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111 条记录 (耗时 0.022 秒)

    Analgesic benzomorphan derivatives
    1.
    发明授权
    Analgesic benzomorphan derivatives 失效
    镇痛苯并吗啉衍生物

    公开(公告)号：US4241070A

    公开(公告)日：1980-12-23

    申请号：US736072

    申请日：1976-10-27

    申请人： Junki Katsube ,  Hiroyuki Mizote ,  Shuichi Harada ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Hiroyuki Mizote ,  Shuichi Harada ,  Hisao Yamamoto

    IPC分类号： A61K31/435 ,  A61P25/04 ,  C07D221/26 ,  A61K31/445

    CPC分类号： C07D221/26 ,  Y02P20/55

    摘要： 2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sub.3 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, with a reactive derivative of an alcohol compound of the formula: ##STR3## wherein X is an optionally protected carbonyl group; and R.sub.3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.

    摘要翻译： 具有下式的2-取代的-2'-甲基-6,7-苯并吗啉衍生物：其中R 1和R 2各自为氢或C 1 -C 3烷基; 并且R3是氢，卤素或C1-C3烷基及其药学上可接受的盐，其可用作具有镇静作用的非上瘾止痛剂，通过下式的6,7-苯并吗啉衍生物的反应制备： [II]其中R1和R2如上所定义，与下式的醇化合物的反应性衍生物：其中X是任选被保护的羰基; 并且R 3如上所定义，任选地随后消除羰基的保护基，或通过下式的6,7-苯并吗啉衍生物的氧化：其中R 1，R 2和R 3是 如上所述。

    Conjugated ketone compounds in preventing platelet thrombosis
    2.
    发明授权
    Conjugated ketone compounds in preventing platelet thrombosis 失效
    共轭酮化合物预防血小板血栓形成

    公开(公告)号：US4418079A

    公开(公告)日：1983-11-29

    申请号：US335522

    申请日：1981-12-29

    申请人： Atsuyuki Kojima ,  Tsunemasa Irie ,  Shuichi Harada ,  Yoshito Kameno ,  Junki Katsube ,  Hisao Yamamoto

    发明人： Atsuyuki Kojima ,  Tsunemasa Irie ,  Shuichi Harada ,  Yoshito Kameno ,  Junki Katsube ,  Hisao Yamamoto

    IPC分类号： C07C29/42 ,  C07D209/44 ,  C07D295/108 ,  C07D307/52 ,  C07D317/58 ,  C07D333/22 ,  A61K27/00 ,  A61K31/135 ,  A61K31/34 ,  A61K31/36 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445

    CPC分类号： C07D295/108 ,  C07C29/42 ,  C07D209/44 ,  C07D307/52 ,  C07D317/58 ,  C07D333/22

    摘要： Conjugated ketone compounds of the formula: ##STR1## wherein Ar is naphthyl, furyl, thienyl, or phenyl optionally bearing one or more substituents selected from the group consisting of chlorine, bromine, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, trifluoromethyl and methylenedioxy, R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.7 -C.sub.8 aralkyl or adamantyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl, or when R.sub.1 and R.sub.2 are taken together with the nitrogen atom to which they are attached, they form a heterocyclic amino group containing up to 8 carbon atoms, A is straight or branched C.sub.1 -C.sub.3 alkylene, N-[4-(p-chlorophenyl)-4-oxo-2-trans-butenyl]morpholine and N-[4-(p-methoxyphenyl)-4-oxo-2-trans-butenyl]piperidine being excluded, and their non-toxic salts, which are useful as blood platelet anti-aggregative agents.

    摘要翻译： 具有下式的共轭酮化合物：其中Ar是萘基，呋喃基，噻吩基或任选具有一个或多个选自氯，溴，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4 烷基硫基，三氟甲基和亚甲二氧基，R 1是C 1 -C 6烷基，C 3 -C 5烯基，C 3 -C 6环烷基，C 7 -C 8芳烷基或金刚烷基，R 2是C 1 -C 6烷基，C 3 -C 5链烯基或C 3 -C 6环烷基， 并且R 2与它们所连接的氮原子一起形成含有至多8个碳原子的杂环氨基，A是直链或支链C1-C3亚烷基，N- [4-（对氯苯基）-4 - 氧代-2-反式 - 丁烯基]吗啉和N- [4-（对甲氧基苯基）-4-氧代-2-反式 - 丁烯基]哌啶，以及它们的无毒盐，其可用作血小板抗体 聚集代理。

    Benzisoxazole derivatives
    3.
    发明授权
    Benzisoxazole derivatives 失效
    苯并异恶唑衍生物

    公开(公告)号：US4217349A

    公开(公告)日：1980-08-12

    申请号：US919221

    申请日：1978-06-26

    申请人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D261/20 ,  A61K31/535 ,  C07D413/06

    CPC分类号： C07D261/20

    摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

    摘要翻译： 新的苯并恶唑化合物，其结构式如下：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 1 -C 3）烷氧基或卤素，或者一起形成C 1 -C 2亚烷基二氧基， Alk是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮的 可含有任何另外的杂原子的杂环，R 5为C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

    Novel cyclopropylmethylamine derivatives
    5.
    发明授权
    Novel cyclopropylmethylamine derivatives 失效
    新型环丙基甲胺衍生物

    公开(公告)号：US4103030A

    公开(公告)日：1978-07-25

    申请号：US635331

    申请日：1975-11-26

    申请人： Atsuyuki Kojima ,  Yoshito Kameno ,  Junki Katsube ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Atsuyuki Kojima ,  Yoshito Kameno ,  Junki Katsube ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A01N9/20 ,  A01N9/24 ,  C07C91/16 ,  C07C91/28

    摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.2 are each as defined above and X is a conventional leaving (removable) group with amines of the formula: ##STR4## wherein R and R' are each as defined above.

