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公开(公告)号：US09758527B2
公开(公告)日：2017-09-12
申请号：US15307719
申请日：2015-05-01
发明人： Jin Yang , Jinwoong Kim , Han Kyu Lee , Jae Hyun Kim , Chang Mo Son , Kyu Hwan Lee , Jeongun Hwang , Hyung-Ho Choi , Daehoon Kim , Jaekeol Rhee
IPC分类号： C07D491/113 , C07D211/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D487/10
CPC分类号： C07D491/113 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/62 , C07D211/72 , C07D211/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D487/10
摘要： The present invention relates to: a cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.
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公开(公告)号：US10821110B2
公开(公告)日：2020-11-03
申请号：US15511955
申请日：2015-10-16
发明人： Jin Yang , Jin Woong Kim , Han Kyu Lee , Jae Hyun Kim , Chang Mo Son , Kyu Hwan Lee , Hyung-Ho Choi , Daehoon Kim , Tae-Young Ha , Jaekeol Rhee
IPC分类号： A61K31/506 , A61K9/00 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/132 , A61K31/357 , A61K31/40 , A61K31/4035 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/47 , A61K31/495 , A61K31/496 , A61K45/06 , C07C59/72 , C07D207/06 , C07D209/44 , C07D211/14 , C07D211/70 , C07D215/06 , C07D295/096 , C07D317/72 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/192
摘要： The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.
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公开(公告)号：US09969723B2
公开(公告)日：2018-05-15
申请号：US14872745
申请日：2015-10-01
发明人： Jin Yang , Jin Woong Kim , Han Kyu Lee , Jae Hyun Kim , Chang Mo Son , kyu hwan Lee , Hyung-Ho Choi , daehoon Kim , Tae-Young Ha , Jaekeol Rhee
IPC分类号： A61K31/497 , C07D413/04 , C07D213/85 , C07D215/06 , C07D217/04 , C07D221/20 , C07D317/72 , C07D239/42 , C07D271/07 , C07D277/82 , C07D209/44 , C07D211/14 , C07D295/073 , C07D295/096 , C07C51/367 , C07C51/373 , C07C59/72 , C07C59/90 , C07D207/06 , C07D211/70 , C07D213/74 , C07D215/04 , C07D217/24 , C07D239/28 , C07D295/155
CPC分类号： C07D413/04 , C07C51/367 , C07C51/373 , C07C59/72 , C07C59/90 , C07D207/06 , C07D209/44 , C07D211/14 , C07D211/70 , C07D213/74 , C07D213/85 , C07D215/04 , C07D215/06 , C07D217/04 , C07D217/24 , C07D221/20 , C07D239/28 , C07D239/42 , C07D271/07 , C07D277/82 , C07D295/073 , C07D295/096 , C07D295/155 , C07D317/72
摘要： The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.
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4.发明申请NOVEL 3-(4(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING METABOLIC DISEASE INCLUDING SAME AS EFFECTIVE INGREDIENT 有权新型3-（4（苄氧基）苯基）十四烷酸衍生物，其制备方法和用于预防和治疗包括其有效成分的代谢疾病的药物组合物公开(公告)号：US20160024063A1
公开(公告)日：2016-01-28
申请号：US14872745
申请日：2015-10-01
发明人： Jin Yang , Jin Woong Kim , Han Kyu Lee , Jae Hyun Kim , Chang Mo Son , kyu hwan Lee , Hyung-Ho Choi , daehoon Kim , Tae-Young Ha , Jaekeol Rhee
IPC分类号： C07D413/04 , C07C59/90 , C07C59/72 , C07D209/44 , C07D211/70 , C07D295/096 , C07D271/07 , C07D217/04 , C07D295/155 , C07D217/24 , C07D211/14 , C07D215/04 , C07D277/82 , C07D239/28 , C07D213/74 , C07D207/06 , C07C51/373 , C07C51/367 , C07D317/72
CPC分类号： C07D413/04 , C07C51/367 , C07C51/373 , C07C59/72 , C07C59/90 , C07D207/06 , C07D209/44 , C07D211/14 , C07D211/70 , C07D213/74 , C07D213/85 , C07D215/04 , C07D215/06 , C07D217/04 , C07D217/24 , C07D221/20 , C07D239/28 , C07D239/42 , C07D271/07 , C07D277/82 , C07D295/073 , C07D295/096 , C07D295/155 , C07D317/72
摘要： The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.
摘要翻译： 本发明涉及一种新型的3-（4-（苄氧基）苯基）己-4-烯酸衍生物及其制备方法，以及包含其作为预防和治疗代谢性疾病的活性成分的药物组合物。 本发明的新型3-（4-（苄氧基）苯基）己-4-烯酸衍生物，其旋光异构体或其药学上可接受的盐具有优异的活化GPR40蛋白并相应地促进胰岛素分泌，但没有 与其他药物共同给药时的毒性。 也就是说，本发明的新型3-（4-（苄氧基）苯基）己-4-烯酸衍生物，其旋光异构体或其药学上可接受的盐可以与其它药物共同给药， 可以显着地激活GPR40蛋白质，使得包含与活性成分相同的组合物可以有效地用作预防和治疗代谢疾病如肥胖症，I型糖尿病，II型糖尿病，不相容的葡萄糖耐量，胰岛素 高血糖症，高脂血症，高甘油三酯血症，高胆固醇血症，血脂异常，X综合征等。
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