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205 条记录 (耗时 0.014 秒)

    2-Benzyl-4-piperidones useful as intermediates in the production of 6,7-benzomorphan derivatives
    61.
    发明授权
    2-Benzyl-4-piperidones useful as intermediates in the production of 6,7-benzomorphan derivatives 失效
    2-苄基-4-哌啶酮可用作6,7-苯并吗啉衍生物生产中的中间体

    公开(公告)号：US4012392A

    公开(公告)日：1977-03-15

    申请号：US543352

    申请日：1975-01-23

    申请人： Antony Marie Akkerman ,  Paul Adriaan Jan Janssen

    发明人： Antony Marie Akkerman ,  Paul Adriaan Jan Janssen

    IPC分类号： C07D211/44 ,  C07D211/48 ,  C07D211/74 ,  C07D211/78 ,  C07D211/86 ,  C07D221/20 ,  C07D221/26

    CPC分类号： C07D221/20 ,  C07D211/44 ,  C07D211/48 ,  C07D211/74 ,  C07D211/78 ,  C07D211/86 ,  C07D221/26

    摘要： 6,7-BENZOMORPHAN DERIVATIVES HAVING ANALGESIC AND MORPHINE-ANTAGONISTIC PROPERTIES ARE OF THE FORMULA ##STR1## in which the substituents R are either lower alkyl groups or groups which, together with the carbon atom to which they are bonded, form a cycloaliphatic ring, and the substituents R.sub.1, R.sub.2 and R.sub. 3 may or may not be made and, if made, R.sub.1 represents either a hydrogen atom or an alkyl, haloalkyl, alkenyl, alkinyl, aralkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl or cycloalkylidine-alkyl group, R.sub. 2 is an alkyl, aryl, heteroaryl or aralkyl group, and R.sub. 3 is a hydrogen atom or an hydroxy, alkoxy, alkoxy-alkoxy or acyloxy group. Such 6,7-benzomorphans may be in the form of their optically active enantiomers and/or their therapeutically acceptable salts. There are also disclosed methods for producing such 6,7-benzomorphan derivatives, and intermediates useful in such production.

    摘要翻译： 具有非线性和吗啡拮抗性的6,7-苯并吡喃衍生物是其中取代基R是低级烷基或与它们键合的碳原子一起形成脂环族基团的基团， 卤代烷基，烯基，炔基，芳烷基，环烯基，环烷基烷基，环烯基烷基或环烷基 - 烷基，R（R），R 2是烷基，芳基，杂芳基或芳烷基，R 3是氢原子或羟基，烷氧基，烷氧基 - 烷氧基或酰氧基。 这样的6,7-苯并呋喃可以是其旋光对映异构体和/或其治疗上可接受的盐的形式。 还公开了用于生产这种6,7-苯并吗啉衍生物的方法和用于这种生产的中间体。

    1,2,3,4,5,6-Hexahydro-1-oxo or hydroxy-3-acyl-2,6-methano-3-benzazocines and corresponding 1-esters thereof
    62.
    发明授权
    1,2,3,4,5,6-Hexahydro-1-oxo or hydroxy-3-acyl-2,6-methano-3-benzazocines and corresponding 1-esters thereof 失效
    1,2,3,4,5,6-六氢-1-氧代或羟基-3-酰基-2,6-亚甲基-3-苯并吖嗪及其相应的1-酯

    公开(公告)号：US3936462A

    公开(公告)日：1976-02-03

    申请号：US369870

    申请日：1973-06-14

    申请人： Noel F. Albertson

    发明人： Noel F. Albertson

    IPC分类号： C07D221/26 ,  C07D263/60

    CPC分类号： C07D221/26 ,  C07D263/60

    摘要： 1,2,3,4,5,6-Hexahydro-1-oxo-3-(hydrocarbon or substituted hydrocarbon)-8-(H or OH)-6-(H or alkyl)-11-(H or alkyl)-2,6-methano-3-benzazocines and 1-hydroxy secondary and tertiary alcohols obtainable therefrom by reduction and by Grignard reactions, and esters of the same, are useful as central nervous system depressants, particularly as analgesics and as analgesic antagonists. The 3-substituent is introduced by alkylation, directly or by N-acylation followed by reduction of the resulting amides, of the corresponding >NH compounds either before or after introduction of the 1-oxo group into the compounds having two hydrogens at the 1-position by chromium (VI) oxidation. Various intermediates and derivatives are also descibed, including 3a,4,5,9b-tetrahydro-3,5-ethanonaphth[2,1-d]oxazol-2(3H)-ones obtained by interacting 1,2,3,4,5,6-hexahydro-1-hydroxy-2,6-methano-3-benzazocines with phosgene or by heating 1,2,3,4,5,6-hexahydro-1-hydroxy-3-carbalkoxy-2,6-methano-3-benzazocines with alkoxide ion.

