JP2022184886A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2022184886A5 JP2022184886A5 JP2022142153A JP2022142153A JP2022184886A5 JP 2022184886 A5 JP2022184886 A5 JP 2022184886A5 JP 2022142153 A JP2022142153 A JP 2022142153A JP 2022142153 A JP2022142153 A JP 2022142153A JP 2022184886 A5 JP2022184886 A5 JP 2022184886A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- azaspiro
- thio
- pyrazin
- methyl
- 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.)
- Pending
Links
- 206010028980 Neoplasm Diseases 0.000 claims 14
- 201000011510 cancer Diseases 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 229940122531 Anaplastic lymphoma kinase inhibitor Drugs 0.000 claims 9
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims 8
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims 8
- 239000003112 inhibitor Substances 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 4
- UCJZOKGUEJUNIO-IINYFYTJSA-N (3S,4S)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound C[C@@H]1OCC2(CCN(CC2)C2=CN=C(SC3=C(Cl)C(N)=NC=C3)C(N)=N2)[C@@H]1N UCJZOKGUEJUNIO-IINYFYTJSA-N 0.000 claims 3
- 206010029260 Neuroblastoma Diseases 0.000 claims 3
- 229950001290 lorlatinib Drugs 0.000 claims 3
- IIXWYSCJSQVBQM-LLVKDONJSA-N lorlatinib Chemical group N=1N(C)C(C#N)=C2C=1CN(C)C(=O)C1=CC=C(F)C=C1[C@@H](C)OC1=CC2=CN=C1N IIXWYSCJSQVBQM-LLVKDONJSA-N 0.000 claims 3
- VCACXGULTWUFOL-CMPLNLGQSA-N (2R,4R)-4-amino-8-[6-amino-5-(2,3-dichloropyridin-4-yl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-2-ol Chemical compound N[C@@H]1C[C@H](O)CC11CCN(CC1)C1=NC(N)=C(SC2=CC=NC(Cl)=C2Cl)N=C1 VCACXGULTWUFOL-CMPLNLGQSA-N 0.000 claims 2
- QRCMRHHVLLNDAD-WCQYABFASA-N (2R,4R)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-2-methyl-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(N=CC(=N1)N1CCC2(C[C@H](C[C@H]2N)C)CC1)SC1=C(C(=NC=C1)N)Cl QRCMRHHVLLNDAD-WCQYABFASA-N 0.000 claims 2
- VCACXGULTWUFOL-ZYHUDNBSSA-N (2S,4R)-4-amino-8-[6-amino-5-(2,3-dichloropyridin-4-yl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-2-ol Chemical compound N[C@@H]1C[C@@H](O)CC11CCN(CC1)C1=NC(N)=C(SC2=CC=NC(Cl)=C2Cl)N=C1 VCACXGULTWUFOL-ZYHUDNBSSA-N 0.000 claims 2
- FDSVUVZQRZMZJD-MGPLVRAMSA-N (3S,4S)-8-[3-(2,3-dichloropyridin-4-yl)-2H-pyrazolo[3,4-b]pyrazin-6-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound ClC1=NC=CC(=C1Cl)C1=NNC2=NC(=CN=C21)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1 FDSVUVZQRZMZJD-MGPLVRAMSA-N 0.000 claims 2
- NIQAQDPFKXLLSZ-MEDUHNTESA-N (3S,4S)-8-[5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=NC=CC(=C1Cl)SC=1N=CC(=NC=1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1 NIQAQDPFKXLLSZ-MEDUHNTESA-N 0.000 claims 2
- ZGMUIFZUVXWGJL-MGPLVRAMSA-N (3S,4S)-8-[5-(6-amino-2,3-dichloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound C[C@@H]1OCC2(CCN(CC2)C2=CN=C(SC3=C(Cl)C(Cl)=NC(N)=C3)C=N2)[C@@H]1N ZGMUIFZUVXWGJL-MGPLVRAMSA-N 0.000 claims 2
