JPWO2021188769A5 - - Google Patents
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- JPWO2021188769A5 JPWO2021188769A5 JP2022556522A JP2022556522A JPWO2021188769A5 JP WO2021188769 A5 JPWO2021188769 A5 JP WO2021188769A5 JP 2022556522 A JP2022556522 A JP 2022556522A JP 2022556522 A JP2022556522 A JP 2022556522A JP WO2021188769 A5 JPWO2021188769 A5 JP WO2021188769A5
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- Prior art keywords
- alkyl
- group
- alkoxy
- haloalkyl
- halogen
- 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 description 147
- 125000003545 alkoxy group Chemical group 0.000 claims description 119
- 229910052736 halogen Inorganic materials 0.000 claims description 86
- 150000002367 halogens Chemical class 0.000 claims description 86
- 150000001875 compounds Chemical class 0.000 claims description 72
- 150000003839 salts Chemical class 0.000 claims description 62
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 57
- 239000012453 solvate Substances 0.000 claims description 44
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 43
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 43
- 229910052799 carbon Inorganic materials 0.000 claims description 43
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 35
- 125000001072 heteroaryl group Chemical group 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 22
- 229910052717 sulfur Inorganic materials 0.000 claims description 22
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 21
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 21
- 125000005842 heteroatom Chemical group 0.000 claims description 21
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000004043 oxo group Chemical group O=* 0.000 claims description 13
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 12
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 12
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims description 11
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims description 11
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 9
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims description 8
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 8
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 8
- 150000001721 carbon Chemical group 0.000 claims description 8
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims description 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 7
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- -1 C1-4alkoxyC1-4alkyl Chemical group 0.000 claims description 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 10
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 229910003827 NRaRb Inorganic materials 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 17
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 description 11
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- 229940124597 therapeutic agent Drugs 0.000 description 8
- 101000831007 Homo sapiens T-cell immunoreceptor with Ig and ITIM domains Proteins 0.000 description 6
- 102100024834 T-cell immunoreceptor with Ig and ITIM domains Human genes 0.000 description 6
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
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- 102000008096 B7-H1 Antigen Human genes 0.000 description 4
- 108010074708 B7-H1 Antigen Proteins 0.000 description 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 4
- 101000834898 Homo sapiens Alpha-synuclein Proteins 0.000 description 4
- 101000611936 Homo sapiens Programmed cell death protein 1 Proteins 0.000 description 4
- 101000652359 Homo sapiens Spermatogenesis-associated protein 2 Proteins 0.000 description 4
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- 102100040678 Programmed cell death protein 1 Human genes 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 description 4
- 125000003118 aryl group Chemical group 0.000 description 3
- 125000000753 cycloalkyl group Chemical group 0.000 description 3
- 230000005855 radiation Effects 0.000 description 3
