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    Esculetin derivatives and method for manufacture thereof, use thereof, and pharmaceutical composition
    2.
    发明授权
    Esculetin derivatives and method for manufacture thereof, use thereof, and pharmaceutical composition 失效
    Esculetin衍生物及其制备方法，其用途和药物组合物

    公开(公告)号：US5736522A

    公开(公告)日：1998-04-07

    申请号：US340421

    申请日：1994-11-15

    申请人： Koju Watanabe ,  Koichi Niimura ,  Junko Miyagawa

    发明人： Koju Watanabe ,  Koichi Niimura ,  Junko Miyagawa

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P29/00 ,  A61P43/00 ,  C07H17/075 ,  C07H1/00 ,  C07H15/00

    CPC分类号： C07H17/075 ,  Y02P20/55

    摘要： A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a monosaccharide residue, a protected monosaccharide residue, or a protecting group for hydroxyl group, but at least one of R.sup.1 and R.sup.2 is a monosaccharide residue or a protected monosaccharide residue, and R.sup.3 is a hydrogen atom, a hydroxyl group, an alkyl group, an aryl group, or an aralkyl group, with the proviso that (1) when R.sup.1 and R.sup.2 are glucose residues at the same time, R.sup.3 is not a hydrogen atom, (2) when R.sup.1 is a hydrogen atom, an acetyl group or a benzyl group and R.sup.2 is a glucose residue, an acetylated glucose residue, or acetalized glucose residue, R.sup.3 is not a hydrogen atom, or (3) when R.sup.1 is a glucose residue and R.sup.2 is a hydrogen atom, R.sup.3 is not a hydrogen atom or a salt thereof is disclosed.

    摘要翻译： 式（I）的化合物：其中R 1和R 2独立地为氢原子，单糖残基，被保护的单糖残基或羟基的保护基，但R 1和R 2中的至少一个为 且R2为单糖残基或被保护的单糖残基，R3为氢原子，羟基，烷基，芳基或芳烷基，条件是（1）R1和R2为葡萄糖残基时 同时，R3不是氢原子，（2）当R1是氢原子，乙酰基或苄基，R2是葡萄糖残基，乙酰化葡萄糖残基或缩醛化葡萄糖残基时，R3不是 氢原子，或（3）当R1是葡萄糖残基且R2是氢原子时，R3不是氢原子或其盐。

    Chondroprotective agents
    3.
    发明授权
    Chondroprotective agents 失效
    软骨保护剂

    公开(公告)号：US5650433A

    公开(公告)日：1997-07-22

    申请号：US519179

    申请日：1995-08-25

    申请人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    发明人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P29/00 ,  A61P43/00 ,  C07D311/30 ,  C07D311/32 ,  C07H17/07

    CPC分类号： A61K31/7048 ,  A61K31/35 ,  A61K31/352 ,  A61K31/70

    摘要： A chondroprotective agent comprising a flavonoid compound of the general formula (I): ##STR1## wherein R.sup.1 to R.sup.9 are, independently, a hydrogen atom, hydroxyl group, or methoxyl group and X is a single bond or a double bond, or a stereoisomer thereof, or a naturally occurring glycoside thereof is disclosed. The above compound strongly inhibits proteoglycan depletion from the chondrocyte matrix and exhibits a function to protect cartilage, and thus, is extremely effective for the treatment of arthropathy.

    摘要翻译： 一种软骨保护剂，其包含通式（I）的类黄酮化合物：其中R 1至R 9独立地为氢原子，羟基或甲氧基，X为单键或双键， 或其立体异构体，或其天然存在的糖苷。 上述化合物强烈地抑制软骨细胞基质中的蛋白多糖消耗，并表现出保护软骨的功能，因此对于治疗关节病是非常有效的。

    Esculetin derivatives and pharmaceutical composition
    4.
    发明授权
    Esculetin derivatives and pharmaceutical composition 失效
    新颖的七叶亭衍生物和药物组成

    公开(公告)号：US5455268A

    公开(公告)日：1995-10-03

    申请号：US204445

    申请日：1994-03-02

    申请人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    发明人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    IPC分类号： A61K31/37 ,  A61P43/00 ,  C07D311/16 ,  A61K31/35

    CPC分类号： A61K31/37 ,  C07D311/16 ,  Y10S514/825

    摘要： A pharmaceutical composition comprising a compound of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a saturated or unsaturated aliphatic acyl having 2 to 25 carbon atoms or benzoyl group and R.sup.3 is a hydrogen atom or alkyl group, and a pharmaceutically acceptable carrier is disclosed. Further, a novel compound of the general formula (I) wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, pivaloyl, capryloyl, lauroyl, palmitoyl, stearoyl, linoleoyl, docosahexaenoyl, or benzoyl group, and R.sup.3 is a hydrogen atom or methyl group, is also disclosed.

