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：US3950526A

公开(公告)日：1976-04-13

申请号：US518070

申请日：1974-10-25

申请人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

发明人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

IPC分类号： C07D239/80 ,  C07D239/82 ,  C07D333/22 ,  C07D401/04 ,  C07D409/04 ,  A61K31/505

CPC分类号： C07D401/04 ,  C07D239/80 ,  C07D239/82 ,  C07D333/22 ,  C07D409/04

摘要： Quinazoline derivatives represented by the formula ##SPC1##Wherein R.sub.1 and R.sub.2 are individually a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a lower alkylthio group or a lower alkylsulfonyl group; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a napthyl group, a furyl group or a thienyl group; R.sub.4 is a lower cycloalkyl group or a trihalomethyl group; and n is an integer of 1 to 3, are novel compounds and have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects with low toxicity. They can be prepared by treating with ammonia a trihaloacetamidophenylketone derivative of the formula, ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above; R is a hydrogen atom or a group of the formula --C.sub.n H.sub.2n --R.sub.4 ; and X is a halogen atom.

摘要翻译： 由式WHEREIN R1和R2表示的喹唑啉衍生物分别为氢原子，卤素原子，低级烷基，低级烷氧基，硝基，低级烷硫基或低级烷基磺酰基; R3是氢原子，低级烷基，低级环烷基，萘基，呋喃基或噻吩基; R4是低级环烷基或三卤代甲基; n为1〜3的整数，为新化合物，具有优异的药理特性，特别是具有低毒性的抗炎镇痛作用。 它们可以通过用氨处理下式的三卤代乙酰胺基苯基酮衍生物，即WHEREIN R1，R2和R3如上所定义; R是氢原子或式-C n H 2n -R 4的基团; X为卤素原子。

公开(公告)号：US3953441A

公开(公告)日：1976-04-27

申请号：US150841

申请日：1971-06-07

申请人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

IPC分类号： C07D211/70 ,  C07D221/26

CPC分类号： C07D221/26 ,  C07D211/70

摘要： A novel process for preparing 2-benzoylalkylbenzomorphan derivatives and salts thereof, represented by the formula ##SPC1##Wherein n, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification. The process comprises reacting a pyridinium derivative of the formula, ##SPC2##Wherein X is a halogen atom and Y' is an ethylenedioxy group; with a Grignard reagent of the formula, ##SPC3##Wherein R' is a hydrogen atom or a C.sub.1 -C.sub.3 alkoxy group and Z is a halogen atom, to yield a 1,2-dihydropyridine derivative of the formula; ##SPC4##And then reducing the said 1,2-dihydropyridine derivative to give a 1,2,5,6-tetrahydropyridine derivative of the formula, ##SPC5##Wherein Y is an oxygen atom or an ethylenedioxy group, and further cyclizing the obtained 1,2,5,6-tetrahydropyridine derivative.

摘要翻译： 由式WHEREIN N，R，R1，R2，R3和R4表示的用于制备2-苯甲酰基烷基苯并喃衍生物及其盐的新方法如本说明书中所定义。 该方法包括使下式的吡啶鎓衍生物WHEREIN X是卤素原子，Y'是亚乙二氧基; 与下式的格利雅试剂，其中R'是氢原子或C1-C3烷氧基，Z是卤素原子，得到下式的1,2-二氢吡啶衍生物; 然后减少所得的1,2-二氢吡啶衍生物，得到本发明的1,2,5,6-四氢吡啶衍生物，其中Y是氧原子或亚乙二氧基，进一步环化得到的1,2,5,6-四氢吡啶衍生物， 6-四氢吡啶衍生物。

公开(公告)号：US4260774A

公开(公告)日：1981-04-07

申请号：US51741

申请日：1979-06-25

申请人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

IPC分类号： C07D233/90

CPC分类号： C07D233/90

摘要： There are provided compounds of the formula: ##STR1## wherein R is an adamantyl group, or a phenyl group unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halogen atom, a nitro group, a cyano group, a methylenedioxy group or an acetamido group, useful as anti-transplanted-tumor agents and immunosuppressants.