- 102100029822 B- and T-lymphocyte attenuator Human genes 0.000 description 2
- 229940127272 CD73 inhibitor Drugs 0.000 description 2
- 102100039498 Cytotoxic T-lymphocyte protein 4 Human genes 0.000 description 2
- 102100034458 Hepatitis A virus cellular receptor 2 Human genes 0.000 description 2
- 101000864344 Homo sapiens B- and T-lymphocyte attenuator Proteins 0.000 description 2
- 101000889276 Homo sapiens Cytotoxic T-lymphocyte protein 4 Proteins 0.000 description 2
- 101001068133 Homo sapiens Hepatitis A virus cellular receptor 2 Proteins 0.000 description 2
- 101001137987 Homo sapiens Lymphocyte activation gene 3 protein Proteins 0.000 description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 description 2
- 102000017578 LAG3 Human genes 0.000 description 2
- 206010025323 Lymphomas Diseases 0.000 description 2
- 229930012538 Paclitaxel Natural products 0.000 description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 229940045799 anthracyclines and related substance Drugs 0.000 description 2
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 2
- 229960004562 carboplatin Drugs 0.000 description 2
- 229960004316 cisplatin Drugs 0.000 description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 2
- 229960004679 doxorubicin Drugs 0.000 description 2
- 208000032839 leukemia Diseases 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
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- 229960001756 oxaliplatin Drugs 0.000 description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 description 2
- 229960001592 paclitaxel Drugs 0.000 description 2
- 229910052697 platinum Inorganic materials 0.000 description 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 2
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- 239000002126 C01EB10 - Adenosine Substances 0.000 description 1
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- 229960005305 adenosine Drugs 0.000 description 1
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- 229960003852 atezolizumab Drugs 0.000 description 1
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- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
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- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062991952P | 2020-03-19 | 2020-03-19 | |
| US62/991,952 | 2020-03-19 | ||
| US202063120875P | 2020-12-03 | 2020-12-03 | |
| US63/120,875 | 2020-12-03 | ||
| PCT/US2021/022912 WO2021188769A1 (en) | 2020-03-19 | 2021-03-18 | Tetralin and tetrahydroquinoline compounds as inhibitors of hif-2alpha |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023518286A JP2023518286A (ja) | 2023-04-28 |
| JPWO2021188769A5 true JPWO2021188769A5 (ru) | 2023-07-12 |
| JP7474861B2 JP7474861B2 (ja) | 2024-04-25 |
Family
ID=75660301
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022556522A Active JP7474861B2 (ja) | 2020-03-19 | 2021-03-18 | Ｈｉｆ－２アルファの阻害剤としてのテトラリン化合物及びテトラヒドロキノリン化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11407712B2 (ru) |
| EP (1) | EP4121409A1 (ru) |
| JP (1) | JP7474861B2 (ru) |
| KR (1) | KR20220155593A (ru) |
| CN (1) | CN115298165A (ru) |
| AU (1) | AU2021240068A1 (ru) |
| BR (1) | BR112022018600A2 (ru) |
| CA (1) | CA3173831A1 (ru) |
| CL (1) | CL2022002515A1 (ru) |
| CO (1) | CO2022013274A2 (ru) |
| CR (1) | CR20220470A (ru) |
| DO (1) | DOP2022000194A (ru) |
| IL (1) | IL295569A (ru) |
| MX (1) | MX2022011534A (ru) |
| PE (1) | PE20230673A1 (ru) |
| TW (1) | TW202144325A (ru) |
| WO (1) | WO2021188769A1 (ru) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL295569A (en) | 2020-03-19 | 2022-10-01 | Arcus Biosciences Inc | Tetralin and tetrahydroquinoline compounds as inhibitors of hif-2alpha |
| WO2022086882A1 (en) | 2020-10-21 | 2022-04-28 | Nikang Therapeutics, Inc. | Diagnostic and therapeutic methods for treatment of cancer with a hif-2(alpha) inhibitor |
| TW202313602A (zh) | 2021-05-21 | 2023-04-01 | 美商阿克思生物科學有限公司 | Axl化合物 |
| EP4341262A1 (en) | 2021-05-21 | 2024-03-27 | Arcus Biosciences, Inc. | Axl inhibitor compounds |
