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1. 发明授权

US4242504A 3"-Acylated macrolide antibiotics 失效
标题翻译： 3“ - 酰化大环内酯抗生素
公开(公告)号：US4242504A
公开(公告)日：1980-12-30
申请号：US37859
申请日：1979-05-10
申请人： Hideo Sakakibara , Osamu Okegawa , Toshiyuki Watanabe , Tatsuro Fujiwara , Susumu Watanabe , Satoshi Omura , Tetsuo Matsuda
发明人： Hideo Sakakibara , Osamu Okegawa , Toshiyuki Watanabe , Tatsuro Fujiwara , Susumu Watanabe , Satoshi Omura , Tetsuo Matsuda
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： 3"-acylated macrolide antibiotics of the formula ##STR1## wherein R.sub.1 is hydrogen or C.sub.2-3 alkanoyl, R.sub.2 is hydrogen or C.sub.2-4 alkanoyl, at least one of R.sub.1 and R.sub.2 being hydrogen, and one of R' and R" being R.sub.3 and the other R.sub.4, R.sub.3 being C.sub.2-6 alkanoyl and R.sub.4 being C.sub.2-5 alkanoyl, or a pharmaceutically acceptable salt thereof.
摘要翻译： 3“ - 酰化大环内酯类抗生素，其中R1是氢或C2-3烷酰基，R2是氢或C2-4烷酰基，R1和R2中的至少一个是氢，R' 和R“为R3且另一个R4，R3为C2-6烷酰基，R4为C2-5烷酰基，或其药学上可接受的盐。

2. 发明授权

US4268665A Derivatives of antibiotic tylosin 失效
标题翻译：抗生素泰乐菌素衍生物
公开(公告)号：US4268665A
公开(公告)日：1981-05-19
申请号：US075661
申请日：1979-09-14
申请人： Hideo Sakakibara , Tatsuro Fujiwara , Osamu Okegawa , Toshiyuki Watanabe , Susumu Watanabe , Tetsuo Matsuda
发明人： Hideo Sakakibara , Tatsuro Fujiwara , Osamu Okegawa , Toshiyuki Watanabe , Susumu Watanabe , Tetsuo Matsuda
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： Derivatives of antibiotic tylosin of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkanoyl, A.sub.1 and A.sub.2 are groups of which one is R.sub.2 and the other is R.sub.3, and R.sub.2 and R.sub.3 are C.sub.2-6 alkanoyl, or a physiologically acceptable salt thereof, have enhanced antibacterial activity against macrolide antibiotic-resistant strains.
摘要翻译：其中R 1为氢或低级烷酰基，A1和A2为其中一个为R 2，另一个为R 3的基团，R 2和R 3为C 2-6烷酰基的基团的抗生素泰乐菌素衍生物，或其生理上可接受的盐对大环内酯类抗生素抗性菌株具有增强的抗菌活性。

