JP2021518395A5 - - Google Patents
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- JP2021518395A5 JP2021518395A5 JP2020550667A JP2020550667A JP2021518395A5 JP 2021518395 A5 JP2021518395 A5 JP 2021518395A5 JP 2020550667 A JP2020550667 A JP 2020550667A JP 2020550667 A JP2020550667 A JP 2020550667A JP 2021518395 A5 JP2021518395 A5 JP 2021518395A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- oxo
- amino
- thio
- pyrazine
- Prior art date
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- -1 naphthalene-1-yl group Chemical group 0.000 claims 171
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 13
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 7
- LPCQBTAOTIZGAE-UHFFFAOYSA-N 2h-pyrimidine-1-carboxamide Chemical compound NC(=O)N1CN=CC=C1 LPCQBTAOTIZGAE-UHFFFAOYSA-N 0.000 claims 6
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 claims 4
- HKSQZEGSMBFHGC-UHFFFAOYSA-N pyrimidine-4-carboxamide Chemical compound NC(=O)C1=CC=NC=N1 HKSQZEGSMBFHGC-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 claims 2
- XQXXOWKUJRCUGZ-UHFFFAOYSA-N (4-methylpiperidin-4-yl)methanamine Chemical compound NCC1(C)CCNCC1 XQXXOWKUJRCUGZ-UHFFFAOYSA-N 0.000 claims 1
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 claims 1
- IBHIUPPGDYCBSV-UHFFFAOYSA-N 1,2-dihydroimidazol-5-one Chemical compound O=C1NCN=C1 IBHIUPPGDYCBSV-UHFFFAOYSA-N 0.000 claims 1
- SCDFILPFVOPDMQ-UHFFFAOYSA-N 1-(3-aminocyclohexyl)-4-(2,3-dichlorophenyl)pyridin-2-one Chemical compound NC1CC(CCC1)N1C(C=C(C=C1)C1=C(C(=CC=C1)Cl)Cl)=O SCDFILPFVOPDMQ-UHFFFAOYSA-N 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Chemical compound C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 1
- IFOXEIWAOZTLPH-APPDUMDISA-N 2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(2,3-dichloroanilino)-3,7-dihydropyrrolo[2,3-d]pyrimidin-4-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1NC(C2=C(N=1)NC=C2NC1=C(C(=CC=C1)Cl)Cl)=O)C IFOXEIWAOZTLPH-APPDUMDISA-N 0.000 claims 1
- KKVLZJPXYUIIIF-KPZWWZAWSA-N 2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(2,3-dichloroanilino)-3-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1N(C(C2=C(N=1)NC=C2NC1=C(C(=CC=C1)Cl)Cl)=O)C)C KKVLZJPXYUIIIF-KPZWWZAWSA-N 0.000 claims 1
- AFVYHLNMSBZECS-KPZWWZAWSA-N 2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(2,3-dichlorophenoxy)-3-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1N(C(C2=C(N=1)NC=C2OC1=C(C(=CC=C1)Cl)Cl)=O)C)C AFVYHLNMSBZECS-KPZWWZAWSA-N 0.000 claims 1
- NRTBXUFMVUIAAD-UHFFFAOYSA-N 2-[4-(aminomethyl)-4-methylpiperidin-1-yl]-5-(2,3-dichlorophenyl)-1-methyl-6-oxopyrimidine-4-carbonitrile Chemical compound NCC1(CCN(CC1)C=1N(C(C(=C(N=1)C#N)C1=C(C(=CC=C1)Cl)Cl)=O)C)C NRTBXUFMVUIAAD-UHFFFAOYSA-N 0.000 claims 1
- PFWXRXTXRFAYGY-UHFFFAOYSA-N 2-[4-(aminomethyl)-4-methylpiperidin-1-yl]-5-(2,3-dichlorophenyl)sulfanyl-3H-pyrido[3,4-d]pyrimidin-4-one Chemical compound NCC1(CCN(CC1)C=1NC(C2=C(N=1)C=NC=C2SC1=C(C(=CC=C1)Cl)Cl)=O)C PFWXRXTXRFAYGY-UHFFFAOYSA-N 0.000 claims 1
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 claims 1
- SYWOGGKKFGSXNS-UHFFFAOYSA-N 3-(2-aminospiro[bicyclo[3.1.0]hexane-3,4'-piperidine]-1'-yl)-6-(2,3-dichlorophenyl)sulfanyl-1-methylpyrazin-2-one Chemical compound NC1C2CC2CC11CCN(CC1)C=1C(N(C(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)C)=O SYWOGGKKFGSXNS-UHFFFAOYSA-N 0.000 claims 1
