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11 条记录 (耗时 0.05 秒)

    Selective etherification
    3.
    发明授权
    Selective etherification 失效
    选择性醚化

    公开(公告)号：US5008405A

    公开(公告)日：1991-04-16

    申请号：US467419

    申请日：1990-01-19

    申请人： Chitoshi Hatanaka ,  Satoru Oi

    发明人： Chitoshi Hatanaka ,  Satoru Oi

    IPC分类号： C07D307/62 ,  C07D407/04

    CPC分类号： C07D307/62

    摘要： There is disclosed an improved process for substitution of the hydroxy group at 2-position of an ascorbic acid derivative according to the following reaction scheme: ##STR1## wherein R.sup.0 is hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or a group of the formula ##STR2## (wherein X is two hydrogen atoms, or acetal or ketal residue); R.sup.1 is an alkyl or alkenyl group having up to 22 carbon atoms which may be substituted with phenyl or alkoxy having 1 to 22 carbon atoms; Y is halogen or optionally substituted sulfonyloxy; R is hydrogen, or primary, secondary or tertiary alkyl having 1 to 10 carbon atoms; and Z is an alkali metal or an alkali earth metal. There is also disclosed hydrolysis of the following scheme: ##STR3## wherein R.sup.1 is as defined above; and X is acetal or ketal residue.

    Fused heterocyclic compounds
    4.
    发明申请
    Fused heterocyclic compounds 失效
    稠合杂环化合物

    公开(公告)号：US20060135530A1

    公开(公告)日：2006-06-22

    申请号：US10523531

    申请日：2003-08-07

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    IPC分类号： A61K31/496 ,  C07D215/38 ,  A61K31/47 ,  C07D403/02

    CPC分类号： C07D401/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

    摘要： A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each is a bound, —O—, —S—, —SO—, —SO?2#191- or —NR3— (R3 is a hydrogen atom or an optionally substituted hydrocarbon group); and L is a divalent hydrocarbon group, or a salt thereof shows a superior peptidase-inhibitory activity and is useful as a prophylactic or therapeutic agent of diabetes and the like.

    摘要翻译： 由下式表示的化合物其中环A是任选取代的5至10元芳环; R 1和R 2相同或不同，各自为任选取代的烃基或任选取代的杂环基; X和Y相同或不同，并且各自为结合的-O - ， - S - ， - SO - ， - SO 2＃191-或-NR 3 - 3是氢原子或任选取代的烃基）; L是二价烃基，或其盐表现出优异的肽酶抑制活性，可用作糖尿病等的预防或治疗剂。

    Fused heterocyclic compounds
    5.
    发明授权
    Fused heterocyclic compounds 失效
    稠合杂环化合物

    公开(公告)号：US07034039B2

    公开(公告)日：2006-04-25

    申请号：US10470805

    申请日：2002-02-01

    申请人： Satoru Oi ,  Koji Ikedou ,  Koji Takeuchi ,  Masaki Ogino ,  Yoshihiro Banno ,  Hiroyuki Tawada ,  Taihei Yamane

    发明人： Satoru Oi ,  Koji Ikedou ,  Koji Takeuchi ,  Masaki Ogino ,  Yoshihiro Banno ,  Hiroyuki Tawada ,  Taihei Yamane

    IPC分类号： C07D217/02 ,  A61K31/47

    CPC分类号： C07D401/04 ,  C07D217/24 ,  C07D217/26 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  C07D495/04

    摘要： The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

    摘要翻译： 本发明提供下式的化合物：其中环A是任选取代的5至10元芳环; R 1和R 2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基; X是一个键等; 和L是二价烃基及其盐，除了3-（氨基甲基）-2,6,7-三甲基-4-苯基-1（2H） - 异喹啉酮，3-（氨基甲基）-2-甲基-4 - 苯基-1（2H） - 异喹啉酮，3-（氨基甲基）-6-氯-2-甲基-4-苯基-1（2H） - 异喹啉酮和3-（氨基甲基）-2-异丙基-4-苯基-1 （2H） - 异喹啉酮。 该化合物显示出优异的肽酶抑制活性，并且可用作预防或治疗糖尿病等的药剂。

    Lactol derivatives, their production and use
    7.
    发明授权
    Lactol derivatives, their production and use 失效
    乳糖衍生物，其生产和使用

    公开(公告)号：US5496834A

    公开(公告)日：1996-03-05

    申请号：US300738

    申请日：1994-09-02

    申请人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    发明人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/078 ,  A61K31/44 ,  A61K31/35 ,  A61K31/40

    CPC分类号： C07K5/06139 ,  C07K5/06043 ,  A61K38/00

    摘要： The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.

