JP2019511564A5 - - Google Patents
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- JP2019511564A5 JP2019511564A5 JP2018560435A JP2018560435A JP2019511564A5 JP 2019511564 A5 JP2019511564 A5 JP 2019511564A5 JP 2018560435 A JP2018560435 A JP 2018560435A JP 2018560435 A JP2018560435 A JP 2018560435A JP 2019511564 A5 JP2019511564 A5 JP 2019511564A5
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- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- atom bonded
- compound
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052799 carbon Inorganic materials 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 15
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 15
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- -1 nitro, cyano, amino Chemical group 0.000 claims 12
- 201000011510 cancer Diseases 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 102000001253 Protein Kinases Human genes 0.000 claims 9
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 8
- 108060006633 Protein Kinases Proteins 0.000 claims 8
- 102100004939 PDGFRB Human genes 0.000 claims 6
- 101710018346 PDGFRB Proteins 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 6
- 102000003989 Aurora Kinases Human genes 0.000 claims 5
- 108090000433 Aurora Kinases Proteins 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 102100019002 ABL1 Human genes 0.000 claims 4
- 101700000782 ABL1 Proteins 0.000 claims 4
- 101710019578 BZIP46 Proteins 0.000 claims 4
- 101700035468 LYN Proteins 0.000 claims 4
- 206010025650 Malignant melanoma Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 102100015703 BLK Human genes 0.000 claims 3
- 101700039697 BLK Proteins 0.000 claims 3
- 102100005175 CSF1R Human genes 0.000 claims 3
- 101700063802 CSF1R Proteins 0.000 claims 3
- 102100006837 DDR1 Human genes 0.000 claims 3
- 101700058746 DDR1 Proteins 0.000 claims 3
- 102100004573 FLT3 Human genes 0.000 claims 3
- 102100013182 FLT4 Human genes 0.000 claims 3
- 101710030894 FLT4 Proteins 0.000 claims 3
- 102100013180 KDR Human genes 0.000 claims 3
- 102000002576 MAP Kinase Kinase 1 Human genes 0.000 claims 3
- 108010068342 MAP Kinase Kinase 1 Proteins 0.000 claims 3
- 101710009384 SRC Proteins 0.000 claims 3
- 102000001332 SRC Human genes 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 108091007928 VEGF receptors Proteins 0.000 claims 3
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 3
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 3
- 108010003374 fms-Like Tyrosine Kinase 3 Proteins 0.000 claims 3
- 125000004430 oxygen atoms Chemical group O* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims 2
- 206010004593 Bile duct cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 102100000359 FGR Human genes 0.000 claims 2
- 101700006624 FGR Proteins 0.000 claims 2
- 102200039431 FLT3 D835Y Human genes 0.000 claims 2
- 206010017758 Gastric cancer Diseases 0.000 claims 2
- 208000003884 Gestational Trophoblastic Disease Diseases 0.000 claims 2
- 206010073071 Hepatocellular carcinoma Diseases 0.000 claims 2
- 206010020243 Hodgkin's disease Diseases 0.000 claims 2
- 206010021042 Hypopharyngeal cancer Diseases 0.000 claims 2
- 208000000429 Leukemia, Lymphocytic, Chronic, B-Cell Diseases 0.000 claims 2
- 208000008456 Leukemia, Myelogenous, Chronic, BCR-ABL Positive Diseases 0.000 claims 2
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 102100016102 NTRK1 Human genes 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010031096 Oropharyngeal cancer Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000007452 Plasmacytoma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 102200006097 RET V804L Human genes 0.000 claims 2
