JPWO2022212894A5 - - Google Patents
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- JPWO2022212894A5 JPWO2022212894A5 JP2023560831A JP2023560831A JPWO2022212894A5 JP WO2022212894 A5 JPWO2022212894 A5 JP WO2022212894A5 JP 2023560831 A JP2023560831 A JP 2023560831A JP 2023560831 A JP2023560831 A JP 2023560831A JP WO2022212894 A5 JPWO2022212894 A5 JP WO2022212894A5
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- Prior art keywords
- optionally substituted
- membered
- alkyl
- hydrogen
- attached
- Prior art date
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 463
- 239000001257 hydrogen Substances 0.000 claims description 458
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 368
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 348
- 150000002431 hydrogen Chemical group 0.000 claims description 339
- 229910052799 carbon Inorganic materials 0.000 claims description 298
- 229910052736 halogen Inorganic materials 0.000 claims description 225
- 150000002367 halogens Chemical group 0.000 claims description 225
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 165
- 150000001721 carbon Chemical group 0.000 claims description 136
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 133
- 125000005549 heteroarylene group Chemical group 0.000 claims description 122
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 118
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 110
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 102
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 100
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 100
- 125000000732 arylene group Chemical group 0.000 claims description 99
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims description 99
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 98
- 229910052760 oxygen Inorganic materials 0.000 claims description 92
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 86
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 86
- 125000003118 aryl group Chemical group 0.000 claims description 81
- -1 cyano, hydroxy Chemical group 0.000 claims description 81
- 125000004429 atom Chemical group 0.000 claims description 72
- 102000016914 ras Proteins Human genes 0.000 claims description 71
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 66
- 239000003112 inhibitor Substances 0.000 claims description 62
- 125000005843 halogen group Chemical group 0.000 claims description 57
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 56
- 125000000217 alkyl group Chemical group 0.000 claims description 49
- 125000005647 linker group Chemical group 0.000 claims description 49
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims description 47
- 150000003839 salts Chemical class 0.000 claims description 47
- GKQLYSROISKDLL-UHFFFAOYSA-N EEDQ Chemical compound C1=CC=C2N(C(=O)OCC)C(OCC)C=CC2=C1 GKQLYSROISKDLL-UHFFFAOYSA-N 0.000 claims description 42
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 38
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 37
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 35
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims description 34
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims description 34
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 34
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 33
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 33
- 229910052717 sulfur Inorganic materials 0.000 claims description 33
- 229910052757 nitrogen Inorganic materials 0.000 claims description 30
- 125000002947 alkylene group Chemical group 0.000 claims description 29
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 19
- 150000001875 compounds Chemical class 0.000 claims description 17
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 14
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 claims description 14
- LIJLYNWYKULUHA-UHFFFAOYSA-N 2-chloroethyl carbamate Chemical compound NC(=O)OCCCl LIJLYNWYKULUHA-UHFFFAOYSA-N 0.000 claims description 14