    摘要翻译： 本发明提供新的式（Ia）或（I）化合物：其中Q是一个或两个可被取代的氨基酸残基; R3是可被酯化的羧基或酰基; A是亚烷基; B是氢或可以被取代的烷基或酰基; 或其盐; （I）其中R 1和R 2可以相同或不同，各自为氢或可被取代的烃残基; R3，A和B具有与上述相同的定义; m和n各自为0或1; 条件是当m和n都等于0时，R 3是可被酯化的羧基或具有不少于7个碳原子的酰基; 或其盐。 化合物（Ia）或（I）表示组织蛋白酶L抑制和骨吸收抑制活性，可用作骨质疏松症的预防/治疗剂。

    Fused heterocyclic compounds as peptidase inhibitors
    8.
    发明授权
    Fused heterocyclic compounds as peptidase inhibitors 失效
    稠合杂环化合物作为肽酶抑制剂

    公开(公告)号：US07547710B2

    公开(公告)日：2009-06-16

    申请号：US10523531

    申请日：2003-08-07

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    IPC分类号： A61K31/47 ,  C07D215/12

    CPC分类号： C07D401/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

    摘要： A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each is a bound, —O—, —S—, —SO—, —SO?2#191- or —NR3— (R3 is a hydrogen atom or an optionally substituted hydrocarbon group); and L is a divalent hydrocarbon group, or a salt thereof shows a superior peptidase-inhibitory activity and is useful as a prophylactic or therapeutic agent of diabetes and the like.

    摘要翻译： 由下式表示的化合物其中环A是任选取代的5至10元芳环; R1和R2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基; X和Y相同或不同，各自为结合的-O - ， - S - ， - SO - ， - SO 2＃191-或-NR 3 - （R 3为氢原子或任选取代的烃基） ; L是二价烃基，或其盐表现出优异的肽酶抑制活性，可用作糖尿病等的预防或治疗剂。

    Pyridine compounds as inhibitors of dipeptidyl peptidase IV
    9.
    发明申请
    Pyridine compounds as inhibitors of dipeptidyl peptidase IV 审中-公开
    吡啶化合物作为二肽基肽酶IV的抑制剂

    公开(公告)号：US20070037807A1

    公开(公告)日：2007-02-15

    申请号：US10577561

    申请日：2004-10-29

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Nobuhiro Suzuki

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Nobuhiro Suzuki

    IPC分类号： A61K31/5377 ,  A61K31/4439 ,  A61K31/44 ,  C07D413/02

    CPC分类号： C07D213/80 ,  C04B35/632 ,  C07D213/12 ,  C07D213/55 ,  C07D213/56 ,  C07D213/59 ,  C07D213/71 ,  C07D213/75 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/58

    摘要： A compound represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted hydroxy group; R3 is an optionally substituted aromatic group; R4 is an optionally substituted amino group; L is a divalent chain hydrocarbon group; Q is a bond or a divalent chain hydrocarbon group; and X is a hydrogen atom, a cyano group, a nitro group, an acyl group, a substituted hydroxy group, an optionally substituted thiol group, an optionally substituted amino group or an optionally substituted cyclic group; provided that when X is an ethoxycarbonyl group, then Q is a divalent chain hydrocarbon group. The compound has a peptidase inhibitory action, is useful as an agent for the prophylaxis or treatment of diabetes and the like, and is superior in efficacy, duration of action, specificity, lower toxicity and the like.

    摘要翻译： 由下式表示的化合物其中R 1和R 2各自相同或不同，并且各自为任选取代的烃基或任选取代的羟基; R 3是任选取代的芳族基团; R 4是任选取代的氨基; L是二价链烃基; Q是键或二价链烃基; X为氢原子，氰基，硝基，酰基，取代羟基，任选取代的硫醇基，任选取代的氨基或任意取代的环状基团; 条件是当X是乙氧基羰基时，则Q是二价链烃基。 该化合物具有肽酶抑制作用，可用作预防或治疗糖尿病等的药剂，其功效，作用时间，特异性，低毒性等优异。