JPWO2019140322A5 - - Google Patents
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- JPWO2019140322A5 JPWO2019140322A5 JP2020558865A JP2020558865A JPWO2019140322A5 JP WO2019140322 A5 JPWO2019140322 A5 JP WO2019140322A5 JP 2020558865 A JP2020558865 A JP 2020558865A JP 2020558865 A JP2020558865 A JP 2020558865A JP WO2019140322 A5 JPWO2019140322 A5 JP WO2019140322A5
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- JP
- Japan
- Prior art keywords
- alkyl
- rings
- cycloalkyl
- cycloalkenyl
- aromatic
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims description 90
- 125000000623 heterocyclic group Chemical group 0.000 claims description 88
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 82
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 81
- 125000003118 aryl group Chemical group 0.000 claims description 80
- 125000001072 heteroaryl group Chemical group 0.000 claims description 69
- 229910052736 halogen Inorganic materials 0.000 claims description 61
- 150000002367 halogens Chemical class 0.000 claims description 61
- 102100021455 Histone deacetylase 3 Human genes 0.000 claims description 60
- 229910052739 hydrogen Inorganic materials 0.000 claims description 56
- 239000001257 hydrogen Substances 0.000 claims description 53
- 150000002431 hydrogen Chemical class 0.000 claims description 42
- 239000003112 inhibitor Substances 0.000 claims description 42
- 229920006395 saturated elastomer Polymers 0.000 claims description 42
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 239000000651 prodrug Substances 0.000 claims description 10
- 229940002612 prodrug Drugs 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 239000012453 solvate Substances 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 7
- 229910052805 deuterium Inorganic materials 0.000 claims description 7
- -1 fluoro (C1-C6) alkyl Chemical group 0.000 claims description 7
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 150000001721 carbon Chemical group 0.000 claims description 5
- 125000004429 atom Chemical group 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 108010074724 histone deacetylase 3 Proteins 0.000 claims 58
- 125000003342 alkenyl group Chemical group 0.000 claims 31
- 125000000304 alkynyl group Chemical group 0.000 claims 31
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 206010028980 Neoplasm Diseases 0.000 claims 24
- 201000011510 cancer Diseases 0.000 claims 24
- 239000002955 immunomodulating agent Substances 0.000 claims 16
- 210000004027 cell Anatomy 0.000 claims 11
- 230000000694 effects Effects 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 10
- 230000002401 inhibitory effect Effects 0.000 claims 8
- 102100029966 HLA class II histocompatibility antigen, DP alpha 1 chain Human genes 0.000 claims 7
- 101000864089 Homo sapiens HLA class II histocompatibility antigen, DP alpha 1 chain Proteins 0.000 claims 7
- 101000930802 Homo sapiens HLA class II histocompatibility antigen, DQ alpha 1 chain Proteins 0.000 claims 7
- 101000968032 Homo sapiens HLA class II histocompatibility antigen, DR beta 3 chain Proteins 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- 230000001939 inductive effect Effects 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 230000010261 cell growth Effects 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 4
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 4
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 102100040678 Programmed cell death protein 1 Human genes 0.000 claims 3
- 101710089372 Programmed cell death protein 1 Proteins 0.000 claims 3
- 230000004611 cancer cell death Effects 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 230000034994 death Effects 0.000 claims 3
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 108700018351 Major Histocompatibility Complex Proteins 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000000467 secondary amino group Chemical class [H]N([*:1])[*:2] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 230000020382 suppression by virus of host antigen processing and presentation of peptide antigen via MHC class I Effects 0.000 claims 2