- CBTBEOJTLGXQBZ-UHFFFAOYSA-N 3-(4-amino-2-oxa-8-azaspiro[4.5]decan-8-yl)-6-(2,3-dichlorophenyl)sulfanyl-1-methylpyrazin-2-one Chemical compound NC1COCC11CCN(CC1)C=1C(N(C(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)C)=O CBTBEOJTLGXQBZ-UHFFFAOYSA-N 0.000 claims 1
- OQJHFEOXMDSFMI-UHFFFAOYSA-N 3-(4-amino-2-oxa-8-azaspiro[4.5]decan-8-yl)-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NC1COCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O OQJHFEOXMDSFMI-UHFFFAOYSA-N 0.000 claims 1
- TVNBISXYSAIDKO-UHFFFAOYSA-N 3-(6-amino-3-azabicyclo[3.1.0]hexan-3-yl)-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NC1C2CN(CC12)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O TVNBISXYSAIDKO-UHFFFAOYSA-N 0.000 claims 1
- UJRCFTNATREODD-OAQYLSRUSA-N 3-[(1S)-1-amino-4-methoxyspiro[1,3-dihydroindene-2,4'-piperidine]-1'-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1C2=CC=CC(=C2CC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)OC UJRCFTNATREODD-OAQYLSRUSA-N 0.000 claims 1
- UNRCWEPFQCACOS-HXUWFJFHSA-N 3-[(1S)-1-aminospiro[1,3-dihydroindene-2,4'-piperidine]-1'-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1C2=CC=CC=C2CC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O UNRCWEPFQCACOS-HXUWFJFHSA-N 0.000 claims 1
- QUDYOUIUXBQJBP-XJKSGUPXSA-N 3-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1-methylpyrazin-2-one Chemical compound N[C@@H]1C[C@@H](CC11CCN(CC1)C=1C(N(C(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)C)=O)C QUDYOUIUXBQJBP-XJKSGUPXSA-N 0.000 claims 1
- KUOXDSAASAJNGS-IINYFYTJSA-N 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichloropyridin-4-yl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=NC=C1)Cl)Cl)=O)C KUOXDSAASAJNGS-IINYFYTJSA-N 0.000 claims 1
- NXGCMWDNLSXJON-MEDUHNTESA-N 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2-chloro-3-fluorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)F)Cl)=O)C NXGCMWDNLSXJON-MEDUHNTESA-N 0.000 claims 1
- CDCDRNUWELNRQH-XHDPSFHLSA-N 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(3-chloro-1-methyl-2-oxopyridin-4-yl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(N(C=C1)C)=O)Cl)=O)C CDCDRNUWELNRQH-XHDPSFHLSA-N 0.000 claims 1
- FGOMPCFISFVIAW-XHDPSFHLSA-N 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(3-chloro-2-methoxypyridin-4-yl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=NC=C1)OC)Cl)=O)C FGOMPCFISFVIAW-XHDPSFHLSA-N 0.000 claims 1
- SXRNTXDHSFPIIM-IINYFYTJSA-N 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-[(3-chloro-2-oxo-1H-pyridin-4-yl)sulfanyl]-1H-pyrazin-2-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(NC=C1)=O)Cl)=O)C SXRNTXDHSFPIIM-IINYFYTJSA-N 0.000 claims 1
- ILPTXIJRMXVQQY-CYBMUJFWSA-N 3-[(4R)-4-amino-2,2-difluoro-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1CC(CC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)(F)F ILPTXIJRMXVQQY-CYBMUJFWSA-N 0.000 claims 1
- SIULRGIDMNPONH-SBXXRYSUSA-N 3-[(4R)-4-amino-2-fluoro-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1CC(CC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)F SIULRGIDMNPONH-SBXXRYSUSA-N 0.000 claims 1
- OQJHFEOXMDSFMI-ZDUSSCGKSA-N 3-[(4R)-4-amino-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@H]1COCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O OQJHFEOXMDSFMI-ZDUSSCGKSA-N 0.000 claims 1