- 102200006095 RET Y791F Human genes 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010046766 Uterine cancer Diseases 0.000 claims 2
- 206010047802 Waldenstrom's macroglobulinaemias Diseases 0.000 claims 2
- 201000005510 acute lymphocytic leukemia Diseases 0.000 claims 2
- 125000005418 aryl aryl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 201000006934 chronic myeloid leukemia Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000002124 endocrine Effects 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 201000010175 gallbladder cancer Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 201000006866 hypopharynx cancer Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 2
- 201000005831 male reproductive organ cancer Diseases 0.000 claims 2
- 201000009251 multiple myeloma Diseases 0.000 claims 2
- 201000003793 myelodysplastic syndrome Diseases 0.000 claims 2
- 230000001537 neural Effects 0.000 claims 2
- 230000000955 neuroendocrine Effects 0.000 claims 2
- 201000006958 oropharynx cancer Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 201000002314 small intestine cancer Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 241000282324 Felis Species 0.000 claims 1
- 102000018473 Interleukin-1 Receptor-Like 1 Protein Human genes 0.000 claims 1
- 108010066572 Interleukin-1 Receptor-Like 1 Protein Proteins 0.000 claims 1
- 102100016985 KIT Human genes 0.000 claims 1
- 101710009391 KIT Proteins 0.000 claims 1
- 102100009453 LYN Human genes 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 210000004698 Lymphocytes Anatomy 0.000 claims 1
- 101700043017 NTRK1 Proteins 0.000 claims 1
- 108091007929 PDGF receptors Proteins 0.000 claims 1
- 108091000081 Phosphotransferases Proteins 0.000 claims 1
- 102000011653 Platelet-Derived Growth Factor Receptors Human genes 0.000 claims 1
- 102100009301 TPM3 Human genes 0.000 claims 1
- 101700003022 TPM3 Proteins 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 102100017976 YES1 Human genes 0.000 claims 1
- 101710044326 YES1 Proteins 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- 101700012475 kita Proteins 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 238000001890 transfection Methods 0.000 claims 1
- 230000003612 virological Effects 0.000 claims 1
- 0 Cc1cc(-c2cnc(Nc3nc(C)nc(N4CCN(CCI)CC4)c3)[s]2)ccc1NC(NC1=N*C(C2CC2)=C1)=O Chemical compound Cc1cc(-c2cnc(Nc3nc(C)nc(N4CCN(CCI)CC4)c3)[s]2)ccc1NC(NC1=N*C(C2CC2)=C1)=O 0.000 description 4
- HWTSERGWWBBNRB-UHFFFAOYSA-N CCc1cc(NC(Nc(cc2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 Chemical compound CCc1cc(NC(Nc(cc2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 HWTSERGWWBBNRB-UHFFFAOYSA-N 0.000 description 2
- AAZWOYHDKCZELR-UHFFFAOYSA-N CC(C)(C)c1cc(NC(Nc(cc2)c(C)cc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 Chemical compound CC(C)(C)c1cc(NC(Nc(cc2)c(C)cc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 AAZWOYHDKCZELR-UHFFFAOYSA-N 0.000 description 1
- QILCGQUUZGDEJE-UHFFFAOYSA-N CCCN(CC1)CCN1c1cc(Nc2ncc(-c(cc3C)ccc3NC(Nc3n[o]c(CC)c3)=O)[s]2)nc(SC)n1 Chemical compound CCCN(CC1)CCN1c1cc(Nc2ncc(-c(cc3C)ccc3NC(Nc3n[o]c(CC)c3)=O)[s]2)nc(SC)n1 QILCGQUUZGDEJE-UHFFFAOYSA-N 0.000 description 1
- UZLXIMKAXYTBNH-UHFFFAOYSA-N CCc1cc(NC(Nc(c(C)c2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 Chemical compound CCc1cc(NC(Nc(c(C)c2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 UZLXIMKAXYTBNH-UHFFFAOYSA-N 0.000 description 1
- PAPZQLQHTIAXCM-UHFFFAOYSA-N CCc1cc(NC(Nc(c(C)c2)ccc2-c2cnc(Nc3nc(SC)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 Chemical compound CCc1cc(NC(Nc(c(C)c2)ccc2-c2cnc(Nc3nc(SC)nc(N4CCN(CCO)CC4)c3)[s]2)=O)n[o]1 PAPZQLQHTIAXCM-UHFFFAOYSA-N 0.000 description 1
