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1. 发明授权

US5064953A Intermediates cephalosporin derivatives 失效
标题翻译：中间体CEPHALOSPORIN衍生物
公开(公告)号：US5064953A
公开(公告)日：1991-11-12
申请号：US412992
申请日：1989-09-26
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D239/40 , C07D239/46 , C07D277/20 , C07D417/12 , C07D487/04 , C07D501/36 , C07D513/04
CPC分类号： C07D239/47 , C07D239/40 , C07D277/587 , C07D417/12 , C07D487/04 , C07D513/04
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
摘要翻译：本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物合成中的中间体化合物及其制备方法。根据本发明的新型头孢菌素衍生物含有缩合杂环基团，特别是作为头孢烯骨架3位的取代基的三唑并嘧啶环或噻二唑嘧啶环，作为7-位上的取代基的羟基亚氨基，烷氧基亚氨基或酰氧基亚氨基部分，头脑骨架的位置。含有上述取代基的本发明化合物对革兰氏阴性细菌和包括耐甲氧西林金黄色葡萄球菌的革兰氏阳性细菌具有很强的抗菌活性。这些化合物对治疗感染性疾病非常有用。

2. 发明授权

US4888332A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4888332A
公开(公告)日：1989-12-19
申请号：US687455
申请日：1984-12-28
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D519/00 , A61K31/545 , A61K31/546 , A61P31/04 , C07D239/40 , C07D239/46 , C07D277/20 , C07D417/12 , C07D487/04 , C07D501/36 , C07D513/04 , C07D519/06
CPC分类号： C07D239/47 , C07D239/40 , C07D277/587 , C07D417/12 , C07D487/04 , C07D513/04 , Y02P20/55
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
摘要翻译：本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物合成中的中间体化合物及其制备方法。根据本发明的新型头孢菌素衍生物含有缩合杂环基团，特别是作为头孢烯骨架3位的取代基的三唑并嘧啶环或噻二唑嘧啶环，作为7-位上的取代基的羟基亚氨基，烷氧基亚氨基或酰氧基亚氨基部分，头脑骨架的位置。含有上述取代基的本发明化合物对革兰氏阴性细菌和包括耐甲氧西林金黄色葡萄球菌的革兰氏阳性细菌具有很强的抗菌活性。这些化合物对治疗感染性疾病非常有用。

3. 发明授权

US4440770A Diuretic, hypotensive and antiedemic quinoline oximes 失效
标题翻译：利尿，降血压和抗胆碱喹啉肟
公开(公告)号：US4440770A
公开(公告)日：1984-04-03
申请号：US281242
申请日：1981-07-07
申请人： Ei Mochida , Haruo Ohnishi , Kazuo Yamaguchi , Yasuo Suzuki , Hiroshi Kosuzume
发明人： Ei Mochida , Haruo Ohnishi , Kazuo Yamaguchi , Yasuo Suzuki , Hiroshi Kosuzume
IPC分类号： A61K31/47 , C07D215/42
CPC分类号： C07D215/42 , A61K31/47 , Y10S514/869 , Y10S514/87
摘要： A pharmaceutical composition having diuretic, hypotensive and antiedemic effects which contains a 6-halo-4-oximino-1,2,3,4-tetrahydroquinoline derivative or a salt thereof, and a method to use the above-described derivative or a salt thereof as a diuretic, hypotensive and antiedemic agent.
摘要翻译：含有6-卤代肟基-1,2,3,4-四氢喹啉衍生物或其盐的具有利尿，降血压和抗血症作用的药物组合物和使用上述衍生物或其盐的方法作为利尿剂，降血压药和止血剂。

4. 发明授权

US4840945A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4840945A
公开(公告)日：1989-06-20
申请号：US838309
申请日：1986-03-10
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D209/48 , C07D277/20 , C07D277/40 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59 , C07D519/00
CPC分类号： C07D209/48 , C07D277/587 , C07D501/36 , C07D501/46 , C07D519/00
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
摘要翻译：本发明涉及新型头孢菌素衍生物，其制备方法，用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物，以及头孢菌素衍生物的合成中的中间体化合物及其制备方法。本发明基于选择含有缩合杂环，特别是三唑并嘧啶环或噻二唑并嘧啶环作为头孢烯骨架3位上的取代基的基团，以及含有儿茶酚部分，特别是儿茶酚羧甲氧基亚氨基部分的基团或邻苯二酚羧基亚氨基部分作为头孢烯骨架的7-位上的取代基。含有上述取代基的本发明化合物对革兰氏阴性菌具有很强的抗菌活性，对抗耐甲氧西林金黄色葡萄球菌的革兰氏阳性菌具有很强的抗菌活性。这些化合物对治疗感染性疾病非常有用。

