosada Sugihara ,  Zenichi Terashita ,  Hideto Fukushi

    IPC分类号： A61K38/00 ,  C07K5/087 ,  A61K31/495 ,  C07D241/04

    CPC分类号： C07K5/0812 ,  A61K38/00

    摘要： Compounds of the formula ##STR1## wherein A represents amidino group or an optionally substituted aminoethyl; R.sup.10 represents one species selected from a group consisting of nitro group, a halogen atom, a lower alkenyl group, a lower alkynyl group, a lower alkyloxycarbonyl group and a group represented by the formula OR.sup.11 (wherein R.sup.11 is hydrogen atom or a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group or a methanesulfonyl group, each of which may be substituted; R.sup.12 and R.sup.13 respectively represent hydrogen atom, hydroxyl group, a lower alkoxy group or a halogen atom; X represents hydroxyl group, p-hydroxyphenyl group or an optionally esterified or amidated carboxyl group; Y represents an optionally esterified or amidated carboxyl group; and n denotes 1 or 2, or a salt thereof and an agent for inhibiting adhesion of cells which comprise these compounds are desclosed. These have more potent and long lasting activities of inhibiting cell-adhesion, thus being useful as an orally administrable anti-thrombotic agent.

    摘要翻译： 式IMA的化合物，其中A表示脒基或任选取代的氨基乙基; R 10表示选自硝基，卤素原子，低级烯基，低级炔基，低级烷氧基羰基，或由式OR 11表示的基团中的一种（其中，R 11为氢原子或低级烷基 ，可以被取代的低级烯基，低级炔基，低级烷酰基，氨基甲酰基或甲磺酰基; R 12和R 13分别表示氢原子，羟基，低级烷氧基或卤素原子 ; X表示羟基，对羟基苯基或任选酯化或酰胺化的羧基; Y表示任选酯化或酰胺化的羧基; n表示1或2，或其盐和用于抑制细胞粘附的试剂，其包含 这些化合物具有抑制细胞粘附的作用，具有更有效和持久的活性，作为可口服给药的抗血栓形成剂有用。

    Trisubstituted piperazine compounds, their production and use
    8.
    发明授权
    Trisubstituted piperazine compounds, their production and use 失效
    三取代哌嗪化合物，其生产和使用

    公开(公告)号：US4997836A

    公开(公告)日：1991-03-05

    申请号：US433990

    申请日：1989-11-09

    申请人： Hirosada Sugihara ,  Kohei Nishikawa

    发明人： Hirosada Sugihara ,  Kohei Nishikawa

    IPC分类号： C07D241/04 ,  C07D405/12 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

    CPC分类号： C07D405/12 ,  C07D241/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

    摘要： Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are lower alkyl groups; A is a phenyl group, a hydrocarbon group formed by condensation of two or three 5- to 8-membered rings, a monocyclic 5- to 8-membered heterocyclic group containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, a dicyclic heterocyclic group formed by condensation of a benzene ring with a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, a tricyclic heterocyclic group formed by condensation of (i) a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, and (ii) a benzene ring, and (iii) a benzene ring or a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, or a styryl group of the formula: Ar--CR.sup.4 .dbd.CR.sup.5 -- wherein Ar is a phenyl group, and R.sup.4 and R.sup.5 are independently hydrogen or a lower alkyl group, the phenyl group represented by A or Ar, the hydrocarbon group represented by A, the monocyclic 5- to 8-membered heterocyclic group represented by A, the dicyclic heterocyclic group represented by A and the tricyclic heterocyclic group represented by A being unsubstituted or substituted by one or more substituents selected from the class consisting of a lower alkyl group, a halo lower alkyl group, a hydroxy lower alkyl group, an acyloxy lower alkyl group, a lower alkoxy lower alkyl group, a lower alkoxy group, a halo lower alkoxy group, a lower alkoxycarbonyl lower alkoxy group, a lower alkenyloxy group, aralkyloxy group, a lower alkoxy lower alkoxy group, a lower alkoxycarbonyl group, carboxyl group, carbamoyl group, an N,N-di-lower alkylcarbamoyl group, an N-lower alkylcarbamoyl group, halo group, cyano group, nitro group, hydroxy group, acyloxy group, amino group, a lower alkylsulfonylamino group, acylamino group, a lower alkoxycarbonylamino group, acyl group, mercapto group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group and oxo group; X is methylene group, carbonyl group or thiocarbonyl group and G is a group of the formula: --CH.sub.2 --.sub.n Z--R.sup.6 wherein n is an integer of 0 to 2, Z is a chemical bond, O, S, SO, SO.sub.2, CO, COO, OCO, OCONR.sup.7, CONR.sup.7 or NR.sup.7 (wherein R.sup.7 is hydrogen, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group or a lower alkoxycarbonyl group), and R.sup.6 is hydrogen, a lower alkyl group, a lower haloalkyl group or a lower alkenyl group, provided that, when n is O and Z is chemical bond, R.sup.6 is not hydrogen or a lower alkyl group are useful as a platelet activating factor antagonist.

