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公开(公告)号：US4283422A
公开(公告)日：1981-08-11
申请号：US120834
申请日：1980-02-12
IPC分类号： A61K31/13 , A61P25/00 , A61P31/12 , C07C67/00 , C07C209/00 , C07C209/50 , C07C211/38 , C07C211/41 , C07C87/40
CPC分类号： C07C211/41 , C07C2103/70
摘要： Novel 3-amino-4-homoisotwistane derivatives of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, and R.sub.2 is a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.5 alkenyl group, or non-toxic pharmaceutically acceptable salts thereof, which are very valuable as medicines for the treatment of virus-caused diseases and as antiviral agents for animals and useful for the treatment of parkinsonean disease.
摘要翻译： 新颖的下式的3-氨基-4-异亮氨酸衍生物，其中R1是氢原子，C1-C4烷基或C3-C5烯基，R2是C1-C4烷基或C3- C5烯基或其无毒的药学上可接受的盐，其作为用于治疗病毒引起的疾病的药物和用作动物的抗病毒剂是非常有价值的，并且可用于治疗帕金森病。
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2.发明授权Antitumor and immunosuppresive 4-carbamoyl imidazolium-5-olate derivatives, pharmaceutical composition and production thereof 失效抗肿瘤和免疫抑制性4-氨基甲酰基咪唑鎓-5-醇酸酯衍生物，药物组合物及其制备方法
公开(公告)号：US4332806A
公开(公告)日：1982-06-01
申请号：US205980
申请日：1980-11-12
IPC分类号： A61K31/415 , A61P35/00 , C07D233/90
CPC分类号： C07D233/90 , Y10S514/885
摘要： There are provided compounds of the formula: ##STR1## wherein R is an adamantoyl group substituted with a lower alkyl group, a lower alkoxy group, a hydroxy group, a lower alkanoyloxy group, an aroyloxy group, a halogen atom, an acetamido group, a nitro group, an azide group, a trifluoromethyl group or a phenyl group which may be substituted with a nitro group, a halogen atom, a lower alkyl group or a lower alkoxy group and a process producing them. These compounds are useful as antitumor agents and immunosuppressants.
摘要翻译： 提供下式的化合物：其中R是被低级烷基，低级烷氧基，羟基，低级烷酰氧基，芳酰氧基，卤素原子，乙酰氨基基团取代的亚甲酰基， 硝基，叠氮基，三氟甲基或可以被硝基，卤素原子，低级烷基或低级烷氧基取代的苯基，以及制备它们的方法。 这些化合物可用作抗肿瘤剂和免疫抑制剂。
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公开(公告)号：US4464531A
公开(公告)日：1984-08-07
申请号：US366423
申请日：1982-04-07
CPC分类号： C07H17/02
摘要： There are provided compounds of the formula: ##STR1## wherein either R.sub.1 or R.sub.2 is a hydrogen atom, a hydroxy group, an acyloxy group, a phthalimido group or an acetamido group and the other is a hydrogen atom; either R.sub.3 or R.sub.4 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.5 or R.sub.6 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.7 or R.sub.8 is a hydrogen atom, a methyl group, a hydroxymethyl group, an acyloxymethyl group, an alkoxycarbonyl group, a group of the formula: ##STR2## (wherein X.sub.1 and X.sub.2 are a hydrogen atom or a lower alkyl group), or a carboxyl group and the other is a hydrogen atom; either R.sub.11 or R.sub.12 is a hydrogen atom, a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.13 or R.sub.14 is a hydroxy group or an acyloxy group and the other is a hydrogen atom; either R.sub.15 or R.sub.16 is a methyl group, a hydroxymethyl group or an acyloxymethyl group and the other is a hydrogen atom; and a process for producing them. These compounds are useful as antitumor agents.
