JPWO2020061086A5 - - Google Patents
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- Publication number
- JPWO2020061086A5 JPWO2020061086A5 JP2021539486A JP2021539486A JPWO2020061086A5 JP WO2020061086 A5 JPWO2020061086 A5 JP WO2020061086A5 JP 2021539486 A JP2021539486 A JP 2021539486A JP 2021539486 A JP2021539486 A JP 2021539486A JP WO2020061086 A5 JPWO2020061086 A5 JP WO2020061086A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- cycloalkyl
- pharmaceutically acceptable
- acceptable salt
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- -1 4-ethoxyphenyl Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 4
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 4
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 4
- 229960002448 dasatinib Drugs 0.000 claims 4
- 229960002411 imatinib Drugs 0.000 claims 4
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 4
- 208000032839 leukemia Diseases 0.000 claims 4
- 229960001346 nilotinib Drugs 0.000 claims 4
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 239000003840 Bafetinib Substances 0.000 claims 3
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 3
- 239000002145 L01XE14 - Bosutinib Substances 0.000 claims 3
- 239000002137 L01XE24 - Ponatinib Substances 0.000 claims 3
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229950002365 bafetinib Drugs 0.000 claims 3
- ZGBAJMQHJDFTQJ-DEOSSOPVSA-N bafetinib Chemical compound C1[C@@H](N(C)C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=NC=3)C(C)=CC=2)C=C1C(F)(F)F ZGBAJMQHJDFTQJ-DEOSSOPVSA-N 0.000 claims 3
- 229960003736 bosutinib Drugs 0.000 claims 3
- UBPYILGKFZZVDX-UHFFFAOYSA-N bosutinib Chemical compound C1=C(Cl)C(OC)=CC(NC=2C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=CC=2C#N)=C1Cl UBPYILGKFZZVDX-UHFFFAOYSA-N 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 229960001131 ponatinib Drugs 0.000 claims 3
- PHXJVRSECIGDHY-UHFFFAOYSA-N ponatinib Chemical compound C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 PHXJVRSECIGDHY-UHFFFAOYSA-N 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- VVQNAFBGAWCMLU-UHFFFAOYSA-N 1h-benzimidazole-4-carboxylic acid Chemical compound OC(=O)C1=CC=CC2=C1N=CN2 VVQNAFBGAWCMLU-UHFFFAOYSA-N 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002255 enzymatic effect Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 102000037865 fusion proteins Human genes 0.000 claims 1
- 108020001507 fusion proteins Proteins 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 238000011301 standard therapy Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 208000016595 therapy related acute myeloid leukemia and myelodysplastic syndrome Diseases 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024227127A JP2025066704A (ja) | 2018-09-18 | 2024-12-24 | 特定の白血病を治療するための化合物 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862733029P | 2018-09-18 | 2018-09-18 | |
| US62/733,029 | 2018-09-18 | ||
| US201962816637P | 2019-03-11 | 2019-03-11 | |
| US62/816,637 | 2019-03-11 | ||
| US201962889929P | 2019-08-21 | 2019-08-21 | |
| US62/889,929 | 2019-08-21 | ||
| PCT/US2019/051567 WO2020061086A2 (en) | 2018-09-18 | 2019-09-17 | Compounds for treating certain leukemias |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024227127A Division JP2025066704A (ja) | 2018-09-18 | 2024-12-24 | 特定の白血病を治療するための化合物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022501429A JP2022501429A (ja) | 2022-01-06 |
| JP2022501429A5 JP2022501429A5 (https=) | 2022-09-27 |
| JPWO2020061086A5 true JPWO2020061086A5 (https=) | 2022-09-27 |
| JP7611832B2 JP7611832B2 (ja) | 2025-01-10 |
Family
ID=69774840
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021539486A Active JP7611832B2 (ja) | 2018-09-18 | 2019-09-17 | 特定の白血病を治療するための化合物 |