    Spiro compounds, their production and use
    9.
    发明授权
    Spiro compounds, their production and use 失效
    螺环化合物，其生产和使用

    公开(公告)号：US4362740A

    公开(公告)日：1982-12-07

    申请号：US188834

    申请日：1980-09-19

    申请人： Isuke Imada ,  Hirosada Sugihara ,  Mitsuru Kawada

    发明人： Isuke Imada ,  Hirosada Sugihara ,  Mitsuru Kawada

    IPC分类号： C07D333/78 ,  A61K31/38 ,  A61K31/381 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D307/33 ,  C07D333/50 ,  C07D495/10 ,  C07D333/64

    CPC分类号： C07D307/33 ,  C07D333/50 ,  C07D495/10

    摘要： New spiro compounds of the formula: ##STR1## wherein n is an integer of 1 to 4, and X is halogen, lower alkyl, nitro, amino which may be substituted, hydroxyl which may be substituted, acyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may be substituted, sulfamoyl which may be substituted, lower alkylthio or lower alkylsulfonyl, or two of X at the 5- and 6-positions together form --CH.dbd.CH--CH.dbd.CH--, exhibit inhibitory activity to thrombocyte aggregation and are useful for the prophylaxis or treatment of cardiovascular disturbance such as thrombosis.

    摘要翻译： 新的具有下式的螺环化合物：其中n为1〜4的整数，X为卤素，低级烷基，硝基，可被取代的氨基，可被取代的羟基，酰基，羧基，低级烷氧基羰基，氨基甲酰基 其可以被取代，可以被取代的氨磺酰基，低级烷硫基或低级烷基磺酰基，或者在5-和6-位X上的两个一起形成-CH = CH-CH = CH-，表现出对血小板聚集的抑制活性，并且是有用的 用于预防或治疗心血管疾病如血栓形成。

    1-Azaxanthone derivatives
    10.
    发明授权
    1-Azaxanthone derivatives 失效
    1-氮杂酮衍生物

    公开(公告)号：US4299963A

    公开(公告)日：1981-11-10

    申请号：US177580

    申请日：1980-08-13

    申请人： Akira Nohara ,  Hirosada Sugihara ,  Kiyoshi Ukawa

    发明人： Akira Nohara ,  Hirosada Sugihara ,  Kiyoshi Ukawa

    IPC分类号： C07D311/58 ,  C07D491/04 ,  C07D491/052

    CPC分类号： C07D491/04 ,  C07D311/58

    摘要： The present invention relates to novel 1-azaxanthone-3-carboxylic acid and its derivatives usable for effective medicines for the treatment of allergic diseases, which are shown by the following formula (I) ##STR1## wherein R.sub.1 is hydrogen, alkyl, phenyl, carboxyl, hydroxyl, alkoxy or amino group which may be unsubstituted or substituted by one alkyl, m is 0, 1 or 2 and R.sub.2 is alkyl, alkoxy, halogen, nitro, hydroxy, carboxyl, butadienylene (--CH.dbd.CH--CH.dbd.CH--) which forms a benzene ring with any adjacent carbon atoms or amino group which may be unsubstituted or substituted by at least one alkyl, and their physiologically acceptable salts.

    摘要翻译： 本发明涉及可用于治疗过敏性疾病的有效药物的新型1-氮杂酮-3-羧酸及其衍生物，其由下式（I）表示：其中R 1为氢，烷基 ，可以是未取代的或被一个烷基取代的苯基，羧基，羟基，烷氧基或氨基，m是0,1或2，R2是烷基，烷氧基，卤素，硝基，羟基，羧基，丁二烯基（-CH = CH- CH = CH-），其形成具有任何相邻碳原子的苯环或可被未取代或被至少一个烷基取代的氨基，及其生理上可接受的盐。