公开(公告)号：US20220213051A1

公开(公告)日：2022-07-07

申请号：US17613983

申请日：2020-05-29

Applicant: HYUNDAI PHARM CO., LTD.

Inventor： Jeong Un HWANG ,  Jin Woong KIM ,  Kyu Hwan LEE ,  Eun Young KIM ,  Su Kyoung CHOI

IPC: C07D317/72

Abstract: The present invention relates to a novel crystal form of a 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method therefore and a pharmaceutical composition comprising same. A crystal form I of a compound of chemical formula 1, according to the present invention, exhibits more excellent physicochemical properties such as thermal stability, static electricity-inducing capability, compressibility, etc. compared to an amorphous form or a crystal form II, and thus is especially useful for preparation and long-term storage.

公开(公告)号：US09758527B2

公开(公告)日：2017-09-12

申请号：US15307719

申请日：2015-05-01

Applicant: HYUNDAI PHARM CO., LTD.

Inventor： 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: C07D491/113 ,  C07D211/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D487/10

CPC classification number: 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

Abstract: 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.

公开(公告)号：US10723699B2

公开(公告)日：2020-07-28

申请号：US15771909

申请日：2016-10-31

Applicant: Hyundai Pharm Co., Ltd.

Inventor： Jin Yang ,  Jin Woong Kim ,  Han Kyu Lee ,  Jae Hyun Kim ,  Chang Mo Son ,  Kyu Hwan Lee ,  Jeong Un Hwang ,  Hyung Ho Choi ,  Dae Hoon Kim ,  Jae Keol Rhee

IPC: C07D211/22 ,  C07D405/12 ,  C07D401/14 ,  C07D491/113 ,  C07D401/04 ,  C07D413/14 ,  C07D413/04 ,  C07D401/12 ,  C07D487/10 ,  A61P3/06 ,  A61P3/04

Abstract: The present invention relates to a cyclohexene derivative, a preparation method thereof, and a pharmaceutical composition for preventing or treating metabolic disease containing the cyclohexene derivative 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.

公开(公告)号：US20160355483A1

公开(公告)日：2016-12-08

申请号：US15244821

申请日：2016-08-23

Applicant: Hyundai Pharm Co., Ltd.

Inventor： In Hee LEE ,  Hee Il CHAE ,  Se hoan KIM ,  Soon Young MOON ,  Tae Young HA ,  Hyo sun CHOI ,  Young Seok KIM ,  Chun hwa KIM ,  Jae Keol RHEE

IPC: C07D215/48 ,  C07D401/12 ,  C07D405/12 ,  C07D265/36 ,  C07D413/12

CPC classification number: C07D215/48 ,  C07D265/36 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

Abstract: The present invention relates to a compound inhibiting CDK5-mediated PPARG phosphorylation and a pharmaceutical composition for treating PPARG-related diseases containing the same as an active ingredient. A compound represented by formula 1 or an optical isomer thereof according to the present invention that binds to PPARG at a high affinity level, but does not act as an agonist, thereby inducing no gene transcription; blocks CDK5, which is a cause of PPARG phosphorylation, thereby causing no side effects of existing anti-diabetic drugs; can be formulated into drugs due to improved pharmacological properties thereof; and can be favorably used as a pharmaceutical composition for treating PPARG-related diseases due to favorable treatment effects on PPARG-related diseases.

Abstract translation: 本发明涉及一种抑制CDK5介导的PPARG磷酸化合物的化合物和用于治疗含有其作为活性成分的PPARG相关疾病的药物组合物。 由式1表示的化合物或其根据本发明的光学异构体以高亲和力水平与PPARG结合但不作为激动剂，从而不诱导基因转录; 阻断CDK5，这是PPARG磷酸化的原因，从而不会引起现有抗糖尿病药物的副作用; 由于其药理学性质的改善，可以配制成药物; 并且由于对PPARG相关疾病的有利治疗作用，可以有利地用作治疗PPARG相关疾病的药物组合物。

公开(公告)号：US20240197674A1

公开(公告)日：2024-06-20

申请号：US18552988

申请日：2022-03-10

Applicant: Hyundai Pharm Co., Ltd.

Inventor： Hye Jin Yoo ,  Hwan Jin Hwang

IPC: A61K31/357 ,  A61P21/00

CPC classification number: A61K31/357 ,  A61P21/00

Abstract: A 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative according to the present invention promotes the expression of the myogenic factors MyoG and MyHC while inhibiting the expression of the muscle atrophy factor atrogin-1, promotes the formation of myotubes, and inhibits myocyte apoptosis, and thus can promote myogenesis and inhibit muscle atrophy.

