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11. 发明授权

US4318925A 4-Homoisotwistane derivatives 失效
标题翻译： 4-Homoisotwistane衍生物
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。

12. 发明授权

US4209525A Imidazole acetic acid derivatives 失效
标题翻译：咪唑乙酸衍生物
公开(公告)号：US4209525A
公开(公告)日：1980-06-24
申请号：US971826
申请日：1978-12-19
申请人： Toshio Atsumi , Yuzo Tarumi , Takao Kiyohara
发明人： Toshio Atsumi , Yuzo Tarumi , Takao Kiyohara
IPC分类号： A61K31/415 , A61P37/04 , C07D233/90
CPC分类号： C07D233/90 , Y10S514/885
摘要： Imidazole derivatives represented by the formula: ##STR1## wherein Y is a hydroxy group, a lower alkoxy group or an amino group, and their non-toxic, pharmaceutically acceptable salts, which have a potent immunostimulating activity and are useful for the immunostimulatory therapy of various diseases, and their preparation and use.
摘要翻译：由下式表示的咪唑衍生物：其中Y是羟基，低级烷氧基或氨基，及其无毒的药学上可接受的盐，它们具有有效的免疫刺激活性，可用于免疫刺激性治疗各种疾病及其准备和使用。

13. 发明授权

US3682914A 2,6-diphenyl-4,5-dihydro-3(2h)-pyridizinone derivatives 失效
标题翻译： 2,6-二氢-4,5-二氢-3（2H） - 吡啶酮衍生物
公开(公告)号：US3682914A
公开(公告)日：1972-08-08
申请号：US3682914D
申请日：1968-11-21
申请人： HISAO YAMAMOTO , TOSHIO ATSUMI , HIROSHI AWATA
发明人： YAMAMOTO HISAO , ATSUMI TOSHIO , AWATA HIROSHI
IPC分类号： B60B23/00 , C07D237/04 , C07D51/04
CPC分类号： C07D237/04 , B60B23/00 , Y10S514/924
摘要： A novel 2,6-diphenyl-4,5-dihydro-3(2H)-pyridazinone derivative having remarkable anti-inflammatory, anti-tuberculous and antivirus actions represented by the general formula:

WHEREIN R1 represents a lower alkyl group of from 1-4 carbon atoms, a lower alkoxyl group of from 1-4 carbon atoms, or a lower alkylthio group of from 1-4 carbon atoms; R2 represents a hydrogen or a methyl group; and X represents a halogen atom and a lower alkoxy group which is prepared by reacting a hydrazine derivative with a Beta -benzoylpropionic acid derivative.
摘要翻译：一种新颖的2,6-二苯基-4,5-二氢-3（2H） - 哒嗪酮衍生物，具有显着的抗炎，抗结核和抗病毒作用，由以下通式表示：

14. 发明授权

US4849434A Novel thiazolidin-4-one derivatives and acid addition salts therof 失效
标题翻译：新型噻唑烷-4-酮衍生物和酸加成盐
公开(公告)号：US4849434A
公开(公告)日：1989-07-18
申请号：US74873
申请日：1987-07-17
申请人： Masao Enomoto , Masami Muraoka , Keiichi Ono , Atsuyuki Kojima , Toshio Atsumi , Yoshihiro Komuro , Yuzuru Sanemitsu , Masato Mizutani
发明人： Masao Enomoto , Masami Muraoka , Keiichi Ono , Atsuyuki Kojima , Toshio Atsumi , Yoshihiro Komuro , Yuzuru Sanemitsu , Masato Mizutani
IPC分类号： A61K31/44 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , C07D417/04
CPC分类号： C07D417/04
摘要： A novel 2-pyridylthiazolidin-4-one derivative represented by the general formula ##STR1## wherein Ar denotes an aryl group unsubstituted or substituted with a halogen atom or with a lower alkoxy group; X denotes a straight-chain or branched-chain lower alkylene group or a single bond; R denotes a hydrogen atom, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, acyloxy, di(lower alkyl) amino, hydroxyl or aryl group, or denotes an aryl group substituted with a lower alkoxy group; and Py denotes a pyridyl group, and the acid addition salt thereof, which have an excellent platelet activating factor antagonsm.

