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1. 发明授权

US4026927A Novel prostaglandin derivatives 失效
标题翻译：新型前列腺素衍生物
公开(公告)号：US4026927A
公开(公告)日：1977-05-31
申请号：US508252
申请日：1974-09-23
申请人： Masuo Murakami , Noriyoshi Inukai , Hidenori Iwamoto , Toshinari Tamura , Isao Yanagisawa , Osamu Hasegawa , Yoshio Ishii , Hideya Matsuda , Tetsuya Shiozaki , Kenichi Tomioka
发明人： Masuo Murakami , Noriyoshi Inukai , Hidenori Iwamoto , Toshinari Tamura , Isao Yanagisawa , Osamu Hasegawa , Yoshio Ishii , Hideya Matsuda , Tetsuya Shiozaki , Kenichi Tomioka
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Novel prostaglandin derivatives are provided having the formula: ##STR1## wherein A represents ##STR2## one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other of them represents a lower alkyl group; one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other of them represents a hydroxyl group; and one of R.sub.7 and R.sub.8 represents a hydrogen atom and the other of them represents a lower alkyl group.The compounds of this invention have excellent effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.sub..alpha..
摘要翻译：提供了具有下式的新型前列腺素衍生物：其中A表示R 3中的一个，R 4表示氢原子，另一个表示低级烷基; R5和R6之一表示氢原子，另一个表示羟基; R 7和R 8中的一个表示氢原子，另一个表示低级烷基。

2. 发明授权

US4246280A 20-Alkoxy-16-alkyl-prostadienoic acid derivatives 失效
标题翻译： 20-烷氧基-16-烷基 - 前列腺烯酸衍生物
公开(公告)号：US4246280A
公开(公告)日：1981-01-20
申请号：US16070
申请日：1979-02-28
申请人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Kenichi Tomioka , Tetsuya Shiozaki, deceased
发明人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Kenichi Tomioka , Tetsuya Shiozaki, deceased
IPC分类号： C07C405/00 , C07D307/935 , C07D309/12 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12
摘要： There are disclosed 20-alkoxy-16-alkyl-prostadienoic acid derivatives of the formula: ##STR1## wherein A represents ##STR2## R and R.sup.5, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group, and the pharmaceutically acceptable non-toxic salts thereof. These compounds have excellent pharmacological effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.alpha..
摘要翻译：公开了下式的20-烷氧基-16-烷基 - 前列腺烯酸衍生物：其中A表示R和R 5可以相同或不同，各自表示氢原子或低级烷基; 和可以相同或不同的R 1和R 4各自表示低级烷基及其药学上可接受的无毒盐。这些化合物具有优异的药理作用，如前列腺素E2和前列腺素F2α。

3. 发明授权

US4055589A 20-Alkoxy-16-alkyl prostadienoic acid derivatives 失效
标题翻译： 20-烷氧基-16-烷基前列腺素衍生物
公开(公告)号：US4055589A
公开(公告)日：1977-10-25
申请号：US640497
申请日：1975-12-15
申请人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Kenichi Tomioka , Tetsuya Shiozaki, deceased
发明人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Kenichi Tomioka , Tetsuya Shiozaki, deceased
IPC分类号： C07C405/00 , C07D307/935 , C07D309/12 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12
摘要： A 20-alkoxy-16-alkyl-prostadienoic acid derivative shown by the formula ##STR1## wherein A represents ##STR2## R and R.sup.5, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group,And the pharmacologically acceptable nontoxic salts thereof.The compounds have excellent effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.alpha..
摘要翻译：其中A表示R和R 5可以相同或不同，表示氢原子或低级烷基的式“IMAGE”所示的20-烷氧基-16-烷基 - 前列腺二烯酸衍生物。并且可以相同或不同的R 1和R 4各自表示低级烷基，并且其药理学上可接受的非共价键。

4. 发明授权

US4058665A Novel 3,15-dilower alkyl PGE.sub.2 derivatives 失效
标题翻译：新型3,15-二烯烷基PGE {HD 2 {B衍生物
公开(公告)号：US4058665A
公开(公告)日：1977-11-15
申请号：US629568
申请日：1975-11-06
申请人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Tetsuya Shizaoki , Kenichi Tomioka , Tokuichi Takagi
发明人： Noriyoshi Inukai , Masuo Murakami , Hidenori Iwamoto , Isao Yanagisawa , Toshinari Tamura , Yoshio Ishii , Tetsuya Shizaoki , Kenichi Tomioka , Tokuichi Takagi
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： 3,15-Dilower alkyl prostaglandin E.sub.2 derivatives and 3,15-dilower alkyl prostaglandin D.sub.2 derivatives are disclosed. These compounds have antigastric ulcer activity without undesirable side effects to intestinal organs.
摘要翻译：公开了3,15-二烷基前列腺素E2衍生物和3,15-二代烷基前列腺素D2衍生物。这些化合物具有抗胃溃疡活性，对肠器官无不良副作用。