3. 发明授权

US4345069A Deformyltylosin derivatives 失效
标题翻译：甲状腺素衍生物
公开(公告)号：US4345069A
公开(公告)日：1982-08-17
申请号：US184375
申请日：1980-09-05
申请人： Hideo Sakakibara , Tatsuro Fujiwara , Osamu Okegawa , Eiichi Honda , Susumu Watanabe , Tetsuo Matsuda
发明人： Hideo Sakakibara , Tatsuro Fujiwara , Osamu Okegawa , Eiichi Honda , Susumu Watanabe , Tetsuo Matsuda
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Deformyltylosin derivatives of the formula ##STR1## wherein A is ##STR2## --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R.sub.1 is hydrogen, lower alkanoyl or aryl-lower alkanoyl, X.sub.1 and X.sub.2 are hydrogen or are connected to form a valence bond, Y.sub.1 and Y.sub.2 are hydrogen or are connected to form a valence bond, Q.sub.1 is hydrogen or methyl, Q.sub.2 is hydrogen or ##STR3## R.sub.2 is hydrogen or lower alkanoyl, R is hydrogen or ##STR4## R.sub.3 is hydrogen or C.sub.2-5 alkanoyl, and R.sub.4 is hydrogen or C.sub.2-6 alkanoyl, and when R.sub.3 is not hydrogen, then R.sub.4 is not hydrogen, or a pharmaceutically acceptable salt thereof, have strong antibacterial activities as compared to the known antibiotic tylosin, and also have enhanced antibacterial activities against all macrolide antibiotic-resistant strains such as A, B and C group strains, and have higher blood levels as compared with tylosin.
摘要翻译：其中A为-CH = CH-或-CH 2 -CH 2 - ，R 1为氢，低级烷酰基或芳基 - 低级烷酰基，X 1和X 2为氢或连接形成价数的式键，Y1和Y2是氢或连接形成价键，Q1是氢或甲基，Q2是氢或R2是氢或低级烷酰基，R是氢或者R3是氢或C2-5 烷酰基，R4为氢或C2-6烷酰基，当R3不为氢时，R4为氢，或其药学上可接受的盐与已知抗生素泰乐菌素相比具有较强的抗菌活性，并且还具有增强的抗菌活性对抗所有大环内酯抗生素抗性菌株如A，B和C组菌株，并且与泰乐菌素相比具有较高的血液水平。

4. 发明授权

US4421911A Deoxydesmycosin 失效
标题翻译：脱氧霉素
公开(公告)号：US4421911A
公开(公告)日：1983-12-20
申请号：US358805
申请日：1982-03-16
申请人： Tatsuro Fujiwara , Eiichi Honda , Hideo Sakakibara , Takao Hirano
发明人： Tatsuro Fujiwara , Eiichi Honda , Hideo Sakakibara , Takao Hirano
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or hydroxy and at least one of R.sub.1 and R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof, has strong antimicrobial and antibacterial activity..
摘要翻译：其中R 1和R 2是氢或羟基，R 1和R 2中的至少一个是氢的化合物或其药学上可接受的盐具有很强的抗菌和抗菌活性。

5. 发明授权

US4415730A 19-Deformyl-deoxy-desmycosin 失效
标题翻译： 19-脱甲基脱氧 - 去霉菌素
公开(公告)号：US4415730A
公开(公告)日：1983-11-15
申请号：US391284
申请日：1982-06-23
申请人： Tatsuro Fujiwara , Eiichi Honda , Hideo Sakakibara , Takao Hirano
发明人： Tatsuro Fujiwara , Eiichi Honda , Hideo Sakakibara , Takao Hirano
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or hydroxyl and at least one of R.sub.1 and R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof, has antibacterial activity against Gram positive bacteria and against macrolide-resistant A group bacteria.
摘要翻译：其中R1和R2是氢或羟基并且R1和R2中的至少一个是氢的式或其药学上可接受的盐的式（IMAGE）化合物对革兰氏阳性细菌和抗大环内酯抗性A组细菌具有抗菌活性。

6. 发明授权

US4868290A 4'-Deoxy-3"-demethoxy-3"-methylenedesmycosin derivatives and synthetic intermediates thereof 失效
标题翻译： 4'-脱氧-3' - 脱甲氧基-3“ - 亚甲基二氢马来酸衍生物及其合成中间体
公开(公告)号：US4868290A
公开(公告)日：1989-09-19
申请号：US125155
申请日：1987-11-25
申请人： Tatsuro Fujiwara , Tomoko Yashiro , Hideo Sakakibara
发明人： Tatsuro Fujiwara , Tomoko Yashiro , Hideo Sakakibara
IPC分类号： A61K31/35 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08 , Y02P20/55
摘要： 4"-deoxy-3"-demethoxy-3"-methylene-desmycosin derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen, acyl or substituted carbamoyl,R.sub.2 is ##STR2## R.sub.3 is hydrogen or a protective group for hydroxy, R.sub.4 is hydrogen, hydroxy or protected hydroxy, and Me is --CH.sub.3, and pharmaceutically acceptable salts thereof are produced.These novel derivatives have antibiotic properties superior to the known related antibiotics tylosin and desmycosin.