- YGFOFLRRLIUMBV-CQSZACIVSA-N 3-[(4R)-4-amino-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1CCCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O YGFOFLRRLIUMBV-CQSZACIVSA-N 0.000 claims 1
- OQJHFEOXMDSFMI-CYBMUJFWSA-N 3-[(4S)-4-amino-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1COCC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O OQJHFEOXMDSFMI-CYBMUJFWSA-N 0.000 claims 1
- VFNBGRKGBQBPJF-LJQANCHMSA-N 3-[(5S)-5-aminospiro[5,7-dihydrocyclopenta[b]pyridine-6,4'-piperidine]-1'-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1C=2C(=NC=CC=2)CC11CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O VFNBGRKGBQBPJF-LJQANCHMSA-N 0.000 claims 1
- DXEIVWFORALKLE-SNVBAGLBSA-N 3-[(6R)-6-amino-2-azaspiro[3.4]octan-2-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@H]1CC2(CN(C2)C=2C(NC(=CN=2)SC2=C(C(=CC=C2)Cl)Cl)=O)CC1 DXEIVWFORALKLE-SNVBAGLBSA-N 0.000 claims 1
- DXEIVWFORALKLE-JTQLQIEISA-N 3-[(6S)-6-amino-2-azaspiro[3.4]octan-2-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound N[C@@H]1CC2(CN(C2)C=2C(NC(=CN=2)SC2=C(C(=CC=C2)Cl)Cl)=O)CC1 DXEIVWFORALKLE-JTQLQIEISA-N 0.000 claims 1
- CUCPROKEXAIMCC-UHFFFAOYSA-N 3-[3-(aminomethyl)-3-methylpyrrolidin-1-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)C CUCPROKEXAIMCC-UHFFFAOYSA-N 0.000 claims 1
- LNZNZGGVJFERLM-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-fluoropiperidin-1-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)F LNZNZGGVJFERLM-UHFFFAOYSA-N 0.000 claims 1
- WHUNDUIZDAWWGK-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-hydroxypiperidin-1-yl]-6-(2,3-dichlorophenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)Cl)Cl)=O)O WHUNDUIZDAWWGK-UHFFFAOYSA-N 0.000 claims 1
- NAKPYWCEFBAGEU-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-(2,3-dichlorophenyl)-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)C1=C(C(=CC=C1)Cl)Cl)=O)C NAKPYWCEFBAGEU-UHFFFAOYSA-N 0.000 claims 1
- HAAAXABVIGQBOT-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-(2-chloro-3-methoxyphenyl)sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=CC=C1)OC)Cl)=O)C HAAAXABVIGQBOT-UHFFFAOYSA-N 0.000 claims 1
- IGWAIPLFFIMTAQ-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-(3-chloro-2-methoxypyridin-4-yl)sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=C(C(=NC=C1)OC)Cl)=O)C IGWAIPLFFIMTAQ-UHFFFAOYSA-N 0.000 claims 1
- VCHHVKLUGGQAET-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-[2-(trifluoromethyl)phenyl]sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=C(C=CC=C1)C(F)(F)F)=O)C VCHHVKLUGGQAET-UHFFFAOYSA-N 0.000 claims 1
- SVRUKQKRAHSRTQ-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-[2-(trifluoromethyl)pyridin-3-yl]sulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC=1C(=NC=CC=1)C(F)(F)F)=O)C SVRUKQKRAHSRTQ-UHFFFAOYSA-N 0.000 claims 1
- VGNPATCUBXRDBE-UHFFFAOYSA-N 3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-6-naphthalen-1-ylsulfanyl-1H-pyrazin-2-one Chemical compound NCC1(CCN(CC1)C=1C(NC(=CN=1)SC1=CC=CC2=CC=CC=C12)=O)C VGNPATCUBXRDBE-UHFFFAOYSA-N 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- SQDOXGXCLKGIAT-UHFFFAOYSA-N 4-amino-2-(6-amino-2-azaspiro[3.4]octan-2-yl)-5-(2,3-dichlorophenyl)sulfanyl-1H-pyrimidin-6-one Chemical compound NC1=C(C(NC(=N1)N1CC2(C1)CC(CC2)N)=O)SC1=C(C(=CC=C1)Cl)Cl SQDOXGXCLKGIAT-UHFFFAOYSA-N 0.000 claims 1
