JPWO2020033828A5 - - Google Patents
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- JPWO2020033828A5 JPWO2020033828A5 JP2021506929A JP2021506929A JPWO2020033828A5 JP WO2020033828 A5 JPWO2020033828 A5 JP WO2020033828A5 JP 2021506929 A JP2021506929 A JP 2021506929A JP 2021506929 A JP2021506929 A JP 2021506929A JP WO2020033828 A5 JPWO2020033828 A5 JP WO2020033828A5
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- JP
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- group
- alkyl
- independently selected
- halo
- amino
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims 48
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000005843 halogen group Chemical group 0.000 claims 31
- 125000003282 alkyl amino group Chemical group 0.000 claims 22
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims 21
- 125000005842 heteroatoms Chemical group 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 18
- 125000004103 aminoalkyl group Chemical group 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 229910052760 oxygen Inorganic materials 0.000 claims 16
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 14
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- -1 hydroxy, amino Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 7
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 102100017818 PTPN11 Human genes 0.000 claims 5
- 101710018405 PTPN11 Proteins 0.000 claims 5
- 125000004432 carbon atoms Chemical group C* 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000003368 amide group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 230000001404 mediated Effects 0.000 claims 4
- 229910052698 phosphorus Inorganic materials 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 3
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010017758 Gastric cancer Diseases 0.000 claims 2
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 2
- 206010024324 Leukaemias Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025650 Malignant melanoma Diseases 0.000 claims 2
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 2
- 206010029748 Noonan syndrome Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000005418 aryl aryl group Chemical group 0.000 claims 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023132960A JP2023144075A (ja) | 2018-08-10 | 2023-08-17 | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６－（４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル）－３－（２，３－ジクロロフェニル）－２－メチルピリミジン－４（３ｈ）－オン誘導体及び関連化合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862717588P | 2018-08-10 | 2018-08-10 | |
| US62/717,588 | 2018-08-10 | ||
| US201862773921P | 2018-11-30 | 2018-11-30 | |
| US62/773,921 | 2018-11-30 | ||
| PCT/US2019/045903 WO2020033828A1 (en) | 2018-08-10 | 2019-08-09 | 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023132960A Division JP2023144075A (ja) | 2018-08-10 | 2023-08-17 | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６－（４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル）－３－（２，３－ジクロロフェニル）－２－メチルピリミジン－４（３ｈ）－オン誘導体及び関連化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021534124A JP2021534124A (ja) | 2021-12-09 |
| JPWO2020033828A5 true JPWO2020033828A5 (pt-PT) | 2022-08-18 |
Family
ID=67766350
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506929A Ceased JP2021534124A (ja) | 2018-08-10 | 2019-08-09 | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６−（４−アミノ−３−メチル−２−オキサ−８−アザスピロ［４．５］デカン−８−イル）−３−（２，３−ジクロロフェニル）−２−メチルピリミジン−４（３ｈ）−オン誘導体及び関連化合物 |
| JP2023132960A Pending JP2023144075A (ja) | 2018-08-10 | 2023-08-17 | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６－（４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル）－３－（２，３－ジクロロフェニル）－２－メチルピリミジン－４（３ｈ）－オン誘導体及び関連化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023132960A Pending JP2023144075A (ja) | 2018-08-10 | 2023-08-17 | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６－（４－アミノ－３－メチル－２－オキサ－８－アザスピロ［４．５］デカン－８－イル）－３－（２，３－ジクロロフェニル）－２－メチルピリミジン－４（３ｈ）－オン誘導体及び関連化合物 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US11104675B2 (pt-PT) |
| EP (2) | EP3833670B1 (pt-PT) |
| JP (2) | JP2021534124A (pt-PT) |
| CN (1) | CN112601750B (pt-PT) |
| AU (1) | AU2019319971A1 (pt-PT) |
| BR (1) | BR112021002327A2 (pt-PT) |
| CA (1) | CA3109181A1 (pt-PT) |
| CL (1) | CL2021000355A1 (pt-PT) |
| CO (1) | CO2021003074A2 (pt-PT) |
| CR (1) | CR20210132A (pt-PT) |
| DK (1) | DK3833670T3 (pt-PT) |
| FI (1) | FI3833670T3 (pt-PT) |
| IL (2) | IL307361B1 (pt-PT) |
| LT (1) | LT3833670T (pt-PT) |
| MX (2) | MX2021001608A (pt-PT) |
| PE (1) | PE20211050A1 (pt-PT) |
| PH (1) | PH12021550268A1 (pt-PT) |
| PL (1) | PL3833670T3 (pt-PT) |
| PT (1) | PT3833670T (pt-PT) |
| RS (1) | RS65728B1 (pt-PT) |
| SG (1) | SG11202100199UA (pt-PT) |
| SI (1) | SI3833670T1 (pt-PT) |
| TW (1) | TWI827646B (pt-PT) |
| UA (1) | UA128559C2 (pt-PT) |
| WO (1) | WO2020033828A1 (pt-PT) |
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| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| AU2017274199B2 (en) | 2016-05-31 | 2021-09-23 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| WO2018081091A1 (en) | 2016-10-24 | 2018-05-03 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| EP3630770B1 (en) | 2017-05-26 | 2024-08-28 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| WO2019067843A1 (en) | 2017-09-29 | 2019-04-04 | Relay Therapeutics, Inc. | PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2 |
| TW202003471A (zh) | 2018-03-21 | 2020-01-16 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| WO2019213318A1 (en) | 2018-05-02 | 2019-11-07 | Board Of Regents, The University Of Texas System | Substituted heterocyclic inhibitors of ptpn11 |
| JP2021534124A (ja) | 2018-08-10 | 2021-12-09 | ナビール ファーマ，インコーポレイティド | 癌治療用ｐｔｐｎ１１（ｓｈｐ２）阻害剤としての６−（４−アミノ−３−メチル−２−オキサ−８−アザスピロ［４．５］デカン−８−イル）−３−（２，３−ジクロロフェニル）−２−メチルピリミジン−４（３ｈ）−オン誘導体及び関連化合物 |
| SG11202102679QA (en) | 2018-09-18 | 2021-04-29 | Nikang Therapeutics Inc | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| TW202039426A (zh) | 2018-11-30 | 2020-11-01 | 美商彗星製藥公司 | 泛硫醇（Ｐａｎｔｅｔｈｅｉｎｅ）衍生物及其用途 |
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| CR20230570A (es) | 2021-05-05 | 2024-01-22 | Revolution Medicines Inc | Inhibidores de ras |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
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