15. 发明授权

US4218457A 2-Substituted 5-hydroxy-1H-imidazole-4-carboxamide derivatives and use 失效
标题翻译： 2-取代的5-羟基-1H-咪唑-4-甲酰胺衍生物和用途
公开(公告)号：US4218457A
公开(公告)日：1980-08-19
申请号：US940131
申请日：1978-09-06
申请人： Toshio Atsumi , Yuzo Tarumi , Noboru Yoshida
发明人： Toshio Atsumi , Yuzo Tarumi , Noboru Yoshida
IPC分类号： C07D233/90 , A61K31/415 , A61K31/44 , C07D233/32 , C07D403/04
CPC分类号： C07D233/90
摘要： Compounds of the formula, ##STR1## wherein R is C.sub.2 -C.sub.17 alkyl group, C.sub.3 -C.sub.7 cycloalkyl group, 1-adamantyl group, pyridyl group, pyridine N-oxide, diphenylmethyl group, benzyl group which may or may not be substituted with nitro group, halogen atom, C.sub.1 -C.sub.3 alkyl group or C.sub.1 -C.sub.3 alkoxy group, or phenyl group which may or may not be substituted with nitro group, halogen atom, hydroxy group, C.sub.1 -C.sub.3 alkyl group, C.sub.1 -C.sub.3 alkoxy group, carboxy group, C.sub.2 -C.sub.4 alkoxycarbonyl group, phenoxycarbonyl group, carbamoyl group, N-phenylcarbamoyl group, N-adamantylcarbamoyl group, benzoylamino group, trifluoromethyl group, C.sub.2 -C.sub.4 alkanoyloxy group, 1-adamantoyloxy group or benzoyloxy group and salts thereof have an anticancer activity and an immunostimulating activity.
摘要翻译：下式的化合物，其中R是C 2 -C 17烷基，C 3 -C 7环烷基，1-金刚烷基，吡啶基，吡啶N-氧化物，二苯基甲基，可以是也可以不是被硝基，卤原子，C1-C3烷基或C1-C3烷氧基取代的苯基，或可以被硝基，卤素原子，羟基，C1-C3烷基，C1-C3烷氧基取代的苯基基团，羧基，C 2 -C 4烷氧基羰基，苯氧基羰基，氨基甲酰基，N-苯基氨基甲酰基，N-金刚烷基氨基甲酰基，苯甲酰氨基，三氟甲基，C 2 -C 4烷酰氧基，1-酰胺基氧基或苯甲酰氧基及其盐抗癌活性和免疫刺激活性。

16. 发明授权

US4140788A N-Substituted imidazolecarboxamide derivatives 失效
标题翻译： N-取代的咪唑甲酰胺衍生物
公开(公告)号：US4140788A
公开(公告)日：1979-02-20
申请号：US849515
申请日：1977-11-07
申请人： Toshio Atsumi , Yuzo Tarumi , Norboru Yoshida
发明人： Toshio Atsumi , Yuzo Tarumi , Norboru Yoshida
IPC分类号： C07C271/22 , C07D233/90 , A61K31/415 , C07D233/64
CPC分类号： C07C271/22 , C07D233/90
摘要： N-Substituted imidazolecarboxamide compounds represented by the formula; ##STR1## wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, R.sub.2 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, 1-adamantyl, R.sub.3 is hydrogen atom, lower alkyl, aralkyl; with the proviso that one of R.sub.1, R.sub.2 or R.sub.3 is not hydrogen when the other two are hydrogen, are produced by reacting aminomalonamide derivative with orthoformate derivative in high yields. The compounds (I) exhibit anti-tumor activity against experimental tumors such as Sarcoma 180 in mice.
摘要翻译：由式表示的N-取代的咪唑酰甲酰胺化合物; （I）其中R 1是氢原子，低级烷基，低级烯基，芳烷基，R 2是氢原子，低级烷基，低级烯基，芳烷基，1-金刚烷基，R 3是氢原子，低级烷基，芳烷基。条件是当另外两个是氢时，R 1，R 2或R 3中的一个不是氢，是通过氨基马来酰亚胺衍生物与原甲酸酯衍生物以高收率反应制备的。化合物（I）对小鼠的实验性肿瘤如肉瘤180具有抗肿瘤活性。

17. 发明授权

US3953441A Preparation of 2-benzoylalkylbenzomorphan 失效
标题翻译： 2-苯甲酰基烷基苯并咪唑的制备
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。

18. 发明授权

US3951984A 3-Benzazocine compounds 失效
标题翻译： 3-苯并吖嗪化合物
公开(公告)号：US3951984A
公开(公告)日：1976-04-20
申请号：US425717
申请日：1973-12-18
申请人： Michio Kimura , Takeshi Nakajima , Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Shigeho Inaba , Hisao Yamamoto
发明人： Michio Kimura , Takeshi Nakajima , Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D471/08 , C07D221/26
CPC分类号： C07D471/08
摘要： A 3-benzazocine compound of the formula: ##SPC1##Wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.8 are each hydrogen or lower alkyl, R.sub.2 is hydrogen, lower alkyl or phenyl and R.sub.6 and R.sub.7 are each lower alkyl, and its pharmaceutically acceptable acid addition salts, which are useful as analgesics and can be produced by reacting a tetrahydropyridine compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each as defined above or its salt with a Lewis acid.
摘要翻译：下式的3-苯并吖嗪化合物：

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