- LPHIYODDPREOBQ-UHFFFAOYSA-N CCc1cc(NC(Nc(cc2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCF)CC4)c3)[s]2)=O)n[o]1 Chemical compound CCc1cc(NC(Nc(cc2)ccc2-c2cnc(Nc3nc(C)nc(N4CCN(CCF)CC4)c3)[s]2)=O)n[o]1 LPHIYODDPREOBQ-UHFFFAOYSA-N 0.000 description 1
- TXBJBHBDLIYNMC-UHFFFAOYSA-N Cc(cc(cc1)-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)c1NC(Nc1n[o]c(C2CC2)c1)=O Chemical compound Cc(cc(cc1)-c2cnc(Nc3nc(C)nc(N4CCN(CCO)CC4)c3)[s]2)c1NC(Nc1n[o]c(C2CC2)c1)=O TXBJBHBDLIYNMC-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662291667P | 2016-02-05 | 2016-02-05 | |
US62/291,667 | 2016-02-05 | ||
PCT/US2017/015765 WO2017136315A1 (en) | 2016-02-05 | 2017-01-31 | Aminothiazole compounds and use thereof |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2019511564A JP2019511564A (ja) | 2019-04-25 |
JP2019511564A5 true JP2019511564A5 (US20040106767A1-20040603-C00005.png) | 2019-11-14 |
JP6883049B2 JP6883049B2 (ja) | 2021-06-02 |
Family
ID=59496120
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018560435A Active JP6883049B2 (ja) | 2016-02-05 | 2017-01-31 | アミノチアゾール化合物及びその使用 |
Country Status (9)
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2534335T3 (es) | 2010-05-20 | 2015-04-21 | Array Biopharma, Inc. | Compuestos macrocíclicos como inhibidores de la Trk cinasa |
DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
JP7061195B2 (ja) | 2018-01-18 | 2022-04-27 | アレイ バイオファーマ インコーポレイテッド | RETキナーゼ阻害剤としての置換ピラゾロ[3,4-d]ピリミジン化合物 |
EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
KR20210016397A (ko) | 2018-05-25 | 2021-02-15 | 에르덴 바놀루 | 신종 항암제 후보로서, 매우 강력한 tacc3 억제제 |
CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
JP2024518711A (ja) * | 2021-04-12 | 2024-05-02 | エーツーエー ファーマシューティカルズ インコーポレーテッド | 癌を処置するための組成物及び方法 |
WO2023183520A1 (en) | 2022-03-24 | 2023-09-28 | A2A Pharmaceuticals, Inc. | Compositions and methods for treating cancer |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3222619A1 (en) * | 1999-04-15 | 2017-09-27 | Bristol-Myers Squibb Holdings Ireland | Cyclic protein tyrosine kinase inhibitors |
WO2002050071A1 (en) * | 2000-12-21 | 2002-06-27 | Bristol-Myers Squibb Company | Thiazolyl inhibitors of tec family tyrosine kinases |
EP1558609A4 (en) * | 2002-10-30 | 2008-05-28 | Merck & Co Inc | KINASE INHIBITORS |
KR100919905B1 (ko) * | 2005-01-26 | 2009-10-06 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
KR101579999B1 (ko) | 2008-04-21 | 2015-12-23 | 타이젠 바이오테크놀러지 컴퍼니 리미티드 | 헤테로사이클릭 화합물 |
WO2010046780A2 (en) | 2008-10-22 | 2010-04-29 | Institut Pasteur Korea | Anti viral compounds |
WO2012020762A1 (ja) | 2010-08-10 | 2012-02-16 | アステラス製薬株式会社 | へテロ環化合物 |
US9255072B2 (en) * | 2011-03-04 | 2016-02-09 | National Health Rsearch Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
WO2013046136A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
CN104024246B (zh) * | 2012-03-27 | 2016-03-02 | 广东东阳光药业有限公司 | 作为欧若拉激酶抑制剂的取代嘧啶衍生物 |
-
2017
- 2017-01-26 TW TW106103165A patent/TWI620748B/zh active
- 2017-01-30 US US15/419,183 patent/US10047078B2/en active Active
- 2017-01-31 JP JP2018560435A patent/JP6883049B2/ja active Active
- 2017-01-31 KR KR1020187024997A patent/KR102449712B1/ko active IP Right Grant
- 2017-01-31 CN CN201780010118.4A patent/CN109069504B/zh active Active
- 2017-01-31 EP EP17747997.9A patent/EP3411035B1/en active Active
- 2017-01-31 WO PCT/US2017/015765 patent/WO2017136315A1/en active Application Filing
- 2017-01-31 ES ES17747997T patent/ES2909612T3/es active Active
-
2019
- 2019-01-22 HK HK19101067.5A patent/HK1258689A1/zh unknown