7. 发明授权

US4661588A 23-O-substituted carbamoyl-23-demycinosyldesmycosin 失效
标题翻译： 23-O-取代的氨基甲酰基-23-脱霉霉素二十二碳三烯酸
公开(公告)号：US4661588A
公开(公告)日：1987-04-28
申请号：US790805
申请日：1985-10-25
申请人： Tatsuro Fujiwara , Kazuyo Ohta , Eiichi Honda , Takao Hirano , Hideo Sakakibara
发明人： Tatsuro Fujiwara , Kazuyo Ohta , Eiichi Honda , Takao Hirano , Hideo Sakakibara
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl, phenyl substituted by one or more lower alkyl or halogen, phenyl-lower alkyl optionally substituted in its side chain by lower alkyl or lower alkoxycarbonyl, thienylmethyl or thiazolyl, R.sub.2 is hydrogen or lower alkyl, or ##STR2## constitutes a 3-7-membered nitrogen-containing heterocyclic ring in which R.sub.1 and R.sub.2 are connected, R.sub.3 is hydrogen or hydroxyl, and X is oxygen or sulfur, or a non-toxic salt thereof. These compounds have stronger antibacterial activity as compared with known clinically used macrolide antibiotics such as erythromycin, oleandomycin, josamycin and leucomycin, and also have strong antibacterial activity against all macrolide antibiotic-resistant strains such as macrolide-resistant A group strains (clinical isolates or erythromycin, oleandomycin and 16-membered macrolide antibiotic resistant strains). These compounds are also stable in vivo and hence may be used for treatment of infectious diseases and also are useful for feed additives and growth stimulants.
摘要翻译：其中R 1是低级烷基，低级烷氧基羰基 - 低级烷基，苯基，被一个或多个低级烷基或卤素取代的苯基，在其侧链中被低级烷基或低级烷氧基羰基任意取代的苯基 - 低级烷基，噻吩基甲基或噻唑基，R2是氢或低级烷基，或者“IMAGE”构成其中R1和R2连接的3-7元含氮杂环，R3是氢或羟基，X是氧或硫，其盐酸盐。这些化合物与已知的临床使用的大环内酯类抗生素如红霉素，木兰霉素，喜马霉素和精氨酸霉素相比具有更强的抗菌活性，并且对所有大环内酯抗生素抗性菌株如大环内酯抗性A组菌株（临床分离株或红霉素）具有强抗菌活性，木兰霉素和16-元大环内酯抗生素抗性菌株）。这些化合物在体内也稳定，因此可用于治疗感染性疾病，并且还可用于饲料添加剂和生长兴奋剂。

8. 发明授权

US4515941A 23-Demycinosyldesmycosin derivatives 失效
标题翻译： 23-去霉霉素赖氨酸衍生物
公开(公告)号：US4515941A
公开(公告)日：1985-05-07
申请号：US480398
申请日：1983-03-30
申请人： Tatsuro Fujiwara , Hideyuki Watanabe , Takao Hirano , Hideo Sakakibara
发明人： Tatsuro Fujiwara , Hideyuki Watanabe , Takao Hirano , Hideo Sakakibara
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Novel 23-demycinosyldesmycosin derivatives are disclosed of the formula ##STR1## wherein A is oxygen or sulfur, R.sub.1 is optionally substituted phenyl or ##STR2## group, in which R.sub.3 is optionally substituted phenyl and R.sub.4 and R.sub.5 are the same or different and are hydrogen, lower alkyl or optionally substituted phenyl, and R.sub.2 is hydrogen or hydroxyl. The compounds or non-toxic salts thereof are useful as antibiotics.
摘要翻译：公开了新颖的23-去霉霉素赖氨酸衍生物，其中A是氧或硫，R1是任选取代的苯基或者IMAGE基团，其中R 3是任选取代的苯基，并且R 4和R 5是相同或不同的并且是氢，低级烷基或任意取代的苯基，R 2是氢或羟基。化合物或其无毒盐可用作抗生素。