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- BXDZOYLPNAIDOC-UHFFFAOYSA-N N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-[2-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethylamino]-2-oxoethyl]piperidine-4-carboxamide Chemical compound CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(CC(=O)NCCOCCOCCOCCNc4cccc5C(=O)N(C6CCC(=O)NC6=O)C(=O)c45)CC3)s2)o1 BXDZOYLPNAIDOC-UHFFFAOYSA-N 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 210000001151 cytotoxic T lymphocyte Anatomy 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- APXRYINGSDDHKM-UHFFFAOYSA-N n-[7-(2-aminoanilino)-7-oxoheptyl]-3-phenylbenzamide Chemical compound NC1=CC=CC=C1NC(=O)CCCCCCNC(=O)C1=CC=CC(C=2C=CC=CC=2)=C1 APXRYINGSDDHKM-UHFFFAOYSA-N 0.000 claims 1
- RPWGAGSAMOSCDJ-UHFFFAOYSA-N n-[7-(2-aminoanilino)-7-oxoheptyl]-6-phenylpyridine-3-carboxamide Chemical compound NC1=CC=CC=C1NC(=O)CCCCCCNC(=O)C1=CC=C(C=2C=CC=CC=2)N=C1 RPWGAGSAMOSCDJ-UHFFFAOYSA-N 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 description 6
- 125000002950 monocyclic group Chemical group 0.000 description 5
- 101000899282 Homo sapiens Histone deacetylase 3 Proteins 0.000 description 2
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024015651A JP2024099510A (ja) | 2018-01-12 | 2024-02-05 | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862616831P | 2018-01-12 | 2018-01-12 | |
| US62/616,831 | 2018-01-12 | ||
| PCT/US2019/013375 WO2019140322A1 (en) | 2018-01-12 | 2019-01-11 | Combination of a selective histone deacetylase 3 (hdac3) inhibitor and an immunotherapy agent for the treatment of cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024015651A Division JP2024099510A (ja) | 2018-01-12 | 2024-02-05 | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021510733A JP2021510733A (ja) | 2021-04-30 |
| JPWO2019140322A5 true JPWO2019140322A5 (https=) | 2022-02-08 |
| JP2021510733A5 JP2021510733A5 (https=) | 2022-02-08 |
Family
ID=65516716
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020558865A Pending JP2021510733A (ja) | 2018-01-12 | 2019-01-11 | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
| JP2024015651A Pending JP2024099510A (ja) | 2018-01-12 | 2024-02-05 | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024015651A Pending JP2024099510A (ja) | 2018-01-12 | 2024-02-05 | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US12128018B2 (https=) |
| EP (1) | EP3737362B1 (https=) |
| JP (2) | JP2021510733A (https=) |
| CN (1) | CN112135610A (https=) |
| CA (1) | CA3125731A1 (https=) |
| ES (1) | ES3057234T3 (https=) |
| WO (1) | WO2019140322A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2701699B1 (en) * | 2011-04-28 | 2019-10-16 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
| JP6337255B2 (ja) | 2012-07-27 | 2018-06-06 | ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. | ヒストンデアセチラーゼの阻害剤 |
| CA3125731A1 (en) | 2018-01-12 | 2019-07-18 | KDAc Therapeutics, Inc. | Combination of a selective histone deacetylase 3 (hdac3) inhibitor and an immunotherapy agent for the treatment of cancer |
| CR20200553A (es) | 2018-04-18 | 2021-04-08 | Constellation Pharmaceuticals Inc | Moduladores de enzimas modificadoras de metilo, composiciones y usos de estos |
| CN120097995A (zh) | 2018-05-21 | 2025-06-06 | 星座制药公司 | 甲基修饰酶的调节剂、其组合物和用途 |
| WO2021016414A1 (en) | 2019-07-24 | 2021-01-28 | Constellation Pharmaceuticals, Inc. | Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide |
| US20240226039A1 (en) * | 2021-05-24 | 2024-07-11 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Immune checkpoint inhibitor and hdac inhibitor combination therapy strategy |
| WO2023034440A1 (en) | 2021-09-01 | 2023-03-09 | Case Western Reserve University | Treatment of neurodegenerative diseases with hdac inhibitors |
| CN113754587B (zh) * | 2021-09-22 | 2023-07-14 | 沈阳药科大学 | 一种苯基吡唑类化合物及应用 |
| KR20230084416A (ko) * | 2021-12-03 | 2023-06-13 | 연세대학교 산학협력단 | Wnk3 억제제를 유효성분으로 포함하는 면역관문 억제용 조성물 |
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-
2019
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- 2019-01-11 WO PCT/US2019/013375 patent/WO2019140322A1/en not_active Ceased
- 2019-01-11 US US16/246,320 patent/US12128018B2/en active Active
- 2019-01-11 ES ES19706776T patent/ES3057234T3/es active Active
- 2019-01-11 JP JP2020558865A patent/JP2021510733A/ja active Pending
- 2019-01-11 CN CN201980018750.2A patent/CN112135610A/zh active Pending
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