- FKQWUTABUJVAQU-UHFFFAOYSA-N 2-chloroethylcarbamothioic s-acid Chemical compound SC(=O)NCCCl FKQWUTABUJVAQU-UHFFFAOYSA-N 0.000 claims description 14
- MSPOLKDRZJCLMQ-UHFFFAOYSA-N 2-chloroethylthiourea Chemical compound NC(=S)NCCCl MSPOLKDRZJCLMQ-UHFFFAOYSA-N 0.000 claims description 14
- BITBMHVXCILUEX-UHFFFAOYSA-N 2-chloroethylurea Chemical compound NC(=O)NCCCl BITBMHVXCILUEX-UHFFFAOYSA-N 0.000 claims description 14
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims description 14
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 14
- UGJBHEZMOKVTIM-UHFFFAOYSA-N N-formylglycine Chemical compound OC(=O)CNC=O UGJBHEZMOKVTIM-UHFFFAOYSA-N 0.000 claims description 14
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 14
- 150000001718 carbodiimides Chemical class 0.000 claims description 14
- AFOSIXZFDONLBT-UHFFFAOYSA-N divinyl sulfone Chemical compound C=CS(=O)(=O)C=C AFOSIXZFDONLBT-UHFFFAOYSA-N 0.000 claims description 14
- 150000002118 epoxides Chemical class 0.000 claims description 14
- 150000002148 esters Chemical class 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- VBZWSGALLODQNC-UHFFFAOYSA-N hexafluoroacetone Chemical compound FC(F)(F)C(=O)C(F)(F)F VBZWSGALLODQNC-UHFFFAOYSA-N 0.000 claims description 14
- ZCQWOFVYLHDMMC-UHFFFAOYSA-O hydron;1,3-oxazole Chemical compound C1=COC=[NH+]1 ZCQWOFVYLHDMMC-UHFFFAOYSA-O 0.000 claims description 14
- UCUUFSAXZMGPGH-UHFFFAOYSA-N penta-1,4-dien-3-one Chemical compound C=CC(=O)C=C UCUUFSAXZMGPGH-UHFFFAOYSA-N 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- CBDKQYKMCICBOF-UHFFFAOYSA-N thiazoline Chemical compound C1CN=CS1 CBDKQYKMCICBOF-UHFFFAOYSA-N 0.000 claims description 14
- 125000005179 haloacetyl group Chemical group 0.000 claims description 7
- 125000003368 amide group Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 43
- 125000003275 alpha amino acid group Chemical group 0.000 claims 15
- 238000006467 substitution reaction Methods 0.000 claims 15
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 13
- 102200006538 rs121913530 Human genes 0.000 claims 8
- 102200006539 rs121913529 Human genes 0.000 claims 7
- 102200006532 rs112445441 Human genes 0.000 claims 5
- 102200006531 rs121913529 Human genes 0.000 claims 5
- 102200006657 rs104894228 Human genes 0.000 claims 4
- 102200006520 rs121913240 Human genes 0.000 claims 4
- 102100029974 GTPase HRas Human genes 0.000 claims 3
- 102100030708 GTPase KRas Human genes 0.000 claims 3
- 102100039788 GTPase NRas Human genes 0.000 claims 3
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims 3
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 3
- 102200006562 rs104894231 Human genes 0.000 claims 3
- 102220014333 rs112445441 Human genes 0.000 claims 3
- 102200006525 rs121913240 Human genes 0.000 claims 3
- 102200006537 rs121913529 Human genes 0.000 claims 3
- 102200006540 rs121913530 Human genes 0.000 claims 3
- 102200006541 rs121913530 Human genes 0.000 claims 3
- 102200006533 rs121913535 Human genes 0.000 claims 3
- 102200006564 rs121917759 Human genes 0.000 claims 3
- 102200007373 rs17851045 Human genes 0.000 claims 3
- 102200006648 rs28933406 Human genes 0.000 claims 3
- 102200006593 rs727503093 Human genes 0.000 claims 3
- PEMUGDMSUDYLHU-ZEQRLZLVSA-N 2-[(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile Chemical compound ClC=1C=CC=C2C=CC=C(C=12)N1CC=2N=C(N=C(C=2CC1)N1C[C@@H](N(CC1)C(C(=C)F)=O)CC#N)OC[C@H]1N(CCC1)C PEMUGDMSUDYLHU-ZEQRLZLVSA-N 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 229940124988 adagrasib Drugs 0.000 claims 2
- 208000021780 appendiceal neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 102200007376 rs770248150 Human genes 0.000 claims 2
- NXQKSXLFSAEQCZ-SFHVURJKSA-N sotorasib Chemical group FC1=CC2=C(N(C(N=C2N2[C@H](CN(CC2)C(C=C)=O)C)=O)C=2C(=NC=CC=2C)C(C)C)N=C1C1=C(C=CC=C1O)F NXQKSXLFSAEQCZ-SFHVURJKSA-N 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 1