5. 发明授权

US4608253A Process for removing immune complex in blood by use of the immobilized pepsin 失效
标题翻译：通过使用固定的胃蛋白酶除去血液中的免疫复合物的方法
公开(公告)号：US4608253A
公开(公告)日：1986-08-26
申请号：US556709
申请日：1983-11-15
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
IPC分类号： A61K35/14 , B01J20/32 , C12N11/00 , C12N11/08 , C12N11/10 , C12N11/14 , A61K37/54
CPC分类号： C12N11/10 , A61K35/14 , B01J20/28033 , B01J20/28038 , B01J20/3092 , B01J20/3204 , B01J20/3212 , B01J20/3248 , B01J20/3274 , C12N11/00 , C12N11/08 , C12N11/14 , B01J2220/58 , B01J2220/64 , B01J2220/86
摘要： The present invention relates to immobilized pepsin for use in removing immune complex which comprises pepsin fixed on a suitable carrier, and to a process for removing immune complex which comprises bringing blood or plasma from a patient suffering from an immune complex disease, such as rheumatoid arthritis and systemic erythematosus, into contact with the immobilized pepsin.
摘要翻译： PCT No.PCT / JP82 / 00212 Sec。 371日期：1983年11月15日 102（e）日期1983年11月15日PCT提交日期为1982年5月31日PCT公布。公开号WO83 / 04180 日期为1983年12月8日。本发明涉及用于去除包含固定在合适载体上的胃蛋白酶的免疫复合物的固定化胃蛋白酶，以及用于除去免疫复合物的方法，其包括使患有免疫的患者的血液或血浆复杂疾病，例如类风湿性关节炎和全身性红斑狼疮，与固定的胃蛋白酶接触。

6. 发明授权

US4956474A Intermediates of cephalosporin compounds 失效
标题翻译：头孢菌素化合物的中间体
公开(公告)号：US4956474A
公开(公告)日：1990-09-11
申请号：US368846
申请日：1989-06-20
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D209/48 , C07D277/20 , C07D277/40 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59 , C07D519/00
CPC分类号： C07D209/48 , C07D277/587 , C07D501/36 , C07D501/46 , C07D519/00
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

7. 发明授权

US4904791A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4904791A
公开(公告)日：1990-02-27
申请号：US174518
申请日：1988-03-28
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D209/48 , C07D277/20 , C07D277/40 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59 , C07D519/00
CPC分类号： C07D209/48 , C07D277/587 , C07D501/36 , C07D501/46 , C07D519/00
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

8. 发明授权

US4476127A 7-Diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine and pharmaceutical composition containing same 失效
标题翻译： 7-二乙基氨基-5-甲基 - 噻唑并[5,4-d]嘧啶和含有它们的药物组合物
公开(公告)号：US4476127A
公开(公告)日：1984-10-09
申请号：US433206
申请日：1982-09-29
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D513/04 , A61K31/495 , C07D417/02
CPC分类号： C07D513/04
摘要： The compound related to this invention is 7-diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine.The compound related to this invention possesses vasodilating action, hypotensive action, inhibitory action on platelet aggregation, and lowering action on cholesterol levels in blood, and is useful as a therapeutic agent for cardiovascular diseases.
摘要翻译： PCT No.PCT / JP82 / 00046 Sec。 371日期：1982年9月29日 102（e）1982年9月29日PCT PCT 1982年9月19日PCT公布。出版物WO83 / 02945 1983年9月1日。与本发明有关的化合物是7-二乙基氨基-5-甲基 - 噻唑并[5,4-d]嘧啶。本发明涉及的化合物具有血管舒张作用，降血压作用，对血小板聚集的抑制作用，降低血液中胆固醇水平的作用，可用作心血管疾病的治疗剂。

9. 发明授权

US5001121A Cephalosporin compounds and pharmaceutical compositions thereof 失效
标题翻译：头孢菌素化合物及其药物组合物
公开(公告)号：US5001121A
公开(公告)日：1991-03-19
申请号：US368830
申请日：1989-06-20
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Masahiro Mizota , Yasuo Suzuki , Ei Mochida
IPC分类号： C07D209/48 , C07D277/20 , C07D277/40 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59 , C07D519/00
CPC分类号： C07D209/48 , C07D277/587 , C07D501/36 , C07D501/46 , C07D519/00
摘要： The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.

10. 发明授权

US4591504A Human leucocyte pepsin-like enzyme as a therapeutic agent for treating allergic disorders and immune complex diseases 失效
标题翻译：人类白细胞胃蛋白酶样酶作为治疗过敏性疾病和免疫复合物疾病的治疗剂
公开(公告)号：US4591504A
公开(公告)日：1986-05-27
申请号：US498506
申请日：1983-05-26
申请人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
发明人： Haruo Ohnishi , Hiroshi Kosuzume , Yasuo Suzuki , Ei Mochida
IPC分类号： A61K20060101 , A61K9/127 , A61K38/00 , C12N20060101 , C12N9/64 , C12N15/00 , C12P20060101 , A61K37/48 , C12N9/48
CPC分类号： C12N9/6481 , A61K9/127 , C12N15/00 , A61K38/00
摘要： This invention provides a human leucocyte pepsin-like enzyme and a therapeutic agent and method for treating allergic disorders, immune complex diseases and tumors, the agent containing the enzyme as an effective ingredient. The human leucocyte pepsin-like enzyme of this invention is a protein of human origin and, therefore, a therapeutic agent containing said enzyme as an effective ingredient shows extremely little adverse reactions such as anaphylaxis and thus is highly safe.
摘要翻译：本发明提供人类白细胞胃蛋白酶样酶，以及用于治疗过敏性疾病，免疫复合物疾病和肿瘤的治疗剂和方法，所述药物含有酶作为有效成分。本发明的人白细胞胃蛋白酶样酶是人源性蛋白质，因此含有所述酶作为有效成分的治疗剂显示极少的不良反应，如过敏反应，因此是高度安全的。

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