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公开(公告)号：US20070105913A1
公开(公告)日：2007-05-10
申请号：US10565538
申请日：2004-07-20
IPC分类号： A61K31/44 , A61K31/40 , A61K31/24 , A61K31/195 , A61K31/16
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译： 本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症 - 高胆固醇血症，多囊卵巢综合征（PCOS）。 特别地，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。 （I'）A是C 2 -C 15炔基，C 2 -C 6 - 炔基芳基 C 2 -C 6 - 炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是芳基，其可任选地被3-8元环烷基稠合。 R 1和R 2彼此独立地选自氢或（C 1 -C 6 - / SUB）烷基。 R 4和R 5各自彼此独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 3烷基羧基，C 2 -C 3链烯基羧基，C 2 -C 3烷基羧基，C 1 -C 3烷基羧基， 亚磺酰基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，由此R 4中的至少一个 或者R 5不是氢或C 1 -C 6烷基。
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2.发明授权1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP 1-B inhibitors 有权1,1'-（1,2-乙炔二基）双苯衍生物作为PTP 1-B抑制剂公开(公告)号：US07947851B2
公开(公告)日：2011-05-24
申请号：US11547861
申请日：2005-03-29
IPC分类号： C07D333/34 , C07C65/03 , C07C211/44 , C07C233/65 , C07C311/15 , A61K31/165 , A61P3/10
CPC分类号： C07D319/08 , A61K38/28 , C07C33/28 , C07C51/31 , C07C63/66 , C07C65/28 , C07C67/343 , C07C69/76 , C07C211/29 , C07C217/58 , C07C229/38 , C07C229/60 , C07C229/64 , C07C233/31 , C07C233/81 , C07C233/87 , C07C235/46 , C07C235/84 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/42 , C07C311/04 , C07C311/13 , C07C311/19 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D333/34
摘要： The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
摘要翻译： 本发明涉及式（I）的羧酸及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖，葡萄糖耐量不足， 胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。 特别地，本发明涉及式（I）的羧酸的用途，特别是抑制PTP的活性。
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公开(公告)号：US07589232B2
公开(公告)日：2009-09-15
申请号：US10565538
申请日：2004-07-20
IPC分类号： C07C299/34 , A61K31/195
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译： 本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症 - 高胆固醇血症，多囊卵巢综合征（PCOS）。 特别地，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。 （I'）A是C 2 -C 15炔基，C 2 -C 6炔基芳基，C 2 -C 6炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是可以任选被3-8元环烷基稠合的芳基。 R 1和R 2彼此独立地选自氢或（C 1 -C 6）烷基。 R 4和R 5各自独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 3烷基羧基，C 2 -C 3烯基羧基，C 2 -C 3炔基羧基，氨基或R 4和R 5可以形成不饱和或饱和的杂环， 或者R 5不是氢或C 1 -C 6烷基。
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公开(公告)号：US20080021028A1
公开(公告)日：2008-01-24
申请号：US11572761
申请日：2005-07-25
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
IPC分类号： A61K31/445 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/5375 , A61P29/00 , C07D211/04 , C07D239/02 , C07D401/02 , C07D403/02 , C07D413/02
CPC分类号： C07D211/46 , C07D211/58 , C07D213/74 , C07D215/46 , C07D239/42 , C07D241/20 , C07D285/08 , C07D295/185 , C07D401/12 , C07D487/08
摘要： The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是用于治疗和/或预防自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多种 硬化症，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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公开(公告)号：US08247437B2
公开(公告)日：2012-08-21
申请号：US13155411
申请日：2011-06-08
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
IPC分类号： C07D211/70 , C07D405/06 , A61K31/4418
CPC分类号： C07D211/46 , C07D211/58 , C07D213/74 , C07D215/46 , C07D239/42 , C07D241/20 , C07D285/08 , C07D295/185 , C07D401/12 , C07D487/08
摘要： The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化症 ，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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6.发明申请1,1'-(1,2-Ethynediyl)Bis-Benzene Derivatives As Ptp 1-B Inhibitors 有权1,1'-（1,2-乙炔二基）双苯衍生物作为Ptp 1-B抑制剂公开(公告)号：US20090029903A1