- MQHUNAGZKZJLQU-APPDUMDISA-N (3S,4S)-8-[6-amino-5-(2,3-dichlorophenyl)pyrazin-2-yl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(N=CC(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C1=C(C(=CC=C1)Cl)Cl MQHUNAGZKZJLQU-APPDUMDISA-N 0.000 claims 2
- BSPKRXNBXSLYTO-XHDPSFHLSA-N (3S,4S)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-ethyl-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(N=CC(=N1)N1CCC2([C@@H]([C@@H](OC2)CC)N)CC1)SC1=C(C(=NC=C1)N)Cl BSPKRXNBXSLYTO-XHDPSFHLSA-N 0.000 claims 2
- OVNZJLIYRSOHHB-RGUGMKFQSA-N (4R)-8-[5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-8-azaspiro[4.5]decan-4-amine Chemical compound CC1CCC2(CCN(CC2)C2=CN=C(SC3=CC=NC(N)=C3Cl)C=N2)[C@@H]1N OVNZJLIYRSOHHB-RGUGMKFQSA-N 0.000 claims 2
- CQASZSQCUYWGME-CYBMUJFWSA-N (4R)-8-[5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=NC=CC(=C1Cl)SC=1N=CC(=NC=1)N1CCC2(CCC[C@H]2N)CC1 CQASZSQCUYWGME-CYBMUJFWSA-N 0.000 claims 2
- DYZZCXHBYCBNEC-CQSZACIVSA-N (4R)-8-[6-amino-5-(2,3-dichlorophenyl)pyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(N=CC(=N1)N1CCC2(CCC[C@H]2N)CC1)C1=C(C(=CC=C1)Cl)Cl DYZZCXHBYCBNEC-CQSZACIVSA-N 0.000 claims 2
- DIFDDGZESHEIPC-JOPIAHFSSA-N (4R)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-3-methyl-8-azaspiro[4.5]decan-4-amine Chemical compound CC1CCC2(CCN(CC2)C2=CN=C(SC3=CC=NC(N)=C3Cl)C(N)=N2)[C@@H]1N DIFDDGZESHEIPC-JOPIAHFSSA-N 0.000 claims 2
- YXXCYOPEUVHPLV-GFCCVEGCSA-N (4R)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(N=CC(=N1)N1CCC2(CCC[C@H]2N)CC1)SC1=C(C(=NC=C1)N)Cl YXXCYOPEUVHPLV-GFCCVEGCSA-N 0.000 claims 2
- AHSZEDCSMMKDNF-GFCCVEGCSA-N (4S)-8-[5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound N[C@@H]1COCC11CCN(CC1)C1=CN=C(SC2=CC=NC(N)=C2Cl)C=N1 AHSZEDCSMMKDNF-GFCCVEGCSA-N 0.000 claims 2
- OMJHHTRDBKAMSN-LLVKDONJSA-N (4S)-8-[6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanylpyrazin-2-yl]-2-oxa-8-azaspiro[4.5]decan-4-amine Chemical compound N[C@@H]1COCC11CCN(CC1)C1=CN=C(SC2=CC=NC(N)=C2Cl)C(N)=N1 OMJHHTRDBKAMSN-LLVKDONJSA-N 0.000 claims 2
- BXVJYYGWZPCIII-YVEFUNNKSA-N 2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(3-chloro-2-methoxypyridin-4-yl)-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=C2C1=C(C(=NC=C1)OC)Cl)=O)C)C BXVJYYGWZPCIII-YVEFUNNKSA-N 0.000 claims 2
- HZDHVNNLNPUGCB-UHFFFAOYSA-N 2-[4-(aminomethyl)-4-methylpiperidin-1-yl]-5-(2,3-dichlorophenyl)-3,7-dihydropyrrolo[2,3-d]pyrimidin-4-one Chemical compound NCC1(CCN(CC1)C=1NC(C2=C(N=1)NC=C2C1=C(C(=CC=C1)Cl)Cl)=O)C HZDHVNNLNPUGCB-UHFFFAOYSA-N 0.000 claims 2
- MLZSINIGJFDNQZ-UHFFFAOYSA-N 6-(1,8-diazaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine Chemical compound ClC1=C(C=CC=C1Cl)C=1C(=NC(=CN=1)N1CCC2(CCCN2)CC1)N MLZSINIGJFDNQZ-UHFFFAOYSA-N 0.000 claims 2
- YGUFCDOEKKVKJK-UHFFFAOYSA-N 6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine Chemical group NC1(CCN(CC1)C1=CN=C(C(=N1)N)C1=C(C(=CC=C1)Cl)Cl)C YGUFCDOEKKVKJK-UHFFFAOYSA-N 0.000 claims 2
