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1. 发明授权

US06310056B1 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06310056B1
公开(公告)日：2001-10-30
申请号：US09355272
申请日：1999-07-28
申请人： Yuko Kano , Kazuhiro Aihara , Yumiko Toyooka , Toshiro Sasaki , Hiromasa Takizawa , Kenichi Fushihara , Kazuko Kobayashi , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Kazuhiro Aihara , Yumiko Toyooka , Toshiro Sasaki , Hiromasa Takizawa , Kenichi Fushihara , Kazuko Kobayashi , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： A61K31429
CPC分类号： C07D519/00
摘要： The carbapenem derivatives represented by the following formula (I) is disclosed. These compounds have strong anti-bacterial activities against bacteria including methicillin resistant Staphylococcus aureus, penicillin resistant Streptococcus pneumoniae, Enterococci, influenza, and &bgr;-lactamase producing bacteria, and have high stabilities to DHP-1 wherein R1 represents hydrogen or methyl, either one of R2, R3, R4, or R5 represents the bond to the 2-position on the carbapenem ring, and the remaining three respectively represent hydrogen, halogen, nitro, cyano, alkyl, cycloalkyl, alkylthio, alkenyl, formyl, alkylcarbonyl, alkoxycarbonyl, aminosulfonyl, aryl carbonyl, aryl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, lower alkoxyiminomethyl, or hydroxyiminomethyl, R6 is not present or represents alkyl, cycloalkyl, or alkenyl, and R is not present, or represents hydrogen or a group which may be metabolically hydrolyzed in the body, provided that when R6 is not present, R represents hydrogen or a group which may be metabolically hydrolyzed in the body, and when R6 is present, R is not present, and the compound forms an inner salt.
摘要翻译：公开了由下式（I）表示的碳青霉烯衍生物。这些化合物对包括耐甲氧西林金黄色葡萄球菌，青霉素耐药性肺炎链球菌，肠球菌，流感和β-内酰胺酶生产细菌在内的细菌具有很强的抗细菌活性，并且对于DHP-1具有高稳定性，其中R 1表示氢或甲基，R 2 ，R 3，R 4或R 5表示碳青霉烯环上2-位的键，其余3个分别表示氢，卤素，硝基，氰基，烷基，环烷基，烷硫基，烯基，甲酰基，烷基羰基，烷氧基羰基，氨基磺酰基，芳基羰基，芳基，氨基甲酰基，N-低级烷基氨基甲酰基，N，N-二低级烷基氨基羰基，低级烷氧基亚氨基甲基或羟基亚氨基甲基，R6不存在或表示烷基，环烷基或烯基，R不存在，或表示氢或可以在体内代谢水解的基团，条件是当R 6不存在时，R代表氢或可以代谢地水解的基团 e体，当R 6存在时，R不存在，且该化合物形成内盐。

2. 发明授权

US06180622B2 Imidazo[5,1-b]thiazol-3-yl carbapenem antimicrobials 失效
标题翻译：咪唑并[5,1-b]噻唑-3-基碳青霉烯类抗生素
公开(公告)号：US06180622B2
公开(公告)日：2001-01-30
申请号：US09117167
申请日：1998-07-23
申请人： Kazuhiro Aihara , Toshiro Sasaki , Yumiko Toyooka , Yuko Kano , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Kazuhiro Aihara , Toshiro Sasaki , Yumiko Toyooka , Yuko Kano , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： C07D51906
CPC分类号： C07D477/20
摘要： Compounds of formula (I) and compounds of formula (II) which have potent antimicrobial activity against a wide range of bacteria including Gram-positive bacteria and Gram-negative bacteria as well as heve potent antimicrobial activity against various &bgr;-lactamase-producing bacteria, MRSA, and resistant Pseudomonas aeruginosa and are very stable against DHP-1.
摘要翻译：对广泛的细菌（包括革兰氏阳性菌和革兰氏阴性细菌）具有强力的抗微生物活性的式（I）化合物和式（II）化合物）以及对各种β-内酰胺酶生产细菌具有强效的抗微生物活性， MRSA和耐药铜绿假单胞菌，对DHP-1非常稳定。

