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1. 发明申请

WO2005011685A1 ARYL DICARBOXAMIDES 审中-公开
公开(公告)号：WO2005011685A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051558
申请日：2004-07-20
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , THOMAS, Russel, J. , SWINNEN, Dominique , PONS, Jean-François , BOMBRUN, Agnès
发明人： THOMAS, Russel, J. , SWINNEN, Dominique , PONS, Jean-François , BOMBRUN, Agnès
IPC分类号： A61K31/426
CPC分类号： A61K31/16 , A61K31/166 , A61K31/167 , A61K31/426 , C07C237/42 , C07C255/57 , C07C2601/08 , C07C2601/14 , C07D277/30 , C07D277/56
摘要： The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an airninocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R 1 and R 2 are independently from each other is selected from the group consisting of hydrogen or C 1 -C 6 -alkyl; R 4 and R 5 are each independently from each other selected from the group consisting of H, hydroxy, C 1 -C 6 alkyl, carboxy, C 1 -C 6 alkoxy, C 1 -C 3 alkyl carboxy, C 2 -C 3 alkenyl carboxy, C 2 -C 3 alkynyl carboxy, amino or R 4 and R 5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R 4 or R 5 is not a hydrogen or C 1 -C 6 alkyl.
摘要翻译：本发明涉及式（I）的芳基二甲酰胺和其用于治疗和/或预防由胰岛素抵抗或高血糖引起的肥胖和/或代谢障碍，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）的芳基二羧酰胺的用途，特别是抑制PTP的活性。 A是空气羰基部分; Cy是芳基，杂芳基，芳基 - 杂芳基，杂芳基 - 芳基，芳基 - 芳基，环烷基或杂环基团; n为0或1; 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，其中R 4或R 5中的至少一个不是氢或C 1 -C 6烷基。

2. 发明申请

WO2003064376A1 SUBSTITUTED METHYLENE AMIDE DERIVATIVES AS MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPS) 审中-公开
标题翻译：作为蛋白质酪氨酸磷酸酯的调节剂的取代的甲基酰胺衍生物
公开(公告)号：WO2003064376A1
公开(公告)日：2003-08-07
申请号：PCT/EP2003/000808
申请日：2003-01-27
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SWINNEN, Dominique , BOMBRUN, Agnès , GONZALEZ, Jerôme , GERBER, Patrick , PITTET, Pierre-André
发明人： SWINNEN, Dominique , BOMBRUN, Agnès , GONZALEZ, Jerôme , GERBER, Patrick , PITTET, Pierre-André
IPC分类号： C07C237/42
CPC分类号： C07D213/40 , C07C2601/14 , C07D211/26 , C07D211/58 , C07D211/96 , C07D271/06 , C07D277/28 , C07D285/06 , C07D307/79 , C07D307/91 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D401/04
摘要： The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).
摘要翻译：本发明涉及式（I）的取代的亚甲基酰胺衍生物及其用于治疗和/或预防由胰岛素抵抗或疟疾引起的代谢紊乱，包括I型和/或II型糖尿病，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，肥胖症，多囊卵巢综合征（PCOS）。特别地，本发明涉及使用式（I）的取代的亚甲基酰胺衍生物来调节，特别是抑制PTP的活性。本发明还涉及治疗II型糖尿病，肥胖症和调节哺乳动物食欲的方法。本发明还涉及新型取代的亚甲基酰胺衍生物及其制备方法。式（I）。

3. 发明申请

WO2006067114A1 SULFONYL AMINO CYCLIC DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：磺酰氨基环状衍生物及其用途
公开(公告)号：WO2006067114A1
公开(公告)日：2006-06-29
申请号：PCT/EP2005/056910
申请日：2005-12-19
申请人： Applied Research Systems ARS Holding N.V. , SWINNEN, Dominique , BOMBRUN, Agnès , GERBER, Patrick , JORAND-LEBRUN, Catherine
发明人： SWINNEN, Dominique , BOMBRUN, Agnès , GERBER, Patrick , JORAND-LEBRUN, Catherine
IPC分类号： C07D317/58 , C07F7/08 , C07D295/22 , C07D213/42 , C07D213/74 , A61K31/495 , A61K31/496 , A61P37/00 , A61P29/00 , C07D211/96 , C07D243/08
CPC分类号： C07D317/58 , C07D211/96 , C07D213/42 , C07D213/74 , C07D243/08 , C07D295/26 , C07F7/0812 , C07F9/591 , C07F9/650958
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。