- PXWVEUAMAFDBCT-SWLSCSKDSA-N 6-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-3-(6-amino-2-methylpyridin-3-yl)-5-methyl-2H-pyrazolo[3,4-d]pyrimidin-4-one Chemical compound C[C@H]1C[C@@H](N)C2(C1)CCN(CC2)c1nc2n[nH]c(-c3ccc(N)nc3C)c2c(=O)n1C PXWVEUAMAFDBCT-SWLSCSKDSA-N 0.000 claims 2
- URUPFUYPXLMTMT-KPZWWZAWSA-N 6-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-[3-chloro-2-(cyclopropylamino)pyridin-4-yl]-5-methyl-2H-pyrazolo[3,4-d]pyrimidin-4-one Chemical compound C[C@@H]1OCC2(CCN(CC2)c2nc3n[nH]c(-c4ccnc(NC5CC5)c4Cl)c3c(=O)n2C)[C@@H]1N URUPFUYPXLMTMT-KPZWWZAWSA-N 0.000 claims 2
- JLWLVSCZOWTUQJ-CYBMUJFWSA-N 6-[(4R)-4-amino-2,2-difluoro-8-azaspiro[4.5]decan-8-yl]-3-(6-amino-2-methylpyridin-3-yl)-5-methyl-2H-pyrazolo[3,4-d]pyrimidin-4-one Chemical compound NC1=CC=C(C(=N1)C)C=1NN=C2N=C(N(C(C2=1)=O)C)N1CCC2(CC(C[C@H]2N)(F)F)CC1 JLWLVSCZOWTUQJ-CYBMUJFWSA-N 0.000 claims 2
- AWCUGJTVKPBYHS-CQSZACIVSA-N 6-[(4R)-4-amino-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-5-methyl-2H-pyrazolo[3,4-d]pyrimidin-4-one Chemical compound N[C@@H]1CCCC11CCN(CC1)C=1N(C(C=2C(N=1)=NNC=2C1=C(C(=CC=C1)Cl)Cl)=O)C AWCUGJTVKPBYHS-CQSZACIVSA-N 0.000 claims 2
- ZAMNYDQBNJFTSZ-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-methylpiperidin-1-yl]-3-(2,3-dichlorophenyl)pyrazin-2-amine Chemical compound CC1(CN)CCN(CC1)C1=CN=C(C(N)=N1)C1=CC=CC(Cl)=C1Cl ZAMNYDQBNJFTSZ-UHFFFAOYSA-N 0.000 claims 2
- JBLYMVJAFCDNOA-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-methylpiperidin-1-yl]-3-[2-(trifluoromethyl)pyridin-3-yl]sulfanylpyrazin-2-amine Chemical compound NCC1(CCN(CC1)C1=CN=C(C(=N1)N)SC=1C(=NC=CC1)C(F)(F)F)C JBLYMVJAFCDNOA-UHFFFAOYSA-N 0.000 claims 2
- YFMXXMJLAJOQKJ-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-phenylpiperidin-1-yl]-3-(2,3-dichlorophenyl)pyrazin-2-amine Chemical compound NCC1(CCN(CC1)C1=CN=C(C(N)=N1)C1=CC=CC(Cl)=C1Cl)C1=CC=CC=C1 YFMXXMJLAJOQKJ-UHFFFAOYSA-N 0.000 claims 2
- GHNNUZAENHZAOE-SWLSCSKDSA-N 6-amino-2-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-3-methyl-5-[3-(trifluoromethyl)pyridin-4-yl]sulfanylpyrimidin-4-one Chemical compound C[C@H]1C[C@@H](N)C2(C1)CCN(CC2)c1nc(N)c(Sc2ccncc2C(F)(F)F)c(=O)n1C GHNNUZAENHZAOE-SWLSCSKDSA-N 0.000 claims 2
- LNQYLYAZNKGMBQ-GOEBONIOSA-N 6-amino-2-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-3-methyl-5-phenylpyrimidin-4-one Chemical compound C[C@H]1C[C@@H](N)C2(C1)CCN(CC2)C1=NC(N)=C(C2=CC=CC=C2)C(=O)N1C LNQYLYAZNKGMBQ-GOEBONIOSA-N 0.000 claims 2
- XNRBIYGXCHMMLM-SWLSCSKDSA-N 6-amino-2-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-5-(2,3-dichlorophenyl)-3-methylpyrimidin-4-one Chemical compound C[C@H]1C[C@@H](N)C2(C1)CCN(CC2)C1=NC(N)=C(C(=O)N1C)C1=CC=CC(Cl)=C1Cl XNRBIYGXCHMMLM-SWLSCSKDSA-N 0.000 claims 2