- ZRBPIAWWRPFDPY-IRXDYDNUSA-N 1-[(3S)-4-[7-[6-amino-4-methyl-3-(trifluoromethyl)pyridin-2-yl]-6-chloro-8-fluoro-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]quinazolin-4-yl]-3-methylpiperazin-1-yl]prop-2-en-1-one Chemical compound NC1=NC(=C(C(=C1)C)C(F)(F)F)C1=C(Cl)C=C2C(N3CCN(C[C@@H]3C)C(=O)C=C)=NC(=NC2=C1F)OC[C@H]1N(C)CCC1 ZRBPIAWWRPFDPY-IRXDYDNUSA-N 0.000 claims 1
- IPFOCHMOYUMURK-UHFFFAOYSA-N 1-[3-[4-[2-[4-chloro-2-hydroxy-5-(1-methylcyclopropyl)anilino]acetyl]piperazin-1-yl]azetidin-1-yl]prop-2-en-1-one Chemical compound C=1C(NCC(=O)N2CCN(CC2)C2CN(C2)C(=O)C=C)=C(O)C=C(Cl)C=1C1(C)CC1 IPFOCHMOYUMURK-UHFFFAOYSA-N 0.000 claims 1
- YNBBKDMAVRSYRE-UHFFFAOYSA-N 1-[4-[7-(2-amino-7-fluoro-1,3-benzothiazol-4-yl)-6-chloro-8-fluoroquinazolin-4-yl]piperazin-1-yl]prop-2-en-1-one Chemical compound NC=1SC2=C(N=1)C(=CC=C2F)C1=C(C=C2C(=NC=NC2=C1F)N1CCN(CC1)C(C=C)=O)Cl YNBBKDMAVRSYRE-UHFFFAOYSA-N 0.000 claims 1
- AZUYLZMQTIKGSC-UHFFFAOYSA-N 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one Chemical compound ClC=1C(=C2C=NNC2=CC=1C)C=1C(=NN(C=1C)C1CC2(CN(C2)C(C=C)=O)C1)C=1C=C2C=NN(C2=CC=1)C AZUYLZMQTIKGSC-UHFFFAOYSA-N 0.000 claims 1
- YRYQLVCTQFBRLD-UIOOFZCWSA-N 2-[(2S)-4-[7-(8-methylnaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-prop-2-enoylpiperazin-2-yl]acetonitrile Chemical compound C(C=C)(=O)N1[C@H](CN(CC1)C=1C2=C(N=C(N=1)OC[C@H]1N(CCC1)C)CN(CC2)C1=CC=CC2=CC=CC(=C12)C)CC#N YRYQLVCTQFBRLD-UIOOFZCWSA-N 0.000 claims 1
- ZRPZPNYZFSJUPA-UHFFFAOYSA-N ARS-1620 Chemical compound Oc1cccc(F)c1-c1c(Cl)cc2c(ncnc2c1F)N1CCN(CC1)C(=O)C=C ZRPZPNYZFSJUPA-UHFFFAOYSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 102220640055 Alpha-mannosidase 2_G12L_mutation Human genes 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 229940126265 GDC-6036 Drugs 0.000 claims 1
- 206010073073 Hepatobiliary cancer Diseases 0.000 claims 1
- 229940126055 JDQ443 Drugs 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- OZUPICRWMLEFCS-LBPRGKRZSA-N NC1=C(C#N)C2=C(S1)C(F)=CC=C2C1=C(F)C=C2C(OCC[C@H]3CN(CCN3C2=O)C(=O)C=C)=C1Cl Chemical compound NC1=C(C#N)C2=C(S1)C(F)=CC=C2C1=C(F)C=C2C(OCC[C@H]3CN(CCN3C2=O)C(=O)C=C)=C1Cl OZUPICRWMLEFCS-LBPRGKRZSA-N 0.000 claims 1
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 102220530637 Putative apolipoprotein(a)-like protein 2_G12F_mutation Human genes 0.000 claims 1
- 208000002669 Sex Cord-Gonadal Stromal Tumors Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000011825 carcinoma of the ampulla of vater Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000003115 germ cell cancer Diseases 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 239000004179 indigotine Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 102200006534 rs104894365 Human genes 0.000 claims 1
- 102200012009 rs111033826 Human genes 0.000 claims 1
- 102220117341 rs11554290 Human genes 0.000 claims 1
- 102220197831 rs121913527 Human genes 0.000 claims 1
- 102220197834 rs121913535 Human genes 0.000 claims 1
- 102220084967 rs121913538 Human genes 0.000 claims 1
- 102200006663 rs121917757 Human genes 0.000 claims 1
- 102220334605 rs1277340795 Human genes 0.000 claims 1
- 102220163944 rs192332761 Human genes 0.000 claims 1
- 102200124922 rs267606920 Human genes 0.000 claims 1
- 102200124915 rs267606921 Human genes 0.000 claims 1
- 102200005817 rs387906918 Human genes 0.000 claims 1
- 102220010996 rs730880471 Human genes 0.000 claims 1
- 102220175510 rs867372893 Human genes 0.000 claims 1
- 208000028467 sex cord-stromal tumor Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 229940073531 sotorasib Drugs 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 12
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 11
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 description 3
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 description 1
- 125000004450 alkenylene group Chemical group 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000004474 heteroalkylene group Chemical group 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 108010014186 ras Proteins Proteins 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163170292P | 2021-04-02 | 2021-04-02 | |
| US63/170,292 | 2021-04-02 | ||