- FGTDIEOPGHWZOR-UHFFFAOYSA-N 4-amino-2-(6-amino-3-azabicyclo[3.1.0]hexan-3-yl)-5-(2,3-dichlorophenyl)sulfanyl-1H-pyrimidin-6-one Chemical compound NC1=C(C(NC(=N1)N1CC2C(C2C1)N)=O)SC1=C(C(=CC=C1)Cl)Cl FGTDIEOPGHWZOR-UHFFFAOYSA-N 0.000 claims 1
- MGSZQRPSSXLWIN-UHFFFAOYSA-N 4-amino-2-(6-amino-3-azabicyclo[3.2.0]heptan-3-yl)-5-(2,3-dichlorophenyl)sulfanyl-1H-pyrimidin-6-one Chemical compound NC1=C(C(NC(=N1)N1CC2CC(C2C1)N)=O)SC1=C(C(=CC=C1)Cl)Cl MGSZQRPSSXLWIN-UHFFFAOYSA-N 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- IQVNXICBINOVNT-UHFFFAOYSA-N 5-[1-(1-aminopropan-2-yl)piperidin-4-yl]-3-(2,3-dichlorophenyl)sulfanyl-1,6-dihydropyrazolo[4,3-d]pyrimidin-7-one Chemical compound NCC(C)N1CCC(CC1)C=1NC(C2=C(N=1)C(=NN2)SC1=C(C(=CC=C1)Cl)Cl)=O IQVNXICBINOVNT-UHFFFAOYSA-N 0.000 claims 1
- QEESQKCQMWEXCC-UHFFFAOYSA-N 6-(2,3-dichlorophenyl)sulfanyl-3-(piperidin-4-ylamino)-1H-pyrazin-2-one Chemical compound ClC1=C(C=CC=C1Cl)SC1=CN=C(C(N1)=O)NC1CCNCC1 QEESQKCQMWEXCC-UHFFFAOYSA-N 0.000 claims 1
- OYYXDXFCUKNPSW-UHFFFAOYSA-N 6-(2-amino-3-chloropyridin-4-yl)sulfanyl-3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-1H-pyrazin-2-one Chemical compound NC1=NC=CC(=C1Cl)SC1=CN=C(C(N1)=O)N1CCC(CC1)(C)CN OYYXDXFCUKNPSW-UHFFFAOYSA-N 0.000 claims 1
- PNLMLGLYVFMTEO-UHFFFAOYSA-N 6-(5-amino-2-chlorophenyl)sulfanyl-3-[4-(aminomethyl)-4-methylpiperidin-1-yl]-1H-pyrazin-2-one Chemical compound NC=1C=CC(=C(C=1)SC1=CN=C(C(N1)=O)N1CCC(CC1)(C)CN)Cl PNLMLGLYVFMTEO-UHFFFAOYSA-N 0.000 claims 1
- BRGIDJLKNGSBSX-MEDUHNTESA-N 6-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichloroanilino)-4-methyl-2H-pyrazolo[3,4-b]pyrazin-5-one Chemical compound N[C@@H]1[C@@H](OCC11CCN(CC1)C=1C(N(C2=C(N=1)NN=C2NC1=C(C(=CC=C1)Cl)Cl)C)=O)C BRGIDJLKNGSBSX-MEDUHNTESA-N 0.000 claims 1
- MSOFATSUYQHEEW-UHFFFAOYSA-N 6-[3-(aminomethyl)-3-methylpyrrolidin-1-yl]-3-(2,3-dichlorophenoxy)-2,5-dihydropyrazolo[3,4-d]pyrimidin-4-one Chemical compound NCC1(CN(CC1)C=1NC(C2=C(N=1)NN=C2OC1=C(C(=CC=C1)Cl)Cl)=O)C MSOFATSUYQHEEW-UHFFFAOYSA-N 0.000 claims 1
- MXRKHCMUIGDXSN-UHFFFAOYSA-N 6-[3-(aminomethyl)-3-methylpyrrolidin-1-yl]-3-(2,3-dichlorophenoxy)-5-methyl-2H-pyrazolo[3,4-d]pyrimidin-4-one Chemical compound NCC1(CN(CC1)C=1N(C(C2=C(N=1)NN=C2OC1=C(C(=CC=C1)Cl)Cl)=O)C)C MXRKHCMUIGDXSN-UHFFFAOYSA-N 0.000 claims 1
- NFJWKKZRQXOAOG-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-methylpiperidin-1-yl]-3-(2,3-dichloroanilino)-2,5-dihydropyrazolo[3,4-d]pyrimidin-4-one Chemical compound NCC1(CCN(CC1)C=1NC(C2=C(N=1)NN=C2NC1=C(C(=CC=C1)Cl)Cl)=O)C NFJWKKZRQXOAOG-UHFFFAOYSA-N 0.000 claims 1
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Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| MX2019008696A (es) | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
| MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| MX2020003579A (es) * | 2017-10-12 | 2020-07-22 | Revolution Medicines Inc | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. |
| BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
| NZ766835A (en) | 2018-03-02 | 2023-09-29 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| SG11202009245TA (en) | 2018-03-21 | 2020-10-29 | Relay Therapeutics Inc | Shp2 phosphatase inhibitors and methods of use thereof |
