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1. 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。

2. 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。

3. 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：

4. 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：

5. 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。

6. 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。

7. 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。

8. 发明授权

US06242437B1 Cephem derivatives 失效
标题翻译： Cephem衍生物
公开(公告)号：US06242437B1
公开(公告)日：2001-06-05
申请号：US09319437
申请日：1999-06-07
申请人： Kazuko Kobayashi , Eijirou Umemura , Kunio Atsumi , Takashi Ida
发明人： Kazuko Kobayashi , Eijirou Umemura , Kunio Atsumi , Takashi Ida
IPC分类号： A61K31546
CPC分类号： C07D519/00
摘要： A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative bacteria including &bgr;-lactamase producing bacteria. In particular, it has higher antimicrobial activity against methicilline-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and imipenem-resistant Pseudomonas aeruginosa than the existing onium salt type cephem derivatives and hence is very useful as a therapeutic agent for infectious diseases derived from various pathogenic bacteria. wherein X represents CH or N, R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or cycloalkyl; any one of R2, R3, R4, and R5 represents R6R7NSO2NH—C1-6 alkyl where R6 and R7, which may be the same or different, represent a hydrogen atom or C1-6 alkyl; and n is 0 or 1.
摘要翻译：公开了由下式（I）表示的化合物。该化合物对革兰氏阳性菌对包括β-内酰胺酶生产细菌在内的Grame-negative细菌的广谱细菌具有有效的抗菌活性。具体而言，与现有的鎓盐型头孢烯衍生物相比，耐甲氧西林金黄色葡萄球菌（MRSA），青霉素耐药性肺炎链球菌（PRSP）和亚胺培南耐药铜绿假单胞菌具有较高的抗菌活性，因此作为治疗剂非常有用用于衍生自各种病原菌的感染性疾病，其中X表示CH或N，R 1表示氢原子，取代或未取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或环烷基; R2，R3，R4和R5中的任一个表示R6R7NSO2NH-C1-6烷基，其中R6和R7可以相同或不同，表示氢原子或C1-6烷基; n为0或1。

9. 发明申请

US20140256203A1 CORE-SHEATH COMPOSITE FIBER AND METHOD FOR PRODUCING SAME 有权
标题翻译：核心复合纤维及其制造方法
公开(公告)号：US20140256203A1
公开(公告)日：2014-09-11
申请号：US14348184
申请日：2012-08-27
申请人： Junichi Mizota , Takashi Ida , Hidetoshi Takanaga
发明人： Junichi Mizota , Takashi Ida , Hidetoshi Takanaga
IPC分类号： D01F8/14 , D01D5/10 , D01F8/12 , D01D5/34 , D03D15/00 , D04B1/16
CPC分类号： D01F8/14 , C08G63/6886 , D01D5/10 , D01D5/253 , D01D5/34 , D01F6/60 , D01F8/12 , D03D15/0027 , D04B1/16 , Y10T428/2929 , Y10T442/30 , Y10T442/3154 , Y10T442/40 , Y10T442/444
摘要： A core-sheath composite fiber includes a core component including an easily alkaline elutable polyester with a main repeating unit constructed of ethylene terephthalate containing 2.0 to 5.5 mol % of an isophthalic acid component containing a metal sulfonate group relative to a total acid component and 3.0 to 6.0 mol % of an adipic acid component relative to the total acid component, and a sheath component including a polyamide.
摘要翻译：芯鞘复合纤维包括芯组分，其包含易碱性可洗涤聚酯，其具有由对苯二甲酸乙二醇酯构成的主重复单元，所述对苯二甲酸乙二醇酯含有相对于总酸成分含有金属磺酸盐基的2.0〜5.5mol％的间苯二甲酸成分，3.0〜己二酸成分相对于总酸成分为6.0摩尔％，鞘成分为聚酰胺。

10. 发明申请

US20140221330A1 NDM INHIBITOR 有权
标题翻译： NDM抑制剂
公开(公告)号：US20140221330A1
公开(公告)日：2014-08-07
申请号：US14234456
申请日：2012-07-26
申请人： Akihiro Morinaka , Kazunori Maebashi , Takashi Ida , Muneo Hikida , Mototsugu Yamada , Takao Abe
发明人： Akihiro Morinaka , Kazunori Maebashi , Takashi Ida , Muneo Hikida , Mototsugu Yamada , Takao Abe
IPC分类号： C07C69/593 , A61K45/06 , C07C69/612 , A61K31/216 , C07C69/618 , C07C69/732 , C07D309/06 , A61K31/351 , C07C69/608 , C07D213/55 , A61K31/4406 , C07D295/108 , A61K31/5375 , C07D211/46 , A61K31/45 , C07D233/64 , A61K31/4174 , C07D207/12 , A61K31/4015 , A61K31/225
CPC分类号： C07C69/593 , A61K31/194 , A61K31/216 , A61K31/225 , A61K31/351 , A61K31/40 , A61K31/4015 , A61K31/407 , A61K31/4164 , A61K31/4174 , A61K31/4406 , A61K31/45 , A61K31/5375 , A61K45/06 , C07C57/13 , C07C57/26 , C07C57/30 , C07C57/42 , C07C57/48 , C07C57/50 , C07C59/46 , C07C59/64 , C07C63/66 , C07C69/608 , C07C69/612 , C07C69/618 , C07C69/732 , C07C217/18 , C07C233/65 , C07C235/20 , C07C237/22 , C07C279/08 , C07D207/12 , C07D211/46 , C07D213/55 , C07D233/64 , C07D295/108 , C07D309/06 , Y02A50/473 , A61K2300/00
摘要： An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):
摘要翻译：本发明的目的是提供一种新型的NDM（新德里金属 - β-内酰胺酶）抑制剂，其作为恢复由NDM分解而灭活的β-内酰胺抗生素的抗菌活性的药物。根据本发明，提供了含有通式（I）表示的化合物的NDM抑制剂：

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