专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5231179A Heterocyclic compounds and their production 失效
标题翻译：杂环化合物及其生产
公开(公告)号：US5231179A
公开(公告)日：1993-07-27
申请号：US684488
申请日：1991-04-12
申请人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
发明人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
IPC分类号： C07D205/08 , C07D233/32 , C07D263/26 , C07D263/52 , C07D263/58 , C07D403/06 , C07D413/06
CPC分类号： C07D263/52 , C07D205/08 , C07D233/32 , C07D263/26 , C07D263/58 , C07D403/06 , C07D413/06
摘要： A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R.sub.1 and R.sub.2 may be combined together to form a lower alkylene group and/or R.sub.3 and R.sub.4 are combined together to form a lower alkylene group, or R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be combined together to form an o-phenylene group, X is a halogen atom and Y is an oxygen atom or a nitrogen atom substituted with lower alkyl or aryl, which is useful as an intermediate in the synthesis of 1.beta.-methylcarbapenem compounds valuable as antibiotics.
摘要翻译：下式的化合物：其中R 1，R 2，R 3和R 4各自为氢原子，低级烷基，芳（低级）烷基或芳基，或者R 1和R 2可以组合一起形成低级亚烷基和/或R 3和R 4结合在一起形成低级亚烷基，或者，R 1，R 2，R 3和R 4可以组合在一起形成邻亚苯基，X是卤素原子，Y 是氧原子或被低级烷基或芳基取代的氮原子，其可用作合成作为抗生素有价值的1β-甲基碳青霉烯化合物的中间体。

2. 发明授权

US07115595B2 Carbapenem compounds 失效
标题翻译：碳青霉烯化合物
公开(公告)号：US07115595B2
公开(公告)日：2006-10-03
申请号：US10465918
申请日：2001-12-25
申请人： Makoto Sunagawa , Akira Sasaki
发明人： Makoto Sunagawa , Akira Sasaki
IPC分类号： C07D477/14 , A61K31/407 , A61K31/5377 , A61K31/496 , A61P31/04
CPC分类号： C07D477/14
摘要： Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: wherein Ring E is benzene ring or thiophene ring; R1 is optionally OH-substituted C1-3 alkyl; R2 and R3 represent each H, optionally substituted lower alkyl, etc.; R is H, or a group which is hydrolyzed in the living body to regenerate a carboxyl group, etc.; X is O or S; and Y represents H, lower alkyl, etc., or pharmaceutically acceptable salts thereof and medicaments containing said compound as the active ingredient. These compounds exhibit an excellent antibacterial activity over a broad range of Gram-positive and Gram-negative bacteria, in particular, penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae.
摘要翻译：具有直接连接到碳青霉烯核的3-位上的取代苯基或取代噻吩的碳青霉烯化合物如下式所示：其中环E是苯环或噻吩环; R 1是任选OH取代的C 1-3烷基; R 2和R 3代表每个H，任选取代的低级烷基等; R是H，或在活体中水解以再生羧基的基团等; X是O或S; 和Y表示H，低级烷基等，或其药学上可接受的盐和含有所述化合物作为活性成分的药物。这些化合物在广泛的革兰氏阳性和革兰氏阴性细菌，特别是青霉素耐药性肺炎链球菌（PRSP）中表现出优异的抗菌活性，其近年来以高频率分离，因此导致严重的临床问题和流感嗜血杆菌，由于青霉素结合蛋白（PBP）突变，如β-内酰胺酶非产生氨苄青霉素（BLNAR）流感嗜血杆菌（BLM），其在广泛范围内对现有的β-内酰胺抗生素具有抗药性。

3. 发明申请

US20050020566A1 Novel carbapenem compounds 失效
标题翻译：新型碳青霉烯类化合物
公开(公告)号：US20050020566A1
公开(公告)日：2005-01-27
申请号：US10494603
申请日：2002-11-01
申请人： Makoto Sunagawa , Akira Sasaki
发明人： Makoto Sunagawa , Akira Sasaki
IPC分类号： A61P31/04 , C07D477/14 , A61K31/407 , C07D487/04
CPC分类号： C07D477/14
摘要： A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.
摘要翻译：由下式表示的化合物或其药学上可接受的盐：本发明是一种碳青霉烯化合物，其在宽范围的革兰氏阴性和革兰氏阳性细菌，特别是耐青霉素的肺炎链球菌（PRSP）中具有强的抗菌活性，其已被分离由于青霉素结合蛋白（PBP）突变如β-内酰胺酶非对称性，近年来出现了严重的临床问题，并且在广泛范围内对现有β-内酰胺类抗生素具有抵抗力的流感嗜血杆菌，生产氨苄青霉素（BLNAR）流感嗜血杆菌，具有优异的口服吸收能力。

