Conjugated ketone compounds in preventing platelet thrombosis
    1.
    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

    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。

    Novel cyclopropylmethylamine derivatives
    2.
    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

    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。

    Cyclopropylmethylamine derivatives
    3.
    发明授权
    Cyclopropylmethylamine derivatives 失效
    环丙基甲胺衍生物

    公开(公告)号:US4110376A

    公开(公告)日:1978-08-29

    申请号:US605012

    申请日:1975-08-15

    CPC分类号: C07D401/12

    摘要: Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, 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 R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

    摘要翻译: 下式的新型环丙基甲胺化合物:其中R 1和R 2各自为氢或卤素,R 3为氢或甲基,及其无毒盐,其具有各种有用的药理活性,可通过还原相应化合物 其中R 1,R 2和R 3各自如上所定义,或其无毒盐,或通过下式的相应化合物的缩合:其中R 1和R 2各自如上所定义,X为 常规的可互换基团如卤素或磺酰氧基与甲胺或二甲胺。

    Novel morpholine derivatives and the treatment of mental depression
    4.
    发明授权
    Novel morpholine derivatives and the treatment of mental depression 失效
    新型吗啉衍生物和精神抑郁症的治疗

    公开(公告)号:US4085210A

    公开(公告)日:1978-04-18

    申请号:US646908

    申请日:1976-01-06

    CPC分类号: C07D265/30 C07D267/10

    摘要: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

    摘要翻译: 式中:R1代表氢或C1-C4烷基,R2代表氢,C1-C4烷基,C3-C5烯基,C3-C5炔基,芳基 - (C1-C4)烷基,(C3 -C 6)环烷基(C 1 -C 4)烷基,多卤代(C 2 -C 4)烷基或羟基(C 2 -C 4)烷基,A表示直链或支链C 2 -C 4亚烷基,B表示选自-CH 2 -CH 2 - , - CH = CH-, -CH 2 -O-,-CH 2 -S-,-S-和-O-,> D-E-代表选自下组的三价基团:CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基,它们的无毒 盐,其可用作抗抑郁药并且可以通过各种方法制备。

    Novel morpholine derivatives and treating depression therewith
    5.
    发明授权
    Novel morpholine derivatives and treating depression therewith 失效
    新型吗啉衍生物和治疗抑郁症

    公开(公告)号:US4169146A

    公开(公告)日:1979-09-25

    申请号:US811944

    申请日:1977-06-30

    CPC分类号: C07D265/30 C07D267/10

    摘要: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

    摘要翻译: 式中:R1代表氢或C1-C4烷基,R2代表氢,C1-C4烷基,C3-C5烯基,C3-C5炔基,芳基 - (C1-C4)烷基,(C3 -C 6)环烷基(C 1 -C 4)烷基,多卤代(C 2 -C 4)烷基或羟基(C 2 -C 4)烷基,A表示直链或支链C 2 -C 4亚烷基,B表示选自-CH 2 -CH 2 - , - CH = CH-, -CH 2 -O-,-CH 2 -S-,-S-和-O-,> DE-表示选自下组的三价基团:CH-CH 2 - 和> C = CH-和C1和C2各自表示任选被一个或多个选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基及其无毒盐, 其可用作抗抑郁药并且可以通过各种方法制备。

    Analgesic benzomorphan derivatives
    6.
    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

    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。

    Benzisoxazole derivatives
    7.
    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

    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。

    9-Formyl-9,10-dihydro-9,10-methanoanthracene
    10.
    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

    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。