| KR102611661B1 (ko) * | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| JP7174143B2 (ja) | 2018-07-24 | 2022-11-17 | 大鵬薬品工業株式会社 | Shp2活性を阻害するヘテロ二環性化合物 |
| LT3833670T (lt) | 2018-08-10 | 2024-06-25 | Navire Pharma, Inc. | 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dichlorfenil)-2-metilpirimidin-4(3h)-ono dariniai ir susiję junginiai kaip ptpn11 (shp2) inhibitoriai, skirti vėžiui gydyti |
| JP7542538B2 (ja) | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス, インコーポレイテッド | Srcホモロジー-2ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| TW202028183A (zh) * | 2018-10-10 | 2020-08-01 | 大陸商江蘇豪森藥業集團有限公司 | 含氮雜芳類衍生物調節劑、其製備方法和應用 |
| EP3866773B1 (en) | 2018-10-16 | 2024-08-28 | Georgia State University Research Foundation, Inc. | Carbon monoxide prodrugs for the treatment of medical disorders |
| US12187721B2 (en) | 2018-10-17 | 2025-01-07 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| CN113365988B (zh) * | 2019-01-31 | 2023-10-03 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| CN111647000B (zh) | 2019-03-04 | 2021-10-12 | 勤浩医药(苏州)有限公司 | 吡嗪类衍生物及其在抑制shp2中的应用 |
| WO2020201991A1 (en) | 2019-04-02 | 2020-10-08 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| CA3127475A1 (en) | 2019-04-08 | 2020-10-15 | Merck Patent Gmbh | Pyrimidinone derivatives as shp2 antagonists |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| AU2020354475A1 (en) | 2019-09-24 | 2022-05-05 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of making and using the same |
| CN112724145A (zh) * | 2019-10-14 | 2021-04-30 | 杭州雷索药业有限公司 | 用于抑制shp2活性的吡嗪衍生物 |
| TW202128688A (zh) | 2019-11-08 | 2021-08-01 | 美商銳新醫藥公司 | 雙環雜芳基化合物及其用途 |
| CN114829362A (zh) * | 2019-12-10 | 2022-07-29 | 成都倍特药业股份有限公司 | 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物 |
| CN117683033A (zh) * | 2019-12-19 | 2024-03-12 | 首药控股(北京)股份有限公司 | 取代的炔基杂环化合物 |
| CN114867720B (zh) * | 2020-01-16 | 2024-10-22 | 浙江海正药业股份有限公司 | 杂芳基类衍生物及其制备方法和用途 |
| WO2021147879A1 (zh) * | 2020-01-21 | 2021-07-29 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| EP4169913A4 (en) * | 2020-06-22 | 2024-10-30 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | SUBSTITUTED PYRAZINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| MX2023003060A (es) | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
| CN115028649B (zh) * | 2021-03-05 | 2026-03-17 | 四川科伦博泰生物医药股份有限公司 | 三并环类化合物,包含其的药物组合物及其用途 |
| CA3217084A1 (en) | 2021-05-05 | 2022-11-10 | Farbod Shojaei | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
| AU2022268962A1 (en) | 2021-05-05 | 2023-12-14 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
| IL308234A (en) | 2021-05-05 | 2024-01-01 | Huyabio Int Llc | Monotherapy with an SHP2 inhibitor and its uses |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| CA3217393A1 (en) | 2021-05-05 | 2022-11-10 | Elena S. Koltun | Ras inhibitors |
| CN113248449B (zh) * | 2021-05-06 | 2022-09-23 | 中国药科大学 | 一种含甲脒的芳基螺环类化合物及其制备方法与应用 |
| TW202244049A (zh) * | 2021-05-12 | 2022-11-16 | 大陸商藥雅科技(上海)有限公司 | Shp2磷酸酶抑制劑的製備及其應用 |
| CN115340559A (zh) * | 2021-05-12 | 2022-11-15 | 药雅科技(上海)有限公司 | Shp2磷酸酶杂环类抑制剂的制备及其应用 |
| CN115340561A (zh) * | 2021-05-14 | 2022-11-15 | 药雅科技(上海)有限公司 | Shp2磷酸酶稠环类抑制剂的制备及其应用 |
| CN115340545A (zh) * | 2021-05-14 | 2022-11-15 | 浙江海正药业股份有限公司 | 双环杂芳基类衍生物及其制备方法和用途 |
| 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 |