3. 发明授权

US5990101A Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US5990101A
公开(公告)日：1999-11-23
申请号：US737232
申请日：1997-03-12
申请人： Kazuhiro Aihara , Yuko Kano , Sohjiro Shiokawa , Toshiro Sasaki , Fumihito Setsu , Yumiko Toyooka , Miyuki Ishii , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura
发明人： Kazuhiro Aihara , Yuko Kano , Sohjiro Shiokawa , Toshiro Sasaki , Fumihito Setsu , Yumiko Toyooka , Miyuki Ishii , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura
IPC分类号： C07D477/14 , C07D519/00 , C07D519/06 , A61K31/425 , A61K31/495
CPC分类号： C07D477/14
摘要： Novel carbapenem derivatives, represented by the following formula (I), having a substituted or unsubstituted imidazo[5,1-b]thiazolium-6-ylmethyl group at the 2-position are disclosed. The compounds represented by the formula (I) have potent antibacterial activity against a wide spectrum of bacteria from Gram-positive bacteria to Gram-negative bacteria including Pseudomonas aeruginosa and, in addition, have potent antibacterial activity against various .beta.-lactamase-producing bacteria and MRSA and are very stable against DHP-1. ##STR1##
摘要翻译： PCT No.PCT / JP96 / 00573 Sec。 371日期1997年3月12日 102（e）1997年3月12日PCT PCT 1996年3月8日PCT公布。出版物WO96 / 28455 日期：1996年9月19日公开了在2-位具有取代或未取代的咪唑并[5,1-b]噻唑鎓-6-基甲基的新型碳青霉烯衍生物，由下式（I）表示。由式（I）表示的化合物对革兰氏阳性菌对革兰氏阴性细菌（包括铜绿假单胞菌）的广谱细菌具有强力的抗菌活性，另外对各种β-内酰胺酶产生细菌具有强力的抗菌活性， MRSA对DHP-1非常稳定。

4. 发明授权

US06825187B2 Carbapenem derivatives of quarternary salt type 失效
标题翻译：八氯化碳衍生物的季盐型
公开(公告)号：US06825187B2
公开(公告)日：2004-11-30
申请号：US10182180
申请日：2002-07-25
申请人： Yuko Kano , Takahisa Maruyama , Yasuo Yamamoto , Eiki Shitara , Toshiro Sasaki , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Takahisa Maruyama , Yasuo Yamamoto , Eiki Shitara , Toshiro Sasaki , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： C07D51906
CPC分类号： C07D477/14
摘要： An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl; R2 and R3 each independently represent H, halogen, lower alkyl or the like; R4 represents optionally substituted lower alkylthio or the like; and R5 represents optionally substituted lower alkyl or the like.
摘要翻译：本发明的目的是提供对MRSA，PRSP，流感病毒和产生β-内酰胺酶的细菌具有有效抗生素活性的碳青霉烯衍生物，并且对DHP-1是稳定的。根据本发明的化合物是由式（I）表示的化合物或其药学上可接受的盐：其中R 1表示H或甲基; R 2和R 3各自独立地表示H，卤素，低级烷基等; R 4表示任选取代的低级烷硫基等; R 5表示任选取代的低级烷基等。

5. 发明授权

US06677331B2 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06677331B2
公开(公告)日：2004-01-13
申请号：US10217670
申请日：2002-08-14
申请人： Yuko Kano , Toshiro Sasaki , Yumiko Sambongi , Kiyoshi Tanabe , Yoshihisa Akiyama , Hideo Kitagawa , Takahisa Maruyama , Hiromasa Takizawa , Takashi Ando , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Toshiro Sasaki , Yumiko Sambongi , Kiyoshi Tanabe , Yoshihisa Akiyama , Hideo Kitagawa , Takahisa Maruyama , Hiromasa Takizawa , Takashi Ando , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： C07D51906
CPC分类号： C07D477/14
摘要： Disclosed is a novel carbapenem derivative having a substituted imidazo[5,1-b]thiazole group at the 2-position on the carbapenem ring have high anti microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant-Pseudomonas aeruginosa, PRSP, enterococci, and influenza, and high stabilities to DHP-1. According to the present invention, there is provided a compound represented by the formula (I), or a pharmacologically acceptable salt thereof or an ester at the 3-position on the carbapenem ring thereof:
摘要翻译：公开了一种在碳青霉烯环上位置具有取代的咪唑并[5,1-b]噻唑基的新型碳青霉烯衍生物对β-内酰胺酶生产细菌，MRSA，耐药铜绿假单胞菌，PRSP，肠球菌具有高抗微生物活性，流感，以及DHP-1的高稳定性。根据本发明，提供由式（I）表示的化合物或其药理学上可接受的盐或其碳青霉烯环的3-位上的酯：