4. 发明申请

WO2005097773A1 1,1’-(1,2-ETHYNEDIYL)BIS-BENZENE DERIVATIVES AS PTP 1-B INHIBITORS 审中-公开
标题翻译： 1,1' - （1,2-ETHYNEDIYL）BIS-BENZENE衍生物作为PTP 1-B抑制剂
公开(公告)号：WO2005097773A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/051426
申请日：2005-03-29
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GERBER, Patrick , GONZALEZ, Jérôme , BOMBRUN, Agnès
发明人： SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GERBER, Patrick , GONZALEZ, Jérôme , BOMBRUN, Agnès
IPC分类号： C07D333/34
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。

5. 发明申请

WO2002102359A2 ALKYLIDENE PYRAZOLIDINEDIONE DERIVATIVES 审中-公开
标题翻译：烷基吡唑啉衍生物
公开(公告)号：WO2002102359A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006627
申请日：2002-06-14
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , BOMBRUN, Agnès , RUECKLE, Thomas , SWINNEN, Dominique , GONZALEZ, Jérôme , CHURCH, Dennis
发明人： BOMBRUN, Agnès , RUECKLE, Thomas , SWINNEN, Dominique , GONZALEZ, Jérôme , CHURCH, Dennis
IPC分类号： A61K31/00
CPC分类号： C07D401/06 , A61K31/00 , A61K31/4155 , A61K31/4192 , C07D231/32 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要： The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.
摘要翻译：本发明涉及式I的亚烷基吡唑烷二酮衍生物用于治疗和/或预防I型和/或II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，高血糖症，肥胖症和多囊卵巢综合征PCOS的用途。特别地，本发明涉及使用式I的亚烷基吡唑烷二酮衍生物调节，特别是抑制PTP的活性，特别是PTP1B，TC-PTP，SHP和GLEPP-1的活性。本发明还涉及新的亚烷基吡唑烷二酮衍生物。 R1和R2彼此独立地表示未取代或取代的芳基或杂芳基。

6. 发明申请

WO2005012280A1 ALKYNYL ARYL CARBOXAMIDES 审中-公开
标题翻译：亚苄基芳香族碳酰胺
公开(公告)号：WO2005012280A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051557
申请日：2004-07-20
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SWINNEN, Dominique , GERBER, Patrick , GONZALEZ, Jerôme , BOMBRUN, Agnès , JORAND-LEBRUN, Catherine
发明人： SWINNEN, Dominique , GERBER, Patrick , GONZALEZ, Jerôme , BOMBRUN, Agnès , JORAND-LEBRUN, Catherine
IPC分类号： C07D319/08
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 C 2 -C 15 alkynyl, C 2 -C 6 -alkynyl aryl, C 2 -C 6 -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. R 1 and R 2 are independently from each other is selected from the group consisting of hydrogen or (C I -C 6 )alkyl. R 4 and R 5 are each independently from each other selected from the group consisting of H, hydroxy. C 1 -C 6 alkyl, carboxy, C 1 -C 6 alkoxy, C 1 -C 3 alkyl carboxy, C 2 -C 3 alkenyl carboxy, C 2 -C 3 alkynyl carboxy, amino or R 4 and R 5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R 4 or R 5 is not a hydrogen or C 1 -C 6 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）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杂环，其中R 4或R 5中的至少一个不是氢或C 1 -C 6烷基。