摘要翻译： 提供下式的化合物：其中R是金刚烷基，或未取代或被低级烷基，低级烷氧基，低级烷硫基，卤原子，硝基， 氰基，亚甲二氧基或乙酰氨基，可用作抗移植肿瘤剂和免疫抑制剂。

公开(公告)号：US3962446A

公开(公告)日：1976-06-08

申请号：US523412

申请日：1974-11-13

申请人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

IPC分类号： A61K31/395 ,  A61K31/485

CPC分类号： A61K31/395

摘要： An analgesic composition comprising an analgesically effective amount of at least one 6,7-benzomorphan derivative of the formula: ##SPC1##Wherein R is a hydrogen atom, a hydroxyl group, a C.sup.1 - C.sup.3 alkoxy group or a C.sup.1 - C.sup.8 alkanoyloxy group; R.sub.1 is a hydrogen atom, a C.sup.1 - C.sup.5 alkyl group, a phenyl group, a halophenyl group, an alkylphenyl group wherein the alkyl moiety has 1 to 3 carbon atoms, an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms, a trifluoromethylphenyl group, an alkylthiophenyl group wherein the alkylthio moiety has 1 to 3 carbon atoms or a group of the formula (C.sub.m H.sub.2m.sub.-p.sub.+1) - (R.sub.9).sub.p wherein m is an integer of 1 - 6, p is an integer of 1 - 2 and R.sub.9 is a C.sup.1 - C.sup.3 alkoxy group; R.sub. 2 is a hydrogen atom or a C.sup.1 - C.sup.3 alkyl group; R.sub.3 is a hydrogen atom, a C.sup.1 - C.sup.3 alkyl group, a phenyl group or an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms; R.sub.4 is a hydrogen atom or a hydroxyl group, or R.sub.3 and R.sub.4 may form a C.sup.1 - C.sup.3 alkylidene group or a carbonyl group together with a carbon atom to which these substituents are bonded; R.sub.5 is a hydrogen atom or C.sup.1 - C.sup.3 alkyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 and R.sub.8 are independently a hydrogen atom or a C.sup.1 - C.sup.2 alkyl group; and n is an integer of 0 - 2; or an acid addition salt thereof, and a pharmaceutically acceptable carrier or diluent, is disclosed.

摘要翻译： 一种止痛组合物，其包含镇痛有效量的至少一种下式的6,7-苯并吗啉衍生物：WHEREIN R是氢原子，羟基，C1-C3烷氧基或C1-C8烷酰氧基; R1为氢原子，C1-C5烷基，苯基，卤代苯基，烷基部分为碳原子数1〜3的烷基苯基，烷氧基部分为碳原子数1〜3的烷氧基苯基， 三氟甲基苯基，其中烷硫基部分具有1至3个碳原子的烷硫基苯基或式（CmH2m-p + 1） - （R9）p的基团，其中m是1-6的整数，p是整数1 - 2和R9是C1-C3烷氧基; R 2是氢原子或C 1 -C 3烷基; R3是氢原子，C1-C3烷基，苯基或烷氧基苯基，其中烷氧基部分具有1至3个碳原子; R4是氢原子或羟基，或者R3和R4可以与这些取代基结合的碳原子一起形成C1-C3亚烷基或羰基; R5是氢原子或C1-C3烷基; R6是氢原子或甲基; R 7和R 8独立地为氢原子或C 1 -C 2烷基; n为0-2的整数; 或其酸加成盐，以及药学上可接受的载体或稀释剂。

公开(公告)号：US3950346A

公开(公告)日：1976-04-13

申请号：US356807

申请日：1973-05-03

申请人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Kenji Kobayashi ,  Yoshiaki Takebayashi ,  Hisao Yamamoto

IPC分类号： C07D221/26

CPC分类号： C07D221/26

摘要： 2-Ketoethyl-6,7-benzomorphan derivatives of the formula: ##SPC1##And their pharmaceutically acceptable non-toxic salts, which are useful as non-addictive analgesics and pain-relieving agents and can be prepared by reacting the corresponding 6,7-benzomorphan derivative of the formula: ##SPC2##With a vinyl carbonyl compound of the formula: ##EQU1## [wherein R' is a hydrogen atom or a group of the formula: --OR" (wherein R" is a hydrogen atom, an alkanoyl group, an alkyl group, an aralkyl group, an alkoxycarbonylmethyl group or a tetrahydropyranyl group), R.sub.1 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, R.sub.2 is a hydrogen atom or an alkyl group and A is an alkyl group, an alkoxy group, a substituted or unsubstituted aryl group or a substituted or unsubstituted amino group].

公开(公告)号：US4318925A

公开(公告)日：1982-03-09

申请号：US132135

申请日：1980-03-20

申请人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Masaru Fukui ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Masaru Fukui ,  Hisao Yamamoto

IPC分类号： C07C235/14 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07C235/22 ,  C07D209/48 ,  C07D295/088 ,  C07C103/37