4. 发明授权

US5424422A Beta-lactams and their production 失效
标题翻译： β-内酰胺及其生产
公开(公告)号：US5424422A
公开(公告)日：1995-06-13
申请号：US197712
申请日：1994-02-17
申请人： Makoto Sunagawa , Akira Sasaki , Koshiro Goda
发明人： Makoto Sunagawa , Akira Sasaki , Koshiro Goda
IPC分类号： C07D205/08 , C07D477/04 , C07F7/18 , C07F9/572 , C07D487/04
CPC分类号： C07D205/08 , C07D477/04 , C07F7/186 , C07F9/5728 , Y02P20/55
摘要： A beta-lactam compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, the same or different, each a hydrogen atom or a lower alkyl group, R.sub.3.sup.o is a lower alkyl group having a beta-configuration, R.sub.4 is a carboxyl-protecting group, X is a hydrogen atom or a protected hydroxyl group and COZ is a protected thiolcarboxyl group, which is useful as a valuable intermediate in the stereospecific production of 1-alkylcarbapenem compounds.
摘要翻译：下式的β-内酰胺化合物：其中R 1和R 2各自为氢原子或低级烷基，R 30为具有β-构型的低级烷基，R 4为羧基保护基，X是氢原子或保护的羟基，COZ是被保护的硫醇羧基，其可用作1-烷基碳青霉烯化合物的立体特异性生产中的有价值的中间体。

5. 发明授权

US5112966A Beta-lactams 失效
标题翻译： BETA-LACTAMS
公开(公告)号：US5112966A
公开(公告)日：1992-05-12
申请号：US793290
申请日：1985-10-31
申请人： Makoto Sunagawa , Haruki Matsumura , Tsuneo Yano , Akira Sasaki , Shinzi Takata
发明人： Makoto Sunagawa , Haruki Matsumura , Tsuneo Yano , Akira Sasaki , Shinzi Takata
IPC分类号： C07D205/08 , C07D498/04
CPC分类号： C07D205/08 , Y02P20/55
摘要： A beta-lactam compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a 1-hydroxy(lower)alkyl group wherein the hydroxyl group is optionally protected, R.sub.2 is a hydrogen atom or a protective group for the nitrogen atom and R.sub.3 is a methyl group, a halomethyl group, a hydroxymethyl group, a protected hydroxymethyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group or an ar(lower)alkoxycarbonyl group wherein the aryl group is optionally substituted, or R.sub.2 and R.sub.3 are combined together to form an oxaalkylene group and, when taken together with one nitrogen atom and two carbon atoms adjacent thereto, they represent a six-membered cyclic aminoacetal group, which is useful as a valuable intermediate in the stereospecific production of 1-methylcarbapenem compounds.

6. 发明授权

US5075435A Beta-lactams and their production via stereospecific hydrogenation 失效
标题翻译： BETA-LACTAMS及其通过立体加氢的生产
公开(公告)号：US5075435A
公开(公告)日：1991-12-24
申请号：US537149
申请日：1990-06-12
申请人： Makoto Sunagawa , Haruki Matsumura , Tsuneo Yano , Akira Sasaki , Shinzi Takata
发明人： Makoto Sunagawa , Haruki Matsumura , Tsuneo Yano , Akira Sasaki , Shinzi Takata
IPC分类号： C07D205/08 , C07D498/04
CPC分类号： C07D205/08 , Y02P20/55
摘要： A beta-lactam compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a 1-hydroxy(lower)alkyl group wherein the hydroxyl group is optionally protected, R.sub.2 is a hydrogen atom or a protective group for the nitrogen atom and R.sub.3 is a methyl group, a halomethyl group, a hydroxymethyl group, a protected hydroxymethyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group or an ar(lower)alkoxycarbonyl group wherein the aryl group is optionally substituted, or R.sub.2 and R.sub.3 are combined together to form an oxaalkylene group and, when taken together with one nitrogen atom and two carbon atoms adjacent thereto, they represent a six-membered cyclic aminoacetal group, which is useful as a valuable intermediate in the stereospecific production of 1-methylcarbapenem compounds.
摘要翻译：一种下式的β-内酰胺化合物：其中R1是氢原子，低级烷基或1-羟基（低级）烷基，其中羟基被任意保护，R2是氢原子或保护基对于氮原子，R 3是甲基，卤代甲基，羟甲基，被保护的羟甲基，甲酰基，羧基，低级烷氧基羰基或芳（低级）烷氧基羰基，其中芳基是任选的或R 2和R 3结合形成氧杂亚烷基，当与一个氮原子和与其相邻的两个碳原子一起时，它们代表六元环氨基缩醛基团，其可用作立体特异性的有价值的中间体生产1-甲基碳青霉烯化合物。