5. 发明授权

US4610821A 4-substituted-2-azetidinone compound, process of producing the compounds, and medicaments containing the compounds 失效
标题翻译： 4-取代-2-氮杂环丁酮化合物，制备该化合物的方法和含有这些化合物的药物
公开(公告)号：US4610821A
公开(公告)日：1986-09-09
申请号：US785168
申请日：1985-10-07
申请人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
发明人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
IPC分类号： C07D403/14 , C07D205/08 , C07D403/12 , C07K5/078 , C07K5/097 , C07D413/12
CPC分类号： C07D403/12 , C07D205/08 , C07K5/06147
摘要： A novel 4-substituted-2-azetidinone compound shown by the general formula ##STR1## and salts thereof. The compounds of this invention have a strong CNS activity and are useful for improving a disturbance of consciousness in shizophrenia, a head injury, etc., or improving hypobulia, memory loss, etc.

6. 发明授权

US4636567A 4-substituted-2-azetidinone compound 失效
标题翻译： 4-取代-2-氮杂环丁酮化合物
公开(公告)号：US4636567A
公开(公告)日：1987-01-13
申请号：US785169
申请日：1985-10-07
申请人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
发明人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
IPC分类号： C07D403/14 , C07D205/08 , C07D403/12 , C07K5/078 , C07K5/097
CPC分类号： C07D403/12 , C07D205/08 , C07K5/06147
摘要： A novel-4-substituted-2-azetidinone compound shown by the general formula ##STR1## and salts thereof. The compounds of this invention have a strong CNS activity and are useful for improving a disturbance of consciousness in schizophrenia, a head injury, etc., or improving hypobulia, memory loss, etc.

7. 发明授权

US4564609A 4-Substituted-2-azetidinone compound, process of producing the compounds, and medicaments containing the compounds 失效
标题翻译： 4-取代-2-氮杂环丁酮化合物，制备该化合物的方法和含有这些化合物的药物
公开(公告)号：US4564609A
公开(公告)日：1986-01-14
申请号：US592866
申请日：1984-03-23
申请人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
发明人： Toshinari Tamura , Hidenori Iwamoto , Makoto Yoshida , Minoru Yamamoto
IPC分类号： C07D403/14 , C07D205/08 , C07D403/12 , C07K5/078 , C07K5/097 , A61K37/00
CPC分类号： C07D403/12 , C07D205/08 , C07K5/06147
摘要： A novel 4-substituted-2-azetidinone compound shown by the general formula ##STR1## and salts thereof. The compounds of this invention have a strong CNS activity and are useful for improving a disturbance of consciousness in schizophrenia, a head injury, etc., or improving hypobulia, memory loss, etc.
摘要翻译：由通式表示的新型4-取代-2-氮杂环丁酮化合物及其盐。本发明化合物具有较强的CNS活性，可用于改善精神分裂症意识障碍，头部损伤等，或改善低血压，记忆力丧失等。

8. 发明授权

US4719207A CNS active substituted azetidinone compounds 失效
标题翻译： CNS活性取代的氮杂环丁酮化合物
公开(公告)号：US4719207A
公开(公告)日：1988-01-12
申请号：US747018
申请日：1985-06-20
申请人： Toshinari Tamura , Makoto Yoshida , Shin-ichi Tsukamoto , Hidenori Iwamoto , Minoru Yamamoto , Soichi Kagami
发明人： Toshinari Tamura , Makoto Yoshida , Shin-ichi Tsukamoto , Hidenori Iwamoto , Minoru Yamamoto , Soichi Kagami
IPC分类号： C07D205/08 , C07D205/085 , C07F7/10 , C07K5/097 , A61K31/415 , C07D403/12 , C07D403/14
CPC分类号： C07K5/0821 , C07D205/08 , C07D205/085 , C07F7/10
摘要： Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.
摘要翻译：提供具有下式的取代的氮杂环丁酮化合物：其中R 1和R 2之一表示取代的低级烷基，叠氮基，氨基，低级酰氨基，巯基或低级烷硫基另一个表示氢基团，或者都表示氢原子或低级烷基; R3表示氢原子或由下式表示的基团：其中X表示（其中R5表示氢原子或低级烷基），Y表示羟基，低级烷氧基，氨基，一或二低级烷基氨基）; R 4表示氢原子，取代或未取代的低级烷基或由式-CH 2 CO-A（其中A表示氨基或由下式表示的基团：其中X和Y如上所定义）），条件是当R 1和R 2均为氢原子时，至少R 4表示氢原子以外的基团，只要R 3或R 4表示除氢原子以外的基团，则该化合物具有强CNS作用。