| JP2024227127A Pending JP2025066704A (ja) | 2018-09-18 | 2024-12-24 | 特定の白血病を治療するための化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024227127A Pending JP2025066704A (ja) | 2018-09-18 | 2024-12-24 | 特定の白血病を治療するための化合物 |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US10889571B2 (https=) |
| EP (1) | EP3852745A4 (https=) |
| JP (2) | JP7611832B2 (https=) |
| KR (2) | KR20210061377A (https=) |
| CN (3) | CN112770745B (https=) |
| AU (2) | AU2019342102C1 (https=) |
| BR (1) | BR112021004051A2 (https=) |
| CA (1) | CA3110576A1 (https=) |
| CL (1) | CL2021000637A1 (https=) |
| CO (1) | CO2021004704A2 (https=) |
| IL (2) | IL281427B2 (https=) |
| MA (1) | MA53664A (https=) |
| MX (2) | MX2021003093A (https=) |
| NZ (1) | NZ773110A (https=) |
| PE (2) | PE20252740A1 (https=) |
| SG (1) | SG11202102367TA (https=) |
| TW (1) | TWI826525B (https=) |
| WO (1) | WO2020061086A2 (https=) |
| ZA (1) | ZA202101304B (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL281427B2 (en) | 2018-09-18 | 2026-01-01 | Terns Inc | Compounds that inhibit tyrosine kinase activity for use in the treatment of leukemia |
| JP7640458B2 (ja) | 2018-10-05 | 2025-03-05 | アンナプルナ バイオ インコーポレイテッド | Apj受容体活性に関連する状態を処置するための化合物および組成物 |
| CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| US11149009B2 (en) | 2019-03-11 | 2021-10-19 | Inflarx Gmbh | Fused piperidinyl bicyclic and related compounds as modulators of C5A receptor |
| WO2021018194A1 (en) * | 2019-07-29 | 2021-02-04 | Ascentage Pharma (Suzhou) Co., Ltd. | Heterocyclic compounds as bcr-abl inhibitors |
| AU2020336272A1 (en) | 2019-08-23 | 2022-04-14 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| CN114375193B (zh) | 2019-09-12 | 2024-05-14 | 拓臻制药公司 | 甲状腺激素受体β激动剂化合物 |
| CA3212130A1 (en) * | 2021-03-03 | 2022-09-09 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| CN116375650B (zh) * | 2022-12-30 | 2025-08-05 | 浙江美诺华药物化学有限公司 | 一种替戈拉生中间体的制备方法 |
| US20240398794A1 (en) | 2023-04-07 | 2024-12-05 | Terns Pharmaceuticals, Inc. | COMBINATIONS OF GLP-1R AND THRß AGONISTS AND METHODS OF USE THEREOF |
| TW202525293A (zh) * | 2023-08-31 | 2025-07-01 | 美商拓臻製藥公司 | 用於治療癌症之組合 |
| WO2025226724A1 (en) * | 2024-04-23 | 2025-10-30 | Terns Pharmaceuticals, Inc. | Bcr-abl1 inhibitors for use in treating cancer |
| CN120842151A (zh) * | 2024-04-26 | 2025-10-28 | 北京英飞智药科技有限公司 | 一种2-芳基苯并咪唑类化合物及其制备方法与应用 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2236220C2 (ru) | 1998-05-22 | 2004-09-20 | Аванир Фармасьютикэлз | Аналоги бензимидазола в качестве понижающих регуляторов ige |
| SE0003476D0 (sv) | 2000-09-28 | 2000-09-28 | Astrazeneca Ab | Compounds |
| TW200304820A (en) * | 2002-03-25 | 2003-10-16 | Avanir Pharmaceuticals | Use of benzimidazole analogs in the treatment of cell proliferation |
| PE20061378A1 (es) * | 2005-04-20 | 2006-12-03 | Smithkline Beecham Corp | INHIBIDORES DE LA ACTIVIDAD DE Akt |
| AR063311A1 (es) * | 2006-10-18 | 2009-01-21 | Novartis Ag | Compuestos organicos |
| CN101553468A (zh) * | 2006-10-18 | 2009-10-07 | 诺瓦提斯公司 | 有机化合物 |
| GB0800035D0 (en) | 2008-01-02 | 2008-02-13 | Glaxo Group Ltd | Compounds |
| WO2013033093A1 (en) | 2011-08-29 | 2013-03-07 | Biocryst Pharmaceuticals, Inc. | Heterocyclic compounds as janus kinase inhibitors |
| KR20150008406A (ko) | 2012-05-15 | 2015-01-22 | 노파르티스 아게 | Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체 |
| PT2861579T (pt) | 2012-05-15 | 2018-04-27 | Novartis Ag | Derivados de benzamida para inibir a atividade de abl1, abl2 e bcr-abl |
| WO2013171641A1 (en) | 2012-05-15 | 2013-11-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of abl1, abl2 and bcr-abl1 |