6. 发明授权

US06458780B1 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06458780B1
公开(公告)日：2002-10-01
申请号：US09744583
申请日：2001-01-26
申请人： Yuko Kano , Toshiro Sasaki , Yumiko Sambongi , Kiyoshi Tanabe , Yoshihisa Akiyama , Hideo Kitagawa , Takahisa Maruyama , Hiromasa Takizawa , Takashi Ando , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Toshiro Sasaki , Yumiko Sambongi , Kiyoshi Tanabe , Yoshihisa Akiyama , Hideo Kitagawa , Takahisa Maruyama , Hiromasa Takizawa , Takashi Ando , Kazuhiro Aihara , Kunio Atsumi , Katsuyoshi Iwamatsu , Takashi Ida
IPC分类号： A61L31429
CPC分类号： C07D477/14
摘要： Disclosed is a novel carbapenem derivative having a substituted imidazo[5,1-b]thiazole group at the 2-position on the carbapenem ring have high anti-microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant-Pseudomonas aeruginosa, PRSP, enterococci, and influenza, and high stabilities to DHP-1. According to the present invention, there is provided a compound represented by the formula (I), or a pharmacologically acceptable salt thereof or an ester at the 3-position on the carbapenem ring thereof:
摘要翻译：公开了一种在碳青霉烯环上2-位具有取代的咪唑并[5,1-b]噻唑基的新型碳青霉烯衍生物对β-内酰胺酶生产细菌，MRSA，耐药铜绿假单胞菌，PRSP，肠球菌和流感，以及DHP-1的高度稳定性。根据本发明，提供由式（I）表示的化合物或其药理学上可接受的盐或其碳青霉烯环的3-位上的酯：

7. 发明授权

US06908913B2 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06908913B2
公开(公告)日：2005-06-21
申请号：US10344729
申请日：2001-11-22
申请人： Yuko Kano , Yasuo Yamamoto , Takahisa Maruyama , Takehiko Sawabe , Eiki Shitara , Kazuhiro Aihara , Kunio Atsumi , Takashi Ida
发明人： Yuko Kano , Yasuo Yamamoto , Takahisa Maruyama , Takehiko Sawabe , Eiki Shitara , Kazuhiro Aihara , Kunio Atsumi , Takashi Ida
IPC分类号： A61P31/04 , C07D477/14 , C07D519/00 , A61K31/429 , C07D519/06
CPC分类号： C07D477/14
摘要： An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and β-lactamase producing bacteria and are stable to DHP-1. The carbapenem derivatives according to the present invention are compounds represented by formulae (I) and (II) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl, R2 and R3 each independently represent H; halogen; substituted or unsubstituted alkyl; cycloalkyl; substituted or unsubstituted alkylcarbonyl; carbamoyl; substituted or unsubstituted aryl; substituted or unsubstituted alkylthio; morpholinyl; alkylsulfonyl; or formyl, n is 0 (zero) to 4, and Hy represents a substituted or unsubstituted monocyclic or bicyclic heterocyclic group.
摘要翻译：本发明的目的是提供对MRSA，PRSP，流感病毒和产生β-内酰胺酶的细菌具有强抗生素活性并且对DHP-1稳定的碳青霉烯衍生物。根据本发明的碳青霉烯衍生物是由式（I）和（II）表示的化合物或其药学上可接受的盐：其中R 1表示H或甲基，R 2，和R 3各自独立地表示H; 卤素; 取代或未取代的烷基; 环烷基取代或未取代的烷基羰基; 氨基甲酰基; 取代或未取代的芳基; 取代或未取代的烷硫基; 吗啉基烷基磺酰基; 或甲酰基，n为0（零）至4，Hy表示取代或未取代的单环或双环杂环基。