7. 发明申请

US20090029964A1 Novel carbapenem compound 审中-公开
标题翻译：新型碳青霉烯类化合物
公开(公告)号：US20090029964A1
公开(公告)日：2009-01-29
申请号：US11886949
申请日：2006-03-23
申请人： Makoto Sunagawa , Akira Sasaki , Takashi Tsukimura
发明人： Makoto Sunagawa , Akira Sasaki , Takashi Tsukimura
IPC分类号： A61K31/407 , C07D477/00 , A61P31/04
CPC分类号： C07D477/14
摘要： An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R0 represents hydrogen atom or the like; R1 represents C1-C3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH2(CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH2—, —NRaCH2— (wherein Ra represents hydrogen atom, optionally substituted C1-C4 alkyl group or the like) or the like.
摘要翻译：作为活性成分含有下述通式[1]所示的碳青霉烯化合物的口服给药抗菌剂，其中，R 0表示氢原子等; R1表示被羟基取代的C1-C3烷基等; R表示氢原子或通过在活体中水解而再生羧基的基团; L表示单键，亚甲基，-OCH 2（CO） - 等; 并且Het表示由下式[2]表示的基团，其中m和n独立地表示0或1; A和B独立地表示亚甲基，羰基等; Y表示亚甲基，亚乙基，氧原子，-OCH 2 - ， - NR a CH 2 - （其中R a表示氢原子，任选取代的C 1 -C 4烷基等）等。

8. 发明授权

US07205291B2 Carbapenem compounds 失效
标题翻译：碳青霉烯化合物
公开(公告)号：US07205291B2
公开(公告)日：2007-04-17
申请号：US10494603
申请日：2002-11-01
申请人： Makoto Sunagawa , Akira Sasaki
发明人： Makoto Sunagawa , Akira Sasaki
IPC分类号： A61K31/397 , C07D487/06
CPC分类号： C07D477/14
摘要： A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.
摘要翻译：由下式表示的化合物或其药学上可接受的盐：

9. 发明申请

US20060183730A1 Novel carbapenem compounds 失效
标题翻译：新型碳青霉烯类化合物
公开(公告)号：US20060183730A1
公开(公告)日：2006-08-17
申请号：US10550395
申请日：2004-04-06
申请人： Makoto Sunagawa , Akira Sasaki , Seiji Hori
发明人： Makoto Sunagawa , Akira Sasaki , Seiji Hori
IPC分类号： C07D487/08 , A61K31/397 , A61K31/407
CPC分类号： C07D487/04
摘要： Carbapenem compounds represented by the general formula [1] or pharmaceutically acceptable salts thereof: wherein R1 is C1-C3 alkyl or hydroxylated C1-C3 alkyl, R is hydrogen atom or a group which is hydrolyzed in vivo into a carboxy group, and G is a group represented by one of the formulae [G1], [G2], and [G3].
摘要翻译：由通式[1]表示的碳青霉烯化合物或其药学上可接受的盐：其中R 1是C 1 -C 3烷基或羟基化C C 1 -C 3烷基，R 2为氢原子或在体内水解成羧基的基团，G为式[G1 ]，[G2]和[G3]。

10. 发明授权

US5227376A .beta.-lactam compounds and their production 失效
标题翻译：（BETA）-LACTAM化合物及其生产
公开(公告)号：US5227376A
公开(公告)日：1993-07-13
申请号：US928170
申请日：1992-08-14
申请人： Makoto Sunagawa , Akira Sasaki , Hiroshi Yamaga , Masatomo Fukasawa , Hiroshi Nouda
发明人： Makoto Sunagawa , Akira Sasaki , Hiroshi Yamaga , Masatomo Fukasawa , Hiroshi Nouda
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , B65H2301/5142
摘要： A compound of the formula: ##STR1## , which is useful as an antimicrobial agent.
摘要翻译：下式的化合物：，其可用作抗微生物剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式