- IKKUGOCAYJSNOZ-XJKSGUPXSA-N 6-amino-2-[(2R,4R)-4-amino-2-methyl-8-azaspiro[4.5]decan-8-yl]-5-(4-chlorophenyl)-3-methylpyrimidin-4-one Chemical compound C[C@H]1C[C@@H](N)C2(C1)CCN(CC2)C1=NC(N)=C(C2=CC=C(Cl)C=C2)C(=O)N1C IKKUGOCAYJSNOZ-XJKSGUPXSA-N 0.000 claims 2
- NQCUFBIRMAZNJZ-SWLSCSKDSA-N 6-amino-2-[(3S,4S)-4-amino-3-ethyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-methyl-5-[2-(trifluoromethyl)pyridin-3-yl]sulfanylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)CC)N)CC1)C)=O)SC=1C(=NC=CC=1)C(F)(F)F NQCUFBIRMAZNJZ-SWLSCSKDSA-N 0.000 claims 2
- QZHZIDHAIVAHMD-SMDDNHRTSA-N 6-amino-2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-methyl-5-[2-(trifluoromethyl)pyridin-3-yl]sulfanylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C)=O)SC=1C(=NC=CC=1)C(F)(F)F QZHZIDHAIVAHMD-SMDDNHRTSA-N 0.000 claims 2
- DEBVNDHNGLRJKA-XHDPSFHLSA-N 6-amino-2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-methyl-5-[3-(trifluoromethyl)pyridin-4-yl]sulfanylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C)=O)SC1=C(C=NC=C1)C(F)(F)F DEBVNDHNGLRJKA-XHDPSFHLSA-N 0.000 claims 2
- YDOIDJXVWAVDGD-MEDUHNTESA-N 6-amino-2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(2,3-dichlorophenyl)sulfanyl-3-methylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C)=O)SC1=C(C(=CC=C1)Cl)Cl YDOIDJXVWAVDGD-MEDUHNTESA-N 0.000 claims 2
- YQIKHFKYMKSZMC-YVEFUNNKSA-N 6-amino-2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-(2-chloro-3-methoxyphenyl)sulfanyl-3-methylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C)=O)SC1=C(C(=CC=C1)OC)Cl YQIKHFKYMKSZMC-YVEFUNNKSA-N 0.000 claims 2
- FWLRJXKKWWAIIU-MEDUHNTESA-N 6-amino-2-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-[3-amino-2-(trifluoromethyl)phenyl]sulfanyl-3-methylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C)=O)SC1=C(C(=CC=C1)N)C(F)(F)F FWLRJXKKWWAIIU-MEDUHNTESA-N 0.000 claims 2
- OOZUDBICHRCGIM-LLVKDONJSA-N 6-amino-5-(2-amino-3-chloropyridin-4-yl)sulfanyl-2-[(4R)-4-amino-2,2-difluoro-8-azaspiro[4.5]decan-8-yl]-3-methylpyrimidin-4-one Chemical compound NC1=C(C(N(C(=N1)N1CCC2(CC(C[C@H]2N)(F)F)CC1)C)=O)SC1=C(C(=NC=C1)N)Cl OOZUDBICHRCGIM-LLVKDONJSA-N 0.000 claims 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- NYPXMXPABWAYNI-UHFFFAOYSA-N CC1(CN)CCN(CC1)c1cnc(Sc2cccc(NC(=O)c3c(O)nc4CCCCn4c3=O)c2Cl)c(N)n1 Chemical compound CC1(CN)CCN(CC1)c1cnc(Sc2cccc(NC(=O)c3c(O)nc4CCCCn4c3=O)c2Cl)c(N)n1 NYPXMXPABWAYNI-UHFFFAOYSA-N 0.000 claims 2
- SXLOCFFGRYJKJH-UHFFFAOYSA-N CC1(CN)CCN(CC1)c1cnc(Sc2cccc(NC(=O)c3c(O)nc4ccccn4c3=O)c2Cl)c(N)n1 Chemical compound CC1(CN)CCN(CC1)c1cnc(Sc2cccc(NC(=O)c3c(O)nc4ccccn4c3=O)c2Cl)c(N)n1 SXLOCFFGRYJKJH-UHFFFAOYSA-N 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 201000003803 Inflammatory myofibroblastic tumor Diseases 0.000 claims 2
- 206010067917 Inflammatory myofibroblastic tumour Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- JJTYMCPMKUFMGA-UHFFFAOYSA-N N-[3-[3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl]sulfanyl-2-chlorophenyl]-2-benzyl-3-hydroxy-1-methyl-5-oxo-2H-pyrrole-4-carboxamide Chemical compound CN1C(Cc2ccccc2)C(O)=C(C(=O)Nc2cccc(Sc3ncc(nc3N)N3CCC(C)(N)CC3)c2Cl)C1=O JJTYMCPMKUFMGA-UHFFFAOYSA-N 0.000 claims 2