CPC分类号： C07D209/48 ,  C07D295/088

摘要： A new class of 4-homoisotwistane derivatives of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and R.sub.2 is an alkyl group, a phenyl group which may be either unsubstituted or substituted with a C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro group or a halogen atom (hereinafter referred to as "an optionally substituted phenyl group"), a group of the formula, --A--OH in which A is a C.sub.1 -C.sub.3 alkylene group; a group of the formula, --A--B in which A is as defined as above and B is a halogen atom, or a group of the formula, ##STR2## in which A is as defined above and R.sub.3 and R.sub.4 are independently a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group or R.sub.3 and R.sub.4 may, when taken together with the adjacent nitrogen atom to which R.sub.3 and R.sub.4 are linked, form pyrrolidine, piperidine, morpholine, phthalimide or piperazine, which have been found to possess potent antiviral activity, are prepared, for example by reacting a compound of the formula, ##STR3## wherein R.sub.1 is as defined above and X is halogen, with a compound of the formula,R.sub.5 OYwherein R.sub.5 has the same meanings as R.sub.2 with the exception of the group of the formula --A--B wherein A and B are as defined above and Y is alkali metal.

摘要翻译： 一种新的下式的4-异亮氨酸维生素衍生物，其中R1是氢原子或C1-C3烷基，R2是烷基，可以是未取代的或被C1- C3烷基，C1-C3烷氧基，硝基或卤素原子（以下称为“任选取代的苯基”），其中A为C1-C3亚烷基的式-A-OH基团; 其中A如上所定义并且B是卤素原子的式-AB，或其中A如上所定义的式（IMAGE）的基团，且R 3和R 4独立地是氢原子或 C1-C3烷基或R3和R4可以与R3和R4相连的相邻氮原子一起形成已被发现具有强抗病毒活性的吡咯烷，哌啶，吗啉，邻苯二甲酰亚胺或哌嗪，是 例如通过使下式的化合物，其中R 1如上所定义，X是卤素的化合物与下式化合物反应：其中R 5具有与R 2相同的含义， 式-AB其中A和B如上所定义，Y是碱金属。

公开(公告)号：US08669040B2

公开(公告)日：2014-03-11

申请号：US12320226

申请日：2009-01-22

申请人： Hiroshi Tashiro ,  Atsushi Sugasaki ,  Hisao Yamamoto

发明人： Hiroshi Tashiro ,  Atsushi Sugasaki ,  Hisao Yamamoto

IPC分类号： B41N1/00 ,  B41F33/00 ,  G03F7/00 ,  G03F7/26

CPC分类号： B41C1/05

摘要： The invention provides a method of manufacturing a relief printing plate having at least engraving an area which is in a relief forming layer of a relief printing plate precursor for laser engraving and is to be exposed by scanning exposure using a fiber-coupled semiconductor laser which emits laser beam with a wavelength of 700 nm to 1,300 nm. The relief printing plate precursor has at least a relief forming layer provided over a support, and the relief forming layer contains at least a binder polymer and a photo-thermal conversion agent. The invention further provides a relief printing plate precursor for laser engraving which can be used in the method of manufacturing a relief printing plate.

摘要翻译： 本发明提供一种制造凸版印刷版的方法，该凸版印刷板至少雕刻在用于激光雕刻的浮雕印版前体的凸版形成层中的区域，并且通过使用发射的光纤耦合半导体激光器的扫描曝光来曝光 波长为700nm至1300nm的激光束。 凸版印刷版前体至少具有设置在载体上的浮雕形成层，凸版形成层至少含有粘合剂聚合物和光热转换剂。 本发明还提供了可用于制造凸版印刷版的方法中的用于激光雕刻的浮雕印版前体。

公开(公告)号：US07741005B2

公开(公告)日：2010-06-22

申请号：US11730411

申请日：2007-04-02

申请人： Hiromitsu Yanaka ,  Shigeo Koizumi ,  Hisao Yamamoto

发明人： Hiromitsu Yanaka ,  Shigeo Koizumi ,  Hisao Yamamoto

IPC分类号： G03C1/00 ,  G03C1/36

CPC分类号： B41C1/1016 ,  B41C2201/02 ,  B41C2201/10 ,  B41C2201/14 ,  B41C2210/04 ,  B41C2210/06 ,  B41C2210/22 ,  B41C2210/24

摘要： The present invention provides a planographic printing plate precursor, including: a support; and a photosensitive layer containing a polymerizable compound; an oxygen barrier layer; and a protective layer containing a filler (preferably an organic resin particle), the layers being formed in this order on the support. The present invention also provides a stack of planographic printing plate precursors, produced by stacking the planographic printing plate precursors with the photosensitive layer side outermost layer and the support side rear surface of the adjacent plate precursor in direct contact with each other.

摘要翻译： 本发明提供一种平版印刷版原版，包括：载体; 和含有可聚合化合物的感光层; 氧阻隔层; 和含有填料（优选有机树脂颗粒）的保护层，这些层依次形成在载体上。 本发明还提供了通过将平版印刷版前体与感光层侧最外层和邻近的板前体的支撑侧后表面彼此直接接触而堆叠制成的平版印刷版前体的叠层。