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公开(公告)号：US09334295B2
公开(公告)日：2016-05-10
申请号：US14525396
申请日：2014-10-28
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： A61K31/662 , C07F9/60 , C07F9/38 , A61K45/06
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
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公开(公告)号：US20060270721A1
公开(公告)日：2006-11-30
申请号：US11498124
申请日：2006-08-02
申请人： Yongxin Han , John Colucci , Xavier Billot , Marie-Claire Wilson , Robert Young
发明人： Yongxin Han , John Colucci , Xavier Billot , Marie-Claire Wilson , Robert Young
IPC分类号： A61K31/426 , A61K31/421
CPC分类号： C07D263/20 , C07D263/24 , C07D277/14 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/10
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP4N4亚型的有效选择性激动剂，它们在治疗青光眼中的用途或制剂以及与眼睛中的眼内压升高有关的其它病症 患者。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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3.发明授权Oxazolidin-2-one and thiazolidin-2-one derivatives for use as EP4 receptor agonists in the treatment of glaucoma 失效用作治疗青光眼的EP4受体激动剂的恶唑烷-2-酮和噻唑烷-2-酮衍生物公开(公告)号：US07109223B2
公开(公告)日：2006-09-19
申请号：US10521508
申请日：2003-08-25
申请人： Yongxin Han , John Colucci , Xavier Billot , Marie-Claire Wilson , Robert Young
发明人： Yongxin Han , John Colucci , Xavier Billot , Marie-Claire Wilson , Robert Young
IPC分类号： A01N43/74 , A01N43/713 , A01N43/76 , C07D277/04 , C07D257/04 , C07D263/04
CPC分类号： C07D263/20 , C07D263/24 , C07D277/14 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/10
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP4N4亚型的有效选择性激动剂，它们在治疗青光眼中的用途或制剂以及与眼睛中的眼内压升高有关的其它病症 患者。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号：US20050227969A1
公开(公告)日：2005-10-13
申请号：US11146992
申请日：2005-06-07
申请人： Xavier Billot , John Colucci , Yongxin Han , Marie-Claire Wilson , Robert Young
发明人： Xavier Billot , John Colucci , Yongxin Han , Marie-Claire Wilson , Robert Young
IPC分类号： A61K31/4412 , A61K31/558 , A61P27/06 , C07D211/54 , C07D211/74 , C07D211/76 , C07D265/04 , C07D265/10 , C07D279/06 , C07D401/06 , C07D409/06
CPC分类号： C07D211/74 , C07D211/76 , C07D265/10 , C07D401/06 , C07D409/06
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP 4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或制剂，其与眼睛中眼内压升高有关 病人。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号：US08481742B2
公开(公告)日：2013-07-09
申请号：US13418956
申请日：2012-03-13
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
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公开(公告)号：US20120178679A1
公开(公告)日：2012-07-12
申请号：US13418956
申请日：2012-03-13
申请人： John COLUCCI , Marie-Claire WILSON , Yongxin HAN , Claude DUFRESNE , Michel BELLEY , Cheuk K. LAU , Christopher BAYLY
发明人： John COLUCCI , Marie-Claire WILSON , Yongxin HAN , Claude DUFRESNE , Michel BELLEY , Cheuk K. LAU , Christopher BAYLY
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译： 本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。 本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。
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公开(公告)号：US20110237511A1
公开(公告)日：2011-09-29
申请号：US13152586
申请日：2011-06-03
IPC分类号： A61K38/23 , C07D211/76 , C07D409/06 , C07D401/06 , C07D265/10 , A61K31/45 , A61K31/4535 , A61K31/454 , A61K31/535 , A61K31/5377 , A61K31/4704 , A61K38/17 , A61K31/59 , A61K31/565 , A61P35/04 , A61P35/00 , A61P19/10 , A61P19/08 , A61P7/10 , A61P27/02 , A61P27/06 , A61P9/12
CPC分类号： C07D211/74 , C07D211/76 , C07D265/10 , C07D401/06 , C07D409/06
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或其制剂，其与患者眼睛中的眼内压升高有关。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号：USRE42562E1
公开(公告)日：2011-07-19
申请号：US11796044
申请日：2007-04-26
IPC分类号： C07D265/06 , C07D265/32 , A61K31/5355 , A61K31/535 , A61P27/06
CPC分类号： C07D211/74 , C07D211/76 , C07D265/10 , C07D401/06 , C07D409/06
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或其制剂，其与患者眼睛中的眼内压升高有关。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号：US07238710B2
公开(公告)日：2007-07-03
申请号：US11146992
申请日：2005-06-07
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4523 , A61P27/06
CPC分类号： C07D211/74 , C07D211/76 , C07D265/10 , C07D401/06 , C07D409/06
摘要： This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
摘要翻译： 本发明涉及前列腺素E2受体的EP 4亚型的有效选择性激动剂，它们在治疗青光眼和其它病症中的用途或制剂，其与眼睛中眼内压升高有关 病人。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。
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公开(公告)号：US08168815B2
公开(公告)日：2012-05-01
申请号：US12518899
申请日：2008-01-24
申请人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
发明人： John Colucci , Marie-Claire Wilson , Yongxin Han , Claude Dufresne , Michel Belley , Cheuk K. Lau , Christopher Bayly
IPC分类号： C07D215/38
CPC分类号： C07F9/60 , A61K31/662 , A61K45/06 , C07F9/3808 , C07F9/3834 , Y02A50/395
摘要： The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
摘要翻译： 本发明包括由下式表示的新一类化合物，它们是PTP-1B酶的抑制剂。 本发明还包括药物组合物，其包括上述化合物（式I）和治疗或预防PTP-1B介导的疾病包括糖尿病的方法。
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