公开(公告)号：US3966939A

公开(公告)日：1976-06-29

申请号：US558655

申请日：1975-03-17

申请人： Kenji Kobayashi ,  Toshitsugu Fukumaru ,  Hiroyuki Mizote ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Kenji Kobayashi ,  Toshitsugu Fukumaru ,  Hiroyuki Mizote ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： A61K31/395 ,  A61K31/485

CPC分类号： A61K31/395

摘要： Novel 2-substituted 6,7-benzomorphan derivatives of the formula: ##SPC1##And acid addition salts thereof, which are useful as non-addicting analgesics, pain relieving agents and antitussives and can be prepared by reacting 6,7-benzomorphan derivatives of the formula: ##SPC2##With the reactive derivatives of alcohols of the formula: ##EQU1## [wherein R is a hydrogen atom, a hydroxyl group, an alkoxy group or an alkanoyloxy group; R.sub.1 is a hydrogen atom, an alkyl group, an alkoxyalkyl group or a substituted or unsubstituted aryl group; R.sub.3 is a hydrogen atom or a hydroxyl group; R.sub.4 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, or R.sub.3 and R.sub.4 may form an alkylidene group or a carbonyl group together with the carbon atom to which these substituents are bonded; R.sub.2, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are each a hydrogen atom or an alkyl group; A is an alkylene group; and m is an integer of 0 to 2].

摘要翻译： 具有下式的新颖的2-取代的6,7-苯并吗啉衍生物：

公开(公告)号：US3961066A

公开(公告)日：1976-06-01

申请号：US456268

申请日：1974-03-29

申请人： Toshitsugu Fukumaru ,  Kenji Kobayashi ,  Hiroyuki Mizote ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Toshitsugu Fukumaru ,  Kenji Kobayashi ,  Hiroyuki Mizote ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： A61K31/47 ,  A61P25/04 ,  C07D211/70 ,  C07D211/82 ,  C07D221/26

CPC分类号： C07D211/70 ,  C07D221/26 ,  Y02P20/55 ,  Y10S514/849

摘要： A novel 2-substituted-6,7-benzomorphan derivative of the formula: ##SPC1##And its acid addition salts, which are useful as non-addicting analgesics and antitussives and can be prepared by reacting a 2-unsubstituted-6,7-benzomorphan derivative of the formula: ##SPC2##With the reactive derivative of an alcohol of the formula:HOA',optionally followed by elimination of the protective group in the resulting product, wherein R.sub.1 is hydrogen, lower alkyl or acyl; R.sub.2 and R.sub.3 are each lower alkyl; A is lower alkyl, cyano(lower)alkyl, benzoyl(lower)alkyl, ar(lower)alkyl, lower alkenyl or cyclo(lower)alkyl(lower)alkyl; and A' is a group as mentioned in A or benzoyl(lower)alkyl of which the carbonyl group is masked with a suitable protective group.

摘要翻译： 一种下式的新型2-取代-6,7-苯并吗啉衍生物：

公开(公告)号：US3954870A

公开(公告)日：1976-05-04

申请号：US230036

申请日：1972-02-28

申请人： Toshitsugu Fukumaru ,  Yoshio Suzuki

发明人： Toshitsugu Fukumaru ,  Yoshio Suzuki

IPC分类号： B01J25/02 ,  C07C87/28

CPC分类号： C07C209/68 ,  B01J25/02 ,  C07B2200/07

摘要： An optically active .alpha.,.beta.-di-phenylethylamine of the formula, ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 - C.sub.4 alkyl and m and n are each an integer of 1 to 5, is racemized by heating the optically active amine at a temperature between 100.degree.C and the boiling point of the amine in the presence of a dry Raney nickel catalyst in the atmosphere of inert gas. d-Isomers are more useful than the l-isomers as intermediates of optically active fatty acid amides having cholesterol lowering effects.

摘要翻译： 下式的旋光活性α，β-二苯基乙胺WHEREIN R1和R2各自为氢或C1-C4烷基，m和n各自为1至5的整数，通过在温度下加热光学活性胺进行外消旋化 在惰性气体气氛中，在干燥的阮内镍催化剂存在下，在100℃和胺的沸点之间。 d-异构体比具有降低胆固醇效果的光学活性脂肪酸酰胺的中间体的1-异构体更有用。

公开(公告)号：US3995059A

公开(公告)日：1976-11-30

申请号：US174149

申请日：1971-08-23

申请人： Toshitsugu Fukumaru ,  Noritaka Hamma ,  Hiroshi Nakatani ,  Hideaki Fukushima ,  Katsuyuki Toki

发明人： Toshitsugu Fukumaru ,  Noritaka Hamma ,  Hiroshi Nakatani ,  Hideaki Fukushima ,  Katsuyuki Toki

IPC分类号： C07C233/00 ,  C07C233/02 ,  C07D295/185 ,  A01N9/20 ,  A01N9/24

CPC分类号： C07D295/185 ,  C07C233/00 ,  C07C233/02

摘要： A pharmaceutical composition consisting essentially of pharmaceutically effective amount of an N-substituted fatty acid amide of the formula, ##EQU1## wherein R is a C.sub.13 - C.sub.25 aliphatic hydrocarbon chain or a C.sub.13 - C.sub.25 hydroxylated aliphatic hydrocarbon chain and RCO-- is other than isostearoyl; R' is d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl, racemic-, d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl substituted in the benzene ring with one or two substituents selected from the group consisting of C.sub.1 - C.sub.4 alkyl, C.sub.1 - C.sub.4 alkoxy, halogen and nitro, or racemic-, d- or l-.alpha.-benzylbenzyl; R" is hydrogen; or R' and R" together are cyclohexyl; and when RCO-- is isotearoyl R' is alkyl, alkenyl, cycloalkyl, alkylcycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, alkylphenyl, hydroxyphenyl, alkoxyphenyl, halogenophenyl, halogen-alkyl-substituted phenyl, halogenoalkyl- and halogen-substituted phenyl, alkoxy- and halogen-substituted phenyl, benzyl, racemic-, d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl, benzyl substituted in the benzene ring with lower alkyl or lower alkoxy, racemic-, d- or l-.alpha.-benzylbenzyl or hydroxybenzyl, and R" is hydrogen or any one of the groups represented by R', and a pharmaceutically acceptable carrier, which is useful for lowering elevated levels of cholesterol in the blood.

摘要翻译： 基本上由药学有效量的式R'R-CO-N ANGLE R“的N-取代脂肪酸酰胺组成的药物组合物，其中R是C 13 -C 25脂族烃链或C 13 -C 25羟基化脂族烃 链和RCO-不是异硬脂酰基; R'是在苯环中被一个或两个选自C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷氧基，卤素和硝基，或外消旋 - ，d-或1-α-苄基苄基; R“是氢; 或R'和R“一起为环己基; 当RCO-为异月桂酰基R'为烷基，烯基，环烷基，烷基环烷基，羟基环烷基，烷氧基环烷基，烷基苯基，羟基苯基，烷氧基苯基，卤代苯基，卤代 - 烷基取代的苯基，卤代烷基 - 和卤素取代的苯基，烷氧基 - 和卤素取代 苯基，苄基，外消旋 - ，d-或1-α-C 1 -C 4烷基苄基，在苯环中被低级烷基或低级烷氧基取代的苄基，外消旋 - ，d-或1-α-苄基苄基或羟基苄基，R“ 是氢或由R'表示的基团中的任何一个，以及可用于降低血液中胆固醇升高的药学上可接受的载体。