    摘要翻译： 一种药物组合物，其包含通式（I）的化合物：其中R 1和R 2独立地为氢原子，具有2至25个碳原子的饱和或不饱和脂族酰基或苯甲酰基，R 3为 公开了氢原子或烷基，以及药学上可接受的载体。 此外，通式（I）的新化合物，其中R 1和R 2独立地为氢原子，新戊酰基，辛酰基，月桂酰基，棕榈酰基，硬脂酰基，亚油酰基，二十二碳六烯酰基或苯甲酰基，R 3为氢原子或甲基 ，也被披露。

    Chondroprotective agents
    5.
    发明授权
    Chondroprotective agents 失效
    软骨保护剂

    公开(公告)号：US06583118B1

    公开(公告)日：2003-06-24

    申请号：US08805049

    申请日：1997-02-24

    申请人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    发明人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    IPC分类号： A61K3170

    CPC分类号： A61K31/7048 ,  A61K31/35 ,  A61K31/352 ,  A61K31/70

    摘要： A chondroprotective agent comprising a flavonoid compound of the general formula (I): wherein R1 to R9 are, independently, a hydrogen atom, hydroxyl group, or methoxyl group and X is a single bond or a double bond, or a stereoisomer thereof, or a naturally occurring glycoside thereof is disclosed. The above compound strongly inhibits proteoglycan depletion from the chondrocyte matrix and exhibits a function to protect cartilage, and thus, is extremely effective for the treatment of arthropathy.

    摘要翻译： 包含通式（I）的类黄酮化合物的软骨保护剂：其中R 1至R 9独立地为氢原子，羟基或甲氧基，X为单键或双键或其立体异构体，或 公开了其天然存在的糖苷。 上述化合物强烈地抑制软骨细胞基质中的蛋白多糖消耗，并表现出保护软骨的功能，因此对于治疗关节病是非常有效的。

    Chromone compounds, pharmaceutical compositions containing the same, and use of the same
    6.
    发明授权
    Chromone compounds, pharmaceutical compositions containing the same, and use of the same 失效
    色酮化合物，含有它们的药物组合物及其用途

    公开(公告)号：US5698575A

    公开(公告)日：1997-12-16

    申请号：US694934

    申请日：1996-08-09

    申请人： Koju Watanabe ,  Tsuyoshi Saito ,  Koichi Niimura

    发明人： Koju Watanabe ,  Tsuyoshi Saito ,  Koichi Niimura

    IPC分类号： C07D405/04 ,  C07D409/04 ,  C07D407/04

    CPC分类号： C07D405/04 ,  C07D409/04

    摘要： A chromone derivative of the formula (I): ##STR1## wherein R.sup.11 is a pyrazolyl, pyrrolyl, triazolyl, benzotriazolyl, benzimidazolyl, indazolyl, or indolyl group, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 is independently a hydrogen or halogen atom, or a hydroxy or alkoxy group, or an alkoxy group substituted with one or more alkoxy groups, and X is an oxygen or sulfur atom, or a salt thereof is disclosed. The chromone derivative inhibits the activity of matrix metalloproteinase.

    摘要翻译： 式（I）的色酮衍生物：其中R 11是吡唑基，吡咯基，三唑基，苯并三唑基，苯并咪唑基，吲唑基或吲哚基，其中R 11，R 3，R 4和R 5独立地是氢或卤素 或羟基或烷氧基，或被一个或多个烷氧基取代的烷氧基，X是氧或硫原子，或其盐。 色酮衍生物抑制基质金属蛋白酶的活性。

    Chondroprotective agents
    7.
    发明授权
    Chondroprotective agents 失效
    软骨保护剂

    公开(公告)号：US5621009A

    公开(公告)日：1997-04-15

    申请号：US535516

    申请日：1995-09-28

    申请人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    发明人： Koju Watanabe ,  Koichi Niimura ,  Kiyonori Umekawa

    IPC分类号： A61K31/047 ,  A61K31/19 ,  A61K31/192 ,  A61K31/215 ,  A61K31/216 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00

    CPC分类号： A61K31/192 ,  A61K31/19 ,  A61K31/215 ,  A61K31/216 ,  Y10S514/825

    摘要： A chondroprotective agent comprising a carboxylic acid compound of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom or an alkyl group of 1 to 6 carbon atoms, or a cis- or trans-isomer thereof, or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier is disclosed. The above compound strongly inhibits proteoglycan depletion from the chondrocyte matrix and exhibits a function to protect cartilage, and thus, is extremely effective for the treatment of arthropathy.