8. 发明授权

US06680313B2 Carbapenum derivatives 失效
标题翻译：卡巴宾衍生物
公开(公告)号：US06680313B2
公开(公告)日：2004-01-20
申请号：US10182179
申请日：2002-07-25
申请人： Yuko Kano , Takahisa Maruyama , Yumiko Sambongi , Kazuhiro Aihara , Kunio Atsumi , Kastuyoshi Iwamatsu , Takashi Ida
发明人： Yuko Kano , Takahisa Maruyama , Yumiko Sambongi , Kazuhiro Aihara , Kunio Atsumi , Kastuyoshi Iwamatsu , Takashi Ida
IPC分类号： C07D51906
CPC分类号： C07D477/14
摘要： An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl; R2 and R3 represent H, a halogen atom, alkyl or the like; and R4 represents substituted lower alkylthio or the like.
摘要翻译：本发明的目的是提供对MRSA，PRSP，流感病毒和产生β-内酰胺酶的细菌具有有效抗生素活性的碳青霉烯衍生物，并且对DHP-1是稳定的。根据本发明的化合物是由式（I）表示的化合物或其药学上可接受的盐：其中R 1表示H或甲基; R 2和R 3代表H，卤素原子，烷基等; R 4表示取代的低级烷硫基等。

9. 发明申请

US20070004700A1 2-Thioethenyl substituted carbapenem derivatives 失效
标题翻译： 2-噻吩基取代的碳青霉烯衍生物
公开(公告)号：US20070004700A1
公开(公告)日：2007-01-04
申请号：US11401892
申请日：2006-04-12
申请人： Takahisa Maruyama , Yuko Kano , Takashi Ando , Toshiro Sasaki , Takehiko Sawabe , Nobuyoshi Baba , Hiromi Takata , Hisashi Suzuki , Kazuhiro Aihara , Toshiki Fujita
发明人： Takahisa Maruyama , Yuko Kano , Takashi Ando , Toshiro Sasaki , Takehiko Sawabe , Nobuyoshi Baba , Hiromi Takata , Hisashi Suzuki , Kazuhiro Aihara , Toshiki Fujita
IPC分类号： A61K31/407 , C07D487/04
CPC分类号： C07D487/04
摘要： [Objective] An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis. [Structure] The present invention provides 2-ethenylthio-based carbapenem derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof that are effective, for example, against pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including beta-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis:
摘要翻译： [目的]本发明的目的是提供对于引起目前临床问题的各种抗性细菌有效的化合物，例如包括耐青霉素的肺炎链球菌（PRSP），流感嗜血杆菌，包括不产生氨苄青霉素的bata-内酰胺酶的肺炎球菌流感嗜血杆菌（BLNAR）和莫拉氏菌（布拉汉氏菌）卡他氏菌。 [结构]本发明提供了式（I）表示的2-乙烯基硫代碳青霉烯衍生物或其药学上可接受的盐，其可有效地例如针对包括耐青霉素的肺炎链球菌（PRSP）在内的肺炎球菌，包括β-内酰胺酶的流感嗜血杆菌 - 非生产氨苄青霉素耐药性流感嗜血杆菌（BLNAR）和莫拉氏菌（Branhamella）卡他性：

10. 发明授权

US08344154B2 2-thioethenyl substituted carbapenem derivatives 失效
标题翻译： 2-硫代乙烯基取代的碳青霉烯衍生物
公开(公告)号：US08344154B2
公开(公告)日：2013-01-01
申请号：US12656606
申请日：2010-02-04
申请人： Takahisa Maruyama , Yuko Kano , Takashi Ando , Toshiro Sasaki , Kazuhiro Aihara , Toshiki Fujita
发明人： Takahisa Maruyama , Yuko Kano , Takashi Ando , Toshiro Sasaki , Kazuhiro Aihara , Toshiki Fujita
IPC分类号： C07D277/24 , C07D277/26
CPC分类号： C07D487/04
摘要： 2-Ethenylthio-type carbapenem derivatives of formula (I) or pharmaceutically acceptable salts thereof are provided. The compounds according to the present invention have potent antimicrobial activity and a wide antimicrobial spectrum against pneumococci including penicillin resistant Streptococcus pneumoniae (PRSP), Haemophilus influenzae including β-lactamase-negative, ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.
摘要翻译：提供式（I）的2-乙烯基硫代碳代青霉烯衍生物或其药学上可接受的盐。根据本发明的化合物具有有效的抗微生物活性和抗肺炎球菌的广谱抗菌谱，包括耐青霉素肺炎链球菌（PRSP），流感嗜血杆菌，包括β-内酰胺酶阴性，氨苄青霉素抗性流感嗜血杆菌（BLNAR）和莫拉氏菌）卡他氏菌

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