公开(公告)日：2009-01-29
申请号：US11547861
申请日：2005-03-29
IPC分类号： A61K38/28 , C07C229/64 , A61K31/196 , C07D333/34 , A61K31/381
CPC分类号： C07D319/08 , A61K38/28 , C07C33/28 , C07C51/31 , C07C63/66 , C07C65/28 , C07C67/343 , C07C69/76 , C07C211/29 , C07C217/58 , C07C229/38 , C07C229/60 , C07C229/64 , C07C233/31 , C07C233/81 , C07C233/87 , C07C235/46 , C07C235/84 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/42 , C07C311/04 , C07C311/13 , C07C311/19 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D333/34
摘要： The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
摘要翻译： 本发明涉及式（I）的羧酸及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖，葡萄糖耐量不足， 胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。 特别地，本发明涉及式（I）的羧酸的用途，特别是抑制PTP的活性。
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公开(公告)号：US20110263628A1
公开(公告)日：2011-10-27
申请号：US13155411
申请日：2011-06-08
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
IPC分类号： A61K31/4468 , C07D401/12 , C07D211/46 , C07D413/04 , C07D211/18 , A61K31/4545 , A61K31/445 , A61K31/506 , A61K31/454 , A61P29/00 , A61P25/28 , A61P9/00 , A61P35/00 , A61P15/06 , A61P11/00 , A61P11/06 , A61P1/16 , A61P1/18 , A61P17/00 , C07D211/58
CPC分类号： C07D211/46 , C07D211/58 , C07D213/74 , C07D215/46 , C07D239/42 , C07D241/20 , C07D285/08 , C07D295/185 , C07D401/12 , C07D487/08
摘要： The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化症 ，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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公开(公告)号：US08008302B2
公开(公告)日：2011-08-30
申请号：US11572761
申请日：2005-07-25
申请人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Agnes Bombrun , Jerome Gonzalez , Stefano Crosignani , Patrick Gerber , Catherine Jorand-Lebrun
IPC分类号： A61K31/496 , A61K31/506 , C07D213/75 , C07D215/46 , C07D271/07 , C07D285/08 , C07D295/185 , C07D317/34 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/12 , A61K31/454 , A61K31/4418 , C07D211/70 , C07D413/04 , C07D417/12 , C07D487/08
CPC分类号： C07D211/46 , C07D211/58 , C07D213/74 , C07D215/46 , C07D239/42 , C07D241/20 , C07D285/08 , C07D295/185 , C07D401/12 , C07D487/08
摘要： The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是用于治疗和/或预防自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多种 硬化症，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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公开(公告)号：US07973039B2
公开(公告)日：2011-07-05
申请号：US11793474
申请日：2005-12-19
IPC分类号： A61P29/00 , A61P37/00 , A61K31/495 , A61K31/496 , C07D211/96 , C07D213/42 , C07D213/74 , C07D243/08 , C07D295/22 , C07D317/58 , C07F7/08
CPC分类号： C07D317/58 , C07D211/96 , C07D213/42 , C07D213/74 , C07D243/08 , C07D295/26 , C07F7/0812 , C07F9/59 , C07F9/650952
摘要： The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化，关节炎， 肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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公开(公告)号：US20080194520A1
公开(公告)日：2008-08-14
申请号：US11793474
申请日：2005-12-19
IPC分类号： C07D241/04 , A61K31/695 , A61K31/495 , C07F7/02 , C07D401/02 , A61K31/497 , A61K31/675 , C07F9/6509 , C07D211/06 , A61K31/445 , A61K31/551 , C07D243/08 , C07D413/02 , A61K31/5375
CPC分类号： C07D317/58 , C07D211/96 , C07D213/42 , C07D213/74 , C07D243/08 , C07D295/26 , C07F7/0812 , C07F9/59 , C07F9/650952
摘要： The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译： 本发明涉及式（I）的衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化，关节炎， 肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。
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