    摘要翻译： 新的下式的环丙基甲胺化合物：其中Ar 1表示具有一个或多个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基的苯基，其中至少一个存在于 或位置，Ar 2表示未取代的苯基或被一个或多个选自卤素和C 1 -C 4烷基的取代基取代的苯基，R表示氢，C 1 -C 4烷基或C 2 -C 4羟烷基， R'表示C1-C4烷基或C2-C4羟基烷基及其无毒盐，它们具有各种有用的药理活性，可以通过还原相应的下式化合物来制备：其中Ar1，Ar2，R和 R'各自如上所定义，或通过下式的相应化合物的缩合：其中Ar 1和Ar 2各自如上所定义，X是具有下式的胺的常规离去（可除去）基团：其中 R和R'各自如上所定义。

    9-Formyl-9,10-dihydro-9,10-methanoanthracene
    7.
    发明授权
    9-Formyl-9,10-dihydro-9,10-methanoanthracene 失效
    9-甲酰基-9,10-二氢-9,10-甲烷基蒽

    公开(公告)号：US4358620A

    公开(公告)日：1982-11-09

    申请号：US139740

    申请日：1980-04-14

    申请人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    发明人： Makoto Sunagawa ,  Hiromi Sato ,  Junki Katsube ,  Hisao Yamamoto

    IPC分类号： C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/02 ,  C07D295/03 ,  C07D295/125 ,  C07C47/52

    CPC分类号： C07D295/03 ,  C07C47/235 ,  C07C47/238 ,  C07C47/453 ,  C07C57/50 ,  C07C61/39 ,  C07D295/125

    摘要： Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e. 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.

    摘要翻译： 其中A为C 1 -C 4亚烷基或C 3 -C 4亚烯基，R 1和R 2各自为氢，C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基，C 3 -C 4炔基， C 1 -C 8环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基或多卤代（C 2 -C 4）烷基，或与相邻的氮原子一起形成5至7元含氮杂环， 可以含有另外的杂原子及其无毒盐，其可用作抗焦虑剂，抗抑郁剂，主要镇静剂，抗组胺和抗过敏药物，并且可以通过新的关键中间体即9- 甲酰基-9,10-二氢-9,10-甲基蒽，通过各种方法。

    3-(Piperazinoalkyl)-benz-2,1-isoxazoles
    8.
    发明授权
    3-(Piperazinoalkyl)-benz-2,1-isoxazoles 失效
    3-（哌嗪基烷基） - 苯并-2,1 - 异恶唑

    公开(公告)号：US4122176A

    公开(公告)日：1978-10-24

    申请号：US755139

    申请日：1976-12-29

    申请人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D261/20 ,  A61K31/495 ,  C07D413/06 ,  C07D413/14

    CPC分类号： C07D261/20 ,  Y10S514/826

    摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 14 C.sub.3) alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

    摘要翻译： 下式的新型苯并异恶唑化合物：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 11 43 C 3）烷氧基或卤素，或者当它们一起形成C 1 -C 2亚烷基二氧基，Alk 是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮杂环 可以含有任何另外的杂原子的环，R 5是C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

    Novel bicycloheptene derivatives
    9.
    发明授权
    Novel bicycloheptene derivatives 失效
    新型双环庚烯衍生物

    公开(公告)号：US4073933A

    公开(公告)日：1978-02-14

    申请号：US697152

    申请日：1976-06-17

    申请人： Hiromi Shimomura ,  Akihiko Sugie ,  Junki Katsube ,  Hisao Yamamoto

    发明人： Hiromi Shimomura ,  Akihiko Sugie ,  Junki Katsube ,  Hisao Yamamoto

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C07D311/94 ,  C07C177/00 ,  C07C61/38 ,  C07C69/74

    CPC分类号： C07C405/0091 ,  C07C405/00 ,  C07D309/12 ,  C07D311/94 ,  Y10S514/925

    摘要： Novel bicycloheptene compounds of the formula: ##STR1## wherein A is C.sub.2 -C.sub.4 alkylene; X and B are each ethylene or vinylene; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkoxyalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.5 -C.sub.8 cycloalkylalkyl, aryl, C.sub.7 -C.sub.10 arylalkyl, C.sub.7 -C.sub.10 aryloxyalkyl; R.sub.2 is hydrogen, or C.sub.1 -C.sub.4 alkyl; and Z is carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 carbamoyl, and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, central nervous system regulators, and labor inducing agents.

    摘要翻译： 下式的新型双环庚烯化合物：其中A是C 2 -C 4亚烷基; X和B各自为亚乙烯基或亚乙烯基; R1是氢，C1-C8烷基，C4-C8烷氧基烷基，C5-C7环烷基，C5-C8环烷基烷基，芳基，C7-C10芳基烷基，C7-C10芳氧基烷基; R2是氢或C1-C4烷基; Z为羧基，C 2 -C 5烷氧基羰基或C 1 -C 5氨基甲酰基及其无毒盐，其可用作抗溃疡剂，胃分泌抑制剂，中枢神经系统调节剂和劳动诱导剂。