公开(公告)号：US20160317478A1

公开(公告)日：2016-11-03

申请号：US15206780

申请日：2016-07-11

申请人： IMMUNOMET THERAPEUTICS INC.

发明人： 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分类号： A61K31/155 ,  A61K31/341 ,  A61K31/472 ,  A61K31/4406

CPC分类号： 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

摘要： 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.

摘要翻译： 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：US10058558B2

公开(公告)日：2018-08-28

申请号：US14893433

申请日：2014-05-20

申请人： ImmunoMet Therapeutics Inc.

发明人： Sung Wuk Kim ,  Soon Im Lee ,  Yeon Jung Song ,  Min Jae Shin ,  Kook Hwan Oh ,  Kyung Don Ju ,  Eun Kyoung Shin ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Min Jeong Kim ,  Hye Soun Eum

IPC分类号： A61K31/165 ,  A61K31/55 ,  A61K31/155 ,  C07C279/26 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445

CPC分类号： A61K31/55 ,  A61K31/155 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  C07C279/26

摘要： The present invention provides a novel use of N1-cyclic amine-N5-substituted biguanide derivatives for preparing a medicine for preventing or treating fibrosis. The N1-cyclic amine-N5-substituted biguanide derivatives according to the present invention are capable of effectively inhibiting fibrosis by effectively suppressing the EMT.

公开(公告)号：US09539238B2

公开(公告)日：2017-01-10

申请号：US15154788

申请日：2016-05-13

申请人： ImmunoMet Therapeutics, Inc.

发明人： 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分类号： A01N43/52 ,  A61K31/40 ,  A61K31/495

CPC分类号： A61K31/40 ,  A61K31/402 ,  A61K31/495 ,  A61K2300/00

摘要： 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 1 alone or temozolomide alone.

摘要翻译： 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，与单独给予式1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：US20160101112A1

公开(公告)日：2016-04-14

申请号：US14893433

申请日：2014-05-20

申请人： IMMUNOMET THERAPEUTICS INC

发明人： Sung Wuk Kim ,  Soon Im Lee ,  Yeon Jung Song ,  Min Jae Shin ,  Kook Hwan Oh ,  Kyung Don Ju ,  Eun Kyoung Shin ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Min Jeong Kim ,  Hye Soun Eum

IPC分类号： A61K31/55 ,  A61K31/44 ,  A61K31/397 ,  A61K31/445 ,  A61K31/40

CPC分类号： A61K31/55 ,  A61K31/155 ,  A61K31/397 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  C07C279/26

摘要： The present invention provides a novel use of N1-cyclic amine-N5-substituted biguanide derivatives for preparing a medicine for preventing or treating fibrosis. The N1-cyclic amine-N5-substituted biguanide derivatives according to the present invention are capable of effectively inhibiting fibrosis by effectively suppressing the EMT.

摘要翻译： 本发明提供了N1环胺-N5取代双胍衍生物用于制备预防或治疗纤维化的药物的新用途。 根据本发明的N1环胺-N5取代双胍衍生物能够通过有效地抑制EMT而有效地抑制纤维化。

公开(公告)号：US11572341B2

公开(公告)日：2023-02-07

申请号：US16820860

申请日：2020-03-17

申请人： ImmunoMet Therapeutics Inc.

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

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

摘要： 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：US10376480B2

公开(公告)日：2019-08-13

申请号：US15976613

申请日：2018-05-10

申请人： Immunomet Therapeutics Inc.

发明人： 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分类号： 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

摘要： 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

申请人： IMMUNOMET THERAPEUTICS INC.

发明人： 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分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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

申请人： ImmunoMet Therapeutics, Inc.

发明人： 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分类号： A61K31/40 ,  A61K31/495

CPC分类号： A61K31/40 ,  A61K31/402 ,  A61K31/495 ,  A61K2300/00

摘要： 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.

摘要翻译： 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：US10590081B2

公开(公告)日：2020-03-17

申请号：US15569584

申请日：2015-04-30

申请人： ImmunoMet Therapeutics Inc.

发明人： 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分类号： C07D295/215 ,  C07D211/38 ,  C07C279/26 ,  C07D221/20 ,  C07D207/10 ,  C07D277/04 ,  C07D209/52 ,  A61K31/155 ,  A61K31/40 ,  A61K45/06 ,  A61K31/44

摘要： 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：US09993446B2

公开(公告)日：2018-06-12

申请号：US15206780

申请日：2016-07-11

申请人： IMMUNOMET THERAPEUTICS INC.

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

CPC分类号： 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

摘要： 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.