公开(公告)号：US20090148480A1

公开(公告)日：2009-06-11

申请号：US11995500

申请日：2006-07-14

申请人： Nobuyuki Isshiki ,  Noboru Kamada ,  Hideki Takeuchi

发明人： Nobuyuki Isshiki ,  Noboru Kamada ,  Hideki Takeuchi

IPC分类号： A61K9/00 ,  A61P1/00

CPC分类号： A61K9/0065 ,  A61K9/2086 ,  A61K31/341 ,  A61K31/496

摘要： The invention provides a preparation which shows a satisfactory gastric residence time, has such a size that allows for easy ingestion, can quickly disintegrate after expelled from the stomach, and can be prepared readily in an industrial scale. A gastric retentive preparation having a gastric resident layer and a drug release layer is provided, wherein the gastric resident layer does not disintegrate in the stomach and disintegrates in the intestine. Preferably, the gastric resident layer has a minimum diameter of 7 mm or more as measured after stirring the preparation in the first fluid at 200 rpm at 37° C. for 15 hours under the conditions of the paddle method in the dissolution test in accordance with Japanese Pharmacopoeia and has a maximum diameter of 6 mm or less as measured after further stirring the preparation in the second fluid at 200 rpm at 37° C. for 9 hours under the same conditions.

摘要翻译： 本发明提供一种显示令人满意的胃停留时间的制剂，具有允许容易摄入的尺寸，可以在从胃排出后迅速崩解，并且可以以工业规模容易地制备。 提供了具有胃滞留层和药物释放层的胃滞留制剂，其中胃停留层在胃中不分解并在肠中分解。 优选地，胃停留层的最小直径为7mm以上，在第一流体中的制剂在200rpm下在37℃下搅拌15小时时，在桨式方法的条件下根据溶出试验按照 日本药典，并且在相同条件下，在第二流体中以200rpm在37℃下进一步搅拌制备9小时后测得的最大直径为6mm或更小。

公开(公告)号：US20100081674A1

公开(公告)日：2010-04-01

申请号：US12595931

申请日：2008-04-16

申请人： Kohsuke Ohno ,  Noboru Kamada

发明人： Kohsuke Ohno ,  Noboru Kamada

IPC分类号： A61K31/519 ,  C07D495/04

CPC分类号： C07D495/04

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; Q is hydrogen atom, alkyl, alkylsulfonyl, acyl, etc.; X is -(alkylene)-Z, —CO—Y, —SO2—Y, etc. (in which Y is Z or amino, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

摘要翻译： 本发明提供了可用作预防或治疗性激素依赖性疾病等的试剂的化合物。 也就是说，本发明提供具有GnRH拮抗活性的由以下通式（I）表示的稠合杂环衍生物，含有它们的药物组合物，其药用用途等。 在式（I）中，环A是5元环状不饱和烃或5元杂芳基; RA是卤素，烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B是芳基或杂芳基; RB是卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2是氧原子等; Q是氢原子，烷基，烷基磺酰基，酰基等; X是 - （亚烷基）-Z，-CO-Y，-SO2-Y等（其中Y是Z或氨基等; Z是环烷基，杂环烷基，芳基，杂芳基等）

公开(公告)号：US08426427B2

公开(公告)日：2013-04-23

申请号：US12595931

申请日：2008-04-16

申请人： Kohsuke Ohno ,  Noboru Kamada

发明人： Kohsuke Ohno ,  Noboru Kamada

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D495/04

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; Q is hydrogen atom, alkyl, alkylsulfonyl, acyl, etc.; X is -(alkylene)-Z, —CO—Y, —SO2—Y, etc. (in which Y is Z or amino, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

摘要翻译： 本发明提供了可用作预防或治疗性激素依赖性疾病等的试剂的化合物。 也就是说，本发明提供具有GnRH拮抗活性的由以下通式（I）表示的稠合杂环衍生物，含有它们的药物组合物，其药用用途等。 在式（I）中，环A是5元环状不饱和烃或5元杂芳基; RA是卤素，烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B是芳基或杂芳基; RB是卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2是氧原子等; Q是氢原子，烷基，烷基磺酰基，酰基等; X是 - （亚烷基）-Z，-CO-Y，-SO2-Y等（其中Y是Z或氨基等; Z是环烷基，杂环烷基，芳基，杂芳基等）

公开(公告)号：US20100112053A1

公开(公告)日：2010-05-06

申请号：US12523117

申请日：2008-01-10

申请人： Denichi Momose ,  Nobuyuki Isshiki ,  Noboru Kamada

发明人： Denichi Momose ,  Nobuyuki Isshiki ,  Noboru Kamada

IPC分类号： A61K9/24 ,  A61K31/198 ,  A61P25/16 ,  A61K9/20

CPC分类号： A61K9/0065 ,  A61K9/2086 ,  A61K31/198

摘要： The present invention is to provide a levodopa preparation which is able to persistently release levodopa in the stomach, has a sufficient gastric residence time, is in an easily ingestible size and is able to be easily manufactured industrially with an object of maintaining a sustained concentration of levodopa in blood. It is a gastric retentive preparation for levodopa, characterized in that, the preparation contains a gastric resident layer showing a sufficient retentive property due to a high mechanical strength in the stomach and showing a good disintegrating property in an intestinal tract in addition to a drug releasing layer containing levodopa.

摘要翻译： 本发明提供一种能够在胃中持续释放左旋多巴的左旋多巴制剂，具有足够的胃停留时间，容易摄取的尺寸，并且能够容易地在工业上制造，其目的是保持持续浓度 左旋多巴在血液中 它是用于左旋多巴的胃保持制剂，其特征在于，该制剂含有由胃中的高机械强度显示出足够的保留性能的胃停留层，除了药物释放之外还显示出良好的肠道分解性 含有左旋多巴的层。