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公开(公告)号:US08592600B2
公开(公告)日:2013-11-26
申请号:US12939276
申请日:2010-11-04
申请人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
发明人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
IPC分类号: C07D401/12
CPC分类号: C07D401/14
摘要: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
摘要翻译: 本发明涉及外消旋的伊拉唑,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。 本发明还涉及用于抑制胃酸分泌的药物组合物,其包含有效抑制胃酸分泌的量的本发明的伊拉唑结晶形式和药学上可接受的载体。 本发明还提供了治疗各种酸相关胃肠道(GI)障碍的方法。
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公开(公告)号:US07999110B2
公开(公告)日:2011-08-16
申请号:US11966868
申请日:2007-12-28
申请人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
发明人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
IPC分类号: C07D401/14
CPC分类号: C07D401/14
摘要: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2 -pyridinyl)-methyl]sulfinyl]-5-(1 H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
摘要翻译: 本发明涉及外消旋伊拉唑,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。 本发明还涉及用于抑制胃酸分泌的药物组合物,其包含有效抑制胃酸分泌的量的本发明的伊拉唑结晶形式和药学上可接受的载体。 本发明还提供了治疗各种酸相关胃肠道(GI)障碍的方法。
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公开(公告)号:US08592599B2
公开(公告)日:2013-11-26
申请号:US12939266
申请日:2010-11-04
申请人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
发明人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent , Jinyu Shen
IPC分类号: C07D401/12
CPC分类号: C07D401/14
摘要: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl)1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
摘要翻译: 本发明涉及外消旋的伊拉唑,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。 本发明还涉及用于抑制胃酸分泌的药物组合物,其包含有效抑制胃酸分泌的量的本发明的伊拉唑结晶形式和药学上可接受的载体。 本发明还提供了治疗各种酸相关胃肠道(GI)障碍的方法。
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公开(公告)号:US07989632B2
公开(公告)日:2011-08-02
申请号:US11966896
申请日:2007-12-28
申请人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent
发明人: John M. Brackett , David T. Jonaitis , Wei Lai , Jih Hua Liu , Stephan D. Parent
IPC分类号: C07D401/12
CPC分类号: C07D401/14
摘要: The invention relates to crystalline forms of various solvates of ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl)1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising crystalline ilaprazole hydrate according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
摘要翻译: 本发明涉及伊拉帕唑,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-苯并咪唑的各种溶剂合物的结晶形式。 本发明还涉及用于抑制胃酸分泌的药物组合物,其包含有效抑制胃酸分泌的量的本发明的结晶伊拉拉唑水合物和药学上可接受的载体。 本发明还提供了治疗各种酸相关胃肠道(GI)障碍的方法。
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公开(公告)号:US08633243B2
公开(公告)日:2014-01-21
申请号:US13537583
申请日:2012-06-29
IPC分类号: A61K31/21
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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公开(公告)号:US20120071684A1
公开(公告)日:2012-03-22
申请号:US13306043
申请日:2011-11-29
IPC分类号: C07C255/47
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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公开(公告)号:US20090048204A1
公开(公告)日:2009-02-19
申请号:US12191176
申请日:2008-08-13
IPC分类号: A61K31/215 , C07C69/753 , A61K31/7068 , A61P35/00
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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公开(公告)号:US08088824B2
公开(公告)日:2012-01-03
申请号:US12191176
申请日:2008-08-13
IPC分类号: A61K31/21
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
摘要翻译: 三萜化合物,2-氰基-3,12-二氧杂环戊烯-1,9(11) - 二烯-28-甲酸甲酯(CDDO甲酯)具有非结晶的玻璃状固体形式和非水合结晶形式, 可以例如由饱和甲醇溶液制备。 玻璃状的形式显示了非含水结晶形式的增强的生物利用度。 每种形式的CDDO甲酯是通常用于固体剂型的优选候选药物,用于治疗通常与炎症相关的各种疾病状态。
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公开(公告)号:US20120330050A1
公开(公告)日:2012-12-27
申请号:US13537583
申请日:2012-06-29
IPC分类号: C07C255/47
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
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公开(公告)号:US08309601B2
公开(公告)日:2012-11-13
申请号:US13306043
申请日:2011-11-29
IPC分类号: A61K31/21
CPC分类号: A61K31/70
摘要: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
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