公开(公告)号：US20230051318A1

公开(公告)日：2023-02-16

申请号：US17780486

申请日：2020-12-01

Applicant: HYUNDAI PHARM CO., LTD.

Inventor： Han Kyu LEE ,  Jeong-Un HWANG ,  Kyu-Hwan LEE ,  Hyung-Ho CHOI ,  Jung-In JANG ,  Hyuck-Joo LEE ,  Seung-Tae KANG ,  Hyun-Ho YOON ,  Neul HA ,  Hyun-Hwa LA ,  Jin Woong KIM ,  Dae Hoon KIM ,  Myoung Ki BAEK

IPC: C07D401/10 ,  C07D405/14 ,  C07D405/06 ,  C07D235/12 ,  C07D413/06 ,  C07D413/14 ,  C07D409/14 ,  C07D401/14

Abstract: The present invention relates to a compound represented by Formula 1 wherein A, B, L, X, and R1 to R6 are as described herein, or a pharmaceutically acceptable salt thereof, which serves as a GLP-1 receptor agonist and may be useful in the prevention or treatment of a disease associated with GLP-1 activity.

公开(公告)号：US10292955B2

公开(公告)日：2019-05-21

申请号：US14779927

申请日：2014-03-28

Applicant: HYUNDAI PHARM CO., LTD.

Inventor： Dong il Lee ,  Min ji Yoon ,  Pung Sok Lee

IPC: A61K31/195 ,  A61K9/00 ,  A61Q19/02 ,  A61K47/08 ,  A61K47/10 ,  A61K47/14 ,  A61K47/26 ,  A61K9/06 ,  A61K8/44 ,  A61Q19/00

Abstract: Provided is a skin external composition, which includes tranexamic acid or a salt thereof and a skin penetration enhancer, thereby showing remarkably increased skin permeability and improved sense of use, skin irritation, and storage stability.

公开(公告)号：US20180318274A1

公开(公告)日：2018-11-08

申请号：US15771909

申请日：2016-10-31

Applicant: Hyundai Pharm Co., Ltd.

Inventor： Jin YANG ,  Jin Woong KIM ,  Han Kyu LEE ,  Jae Hyun KIM ,  Chang Mo SON ,  Kyu Hwan LEE ,  Jeong Un HWANG ,  Hyung Ho CHOI ,  Dae Hoon KIM ,  Jae Keol RHEE

IPC: A61K31/4427 ,  A61P3/04 ,  A61P3/06 ,  A61P5/48

Abstract: The present invention relates to a cyclohexene derivative, a preparation method thereof, and a pharmaceutical composition for preventing or treating metabolic disease containing the cyclohexene derivative 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.

公开(公告)号：US20170296539A1

公开(公告)日：2017-10-19

申请号：US15511955

申请日：2015-10-16

Applicant: HYUNDAI PHARM CO., LTD.

Inventor： 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: A61K31/506 ,  A61K9/00 ,  C07D403/04 ,  C07D401/04 ,  C07D317/72 ,  C07D295/096 ,  C07D215/06 ,  C07D211/70 ,  C07D211/14 ,  C07D209/44 ,  C07D207/06 ,  C07C59/72 ,  A61K45/06 ,  A61K31/496 ,  A61K31/495 ,  A61K31/47 ,  A61K31/454 ,  A61K31/445 ,  A61K31/44 ,  A61K31/4035 ,  A61K31/40 ,  A61K31/357 ,  A61K31/192 ,  A61K9/48 ,  A61K9/20 ,  A61K9/14 ,  C07D413/04 ,  C07D417/04

Abstract: 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.

公开(公告)号：US20230227465A1

公开(公告)日：2023-07-20

申请号：US17759305

申请日：2021-01-29

Applicant: Hyundai Pharm Co., Ltd.

Inventor： Jeong Un Hwang ,  Kyu Hwan Lee ,  Eun Young Kim ,  Su Kyoung Choi

IPC: C07D493/10 ,  G01N30/88

CPC classification number: C07D493/10 ,  G01N30/88 ,  G01N2030/884 ,  G01N2030/045

Abstract: The present invention provides a related substance of (3S)-3-(4-(3-(1,4-dioxaspiro[4,5]dec-7-en-8-yl)benzyloxy)phenyl)hex-4-inoic acid, and a method for evaluating the quality of (3S)-3-(4-(3-(1,4-dioxaspiro[4,5]dec-7-en yl)benzyloxy)phenyl)hex-4-inoic acid using the same. According to the present invention, it is possible to evaluate the quality, stability and the like of a pharmaceutical composition comprising (3S)-3-(4-(3-(1,4-dioxaspiro[4,5]dec-7-en-8-yl)benzyloxy)phenyl)hex-4-inoic acid using a compound of Chemical Formula 2 or a salt thereof as a reference standard.