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    Novel carbapenem compounds
    1.
    发明申请
    Novel carbapenem compounds 失效
    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]。

    Carbapenem compounds
    2.
    发明授权
    Carbapenem compounds 失效
    碳青霉烯化合物

    公开(公告)号：US07468364B2

    公开(公告)日：2008-12-23

    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： C07D477/14 ,  A61K31/407 ,  A61P31/04 ,  A61K31/4178 ,  A61K31/5377 ,  A61K31/4439 ,  C07F7/18

    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R1为C1-C3烷基或羟基化C1-C3烷基，R为氢原子或在体内水解成羧基的基团，G为 由[G1]，[G2]和[G3]之一表示的基团。

    Carbapenem compounds
    3.
    发明授权
    Carbapenem compounds 失效
    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。

    Novel carbapenem compounds
    4.
    发明申请
    Novel carbapenem compounds 失效
    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。

    Novel carbapenem compound
    5.
    发明申请
    Novel carbapenem compound 审中-公开
    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。

    Carbapenem compounds
    6.
    发明授权
    Carbapenem compounds 失效
    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：

    3(1-hydoxyethyl)azetidinone compounds and their production
    9.
    发明授权
    3(1-hydoxyethyl)azetidinone compounds and their production 失效
    3（1-羟乙基）氮杂环丁酮化合物及其生产

    公开(公告)号：US5134231A

    公开(公告)日：1992-07-28

    申请号：US642531

    申请日：1991-01-17

    申请人： Makoto Sunagawa ,  Yoshihito Nozaki ,  Akira Sasaki ,  Haruki Matsumura

    发明人： Makoto Sunagawa ,  Yoshihito Nozaki ,  Akira Sasaki ,  Haruki Matsumura

    IPC分类号： C07C67/00 ,  C07C229/22 ,  C07C229/24 ,  C07C239/00 ,  C07C271/22 ,  C07C313/00 ,  C07C319/20 ,  C07C323/57 ,  C07C323/58 ,  C07C323/63 ,  C07D205/08 ,  C07D307/52 ,  C07D309/30 ,  C07D405/06 ,  C07D477/00

    CPC分类号： C07D405/06 ,  C07D205/08 ,  C07D307/52 ,  C07D309/30 ,  Y02P20/55

    摘要： An amino acid compound of the formula: ##STR1## wherein R is a lower alkyl group, R.sub.1 is a hydrogen atom or a protecting group for carboxyl, R.sub.2 is a hydrogen atom, a protecting group for amino, an optionally substituted allyl group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group or an aryl group), a beta-hydroxyethyl group in which the hydroxyl group is optionally protected, a formylmethyl group in which the formyl group is optionally protected, a carboxymethyl group in which the carboxyl group is protected or a 2-furylmethyl group and X is an optionally protected carboxyl group, a hydroxymethyl group in which the hydroxyl group is optionally protected or a substituted mercaptomethyl group of the formula:--CH.sub.2 SR.sub.5(wherein R.sub.5 is an aryl group or an ar(lower)alkyl group), which is a useful intermediate in the synthesis of 1-alkylcarbapenem compounds.

    摘要翻译： 下式的氨基酸化合物：其中R是低级烷基，R 1是氢原子或羧基保护基，R 2是氢原子，氨基保护基，任意取代的烯丙基 下式的基团：其中R 3和R 4各自为氢原子，低级烷基或芳基，其中羟基被任意保护的β-羟乙基，甲酰基甲基，其中甲酰基 可任意保护的基团，羧基被保护的羧甲基或2-呋喃基甲基，X是任选保护的羧基，羟基被任选保护的羟甲基或下式的取代的巯基甲基： -CH2SR5（其中R5是芳基或芳（低级）烷基），它是合成1-烷基碳青霉烯化合物的有用中间体。

    Beta-lactams and their production
    10.
    发明授权
    Beta-lactams and their production 失效
    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。