9. 发明授权

US4490524A 23-O-Acyl-23-demycinosyldesmycosin derivatives 失效
标题翻译： 23-O-酰基-23-脱霉霉素赖氨酸衍生物
公开(公告)号：US4490524A
公开(公告)日：1984-12-25
申请号：US460443
申请日：1983-01-24
申请人： Tatsuro Fujiwara , Hideyuki Watanabe , Takao Hirano , Hideo Sakakibara
发明人： Tatsuro Fujiwara , Hideyuki Watanabe , Takao Hirano , Hideo Sakakibara
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, thienyl, 2-amino-4-thiazolyl or 2-chloroacetamido-4-thiazolyl; A is lower alkylene, lower alkenylene, or lower alkylene substituted by lower alkyl, amino, lower alkoxyimino or phenyl-Z-group wherein Z is a single bond or --S-- or --SO.sub.2 --, but when R.sub.1 is 2-amino-4-thiazolyl or 2-chloroacetamido-4-thiazolyl then A is lower alkylene substituted by lower alkoxyimino; R.sub.2 is hydrogen or hydroxyl; X is oxygen or sulfur and n=0 or 1, or a non-toxic salt thereof. These compounds have a stronger antibacterial activity against Gram positive bacteria as compared with known macrolide antibiotics such as erythromycin and tylosin, and also have an equivalent level of antibacterial activity against Gram negative bacteria as compared with that of erythromycin, and hence may be useful for clinical use. These compounds are also useful for feed additives and growth stimulants.
摘要翻译：其中R 1为任选取代的苯基，噻吩基，2-氨基-4-噻唑基或2-氯乙酰氨基-4-噻唑基的式IMA化合物; A是低级亚烷基，低级亚烯基或被低级烷基，氨基，低级烷氧基亚氨基或苯基-Z-基取代的低级亚烷基，其中Z是单键或-S-或-SO 2 - ，但当R 1是2-氨基-4 噻唑基或2-氯乙酰氨基-4-噻唑基，那么A是被低级烷氧基亚氨基取代的低级亚烷基; R2是氢或羟基; X是氧或硫，n = 0或1，或其无毒盐。与红霉素和泰乐菌素等已知的大环内酯类抗生素相比，这些化合物对革兰氏阳性菌具有较强的抗菌活性，与红霉素相比，具有与革兰氏阴性细菌相当的抗菌活性水平，因此可用于临床使用。这些化合物也可用于饲料添加剂和生长兴奋剂。

10. 发明授权

US5281580A Calcitonin-containing emulsion for nasal administration 失效
标题翻译：含降钙素的鼻腔给药乳液
公开(公告)号：US5281580A
公开(公告)日：1994-01-25
申请号：US734637
申请日：1991-07-23
申请人： Nakayuki Yamamoto , Michihiko Sugimoto , Hideo Sakakibara , Masaru Saita , Yuji Shimozono , Takafumi Manako
发明人： Nakayuki Yamamoto , Michihiko Sugimoto , Hideo Sakakibara , Masaru Saita , Yuji Shimozono , Takafumi Manako
IPC分类号： A61K9/00 , A61K9/107 , A61K38/23 , A61K47/22 , A61K47/26 , A61P3/00 , A61K33/24 , A61K9/06 , A61K37/30 , C07K7/36
CPC分类号： A61K38/23 , A61K47/22 , A61K9/0043 , A61K9/1075 , Y10S514/808
摘要： The present invention is to provide emulsion preparations for nasal administration containing calcitonins, which are safely and effectively administrated compared with the conventional calcitonin preparations. The emulsions are prepared by using a calcitonin as the active ingredient, an azacycloalkane derivative as the absorption promotor such as 1-[2-(decylthio)ethyl] azacyclopentan-2-one, and glycyrrhizic acid or its salt.
摘要翻译：本发明提供了含有降钙素的鼻内给药用乳剂，与常规降钙素制剂相比，其安全有效地施用。通过使用降钙素作为活性成分，作为吸收促进剂的氮杂环烷烃衍生物如1-（2-（癸硫基）乙基）氮杂环戊烷-2-酮和甘草酸或其盐制备乳液。

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