摘要翻译： 提供下式的化合物：其中R 1或R 2为氢原子，羟基，酰氧基，苯二甲酰亚氨基或乙酰氨基，其中R 1或R 2为氢原子， 另一个是氢原子; R3或R4是羟基或酰氧基，另一个是氢原子; R5或R6是羟基或酰氧基，另一个是氢原子; R7或R8是氢原子，甲基，羟甲基，酰氧基甲基，烷氧基羰基，下式的基团：其中X1和X2是氢原子或低级烷基， 或羧基，另一个是氢原子; R 11或R 12是氢原子，羟基或酰氧基，另一个是氢原子; R13或R14是羟基或酰氧基，另一个是氢原子; R 15或R 16是甲基，羟甲基或酰氧基甲基，另一个是氢原子; 以及生产它们的过程。 这些化合物可用作抗肿瘤剂。
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公开(公告)号：US4318925A
公开(公告)日：1982-03-09
申请号：US132135
申请日：1980-03-20
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。
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公开(公告)号：US3953441A
公开(公告)日：1976-04-27
申请号：US150841
申请日：1971-06-07
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。
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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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公开(公告)号：US4260774A
公开(公告)日：1981-04-07
申请号：US51741
申请日：1979-06-25
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。
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8.发明授权Analgesic compositions containing 2-cyanoalkylbenzomorphan derivatives and salts thereof 失效含有2-氰基烷基苯并喃衍生物及其盐的止痛组合物
公开(公告)号：US3962446A
公开(公告)日：1976-06-08
申请号：US523412
申请日：1974-11-13
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。
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9.发明授权Novel process for producing 2-ketoethylbenzomorphan derivatives and salts thereof 失效生产2-乙基苯并吡喃衍生物的新方法及其制备方法
公开(公告)号：US3950346A
公开(公告)日：1976-04-13
申请号：US356807
申请日：1973-05-03
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].
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公开(公告)号：US4774319A
公开(公告)日：1988-09-27
申请号：US119279
申请日：1987-11-09
申请人： Keiichi Ono , Yoshiyuki Kai , Yoshiaki Takebayashi , Akihiko Sano , Kazushi Suwa
发明人： Keiichi Ono , Yoshiyuki Kai , Yoshiaki Takebayashi , Akihiko Sano , Kazushi Suwa
CPC分类号： C07K14/60 , A61K38/00 , Y02P20/55 , Y10S930/12
摘要： A process for the manufacture of a polypeptide (I) having the formula: ##STR1## which comprises steps of: (a) coupling, successively and in the order of the sequence of the polypeptide (I), the four protected fragments A, B, C and D or five protected fragments A, B, C, E and F,said fragment A by the formula, Leu-Gin-Asp-Ile-Met-Ser-Arg-NH.sub.2said fragment B by the formula, Gln-Leu-Ser-Ala-Arg-Lys-Leusaid fragment C by the formula, Arg-Lys-Val-Leu-Glysaid fragment D by the formula, Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyrsaid fragment E by the formula, Ile-Phe-Thr-Asn-Ser-Tyrand said fragment F by the formula, Tyr-Ala-Asp-Ala being represented, respectively, and(b) eliminating, at the end of sequence, all the protecting groups to provide the polypeptide (I) which is active on the stimulation of the release of the growth hormone and thus is very useful as medicine for treatment of growth hormone deficiency disease and the like.
摘要翻译： 一种制备具有下式的多肽（I）的方法：其包括以下步骤：（a）依次和按照多肽（I ），四个保护的片段A，B，C和D或五个保护的片段A，B，C，E和F，所述片段A通过式Leu-Gin-Asp-Ile-Met-Ser-Arg-NH2表示 片段B由式Gln-Leu-Ser-Ala-Arg-Lys-Leu表示，由式Arg-Lys-Val-Leu-Gly表示的片段C表示下式的Tyr-Ala-Asp-Ala- Ile-Phe-Thr-Asn-Ser-Tyr分别表示分子式为Ile-Phe-Thr-Asn-Ser-Tyr的片段E和由式Tyr-Ala-Asp-Ala表示的所述片段F，以及 （b）在序列结束时，除去所有保护基以提供在刺激生长激素释放方面具有活性的多肽（I），因此作为治疗生长激素缺乏症的药物非常有用， 类似。
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