- JBTYRLRPDPSWAY-UHFFFAOYSA-N N-[3-[3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyrazin-2-yl]sulfanyl-2-chlorophenyl]-3-hydroxy-5-oxo-1-phenyl-2H-pyrrole-4-carboxamide Chemical compound CC1(N)CCN(CC1)c1cnc(Sc2cccc(NC(=O)C3=C(O)CN(C3=O)c3ccccc3)c2Cl)c(N)n1 JBTYRLRPDPSWAY-UHFFFAOYSA-N 0.000 claims 2
- JZDGMMPURNKFOD-UHFFFAOYSA-N NC=1C(=NC=C(N=1)N1CCC(CC1)(C)N)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)C=CC=C2)O)Cl Chemical compound NC=1C(=NC=C(N=1)N1CCC(CC1)(C)N)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)C=CC=C2)O)Cl JZDGMMPURNKFOD-UHFFFAOYSA-N 0.000 claims 2
- QQGWBWWGXPNCEH-UHFFFAOYSA-N NC=1C(=NC=C(N=1)N1CCC(CC1)(CF)N)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl Chemical compound NC=1C(=NC=C(N=1)N1CCC(CC1)(CF)N)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl QQGWBWWGXPNCEH-UHFFFAOYSA-N 0.000 claims 2
- PVBNSTQJFPASQY-QGZVFWFLSA-N NC=1C(=NC=C(N=1)N1CCC2(CC(C[C@H]2N)(F)F)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl Chemical compound NC=1C(=NC=C(N=1)N1CCC2(CC(C[C@H]2N)(F)F)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl PVBNSTQJFPASQY-QGZVFWFLSA-N 0.000 claims 2
- QZVSNMBRLYUYQI-GOSISDBHSA-N NC=1C(=NC=C(N=1)N1CCC2(CCC[C@H]2N)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl Chemical compound NC=1C(=NC=C(N=1)N1CCC2(CCC[C@H]2N)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl QZVSNMBRLYUYQI-GOSISDBHSA-N 0.000 claims 2
- NGJFCIYVFFUILZ-OYHNWAKOSA-N NC=1C(=NC=C(N=1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl Chemical compound NC=1C(=NC=C(N=1)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)SC=1C(=C(C=CC=1)NC(=O)C1=C(N=C2N(C1=O)CCCC2)O)Cl NGJFCIYVFFUILZ-OYHNWAKOSA-N 0.000 claims 2
- SJVCCJDLEIGCAW-QGZVFWFLSA-N N[C@@H]1COCC11CCN(CC1)C1=NC(N)=C(SC2=CC=CC(NC(=O)C3=C(O)N=C4CCCCN4C3=O)=C2Cl)N=C1 Chemical compound N[C@@H]1COCC11CCN(CC1)C1=NC(N)=C(SC2=CC=CC(NC(=O)C3=C(O)N=C4CCCCN4C3=O)=C2Cl)N=C1 SJVCCJDLEIGCAW-QGZVFWFLSA-N 0.000 claims 2
- ZVBSVBHUEYAOGL-UHFFFAOYSA-N Nc1nc(cnc1Sc1cccc(NC(=O)c2c(O)nc3ccccn3c2=O)c1Cl)N1CCC(N)(CF)CC1 Chemical compound Nc1nc(cnc1Sc1cccc(NC(=O)c2c(O)nc3ccccn3c2=O)c1Cl)N1CCC(N)(CF)CC1 ZVBSVBHUEYAOGL-UHFFFAOYSA-N 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- UOQACRNTVQWTFF-UHFFFAOYSA-N decane-1,10-dithiol Chemical compound SCCCCCCCCCCS UOQACRNTVQWTFF-UHFFFAOYSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762444493P | 2017-01-10 | 2017-01-10 | |
| US62/444,493 | 2017-01-10 | ||
| JP2019536863A JP7503380B2 (ja) | 2017-01-10 | 2018-01-08 | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 |
| PCT/IB2018/050111 WO2018130928A1 (en) | 2017-01-10 | 2018-01-08 | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019536863A Division JP7503380B2 (ja) | 2017-01-10 | 2018-01-08 | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022184886A JP2022184886A (ja) | 2022-12-13 |