| CA3226206A1 (en) * | 2021-07-09 | 2023-01-12 | Kanaph Therapeutics Inc. | Shp2 inhibitor and use thereof |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN119136806A (zh) | 2022-03-08 | 2024-12-13 | 锐新医药公司 | 用于治疗免疫难治性肺癌的方法 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| CN121263418A (zh) | 2023-04-07 | 2026-01-02 | 锐新医药公司 | 大环ras抑制剂 |
| KR20260005904A (ko) | 2023-04-07 | 2026-01-12 | 레볼루션 메디슨즈, 인크. | 매크로사이클릭 ras 억제제 |
| KR20250172857A (ko) | 2023-04-14 | 2025-12-09 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형 |
| AU2024252105A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| CN121568944A (zh) * | 2023-07-11 | 2026-02-24 | 勤浩医药(苏州)股份有限公司 | 用作shp2抑制剂的杂环化合物、包含其的药物组合物及其制备方法和用途 |
| 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 |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶KRas抑制劑 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025081291A1 (en) * | 2023-10-16 | 2025-04-24 | Canwell Biotech Limited | Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (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 |
| 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 (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10238477A1 (de) * | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| WO2004096806A1 (ja) * | 2003-04-30 | 2004-11-11 | Sumitomo Pharmaceuticals Co. Ltd. | 縮合イミダゾール誘導体 |
| US20070219178A1 (en) * | 2003-12-04 | 2007-09-20 | Eisai Co., Ltd. | Preventive or therapeutic agents for multiple sclerosis |
| US7582631B2 (en) * | 2004-01-14 | 2009-09-01 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| MX2007006230A (es) * | 2004-11-30 | 2007-07-25 | Amgen Inc | Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer. |
| US8350043B2 (en) * | 2005-06-07 | 2013-01-08 | Pharmacopeia, Inc. | Azinone and diazinone V3 inhibitors for depression and stress disorders |
| MX2008015648A (es) * | 2006-06-21 | 2009-01-09 | Du Pont | Pirazinonas como inhibidores de proliferacion celular. |
| WO2008107398A2 (en) * | 2007-03-02 | 2008-09-12 | Basf Se | Pyrazine compounds |
| WO2009049098A2 (en) | 2007-10-09 | 2009-04-16 | Indiana University Research & Technology Corporation | Materials and methods for regulating the activity of phosphatases |
| KR101906146B1 (ko) * | 2009-08-17 | 2018-10-10 | 메모리얼 슬로안-케터링 캔서 센터 | 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법 |
| CN102080087B (zh) | 2010-12-08 | 2012-05-30 | 厦门大学 | 蛋白酪氨酸磷酸酶shp2的核酸适体及其制备方法 |
| AU2014256984B2 (en) | 2013-04-26 | 2019-02-14 | Indiana University Research & Technology Corporation | Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) |
| EP3016652A4 (en) | 2013-07-03 | 2017-03-08 | Indiana University Research and Technology Corporation | Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors |
| AR097631A1 (es) * | 2013-09-16 | 2016-04-06 | Bayer Pharma AG | Trifluorometilpirimidinonas sustituidas con heterociclos y sus usos |
| JP6523303B2 (ja) | 2014-01-17 | 2019-05-29 | ノバルティス アーゲー | Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物 |
| CN105899493B (zh) | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| SI3137169T1 (sl) * | 2014-05-01 | 2022-04-29 | Celgene Quanticel Research, Inc. | Inhibitorji lizin specifične demetilaze-1 |
| KR102461419B1 (ko) * | 2014-05-13 | 2022-11-02 | 메모리얼 슬로안 케터링 캔서 센터 | Hsp70 조정물질 및 이의 제조 및 이용 방법 |