9. 发明授权

US4477443A Tylosin derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：泰乐菌素衍生物，它们的制剂和含有它们的药物组合物
公开(公告)号：US4477443A
公开(公告)日：1984-10-16
申请号：US395463
申请日：1982-07-06
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Akihiro Tanaka , Hidenori Iwamoto , Shuichi Sakamoto
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Akihiro Tanaka , Hidenori Iwamoto , Shuichi Sakamoto
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： Tylosin compounds of the formula ##STR1## wherein R.sub.1 represents a hydroxyl group; a halogen atom; ##STR2## group (wherein R.sub.5 is a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group and R.sub.6 is a hydrogen atom, a lower alkyl group which may be substituted by a hydroxyl group, an aryl group, an aralkyl group, a cycloalkyl group having 3-10 carbon atoms, --CO(O).sub.m --R.sub.7 group (wherein m is 0 or 1 and R.sub.7 is a lower alkyl group, an aryl group, an aralkyl group, a furanyl group, or a pyridyl group), or --CH.sub.2 --R.sub.13 group (wherein R.sub.13 is a mono-, di-, or trifluoromethyl group)); --N(CH.sub.2).sub.n group (wherein n is an integer of 2-15) which may be substituted by an oxo group, a hydroxyl group, a lower alkyl group, or a hydroxy lower alkyl group; an imidazolyl group, a morpholino group, or a piperazino group each may be substituted by a lower alkyl group; or --OOCCH.sub.2 --R.sub.8 group (wherein R.sub.8 is ##STR3## group (wherein R.sub.9 and R.sub.10, which may be the same or different, each is a hydrogen atom or a lower alkyl group; said R.sub.9 and R.sub.10 may be combined with each other to form an alkylene group having 3-7 carbon atoms) or --S--R.sub.11 group (wherein R.sub.11 is a furanyl group or a pyridyl group)); R.sub.2 represents a hydrogen atom or a lower alkanoyl group; R.sub.3 represents a methyl group or --CH.sub.2 CHO group; R.sub.4 represents a hydrogen atom or a hydroxyl group; A represents 0.dbd., ##STR4## line represents a single bond or a double bond; and line ---- represents a single bond, a double bond, or ; however, when said R.sub.1 is a hydroxyl group, said R.sub.3 is a methyl group and R.sub.4 is a hydrogen atom, or said line ---- is ; or when said R.sub.1 is a halogen atom, said R.sub.3 is a methyl group of said line ---- is .The foregoing compounds of this invention are useful as antibiotics.
摘要翻译：式“IMAGE”的泰乐菌素化合物，其中R 1表示羟基; 卤素原子; 基（其中R5是氢原子或可被羟基取代的低级烷基，R6是氢原子，可被羟基取代的低级烷基，芳基，芳烷基基团，具有3-10个碳原子的环烷基，-CO（O）m-R7基团（其中m为0或1，R7为低级烷基，芳基，芳烷基，呋喃基或吡啶基）或-CH 2 -R 13基（其中R 13是单 - ，二 - 或三氟甲基））; -N（CH 2）n基（其中n为2-15的整数），其可被氧代基，羟基，低级烷基或羟基低级烷基取代; 咪唑基，吗啉代基或哌嗪子基各自可以被低级烷基取代; 或-OOCCH 2 -R 8基团（其中R 8为<基团）（其中R 9和R 10可以相同或不同，各自为氢原子或低级烷基;所述R 9和R 10可彼此组合形成具有3-7个碳原子的亚烷基）或-S-R11基（其中R11是呋喃基或吡啶基））; R2表示氢原子或低级烷酰基; R3表示甲基或-CH2CHO基; R4表示氢原子或羟基; A代表0 =，线代表单键或双键; 线----代表单键，双键，或; 然而，当所述R 1为羟基时，所述R 3为甲基，R 4为氢原子，或者当所述R 1为卤素原子时，所述R 3为所述线----甲基。本发明的前述化合物可用作抗生素。

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