    摘要翻译： 1,2,3,4,5,6-六氢-1-氧代-3-（烃基或取代的烃）-8-（H或OH）-6-（H或烷基）-11-（H或烷基） -2,6-亚甲基-3-苯并吖嗪和通过还原和格利雅反应得到的1-羟基仲和叔醇及其酯可用作中枢神经系统抑制剂，特别是作为止痛剂和止痛剂拮抗剂。 3-取代基直接或通过N-酰化直接或通过N-酰化，然后还原所得的酰胺，在将1-氧代基引入具有两个氢的化合物之前或之后，在1- 铬（VI）氧化位置。 还描述了各种中间体和衍生物，包括通过相互作用的1,2,3,4和4获得的3a，4,5,9b-四氢-3,5-乙基萘并[2,1-d]恶唑-2（3H） 5,6-六氢-1-羟基-2,6-亚甲基-3-苯并吖嗪与光气或通过加热1,2,3,4,5,6-六氢-1-羟基-3-烷氧基-2,6- 亚烷基-3-苯并吖嗪与醇盐离子。

    Microbiological hydroxylation of 2,6-methano-3-benzazocines
    64.
    发明授权
    Microbiological hydroxylation of 2,6-methano-3-benzazocines 失效
    2,6-亚甲基-3-苯并吖嗪的微生物羟基化

    公开(公告)号：US3919047A

    公开(公告)日：1975-11-11

    申请号：US49223374

    申请日：1974-07-26

    申请人： SCHERING AG

    发明人： VIDIC HANS-JORG ,  KIESLICH KLAUS

    IPC分类号： C12P17/12 ,  C07D221/26 ,  C12D13/02

    CPC分类号： C07D221/26 ,  Y10S435/911

    摘要： WHEREIN Q'' is a benzoyl group, R1 and R2 each are a hydrogen atom or lower alkyl and Z'' is a free, etherified or esterified hydroxy group, are hydroxylated in the 1-position by microorganisms of the family Agaricaceae, e.g., Pellicularia filamentosa f. sp. sasakii.

    2,6-Methano-3-benzazocines of the formula

    摘要翻译： 式WHEREIN Q'是苯甲酰基的2,6-甲磺酰-3-苯并吖嗪类，R1和R2各自是氢原子或低级烷基，Z'是游离醚化或酯化的羟基，在1- 家Ag科的微生物的位置，例如丝状毛球菌f。 sp。 佐佐基

    Novel benzomorphan and their salts as analgesics
    66.
    发明授权
    Novel benzomorphan and their salts as analgesics 失效
    新的BENZOMORPHAN和他们的销售作为理论

    公开(公告)号：US3873706A

    公开(公告)日：1975-03-25

    申请号：US47284074

    申请日：1974-05-23

    申请人： SUMITOMO CHEMICAL CO

    发明人： ATSUMI TOSHIO ,  KOBAYASHI KENJI ,  TAKEBAYASHI YOSHIAKI ,  YAMAMOTO HISAO

    IPC分类号： C07D221/26 ,  A61K27/00

    CPC分类号： C07D221/26

    摘要： Benzomorphan derivatives of the formula:

    WHEREIN R is a hydrogen atom, a C1-C3 alkoxy group, an acyloxy group, a hydroxy group, a nitro group, a halogen atom, a cyano group, an amino group, a carboxyl group, a carbamoyl group or a sulfo group; R1 is a hydrogen atom, a C1-C3 alkyl group or a group of the formula, (CmH(2m p) 1)-(R9)p (wherein m is an integer of 1-6; p is an integer of 1-2, and R9 is a hydroxyl group or a C1-C3 alkoxy group); R2 is a hydrogen atom or a C1-C3 alkyl group; R3 and R4 are independently a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 alkoxy group, a C1-C3 alkylthio group, a nitro group, a trifluoromethyl group, an amino group or a hydroxyl group; R5 is a hydrogen atom or a methyl group; R6 is a hydrogen atom or a C1-C3 alkyl group; R7 is a hydrogen atom, a C1-C3 alkyl group, a phenyl group or a C1-C3 alkoxyphenyl group; R8 is a hydrogen atom or a hydroxyl group, or R7 and R8 may form a C1-C3 alkylidene group or a carbonyl group together with a carbon atom to which these substituents are bonded; and n is an integer of 2-4, provided that, when n is an integer of 2, R1 and R2 are a methyl group, R is a hydrogen atom or a hydroxyl group and R4, R5, R6, R7 and R8 are hydrogen atoms, R3 must be a halogen atom, a C1-C3 alkyl group, a C1-C3 alkoxy group, a C1-C3 alkylthio group, a nitro group, a trifluoromethyl group, an amino group or a hydroxyl group, which are useful as non-addicting, analgesic and pain-relieving agents with calming effect.