| US9550737B2 (en) | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
| CN103113355B (zh) | 2013-02-27 | 2014-08-13 | 无锡爱内特生物科技有限公司 | 一种Bcr/Abl酪氨酸激酶抑制剂及其制备方法和在治疗慢性粒细胞白血病中的应用 |
| GB201401086D0 (en) | 2014-01-23 | 2014-03-12 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| US9931342B2 (en) | 2016-02-02 | 2018-04-03 | Duke University | Compositions and methods for the treatment of cancer |
| JP2019515932A (ja) | 2016-04-29 | 2019-06-13 | アスター バイオテック リミテッド ライアビリティ カンパニー | チロシンキナーゼbcr−abl阻害剤としての新規複素環化合物 |
| US11091462B2 (en) | 2017-01-20 | 2021-08-17 | Shenzhen Targetrx, Inc. | (Hetero)arylamide compound for inhibiting protein kinase activity |
| US10875853B2 (en) | 2017-01-20 | 2020-12-29 | Shenzhen Targetrx, Inc. | (Hetero)arylamide compound for inhibiting protein kinase activity |
| WO2018191146A1 (en) * | 2017-04-10 | 2018-10-18 | Navitor Pharmaceuticals, Inc. | Heteroaryl rheb inhibitors and uses thereof |
| WO2019173761A1 (en) | 2018-03-09 | 2019-09-12 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | C-abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same |
| IL281427B2 (en) | 2018-09-18 | 2026-01-01 | Terns Inc | Compounds that inhibit tyrosine kinase activity for use in the treatment of leukemia |
| US20240262842A1 (en) | 2021-04-27 | 2024-08-08 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant |
| WO2023051681A1 (zh) | 2021-09-30 | 2023-04-06 | 江苏豪森药业集团有限公司 | 四元稠环类化合物及其制备方法和应用 |
| KR20260004344A (ko) | 2023-03-30 | 2026-01-08 | 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 | 4차 융합 고리 화합물의 염 결정 형태, 및 이의 제조 방법 및 이의 용도 |
| TW202525293A (zh) | 2023-08-31 | 2025-07-01 | 美商拓臻製藥公司 | 用於治療癌症之組合 |
-
2019
- 2019-09-17 IL IL281427A patent/IL281427B2/en unknown
- 2019-09-17 MA MA053664A patent/MA53664A/fr unknown
- 2019-09-17 SG SG11202102367TA patent/SG11202102367TA/en unknown
- 2019-09-17 EP EP19862388.6A patent/EP3852745A4/en active Pending
- 2019-09-17 KR KR1020217011001A patent/KR20210061377A/ko active Pending
- 2019-09-17 BR BR112021004051-0A patent/BR112021004051A2/pt unknown
- 2019-09-17 PE PE2025001942A patent/PE20252740A1/es unknown
- 2019-09-17 MX MX2021003093A patent/MX2021003093A/es unknown
- 2019-09-17 CA CA3110576A patent/CA3110576A1/en active Pending
- 2019-09-17 IL IL322515A patent/IL322515A/en unknown
- 2019-09-17 PE PE2021000343A patent/PE20211644A1/es unknown
- 2019-09-17 KR KR1020267002852A patent/KR20260019669A/ko active Pending
- 2019-09-17 CN CN201980060896.3A patent/CN112770745B/zh active Active
- 2019-09-17 NZ NZ773110A patent/NZ773110A/en unknown
- 2019-09-17 CN CN202210968772.9A patent/CN115215838B/zh active Active
- 2019-09-17 AU AU2019342102A patent/AU2019342102C1/en active Active
- 2019-09-17 US US16/573,860 patent/US10889571B2/en active Active
- 2019-09-17 JP JP2021539486A patent/JP7611832B2/ja active Active
- 2019-09-17 CN CN202210969394.6A patent/CN115448908B/zh active Active
- 2019-09-17 TW TW108133432A patent/TWI826525B/zh active
- 2019-09-17 WO PCT/US2019/051567 patent/WO2020061086A2/en not_active Ceased
-
2021
- 2021-02-25 ZA ZA2021/01304A patent/ZA202101304B/en unknown
- 2021-03-16 CL CL2021000637A patent/CL2021000637A1/es unknown
- 2021-03-16 MX MX2023007714A patent/MX2023007714A/es unknown
- 2021-04-15 CO CONC2021/0004704A patent/CO2021004704A2/es unknown
-
2023
- 2023-06-22 US US18/339,516 patent/US12240835B2/en active Active
-
2024
- 2024-12-20 AU AU2024287115A patent/AU2024287115A1/en active Pending
- 2024-12-24 JP JP2024227127A patent/JP2025066704A/ja active Pending
-
2025
- 2025-01-30 US US19/041,557 patent/US20250276961A1/en active Pending
- 2025-03-06 US US19/072,824 patent/US12454524B2/en active Active
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