| WO2023077046A1 (en) * | 2021-10-29 | 2023-05-04 | Arcus Biosciences, Inc. | Inhibitors of hif-2alpha and methods of use thereof |
| WO2023215719A1 (en) | 2022-05-02 | 2023-11-09 | Arcus Biosciences, Inc. | Anti-tigit antibodies and uses of the same |
| US20240124490A1 (en) | 2022-07-15 | 2024-04-18 | Arcus Biosciences, Inc. | Inhibitors of hpk1 and methods of use thereof |
| WO2024020034A1 (en) | 2022-07-20 | 2024-01-25 | Arcus Biosciences, Inc. | Cbl-b inhibitors and methods of use thereof |
| WO2024059142A1 (en) | 2022-09-14 | 2024-03-21 | Arcus Biosciences, Inc. | Dispersions of etrumadenant |
| WO2024067463A1 (zh) * | 2022-09-27 | 2024-04-04 | 苏州阿尔脉生物科技有限公司 | 苯并[7]环烯类衍生物、包含其的药物组合物及其医药用途 |
| WO2024081385A1 (en) | 2022-10-14 | 2024-04-18 | Arcus Biosciences, Inc. | Hpk1 inhibitors and methods of use thereof |
| WO2024086718A1 (en) | 2022-10-20 | 2024-04-25 | Arcus Biosciences, Inc. | Lyophilized formulations of cd73 compounds |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US5952294A (en) | 1996-07-31 | 1999-09-14 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Peptidyl prodrugs and methods of making and using the same |
| WO2002089739A2 (en) | 2001-05-09 | 2002-11-14 | Newbiotics, Inc. | Peptide deformylase activated prodrugs |
| CA2528232C (en) | 2003-06-06 | 2010-05-25 | Fibrogen, Inc. | Novel nitrogen-containing heteroaryl compounds and their use in increasing endogenous erythropoietin |
| TWI380996B (zh) | 2004-09-17 | 2013-01-01 | Hoffmann La Roche | 抗ｏｘ４０ｌ抗體 |
| WO2006105021A2 (en) | 2005-03-25 | 2006-10-05 | Tolerrx, Inc. | Gitr binding molecules and uses therefor |
| BRPI0613361A2 (pt) | 2005-07-01 | 2011-01-04 | Medarex Inc | anticorpo monoclonal humano isolado, composição, imunoconjugado, molécula biespecìfica, molécula de ácido nucleico isolada, vetor de expressão, célula hospedeira, camundongo transgênico, método para modular uma resposta imune num indivìduo, método para inibir crescimento de células tumorais num indivìduo, método para tratar uma doença infecciosa num indivìduo, método para aumentar uma resposta imune a um antìgeno num indivìduo, método para tratar ou prevenir uma doença inflamatória num indivìduo e método para preparar o anticorpo anti-pd-l1 |
| WO2008039359A2 (en) | 2006-09-25 | 2008-04-03 | Janssen Pharmaceutica N.V. | Bicyclic pyrimidine kinase inhibitors |
| GB0704407D0 (en) | 2007-03-07 | 2007-04-18 | Glaxo Group Ltd | Compounds |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| ES2591281T3 (es) | 2007-07-12 | 2016-11-25 | Gitr, Inc. | Terapias de combinación que emplean moléculas de enlazamiento a GITR |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| WO2009099763A1 (en) | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| KR20210060670A (ko) | 2008-12-09 | 2021-05-26 | 제넨테크, 인크. | 항-ｐｄ-ｌ１ 항체 및 ｔ 세포 기능을 향상시키기 위한 그의 용도 |
| PL3023438T3 (pl) | 2009-09-03 | 2020-07-27 | Merck Sharp & Dohme Corp. | Przeciwciała anty-gitr |
| PE20121398A1 (es) | 2009-12-10 | 2012-10-26 | Hoffmann La Roche | Anticuerpos ligantes preferentemente al dominio extracelular 4 de csf1r humano |
| US9150656B2 (en) | 2010-03-04 | 2015-10-06 | Macrogenics, Inc. | Antibodies reactive with B7-H3, immunologically active fragments thereof and uses thereof |
| CN102918060B (zh) | 2010-03-05 | 2016-04-06 | 霍夫曼-拉罗奇有限公司 | 抗人csf-1r抗体及其用途 |
| CA2789071C (en) | 2010-03-05 | 2018-03-27 | F. Hoffmann-La Roche Ag | Antibodies against human csf-1r and uses thereof |
| SI2566517T1 (sl) | 2010-05-04 | 2019-01-31 | Five Prime Therapeutics, Inc. | Protitelesa, ki vežejo CSF1R |
| RU2551963C2 (ru) | 2010-09-09 | 2015-06-10 | Пфайзер Инк. | Молекулы, связывающиеся с 4-1вв |
| KR101970025B1 (ko) | 2011-04-20 | 2019-04-17 | 메디뮨 엘엘씨 | Ｂ7-ｈ1 및 ｐｄ-1과 결합하는 항체 및 다른 분자들 |
| HUE051954T2 (hu) | 2011-11-28 | 2021-03-29 | Merck Patent Gmbh | ANTI-PD-L1 ellenanyagok és alkalmazásaik |
| MX356337B (es) | 2011-12-15 | 2018-05-23 | Hoffmann La Roche | Anticuerpos contra csf-1r humano y sus usos. |
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