公开(公告)号：US10252996B2

公开(公告)日：2019-04-09

申请号：US15841971

申请日：2017-12-14

Applicant: Immunomet Therapeutics Inc.

Inventor： Chang Hee Min ,  Yong Eun Kim ,  Byung Kyu Oh ,  Ji Sun Lee ,  Hye Jin Heo ,  Ju Hoon Oh ,  Woong Cho

IPC: C07D207/20 ,  C07D211/14 ,  C07D211/16 ,  C07D211/70

Abstract: The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.

公开(公告)号：US20180093953A1

公开(公告)日：2018-04-05

申请号：US15569584

申请日：2015-04-30

Applicant: ImmunoMet Therapeutics Inc.

Inventor： Sung Wuk KIM ,  Hong Woo KIM ,  Sang Hee YOO ,  Ji Sun LEE ,  Hye Jin HEO ,  Hong Bum LEE ,  Ji Ae KOOK ,  Young Woo LEE

IPC: C07D211/38 ,  C07D277/04 ,  C07D207/10 ,  C07D221/20 ,  C07D209/52 ,  C07C279/26

CPC classification number: C07D211/38 ,  A61K31/155 ,  A61K31/40 ,  A61K31/44 ,  A61K45/06 ,  C07C279/26 ,  C07D207/10 ,  C07D209/52 ,  C07D221/20 ,  C07D277/04 ,  A61K2300/00

Abstract: The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

公开(公告)号：US20180044283A1

公开(公告)日：2018-02-15

申请号：US15527621

申请日：2015-11-20

Applicant: ImmunoMet Therapeutics Inc.

Inventor： Hong Woo KIM ,  Jae Kap JEONG ,  Ji Sun LEE ,  Hye Jin HEO ,  Hong Bum LEE ,  Ji Ae KOOK ,  Sung Wuk KIM

IPC: C07C279/26 ,  C07D211/10

CPC classification number: C07C279/26 ,  A61K31/155 ,  A61P35/00 ,  C07D211/10 ,  C07D211/34

Abstract: The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.

公开(公告)号：US20160317478A1

公开(公告)日：2016-11-03

申请号：US15206780

申请日：2016-07-11

Applicant: IMMUNOMET THERAPEUTICS INC.

Inventor： Sung Wuk Kim ,  Sung Soo Jun ,  Chang Hee Min ,  Young Woong Kim ,  Min Seok Kang ,  Byung Kyu Oh ,  Se Hwan Park ,  Yong Eun Kim ,  Duck Kim ,  Ji Sun Lee ,  Ju Hoon Oh

IPC: A61K31/155 ,  A61K31/341 ,  A61K31/472 ,  A61K31/4406

CPC classification number: A61K31/155 ,  A61K31/341 ,  A61K31/4406 ,  A61K31/472 ,  C07C277/04 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/16 ,  C07C279/18 ,  C07C279/26 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D213/38 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20

Abstract: A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPKα and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

Abstract translation: 提供了由式1表示的具有N1-N5取代的双胍衍生物化合物或其药学上可接受的盐的制备方法，以及含有其作为活性成分的药物组合物。 与常规药物相比，双胍衍生物可能对AMPKα的活化和低剂量的癌细胞增殖具有优异的作用，因此可用于治疗糖尿病，肥胖症，高脂血症，高胆固醇血症，脂肪肝，冠状动脉疾病 ，骨质疏松症，多囊卵巢综合征，代谢综合征，癌症等

公开(公告)号：US11572341B2

公开(公告)日：2023-02-07

申请号：US16820860

申请日：2020-03-17

Applicant: ImmunoMet Therapeutics Inc.

Inventor： Hong Woo Kim ,  Jae Kap Jeong ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Sung Wuk Kim

IPC: C07C279/26 ,  C07D211/10 ,  C07D211/34 ,  A61K31/155 ,  A61P35/00

Abstract: The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.

公开(公告)号：US20200038347A1

公开(公告)日：2020-02-06

申请号：US16480294

申请日：2018-01-23

Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY ,  IMMUNOMET THERAPEUTICS INC.

Inventor： Jungsik SONG ,  Beom Seok KIM ,  Sang Jun HA ,  Ji Min SON

IPC: A61K31/155 ,  A61K31/436

Abstract: Provided are a pharmaceutical composition for preventing or treating inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof, the pharmaceutical composition including a compound represented by Formula 1, or a stereoisomer, derivative, solvate, or pharmaceutically acceptable salt thereof, and a method using the pharmaceutical composition. The pharmaceutical composition and the method can be used to effectively prevent or treat inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof.

公开(公告)号：US10376480B2

公开(公告)日：2019-08-13

申请号：US15976613

申请日：2018-05-10

Applicant: Immunomet Therapeutics Inc.