| JP2022184886A5 true JP2022184886A5 (enExample) | 2023-06-08 |
Family
ID=61028108
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019536863A Active JP7503380B2 (ja) | 2017-01-10 | 2018-01-08 | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 |
| JP2022142153A Pending JP2022184886A (ja) | 2017-01-10 | 2022-09-07 | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019536863A Active JP7503380B2 (ja) | 2017-01-10 | 2018-01-08 | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20190343836A1 (enExample) |
| EP (1) | EP3568204B1 (enExample) |
| JP (2) | JP7503380B2 (enExample) |
| KR (1) | KR102571130B1 (enExample) |
| CN (1) | CN110730678B (enExample) |
| AU (1) | AU2018207464B2 (enExample) |
| CA (1) | CA3048340A1 (enExample) |
| ES (1) | ES2964956T3 (enExample) |
| IL (1) | IL267617A (enExample) |
| RU (1) | RU2769132C2 (enExample) |
| WO (1) | WO2018130928A1 (enExample) |
Families Citing this family (86)
| 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 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| AU2017226389B2 (en) | 2016-03-04 | 2023-02-02 | Taiho Pharmaceutical Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| CN109311848B (zh) * | 2016-06-07 | 2022-02-01 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| RU2744988C2 (ru) | 2016-06-14 | 2021-03-17 | Новартис Аг | Соединения и композиции для подавления активности shp2 |
| AU2017296289A1 (en) | 2016-07-12 | 2019-01-31 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての二環式化合物 |
| CN110431134A (zh) | 2017-01-23 | 2019-11-08 | 锐新医药公司 | 作为变构shp2抑制剂的吡啶化合物 |
| KR20200051684A (ko) | 2017-09-07 | 2020-05-13 | 레볼루션 메디슨즈, 인크. | 암 치료를 위한 shp2 억제제 조성물 및 방법 |
| US10435389B2 (en) | 2017-09-11 | 2019-10-08 | Krouzon Pharmaccuticals, Inc. | Octahydrocyclopenta[c]pyrrole allosteric inhibitors of SHP2 |
| EP3694848A1 (en) * | 2017-10-12 | 2020-08-19 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| TW201927791A (zh) | 2017-12-15 | 2019-07-16 | 美商銳新醫藥公司 | 作為變構shp2抑制劑的多環化合物 |
| MX2020008754A (es) | 2018-03-02 | 2020-12-07 | Otsuka Pharma Co Ltd | Compuestos farmaceuticos. |
| PL3769765T3 (pl) | 2018-03-19 | 2024-06-10 | Taiho Pharmaceutical Co., Ltd. | Kompozycja farmaceutyczna zawierająca alkilosiarczan sodu |
| AU2019239658A1 (en) | 2018-03-21 | 2020-11-12 | Suzhou Puhe BioPharma Co., Ltd. | SHP2 inhibitors and uses thereof |
| US10954243B2 (en) | 2018-05-02 | 2021-03-23 | Navire Pharma, Inc. | Substituted heterocyclic inhibitors of PTPN11 |
| MX2021000795A (es) * | 2018-07-24 | 2021-04-12 | Taiho Pharmaceutical Co Ltd | Compuestos heterociclicos para inhibir la actividad de shp2. |
