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    Process and intermediates to a tetrahydro-[1,8]- Naphthyridine
    32.
    发明授权
    Process and intermediates to a tetrahydro-[1,8]- Naphthyridine 失效
    四氢 - [1,8] - 萘啶的方法和中间体

    公开(公告)号：US06423845B1

    公开(公告)日：2002-07-23

    申请号：US09718139

    申请日：2000-11-21

    申请人： Nelo R. Rivera ,  Yi Xiao ,  Nobuyoshi Yasuda

    发明人： Nelo R. Rivera ,  Yi Xiao ,  Nobuyoshi Yasuda

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  C07F9/4006

    摘要： A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

    摘要翻译： 提供了一种制备3-（5,6,7,8-四氢 - [1,8] - 萘啶-2-基） - 丙胺的新方法，其可用于合成αphav整联蛋白受体拮抗剂。 还提供了从该方法获得的有用的中间体。

    Process for synthesizing carbapenem intermediates
    33.
    发明授权
    Process for synthesizing carbapenem intermediates 失效
    合成碳青霉烯中间体的方法

    公开(公告)号：US5973142A

    公开(公告)日：1999-10-26

    申请号：US5158

    申请日：1998-01-09

    申请人： Nobuyoshi Yasuda ,  Chunhua Yang

    发明人： Nobuyoshi Yasuda ,  Chunhua Yang

    IPC分类号： C07F7/18 ,  C07D205/08 ,  C07F7/10 ,  C09B49/00

    CPC分类号： C07D205/08 ,  C07F7/186 ,  C07F7/1892 ,  Y02P20/55

    摘要： A process of synthesizing a compound of formula 1: ##STR1## wherein P and P' each independently represent H or a protecting group, R.sup.1 represents H or C.sub.1-4 alkyl, andHal represents a halogen selected from Cl, Br and I, comprising: reacting a compound of formula 2: ##STR2## wherein P, P' and R.sub.1 are as defined above with an N,O-di-C.sub.1-4 alkyl hydroxylamine in the presence of a carbodiimide to produce a compound of formula 3: ##STR3## reacting compound 3 with a compound of formula 4:MetCH.sub.2 SiR.sub.2 R.sub.3 R.sub.4 4wherein Met represents lithium or halomagnesium;R.sub.2, R.sub.3 and R.sub.4 are C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and the halo portion of halomagnesium is Cl, Br or I, to produce a compound of formula 5: ##STR4## and reacting compound 5 with a halogenating agent to produce a compound of formula 1.

    摘要翻译： 合成式1化合物的方法：其中P和P'各自独立地表示H或保护基，R 1表示H或C 1-4烷基，Hal表示选自Cl，Br和I的卤素，其包括：使 式2的化合物：其中P，P'和R 1如上所定义，与碳原子数为3的化合物反应形成式III化合物：使化合物3与化合物 式4：MetCH 2 SiR 2 R 3 R 44，其中Met表示锂或卤代镁; R2，R3和R4是C1-4烷基或C1-4烷氧基，卤代卤素的卤代部分是Cl，Br或I，以产生式5的化合物：使化合物5与卤化剂反应，生成化合物 公式1。

    Cephem compounds
    36.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号：US4420477A

    公开(公告)日：1983-12-13

    申请号：US209988

    申请日：1980-11-24

    申请人： Takao Takaya ,  Yoshikazu Inoue ,  Nobuyoshi Yasuda ,  Masayoshi Murata

    发明人： Takao Takaya ,  Yoshikazu Inoue ,  Nobuyoshi Yasuda ,  Masayoshi Murata

    IPC分类号： C07D501/18 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D209/48 ,  C07D257/04 ,  C07D277/20 ,  C07D295/13 ,  C07D295/205 ,  C07D501/36 ,  C07D501/57

    CPC分类号： C07D209/48 ,  C07D257/04 ,  C07D277/587 ,  C07D295/13 ,  C07D295/205 ,  Y02P20/55

    摘要： This invention relates to novel cephem compounds of high antimicrobial activity, said compounds being of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or a protected amino group; and R.sup.6 is lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cyclo(lower)alkenyl, aryl, ar(lower)alkyl, or halogen-substituted ar(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group;A is hydroxy(lower)alkylene, amino(lower)alkylene, protected amino(lower)alkylene, lower alkenylene, hydroxyimino(lower)alkylene, lower alkoxyimino(lower)alkylene, or lower alkenyloxyimino(lower)alkylene; andR.sup.3 is carboxy or a protected carboxy group, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及高抗微生物活性的新型头孢烯化合物，所述化合物具有下式：其中R 1是下式的基团：其中R 5是氨基或被保护的氨基; 低级烯基，低级炔基，环烷基，环（低级）烯基，芳基，芳（低级）烷基或卤素取代的芳（低级）烷基; R2是羧基或被保护的羧基; A是羟基（低级）亚烷基，氨基（低级）亚烷基，保护的氨基（低级）亚烷基，低级亚烯基，肟基（低级）亚烷基，低级烷氧基亚氨基（低级）亚烷基或低级烯氧基亚氨基（低级） 且R 3为羧基或被保护的羧基，及其药学上可接受的盐。