Inventor： Sung Wuk Kim ,  Sung Soo Jun ,  Chang Hee Min ,  Young Woong Kim ,  Min Seok Kang ,  Byung Kyu Oh ,  Se Hwan Park ,  Yong Eun Kim ,  Duck Kim ,  Ji Sun Lee ,  Ju Hoon Oh

IPC: A61K31/155 ,  A61K31/341 ,  A61K31/472 ,  C07C277/04 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/16 ,  C07C279/18 ,  C07C279/26 ,  C07D213/38 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  A61K31/4406

Abstract: A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPKα and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

公开(公告)号：US20170073331A1

公开(公告)日：2017-03-16

申请号：US15304798

申请日：2015-04-17

Applicant: IMMUNOMET THERAPEUTICS INC.

Inventor： Sung Wuk Kim ,  Hong Woo Kim ,  Sang Hee Yoo ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Young Woo Lee ,  Mi Jeong Kim ,  Woong Cho

IPC: C07D403/12 ,  C07C311/47 ,  C07D295/13 ,  C07D211/14 ,  C07D319/18 ,  C07D333/20 ,  C07D251/18 ,  C07D249/14 ,  C07D211/54 ,  C07C279/04 ,  C07C279/08 ,  C07D209/44 ,  C07C279/16 ,  C07C279/06 ,  C07D233/91 ,  C07D213/38 ,  C07C279/12 ,  C07D239/42 ,  C07C279/24 ,  C07D207/16 ,  C07D277/46 ,  C07D263/48 ,  C07C279/26

CPC classification number: C07D403/12 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/12 ,  C07C279/16 ,  C07C279/24 ,  C07C279/26 ,  C07C311/47 ,  C07C311/49 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74 ,  C07D207/16 ,  C07D209/40 ,  C07D209/44 ,  C07D211/14 ,  C07D211/54 ,  C07D213/38 ,  C07D213/40 ,  C07D233/88 ,  C07D233/91 ,  C07D239/42 ,  C07D249/14 ,  C07D251/18 ,  C07D251/48 ,  C07D263/48 ,  C07D277/46 ,  C07D295/13 ,  C07D317/58 ,  C07D319/18 ,  C07D333/16 ,  C07D333/20

Abstract: The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

Abstract translation: 本发明涉及用于抑制线粒体氧化磷酸化（OXPHOS）的胍化合物及其应用。 更具体地，本发明涉及通过抑制线粒体氧化磷酸化和重新编程细胞代谢来预防或治疗OXPHOS相关疾病，特别是癌症的药物组合物。

公开(公告)号：US20160331724A1

公开(公告)日：2016-11-17

申请号：US15154788

申请日：2016-05-13

Applicant: ImmunoMet Therapeutics, Inc.

Inventor： Seok Gu Kang ,  Ji Hyun Lee ,  Jong Hee Chang ,  Jae Ho Cheong ,  Jun Jeong Choi ,  Sung Wuk Kim ,  Sang Hee Yoo ,  Hong Woo Kim ,  Soon Im Lee

IPC: A61K31/40 ,  A61K31/495

CPC classification number: A61K31/40 ,  A61K31/402 ,  A61K31/495 ,  A61K2300/00

Abstract: The present invention provides novel uses of a biguanide derivative for preventing or treating glioblastoma. The compound of Formula 1 and its pharmaceutically acceptable salts can be used for preventing and treating glioblastoma. Further, the combined treatment of the compound of Formula 1 and temozolomide can provide superior effects compared to the administration of the compound of Formula alone or temozolomide alone.

Abstract translation: 本发明提供双胍衍生物预防或治疗胶质母细胞瘤的新用途。 式1的化合物及其药学上可接受的盐可用于预防和治疗胶质母细胞瘤。 此外，与单独给予化合物或单独使用替莫唑胺相比，式1化合物和替莫唑胺的联合治疗可以提供优异的效果。

公开(公告)号：US11826324B2

公开(公告)日：2023-11-28

申请号：US17126478

申请日：2020-12-18

Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY ,  IMMUNOMET THERAPEUTICS INC.

Inventor： Jungsik Song ,  Beom Seok Kim ,  Sang Jun Ha ,  Ji Min Son

IPC: A61K31/155 ,  A61K31/436 ,  A61K31/40

CPC classification number: A61K31/155 ,  A61K31/40 ,  A61K31/436

Abstract: Provided are a pharmaceutical composition for preventing or treating inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof, the pharmaceutical composition including a compound represented by Formula 1, or a stereoisomer, derivative, solvate, or pharmaceutically acceptable salt thereof, and a method using the pharmaceutical composition. The pharmaceutical composition and the method can be used to effectively prevent or treat inflammatory disease, autoimmune disease, graft rejection responses, or combinations thereof.