    摘要翻译： 一种软骨保护剂，其包含通式（I）的羧酸化合物：其中R 1和R 2独立地为氢原子或1至6个碳原子的烷基，或者顺式或反式 - 其异构体，或其药学上可接受的盐或酯，和药学上可接受的载体。 上述化合物强烈地抑制软骨细胞基质中的蛋白多糖消耗，并表现出保护软骨的功能，因此对于治疗关节病是非常有效的。

    Housing body for deglutition of solid molding for oral ingestion, container for the housing body, and deglutition method
    8.
    发明申请
    Housing body for deglutition of solid molding for oral ingestion, container for the housing body, and deglutition method 审中-公开
    用于口腔摄入的固体成型用于脱脂的壳体，用于壳体的容器和脱脂方法

    公开(公告)号：US20060293641A1

    公开(公告)日：2006-12-28

    申请号：US10556592

    申请日：2004-05-14

    申请人： Fuyuhiko Nishijima ,  Saichi Ono ,  Tadahiko Chiba ,  Yukio Iwase ,  Yoshiaki Osaka ,  Koichi Niimura

    发明人： Fuyuhiko Nishijima ,  Saichi Ono ,  Tadahiko Chiba ,  Yukio Iwase ,  Yoshiaki Osaka ,  Koichi Niimura

    IPC分类号： A61M31/00

    CPC分类号： A61J7/0038 ,  A47G21/183

    摘要： A housing body (10) for deglutition of a shaped solid (5) for oral ingestion which is stored therein, comprising a generally tubular water-resistant envelope (1); an opening-side end part (A) at one end of the envelope, having an unsealable structure part (2), and capable of forming an opening part (22) by removing the unsealable structure part; a shielding-side end part (B) at the other end of the envelope, having a means for preventing the shaped solid for oral ingestion from release, the means allowing liquid to pass therethrough but not allowing the shaped solid for oral ingestion to pass therethrough; and a storage chamber (6) storing the shaped solid for oral ingestion between the opening-side end part and the shielding-side end part is disclosed. A method for swallowing a shaped solid for oral ingestion, wherein an unsealable structure part installed at an opening-side end part of the housing body is removed; the shielding-side end part of the housing body is immersed into liquid in a vessel while the shaped solid for oral ingestion is stored in the storage chamber in the tubular envelope; and an opening part formed at the opening-side end part is held between the lips so that the shaped solid for oral ingestion is sucked in together with the liquid in the vessel is also disclosed.

    摘要翻译： 一种用于口腔成形固体（5）脱水的壳体（10），其用于口腔摄取，其存储在其中，包括大致管状的防水外壳（1）; 在封套的一端处的开口侧端部（A），具有可开封结构部分（2），并且能够通过移除开封结构部分形成开口部分（22）; 在封套的另一端处的屏蔽侧端部（B）具有用于防止成形固体口服摄取的装置，允许液体通过但不允许用于口服摄取的成形固体通过的装置 ; 公开了一种在开口侧端部和屏蔽侧端部之间存储用于口腔摄取的成形固体的储存室（6）。 一种吞咽用于口服摄取的成形固体的方法，其中移除安装在所述壳体的开口侧端部的开封结构部分; 将壳体的屏蔽侧端部浸入容器中的液体中，同时将用于口腔摄取的成形固体储存在管状外壳中的储存室中; 并且形成在开口侧端部处的开口部分保持在唇缘之间，使得用于口服摄取的成形固体与容器中的液体一起被吸入。

    Method for treating prostatic hypertrophy with estradiol derivatives
    10.
    发明授权
    Method for treating prostatic hypertrophy with estradiol derivatives 失效
    用雌二醇衍生物治疗前列腺肥大的方法

    公开(公告)号：US5480878A

    公开(公告)日：1996-01-02

    申请号：US408389

    申请日：1995-03-22

    申请人： Koichi Niimura ,  Takako Kawabe ,  Tsutomu Wada ,  Tsuyoshi Saitoh ,  Kenji Bannai

    发明人： Koichi Niimura ,  Takako Kawabe ,  Tsutomu Wada ,  Tsuyoshi Saitoh ,  Kenji Bannai

    IPC分类号： A61K31/565 ,  A61P35/00 ,  C07J1/00 ,  C07J41/00

    CPC分类号： C07J41/0072 ,  C07J1/0077

    摘要： Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is the treatment of prostatic hypertrophy with an estradiol derivative of the formula (II): ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3; and X is hydroxy or halogen.

    摘要翻译： 公开了一种用式（1'）的雌二醇衍生物 - 烷化剂缀合物治疗前列腺肥大的方法：其中R 1是C 1-4烷基或C 1-4烷氧基; R2为酰基或苄基; m为1〜3的整数。 并且n是0至3的整数。还公开了用式（II）的雌二醇衍生物治疗前列腺肥大：其中R 1是C 1-4烷基或C 1-4烷氧基; R2是酰基或苄基; m为1〜3的整数。 n为0〜3的整数。 X是羟基或卤素。