7. 发明申请

WO2003037328A1 OXINDOLE HYDRAZIDE MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPS) 审中-公开
标题翻译：蛋白酪氨酸磷酸酯（PTPS）的氧化物水解调节剂
公开(公告)号：WO2003037328A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/011919
申请日：2002-10-24
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , BOMBRUN, Agnès , GERBER, Patrick , CHURCH, Dennis
发明人： BOMBRUN, Agnès , GERBER, Patrick , CHURCH, Dennis
IPC分类号： A61K31/404
CPC分类号： C07D257/04 , A61K31/404 , C07D209/38 , C07D209/40 , C07D211/62 , C07D295/096 , C07D307/68 , C07D317/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D513/04
摘要： The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.(I).
摘要翻译：本发明涉及式（I）的羟吲哚酰肼衍生物用于治疗和/或预防由胰岛素抵抗或高血糖介导的代谢紊乱的用途，包括I型和/或II型糖尿病，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，肥胖症，多囊卵巢综合征（PCOS）。特别地，本发明涉及式（I）的羟吲哚酰肼衍生物在特别是抑制PTP的活性，特别是PTP1B，TC-PTP，SHP和GLEPP-1的调节中的应用。本发明还涉及新型羟吲哚酰肼衍生物及其制备方法（I）。

8. 发明授权

EP1268418B1 PHARMACEUTICALLY ACTIVE PYRROLIDINE DERIVATIVES AS BAX INHIBITORS 有权
标题翻译：药学有效吡咯烷衍生物AS BAX抑制剂
公开(公告)号：EP1268418B1
公开(公告)日：2006-06-14
申请号：EP01925491.1
申请日：2001-03-20
申请人： Applied Research Systems ARS Holding N.V.
发明人： HALAZY, Serge , SCHWARZ, Matthias , QUATTROPANI, Anna , THOMAS, Russel , BAXTER, Anthony , BOMBRUN, Agnès
IPC分类号： C07D207/22 , C07D405/12 , C07D405/06 , C07D405/14 , C07D409/12 , C07D403/14 , C07D417/12 , C07D401/12 , C07D403/06 , C07D403/04 , A61K31/4025 , A61K31/401 , A61P25/00
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating - up to an inhibitory - activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CR?6R7, NOR6, NNR6R7¿; A is selected from the group consisting of -(C=O)-, -(C=O)-O-, -C(=NH)-, -(C=O)-NH-, -(C=S)-NH, -SO¿2?-, -SO2NH-; -CH2-; B is either a group -(C=O)-NR?8R9¿ or represents a heterocyclic residue having the formula (II) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.

9. 发明授权

EP1399156B1 ALKYLIDENE PIRAZOLIDINEDIONE DERIVATIVES AND THEIR USE FOR TREATING DIABETES AND OBESITY 有权
标题翻译：亚PIRAZOLIDINEDIONE衍生物及其预防糖尿病和diabesity
公开(公告)号：EP1399156B1
公开(公告)日：2006-11-22
申请号：EP02735418.2
申请日：2002-06-14
申请人： Applied Research Systems ARS Holding N.V.
发明人： BOMBRUN, Agnès , RUECKLE, Thomas , SWINNEN, Dominique , GONZALEZ, Jérôme , CHURCH, Dennis
IPC分类号： A61K31/415 , A61P3/10 , A61P15/08 , C07D405/06
CPC分类号： C07D401/06 , A61K31/00 , A61K31/4155 , A61K31/4192 , C07D231/32 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要： The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.

10. 发明公开

EP1756081A1 1,1'-(1,2-ETHYNEDIYL)BIS-BENZENE DERIVATIVES AS PTP 1-B INHIBITORS 审中-公开
标题翻译：作为PTP 1-B抑制剂的1,1' - （1,2-乙烯基）双苯衍生物
公开(公告)号：EP1756081A1
公开(公告)日：2007-02-28
申请号：EP05717158.9
申请日：2005-03-29
申请人： Applied Research Systems ARS Holding N.V.
发明人： SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GERBER, Patrick , GONZALEZ, Jérôme , BOMBRUN, Agnès
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症和/或代谢病症的用途，其包含I型和/或II型糖尿病，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）的羧酸用于调节，特别是抑制PTP的活性。

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