| US202163192843P | 2021-05-25 | 2021-05-25 | |
| US63/192,843 | 2021-05-25 | ||
| PCT/US2022/023133 WO2022212894A1 (en) | 2021-04-02 | 2022-04-01 | Methods for inhibiting ras |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024512767A JP2024512767A (ja) | 2024-03-19 |
| JPWO2022212894A5 true JPWO2022212894A5 (https=) | 2025-04-08 |
| JP2024512767A5 JP2024512767A5 (https=) | 2025-04-08 |
Family
ID=83456876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023560831A Pending JP2024512767A (ja) | 2021-04-02 | 2022-04-01 | Ｒａｓの阻害方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20240108630A1 (https=) |
| EP (1) | EP4320143A4 (https=) |
| JP (1) | JP2024512767A (https=) |
| KR (1) | KR20240004436A (https=) |
| AU (1) | AU2022249177A1 (https=) |
| BR (1) | BR112023020182A2 (https=) |
| CA (1) | CA3214155A1 (https=) |
| CR (1) | CR20230500A (https=) |
| IL (1) | IL307396A (https=) |
| MX (1) | MX2023011608A (https=) |
| TW (1) | TW202308632A (https=) |
| WO (1) | WO2022212894A1 (https=) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2022005359A (es) | 2019-11-04 | 2022-06-02 | Revolution Medicines Inc | Inhibidores de ras. |
| MX2023003060A (es) | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
| AU2022268962A1 (en) | 2021-05-05 | 2023-12-14 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| WO2023199180A1 (en) * | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| CN119301132A (zh) * | 2022-06-01 | 2025-01-10 | 豪夫迈·罗氏有限公司 | 用于治疗癌症的卤代吲哚大环化合物 |
| CN117720556A (zh) * | 2022-09-19 | 2024-03-19 | 杭州阿诺生物医药科技有限公司 | 一种pan-KRAS抑制剂化合物及其制备方法和用途 |
| EP4582426A4 (en) * | 2022-09-19 | 2025-12-24 | Adlai Nortye Biopharma Co Ltd | PAN-KRAS INHIBITOR COMPOUND |
| CN119522225A (zh) | 2022-09-29 | 2025-02-25 | 广州嘉越医药科技有限公司 | 大环衍生物及其应用 |
| WO2024104364A1 (zh) * | 2022-11-16 | 2024-05-23 | 杭州阿诺生物医药科技有限公司 | 一种pan-KRAS抑制剂化合物 |
| CN117534684A (zh) * | 2022-11-29 | 2024-02-09 | 杭州阿诺生物医药科技有限公司 | 一种pan-KRAS抑制剂化合物 |
| IL322278A (en) * | 2023-02-06 | 2025-09-01 | Bicara Therapeutics Inc | Combined therapy and related methods |
| CR20250329A (es) | 2023-02-14 | 2025-09-12 | Hoffmann La Roche | Compuestos tricíclicos para el tratamiento del cáncer |
| WO2024187174A2 (en) * | 2023-03-09 | 2024-09-12 | Aadigen, Llc | Compositions for treating cancer with kras mutations and uses thereof |
| EP4687905A1 (en) * | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| WO2025051241A1 (zh) * | 2023-09-06 | 2025-03-13 | 劲方医药科技(上海)股份有限公司 | 大环化合物及其抗体-药物偶联物 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025087431A1 (zh) * | 2023-10-27 | 2025-05-01 | 贝达药业股份有限公司 | 泛-kras抑制剂及其在医药上的应用 |
| WO2025093625A1 (en) * | 2023-11-01 | 2025-05-08 | F. Hoffmann-La Roche Ag | Macrocycle compounds for the treatment of cancer |
| WO2025119392A1 (zh) * | 2023-12-08 | 2025-06-12 | 正大天晴药业集团股份有限公司 | 含有酰胺取代的大环类化合物 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025193628A2 (en) * | 2024-03-09 | 2025-09-18 | Aadigen, Llc | Compositions for treating cancer with kras mutations and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025252241A1 (zh) * | 2024-06-07 | 2025-12-11 | 杭州和正医药有限公司 | 一种大环衍生物及其用途 |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015745A1 (en) * | 2024-07-11 | 2026-01-15 | Treeline Biosciences, Inc. | Macrocyclic ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101602876B1 (ko) * | 2014-07-22 | 2016-03-11 | 아주대학교산학협력단 | 완전한 이뮤노글로불린 형태의 세포질 침투능을 갖는 항체를 이용하여 세포내 활성화된 ras를 억제하는 방법 및 그의 이용 |
| KR20210116479A (ko) * | 2018-12-21 | 2021-09-27 | 레볼루션 메디슨즈, 인크. | 공동 결합에 참여하는 화합물 및 그의 용도 |
| MX2023003060A (es) * | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
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- 2022-04-01 WO PCT/US2022/023133 patent/WO2022212894A1/en not_active Ceased
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- 2022-04-01 BR BR112023020182A patent/BR112023020182A2/pt unknown
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- 2023-10-02 US US18/479,500 patent/US20240108630A1/en active Pending
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