公开(公告)号：US08686006B2

公开(公告)日：2014-04-01

申请号：US13124797

申请日：2009-10-22

申请人： Masayuki Umeda ,  Akio Kimura ,  Kenji Ueda ,  Koji Sakanaka

发明人： Masayuki Umeda ,  Akio Kimura ,  Kenji Ueda ,  Koji Sakanaka

IPC分类号： A61K31/44

CPC分类号： A61K31/4409

摘要： An object of the present invention is to provide a pharmaceutical composition that improves intestinal absorption of a compound having a structure represented by the general formula [1]. The composition containing a compound represented by the general formula [1] or a salt thereof and (b) a lipophilic substance improves intestinal absorption of the compound. In the formula, A represents —(NR4)—, —(CR5R6)— or the like; B represents an alkylene group or an alkenylene group; R1 represents an alkyl group, an alkenyl group or the like; R2 represents an adamantylalkyl group or the like; R3 represents an unsaturated heterocyclic ring; R4, R5 and R6 each represent a hydrogen atom or the like; and X represents an oxygen atom or the like.

摘要翻译： 本发明的目的是提供一种改善具有由通式[1]表示的结构的化合物的肠吸收的药物组合物。 包含由通式[1]表示的化合物或其盐和（b）亲脂性物质的组合物改善了化合物的肠吸收。 在该式中，A表示 - （NR 4） - ， - （CR 5 R 6） - 等; B表示亚烷基或亚烯基; R1表示烷基，烯基等; R2表示金刚烷基烷基等; R3表示不饱和杂环; R4，R5和R6各自表示氢原子等; X表示氧原子等。

公开(公告)号：US20110201655A1

公开(公告)日：2011-08-18

申请号：US13124797

申请日：2009-10-22

申请人： Masayuki Umeda ,  Akio Kimura ,  Kenji Ueda ,  Koji Sakanaka

发明人： Masayuki Umeda ,  Akio Kimura ,  Kenji Ueda ,  Koji Sakanaka

IPC分类号： A61K31/4409 ,  A61P35/00 ,  A61P19/10 ,  A61P11/00 ,  A61P17/00 ,  A61P25/00

CPC分类号： A61K31/4409

摘要： An object of the present invention is to provide a pharmaceutical composition that improves intestinal absorption of a compound having a structure represented by the general formula [1]. The composition containing a compound represented by the general formula [1] or a salt thereof and (b) a lipophilic substance improves intestinal absorption of the compound. In the formula, A represents —(NR4)—, —(CR5R6)— or the like; B represents an alkylene group or an alkenylene group; R1 represents an alkyl group, an alkenyl group or the like; R2 represents an adamantylalkyl group or the like; R3 represents an unsaturated heterocyclic ring; R4, R5 and R6 each represent a hydrogen atom or the like; and X represents an oxygen atom or the like.

摘要翻译： 本发明的目的是提供一种改善具有由通式[1]表示的结构的化合物的肠吸收的药物组合物。 包含由通式[1]表示的化合物或其盐和（b）亲脂性物质的组合物改善了化合物的肠吸收。 在该式中，A表示 - （NR 4） - ， - （CR 5 R 6） - 等; B表示亚烷基或亚烯基; R1表示烷基，烯基等; R2表示金刚烷基烷基等; R3表示不饱和杂环; R4，R5和R6各自表示氢原子等; X表示氧原子等。

公开(公告)号：US20120316158A1

公开(公告)日：2012-12-13

申请号：US13580931

申请日：2010-12-16

申请人： Takashi Nagano ,  Koji Sakanaka ,  Masatsugu Nakamura ,  Kouichi Kawazu ,  Hajime Ibuki ,  Kayoko Sakamoto

发明人： Takashi Nagano ,  Koji Sakanaka ,  Masatsugu Nakamura ,  Kouichi Kawazu ,  Hajime Ibuki ,  Kayoko Sakamoto

IPC分类号： A61K31/5383 ,  A61P31/04 ,  A61P29/00 ,  A61P31/00 ,  A61P27/02

CPC分类号： A61K31/5383 ,  A61K9/0048

摘要： Instillation of a 1.5% (w/v) levofloxacin ophthalmic solution three times a day, which is the dosage or dose regimen of the present invention, has features to cure bacterial conjunctivitis in a shorter time than instillation of a 0.5% (w/v) ophthalmic solution three times a day, which is the conventional dosage or dose regimen, and not to increase the rate of occurrence of side effects. Curing the ocular infection in a short time leads to shortening of the duration of exposure of the ocular-infection-causing bacterium to levofloxacin. Therefore, the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention is eventually expected to suppress emergence of the resistant bacterium resulting from the long-term use of the levofloxacin ophthalmic solution in the conventional dosage or dose regimen. In addition, it is confirmed that the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention directly inhibits the ocular-infection-causing bacterium such as Staphylococcus aureus from becoming resistant to levofloxacin, which results from the short-term use of the levofloxacin ophthalmic solution in the conventional dosage or dose regimen.

摘要翻译： 每天三次（即本发明的剂量或剂量方案）滴注1.5％（w / v）左氧氟沙星眼用溶液具有在比滴注0.5％（w / v）的时间更短的时间内治愈细菌性结膜炎的特征 ）眼用溶液每天三次，这是常规剂量或剂量方案，而不是增加副作用的发生率。 在短时间内治疗眼部感染导致引起眼睛感染的细菌暴露于左氧氟沙星的持续时间缩短。 因此，本发明的剂量或剂量方案中的左氧氟沙星眼用溶液最终预期会抑制由常规剂量或剂量方案中长期使用左氧氟沙星眼用溶液引起的耐药性细菌的出现。 此外，证实本发明的剂量或剂量方案中的左氧氟沙星眼用溶液直接抑制例如金黄色葡萄球菌引起的眼睛感染的细菌变得对左氧氟沙星具有抗性，这是由于短期使用 左氧氟沙星眼科溶液在常规剂量或剂量方案中。