    摘要翻译： 下式的苯并吗啉衍生物：

    Benzomorphan derivatives as analgesic agents
    68.
    发明授权
    Benzomorphan derivatives as analgesic agents 失效
    苯并吡喃衍生物作为有效代谢物

    公开(公告)号：US3781431A

    公开(公告)日：1973-12-25

    申请号：US3781431D

    申请日：1972-09-27

    申请人： BAYER AG

    发明人： SCHUBERT H ,  HOFFMEISTER F

    IPC分类号： C07D221/26 ,  A61K27/00

    CPC分类号： C07D221/26

    摘要： AN ANALGESIC COMPOSITIONS IS PRODUCED WHICH COMPRISES AN ANALGESICALLY EFFECTIVE AMOUNT OF A BENZOMORPHAN OF THE FORMULA

    3-R,11-R",6-R'',8-(X-CO-A-O-)-1,2,3,4,5,6-HEXAHYDRO-2,6-

    METHANO-3-BENZAZOCINE

    WHEREIN

    R IS METHYL, CYCLOPROPYLMETHYL OR CYCLOBUTYLMETHYL; R'' AND R" ARE THE SAME OR DIFFERENT, AND ARE METHYL OR ETHYL; A IS STRAIGHT OR BRANCHED CHAIN ALKYLENE OR ALKYLIDENE OF 1 TO 4 CARBON ATOMS OR ALKENYLENE OF 2 TO 4 CARBON ATOMS, UNSUBSTITUTED OR SUBSTITUTED BYPHENYL OR PHENYL SUBSTITUTED BY METHYL, METHOXY, CHLORO, NITRO OR ACETYLAMINO; X IS

    -OH, -O-R''", OR -N(-R4)-R5

    WHEREIN

    R"'' IS A STRAIGHT OR BRANCHED CHAIN ALKYL OF 1 TO 11 CARBON ATOMS OR STRAIGHT OF BRANCHED CHAIN ALKENYL OR 2 TO 11 CARBON ATOMS, AND R4 AND R5 ARE THE SAME OR DIFFERENT, AND ARE HYDROGEN, ALKYL OF 1 TO 4 CARBON ATOMS, OR R4 AND R5 TOGETHER WITH THE NITROGEN ATOM FORM A PYRROLIDINE, PIPERIDINE OR MORPHOLINE RING;

    IN COMBINATION WITH A PHARMACEUTICALLY ACCEPTABLE, NONTOXIC INERT DILUENT OR CARRIER. THE COMPOSITION MAY BE ADMINISTERED ORALLY OR PARENTERALLY.

    1-oxygenated-6-acyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines
    69.
    发明授权
    1-oxygenated-6-acyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines 失效
    1-氧代-6-亚氨基-1,2,3,4,5,6-六氢-2H-吡喃-2,6-甲酰基-3-苯甲酰胺

    公开(公告)号：US3687957A

    公开(公告)日：1972-08-29

    申请号：US3687957D

    申请日：1971-03-11

    申请人： FRED B BLOCK ,  ARTHUR H SCHRODER

    发明人： BLOCK FRED B ,  SCHRODER ARTHUR H

    IPC分类号： C07D221/26 ,  C07D39/00

    CPC分类号： C07D221/26

    摘要： 1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocines characterized by the presence of an alkanoyl or benzoyl group in the 6-position and a hydroxy or oxo group in the 1-position are analgesic agents and are prepared by treating the corresponding 1 Beta -hydroxy-6cyano compound with a Grignard-type reagent. Typical embodiments are 1 Beta -hydroxy-3-methyl-6-acetyl-1,2,3,4,5,6-hexahydro-2,6methano-3-benzazocine and 3,11 Beta -dimethyl-6-propionyl-1 Beta -hydroxy-8-methoxy-1,2,3,4,5,6-hexahydro-2,6-methano-3benzazocines.

    摘要翻译： 特征在于6-位上存在烷酰基或苯甲酰基并且1-位羟基或氧代基的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪是 通过用格氏试剂处理相应的1β-羟基-6-氰基化合物来制备镇痛剂。 典型的实施方案是1β-羟基-3-甲基-6-乙酰基-1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并嗪和3,11β-二甲基-6- 丙酰基-1β-羟基-8-甲氧基-1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪。