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31 条记录 (耗时 0.03 秒)

    Propiophenone derivative and a process for preparing the same
    3.
    发明授权
    Propiophenone derivative and a process for preparing the same 失效
    苯丙酮衍生物及其制备方法

    公开(公告)号：US5830873A

    公开(公告)日：1998-11-03

    申请号：US429567

    申请日：1995-04-27

    申请人： Kenji Tsujihara ,  Mitsuya Hongu ,  Nobuyuki Funami ,  Masanori Inamasu ,  Kenji Arakawa

    发明人： Kenji Tsujihara ,  Mitsuya Hongu ,  Nobuyuki Funami ,  Masanori Inamasu ,  Kenji Arakawa

    IPC分类号： C07H15/203 ,  C07H15/26 ,  A61K31/70 ,  C07K15/00

    CPC分类号： C07H15/203 ,  C07H15/26

    摘要： A propiophenone derivative of the formula �I!: ##STR1## wherein X is O, S or methylene, OY is a protected or unprotected OH, Z is .beta.-D-glucopyranosyl or 4-O-(.alpha.-D-glucopyranosyl)-.beta.-D-glucopyranosyl or wherein one or more hydroxy groups of these groups may optionally be acylated, and the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

    摘要翻译： 式[I]的苯丙酮衍生物：其中X为O，S或亚甲基，OY为被保护或未被保护的OH，Z为β-D-吡喃葡萄糖基或4-O-（α-D- 吡喃葡萄糖基）-β-D-吡喃葡萄糖基或其中这些基团的一个或多个羟基可以任选地被酰化，并且虚线表示双键的存在或不存在或其药学上可接受的盐。 所述化合物具有优异的降血糖活性，因此它们可用于预防或治疗糖尿病。

    Dihydrochalcone derivatives which are hypoglycemic agents
    4.
    发明授权
    Dihydrochalcone derivatives which are hypoglycemic agents 失效
    二氢查耳酮衍生物，它们是降糖药

    公开(公告)号：US5731292A

    公开(公告)日：1998-03-24

    申请号：US426002

    申请日：1995-04-20

    申请人： Kenji Tsujihara ,  Mitsuya Hongu ,  Nobuyuki Funami ,  Masanori Inamasu ,  Kenji Arakawa

    发明人： Kenji Tsujihara ,  Mitsuya Hongu ,  Nobuyuki Funami ,  Masanori Inamasu ,  Kenji Arakawa

    IPC分类号： A61K31/7056 ,  C07H15/203 ,  A61K31/70

    CPC分类号： A61K31/7034 ,  A61K31/7048 ,  A61K31/7056 ,  A61K31/706 ,  C07H15/203 ,  Y10S514/866

    摘要： A method for prophylaxis or treatment of diabetes, which comprises administering to a patient with diabetes an effective amount of a dihydrochalcone derivative of the formula �I!: ##STR1## wherein Ar is an aryl group, R.sup.1 is hydrogen atom or an acyl group, R.sup.2 is a hydrogen atom, an acyl group or .alpha.-D-glucopyranosyl group, or R.sup.1 and R.sup.2 may combine together to form a substituted methylene group, R.sup.3 and R.sup.4 are each a hydrogen atom or an acyl group, OR.sup.5 is a protected or unprotected hydroxy group or a lower alkoxy group, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 一种预防或治疗糖尿病的方法，其包括向糖尿病患者施用有效量的式[I]的二氢查耳酮衍生物：其中Ar是芳基，R 1是氢原子或 酰基，R2是氢原子，酰基或α-D-吡喃葡萄糖基，或者R1和R2可以结合在一起形成取代的亚甲基，R 3和R 4各自为氢原子或酰基，OR 5为 保护或未保护的羟基或低级烷氧基，或其药学上可接受的盐。

    Aromatic amino acid derivatives and medicinal compositions
    6.
    发明授权
    Aromatic amino acid derivatives and medicinal compositions 有权
    芳香族氨基酸衍生物和药物组合物

    公开(公告)号：US07345068B2

    公开(公告)日：2008-03-18

    申请号：US10503125

    申请日：2003-02-03

    申请人： Hitoshi Endou ,  Yoshikatsu Kanai ,  Kenji Tsujihara ,  Kunio Saito

    发明人： Hitoshi Endou ,  Yoshikatsu Kanai ,  Kenji Tsujihara ,  Kunio Saito

    IPC分类号： C07D235/14 ,  C07D263/57 ,  A61K31/54 ,  A61K31/4745

    CPC分类号： C07D207/325 ,  C07C229/36 ,  C07C233/47 ,  C07C233/69 ,  C07C255/54 ,  C07C271/10 ,  C07C2602/10 ,  C07D209/08 ,  C07D213/30 ,  C07D213/74 ,  C07D215/14 ,  C07D235/18 ,  C07D239/42 ,  C07D263/32 ,  C07D263/56 ,  C07D265/36 ,  C07D277/24 ,  C07D277/66 ,  C07D307/79 ,  C07D307/82 ,  C07D307/83 ,  C07D307/91 ,  C07D311/30 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/06 ,  Y02P20/55

    摘要： 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle around (1)} a hydrogen atom, {circle around (2)} an aroylamino group, {circle around (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle around (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle around (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle around (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; l is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5. This compound can inhibit a transporter (LAT1) of essential amino acid which is one of main nutrition for cancer cells and accordingly cause drain of the essential amino acid on the cancer cells and finally can prohibit the multiplication of cancer cells.

    摘要翻译： 1.由式（I）表示的芳族氨基酸衍生物或其药理学上可接受的盐：其中R 1是氢原子或氨基保护基，R 2 O >是卤素原子或烷基，芳烷基或芳基，R 3是（环绕（1个氢原子，{环周围（2个芳酰氨基，{环周（3个苯基） 取代为低级烷基，苯基，苯氧基等。（四个萘基或四氢萘基，任选被羟基，低级烷氧基或二（低级）烷基氨基取代，（环绕（5个含有N的不饱和单环杂环基） O和/或S被低级烷基，苯基，萘基或四氢喹啉基取代，{环绕（6个不饱和或部分饱和的含有N，O和/或S的稠合杂环基，任选被氧代，羧基，氨基，低级烷基， X是卤素原子，烷基或烷氧基; Y是氧原子或氮原子; l是0或1; m 是0，1或2; n是0-5的整数。 该化合物可以抑制作为癌细胞的主要营养素之一的必需氨基酸的转运体（LAT1），因此导致癌细胞上必需氨基酸的排出，最终能够抑制癌细胞的增殖。

    Hair-growth agent
    7.
    发明授权
    Hair-growth agent 失效
    头发生长剂

    公开(公告)号：US5741816A

    公开(公告)日：1998-04-21

    申请号：US466968

    申请日：1995-06-06

    申请人： Kenji Tsujihara ,  Kunio Saito ,  Satoshi Furuuchi

    发明人： Kenji Tsujihara ,  Kunio Saito ,  Satoshi Furuuchi

    IPC分类号： A61K8/44 ,  A61Q7/00 ,  C07C229/22 ,  A01N37/02 ,  A01N37/06

    CPC分类号： A61Q7/00 ,  A61K8/44 ,  C07C229/22 ,  Y10S514/88

    摘要： Disclosed is a hair-growing (restoration) agent which comprises a carnitine compound represented by the formula (I): ##STR1## wherein R.sup.1 to R.sup.3 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.4 represents an aliphatic acyl group having 3 to 31 carbon atoms which may be substituted; R.sup.5 represents an alkyl group having 3 to 31 carbon atoms which may be substituted, or an alkenyl group having 3 to 31 carbon atoms which may be substituted; and X.sup.- represents an anion of a pharmaceutically acceptable acid, as an active ingredient.

    摘要翻译： 公开了包含式（I）表示的肉碱化合物的生发（还原剂）：其中R 1至R 3各自表示具有1至6个碳原子的烷基; R4表示可以被取代的碳原子数3〜31的脂肪族酰基， R5表示可以被取代的碳原子数3〜31的烷基或可以被取代的碳原子数3〜31的烯基; X表示药学上可接受的酸的阴离子作为活性成分。

    Camptothecin derivatives
    9.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US06617456B1

    公开(公告)日：2003-09-09

    申请号：US09624012

    申请日：2000-07-21

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： C07D49800

    CPC分类号： C08B37/0018 ,  A61K47/61 ,  A61K47/65 ,  C08B37/0021

    摘要： A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

    摘要翻译： 包含式[I]化合物的喜树碱衍生物：其中R1，R2，R3，R4和R5是（A）相邻的两个基团结合形成亚烷基，或两者都是H，其余三个基团之一是-Xn -Alkm-R6，另外两个为H，烷基或卤素，或（B）相邻的两个基团结合形成亚烷基，所述亚烷基的一个碳原子被-Xn-Alkm-R6取代，并且 剩余的三个基团是H，烷基或卤素，并且（A）或（B）中的一个或两个亚烷基的-CH 2可以任选地被-O - ， - S-或-NH-替代，X是-O - 或-NH-，Alk为亚烷基或-OH，m和n均为0或1，或m为1，n为0，喜树碱化合物通过氨基酸或肽与具有羧基的多糖结合 ，或其药学上可接受的盐。 所述喜树碱衍生物显示出增强的抗肿瘤活性，但副作用很少，可用作药物。