    Process for the synthesis of carbapenem intermediates, and compounds produced
    39.
    发明授权
    Process for the synthesis of carbapenem intermediates, and compounds produced 失效
    合成碳青霉烯中间体的方法和所生产的化合物

    公开(公告)号：US06489471B1

    公开(公告)日：2002-12-03

    申请号：US09719503

    申请日：2001-03-05

    申请人： Guy R. Humphrey ,  Ross A. Miller ,  Nobuyoshi Yasuda

    发明人： Guy R. Humphrey ,  Ross A. Miller ,  Nobuyoshi Yasuda

    IPC分类号： C07D47714

    CPC分类号： C07D477/14 ,  C07D477/02 ,  Y02P20/55

    摘要： A process of synthesizing a carbapenem compound of formula (6) is disclosed, wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R1 is independently selected from: H, halo, OH, OP wherein P is a protecting group, C1-6 alkyl or C1-6 alkyl substituted with 1-3 of halo, OH, OP, NH2, NHC1-4 alkyl or N(C1-4 alkyl)2, comprising reacting a carbapenem of formula (4′) with a compound of formula (7), wherein R, R1, P and P* are as previously defined and R2 represents acetate, C(O)OR′ or P(O)(OR″)2, wherein R′ and R″ independently represent Clot alkyl, benzyl or aryl, in the presence of a catalyst to produce a compound of formula (6).

    摘要翻译： 公开了合成式（6）的碳青霉烯化合物的方法，其中R表示H或甲基，P和P *独立地表示H或保护基，并且每个R 1独立地选自：H，卤素，OH，OP，其中P为 保护基，C 1-6烷基或被1-3个卤素，OH，OP，NH 2，NHC 1-4烷基或N（C 1-4烷基）2取代的C 1-6烷基，包括使式（4'）的碳青霉烯 ）与式（7）化合物反应，其中R，R 1，P和P *如前所定义，R 2表示乙酸酯，C（O）OR'或P（O）（OR“）2，其中R'和 在催化剂存在下，R“独立地表示稠合烷基，苄基或芳基，以制备式（6）化合物。

    Probe for optical measurement
    40.
    发明授权
    Probe for optical measurement 失效
    光学测量探头

    公开(公告)号：US06449500B1

    公开(公告)日：2002-09-10

    申请号：US09620573

    申请日：2000-07-20

    申请人： Kuniharu Asai ,  Naoki Yanai ,  Motonobu Shiomi ,  Nobuyoshi Yasuda

    发明人： Kuniharu Asai ,  Naoki Yanai ,  Motonobu Shiomi ,  Nobuyoshi Yasuda

    IPC分类号： A61B500

    CPC分类号： A61B5/6843 ,  A61B5/0059 ,  A61B5/14532

    摘要： A second optical component is an optical fiber bundle charged in a clearance between an inner cylinder and an outer cylindrical outer peripheral part in the form of a ring. These elements are integrated with each other, and forward-end-surfaces thereof are on concentric circles. A ring of the forward-end-surface of the outer peripheral part is larger in width than the ring of the forward-end-surface of the second optical component. A first optical component charged with an optical fiber bundle is slidably inserted into and engaged in the cylinder inside the second optical component, so that the forward-end-surface of the first optical component can project or retract from the forward-end-surface of the outer peripheral part. The outer peripheral part is brought into contact with a human body and force for pressing a measured region is changed by sliding the first optical component for measuring absorption spectra between the first and second optical components under different values of pressing force, thereby obtaining a difference absorbance spectrum under different states of pressurization.

    摘要翻译： 第二光学部件是以环形的内筒和外筒部外周部之间的间隙充填的光纤束。 这些元件彼此集成，其前端表面在同心圆上。 外周部的前端面的环的宽度比第二光学部件的前端面的环宽。 装有光纤束的第一光学部件可滑动地插入第二光学部件内并与其接合，从而第一光学部件的前端表面可以从第一光学部件的前端表面突出或缩回 外围部分。 使外周部与人体接触，通过在不同的按压力下滑动用于测量第一和第二光学部件之间的吸收光谱的第一光学部件来改变测量区域的按压力，从而获得差异吸光度 频谱在不同的加压状态。