公开(公告)号：US20160289196A1

公开(公告)日：2016-10-06

申请号：US15083503

申请日：2016-03-29

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Kisoo PARK ,  Hee Jeong SEO ,  Eun-Jung PARK ,  Younggyu KONG ,  Ickhwan SON ,  Sang-ho MA ,  Kwang-Seop SONG ,  Min Ju KIM ,  So Ok PARK ,  Man-Young CHA ,  Mi-Soon KIM ,  Sang Mi KANG ,  Dong Hyuk JANG ,  Jangwon HONG

IPC: C07D231/56 ,  C07D409/12 ,  C07D495/04 ,  C07D409/14 ,  C07D401/12 ,  C07D413/12 ,  C07C53/18 ,  C07D417/12 ,  C07D403/12 ,  C07D413/14 ,  C07D405/12 ,  C07D409/04

CPC classification number: C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04

Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供吡唑衍生物作为TNIK（Traf2-和NCK相互作用激酶），IKKε（I-κB激酶ε）和TBK1（TANK结合激酶1）抑制剂; 根据本发明的吡唑衍生物有效地抑制TNIK，IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞肺 癌症，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌， 骨肉瘤，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。

公开(公告)号：US20160311772A1

公开(公告)日：2016-10-27

申请号：US15134987

申请日：2016-04-21

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Eun-Jung PARK ,  Hee Jeong SEO ,  Younggyu KONG ,  Ickhwan SON ,  Sang-ho MA ,  Man-Young CHA ,  Mi-Soon KIM ,  Kisoo PARK

IPC: C07D209/46 ,  C07D403/04 ,  C07D401/04 ,  C07D403/14 ,  C07D409/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D409/14 ,  C07D403/12 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  C07D217/24 ,  C07D401/12 ,  C07D417/04

CPC classification number: C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

Abstract: Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供作为TNIK（Traf2-和NCK相互作用激酶），IKKε（I-κB激酶ε）和TBK1（TANK结合激酶1）抑制剂的式（I）化合物; 根据本发明的化合物有效地抑制TNIK，IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞肺癌 ，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌，骨肉瘤 ，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。

公开(公告)号：US20160297815A1

公开(公告)日：2016-10-13

申请号：US15080068

申请日：2016-03-24

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Kwang-Seop SONG ,  Hee Jeong SEO ,  Sang-ho MA ,  Eun-Jung PARK ,  Younggyu KONG ,  So Ok PARK ,  Kisoo PARK ,  Ickhwan SON ,  Min Ju KIM ,  Man-Young CHA ,  Mi-Soon KIM ,  Sang Mi KANG ,  Dong Hyuk JANG ,  Jangwon HONG

IPC: C07D471/04 ,  C07D519/00 ,  C07D487/04 ,  C07C53/18

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供作为IKKε（I-kappa-B激酶ε）和TBK1（TANK结合激酶1）抑制剂的7-氮杂吲哚或4,7-二氮杂双环衍生物。 7-氮杂吲哚或4,7-二氮杂双环衍生物有效抑制IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞 肺癌，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌 ，骨肉瘤，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。