公开(公告)号：KR1020090086615A

公开(公告)日：2009-08-13

申请号：KR1020097013519

申请日：2007-12-28

Applicant: 일양약품주식회사

Inventor： 브랙켓,존,엠. ,  조나이티스,데이비드,티. ,  라이,웨이 ,  리우,지,후아 ,  파렌트,스테판,디. ,  쉔,진유

IPC: C07D401/14 ,  A61K31/4439 ,  A61P1/04

CPC classification number: C07D401/14

Abstract: A crystalline racemic ilaprazole is provided to suppress gastric acid secretion as an inhibitor of proton pump and treat various acids related gastrointestinal disease. A pharmaceutical composition for suppressing gastric acid secretion comprises 5-80mg of crystalline racemic ilaprazole and pharmaceutically acceptable carrier. The crystalline racemic ilaprazole has the peak of 15.8^o2theta Π0.2^o2theta in powder X-ray diffraction pattern. The pharmaceutical composition is extended-release type. The therapeutically effective amount of racemic ilaprazole treats gastric inflammatory disease by administering.

Abstract translation: 提供结晶外消旋的伊拉唑，以抑制胃酸分泌作为质子泵的抑制剂，并治疗各种酸相关的胃肠道疾病。 用于抑制胃酸分泌的药物组合物包含5-80mg结晶外消旋伊拉唑和药学上可接受的载体。 结晶外消旋的伊拉唑在粉末X射线衍射图中具有15.8μm±0.2μm的峰值。 药物组合物是延长释放型。 外用伊拉唑的治疗有效量通过给药治疗胃炎。

公开(公告)号：KR1020110091594A

公开(公告)日：2011-08-11

申请号：KR1020117016139

申请日：2007-12-28

Applicant: 일양약품주식회사

Inventor： 브랙켓,존,엠. ,  조나이티스,데이비드,티. ,  라이,웨이 ,  리우,지,후아 ,  파렌트,스테판,디. ,  쉔,진유

IPC: C07D401/14 ,  A61K31/4439 ,  A61P1/04

CPC classification number: C07D401/14

Abstract: PURPOSE: A crystalline form of racemic illaprazole(2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl)1H-Benzimidazole) is provided to treat acids-associated gastrointestinal disease. CONSTITUTION: A crystalline form of racemic illaprazole has 156.1, 143.2, 110.6, and 10.5 ppm of peak at solid phase 13C CP/MAS NMR. The crystalline form has starting temperature at 170°C. The crystalline form has 9.4o2θ ± 0.2o2θ, 17.5o2θ ± 0.2o2θ, 18.8o2θ ± 0.2o2θ, and 32.8o2θ ± 0.2o2θ of peak at a X-ray diffraction pattern. A pharmaceutical composition for suppressing gastric acid secretion contains the crystalline form and pharmaceutically acceptable carrier. The drug composition is a delayed release type.

Abstract translation: 目的：提供外消旋的伊拉帕唑（2 [[（4-甲氧基-3-甲基-2-吡啶基） - 甲基]亚磺酰基] -5-（1H-吡咯-1-基）1H-苯并咪唑的结晶形式 酸相关的胃肠道疾病。 构成：外消旋伊拉波唑的结晶形式在固相13C CP / MAS NMR下具有156.1,143.2,110.6和10.5ppm的峰。 结晶形式的起始温度为170℃。 结晶形式有9.4o2＆amp; ±0.2o2＆thgr; 17.5o2＆thgr ±0.2o2＆thgr; 18.8o2＆thgr; ±0.2o2＆thgr;和32.8o2＆thgr ±0.2o2＆thgr 在X射线衍射图中为峰。 用于抑制胃酸分泌的药物组合物含有结晶形式和药学上可接受的载体。 药物组合物是延迟释放型。

公开(公告)号：KR101052387B1

公开(公告)日：2011-07-28

申请号：KR1020097013519

申请日：2007-12-28

Applicant: 일양약품주식회사

Inventor： 브랙켓,존,엠. ,  조나이티스,데이비드,티. ,  라이,웨이 ,  리우,지,후아 ,  파렌트,스테판,디. ,  쉔,진유

IPC: C07D401/14 ,  A61K31/4439 ,  A61P1/04

CPC classification number: C07D401/14

Abstract: 본 발명은 라세믹 일라프라졸 (2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole)의 결정형에 대한 것이다. 본 발명은 위산분비에 대한 유효량과 약제학적으로 허용되는 담체에 대한 발명에 기초한 라세믹 일라프라졸 결정형이 포함된 위산분비를 저해하는 약제학적 조성물에 대한 것이다. 또한 본 발명은 앞에서 언급된 여러 산 관련 위장관 질환의 치료법을 제공한다.
일라프라졸, 결정형, 위장관 질환

公开(公告)号：KR1020090086121A

公开(公告)日：2009-08-10

申请号：KR1020097013491

申请日：2007-12-28

Applicant: 일양약품주식회사

Inventor： 브랙켓,존,엠. ,  조나이티스,데이비드,티. ,  라이,웨이 ,  파렌트,스테판,디.

IPC: C07D401/14 ,  A61K31/4439 ,  A61P1/04

CPC classification number: C07D401/14

Abstract: A solvated ilaprazole crystalline is provided to treat gastrointestinal diseases (GI) which is related to acid through the suppression of proton pump. A solvated ilaprazole crystalline is 1,4-dioxane/racemic ilaprazole semi-solvate crystalline (C type), THF/racemic ilaprazole semi-solvate crystalline (D type), methanol/racemic ilaprazole solvate crystalline (G type), and racemic ilaprazole hydrate crystalline (K type). The 1,4-dioxane/racemic ilaprazole semi-solvate crystalline (C type) has the onf temperature at 94‹C by differential scanning calorimetry (DSC). A pharmaceutical composition suppressing the secretion of gastric acid comprises therapeutically effective amount of racemic ilaprazole hydrate crystalline and pharmaceutically acceptable carrier. The pharmaceutical composition is sustained release type.

Abstract translation: 提供溶剂化的伊拉唑结晶，通过抑制质子泵来治疗与酸有关的胃肠疾病（GI）。 溶剂化的伊拉唑结晶是1,4-二恶烷/外消旋的伊拉唑半溶剂化物结晶（C型），THF /外消旋的伊拉唑半溶剂化物结晶（D型），甲醇/外消旋的伊拉唑溶剂合物结晶（G型）和外消旋的伊拉唑水合物 结晶（K型）。 1,4-二恶烷/外消旋的伊拉唑半溶剂化物结晶（C型）通过差示扫描量热法（DSC）的温度为94℃。 抑制胃酸分泌的药物组合物包括治疗有效量的外消旋伊拉唑水合物结晶和药学上可接受的载体。 药物组合物为持续释放型。