| RS60658B1 (sr) * | 2014-06-27 | 2020-09-30 | Celgene Quanticel Research Inc | Inhibitori lizin specifične demetilaze-1 |
| WO2016196569A1 (en) | 2015-06-01 | 2016-12-08 | Indiana University Research & Technology Corporation | Small molecule inhibitors of protein tyrosine phosphatases and uses thereof |
| ES2824576T3 (es) * | 2015-06-19 | 2021-05-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| CN112625028B (zh) | 2015-06-19 | 2024-10-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| ES2741746T3 (es) * | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| US9932288B2 (en) | 2015-12-09 | 2018-04-03 | West Virginia University | Chemical compound for inhibition of SHP2 function and for use as an anti-cancer agent |
| WO2017156397A1 (en) * | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| CN107286150B (zh) | 2016-04-11 | 2020-07-07 | 中国科学院上海有机化学研究所 | N-杂环类化合物、其中间体、制备方法、药物组合物和应用 |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| MX383856B (es) * | 2016-06-14 | 2025-03-14 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de shp2. |
| KR102598895B1 (ko) * | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| IL303436A (en) * | 2016-08-10 | 2023-08-01 | Celgene Quanticel Res Inc | Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| US20190343836A1 (en) | 2017-01-10 | 2019-11-14 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| MX2019008696A (es) | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
| CN108341791B (zh) | 2017-01-23 | 2020-09-29 | 中国科学院上海药物研究所 | 苯并噻二唑类化合物、其制备方法及用途 |
| MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
| EP3589647A1 (en) | 2017-02-28 | 2020-01-08 | Novartis AG | Shp inhibitor compositions and uses for chimeric antigen receptor therapy |
| KR20240026521A (ko) | 2017-03-23 | 2024-02-28 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| CA3074690A1 (en) | 2017-09-07 | 2019-03-14 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
| EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| MX2020003579A (es) | 2017-10-12 | 2020-07-22 | Revolution Medicines Inc | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. |
| CN108113984B (zh) | 2017-12-20 | 2021-05-07 | 中国科学院成都生物研究所 | Shp2抑制剂在制备抗肿瘤的药物中的用途 |
| WO2019165073A1 (en) * | 2018-02-21 | 2019-08-29 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| CN108578395B (zh) | 2018-06-21 | 2019-10-25 | 厦门大学 | 苯丙烯酸类化合物在制备Shp2特异性抑制剂中的用途及其制药用途 |
| CN109646441A (zh) | 2019-01-25 | 2019-04-19 | 上海交通大学医学院附属仁济医院 | Shp-2抑制剂在制备靶向前神经元型胶质瘤的药物中的应用 |
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2019
- 2019-03-18 RU RU2020133727A patent/RU2020133727A/ru unknown
- 2019-03-18 JP JP2020550667A patent/JP7265275B2/ja active Active
- 2019-03-18 CA CA3097709A patent/CA3097709A1/en not_active Abandoned
- 2019-03-18 AU AU2019239658A patent/AU2019239658A1/en not_active Abandoned
- 2019-03-18 CN CN201980031603.9A patent/CN112368272B/zh active Active
- 2019-03-18 KR KR1020207030224A patent/KR102724968B1/ko active Active
- 2019-03-18 TW TW108109165A patent/TW201940167A/zh unknown
- 2019-03-18 WO PCT/US2019/022717 patent/WO2019182960A1/en not_active Ceased
- 2019-03-18 EP EP19771115.3A patent/EP3768664B1/en active Active
- 2019-03-18 US US16/356,360 patent/US10561655B2/en active Active
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