| EP3833670B1 (en) | 2018-08-10 | 2024-04-17 | Navire Pharma, Inc. | 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 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| WO2020065452A1 (en) | 2018-09-29 | 2020-04-02 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| MX2021003459A (es) | 2018-09-29 | 2021-06-18 | Novartis Ag | Proceso de fabricacion de un compuesto para la inhibicion de la actividad de shp2. |
| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| CN111153899B (zh) * | 2018-11-08 | 2023-12-01 | 四川科伦博泰生物医药股份有限公司 | 一种取代吡啶化合物、其制备方法和用途 |
| WO2020108590A1 (zh) | 2018-11-30 | 2020-06-04 | 上海拓界生物医药科技有限公司 | 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用 |
| CN113382731A (zh) * | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和瑞博西尼的药物组合 |
| CN113382774A (zh) * | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和krasg12c抑制剂的药物组合 |
| CN113395967A (zh) * | 2019-02-12 | 2021-09-14 | 诺华股份有限公司 | 包含tno155和pd-1抑制剂的药物组合 |
| US20230148450A9 (en) | 2019-03-01 | 2023-05-11 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| US20230096028A1 (en) | 2019-03-01 | 2023-03-30 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
| 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 |
| US11033547B2 (en) | 2019-03-07 | 2021-06-15 | Merck Patent Gmbh | Carboxamide-pyrimidine derivatives as SHP2 antagonists |
| AU2020271838A1 (en) | 2019-04-08 | 2021-08-19 | Merck Patent Gmbh | Pyrimidinone derivatives as SHP2 antagonists |
| EP3991731A4 (en) | 2019-06-28 | 2022-07-20 | Tuojie Biotech (Shanghai) Co., Ltd. | FIVE-MEMBERED NITROGEN-CONTAINING HETEROCYCLIC PYRIMIDINE DERIVATIVE, PROCESS FOR ITS PREPARATION AND ITS PHARMACEUTICAL USE |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| WO2021061515A1 (en) * | 2019-09-23 | 2021-04-01 | Synblia Therapeutics, Inc. | Shp2 inhibitors and uses thereof |
| 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 |
| CN115894606A (zh) | 2019-11-04 | 2023-04-04 | 锐新医药公司 | Ras抑制剂 |
| CA3160142A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2021091967A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| KR20220100903A (ko) | 2019-11-08 | 2022-07-18 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2021110796A1 (en) * | 2019-12-04 | 2021-06-10 | Bayer Aktiengesellschaft | Inhibitors of shp2 |
| CN113135910A (zh) * | 2020-01-19 | 2021-07-20 | 北京诺诚健华医药科技有限公司 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| EP4093406A4 (en) * | 2020-01-24 | 2024-02-28 | Taiho Pharmaceutical Co., Ltd. | IMPROVEMENT OF THE ANTI-TUMORAL ACTIVITY OF SHP2 INHIBITOR PYRIMIDINONE IN COMBINATION WITH NEW ANTI-CANCER DRUGS AGAINST CANCER |
| CN111265529B (zh) * | 2020-02-22 | 2021-07-23 | 南京大学 | 蛋白酪氨酸磷酸酶shp2抑制剂在制备治疗银屑病药物中的应用 |
| CN111393459B (zh) * | 2020-04-16 | 2022-07-22 | 南京安纳康生物科技有限公司 | Shp2抑制剂及其用途 |
| EP4146217A1 (en) * | 2020-05-08 | 2023-03-15 | Novartis AG | Pharmaceutical combination comprising tno155 and nazartinib |
| WO2021236775A1 (en) * | 2020-05-19 | 2021-11-25 | The Regents Of The University Ofmichigan | Small molecule degraders of shp2 protein |
| CN115515946A (zh) * | 2020-06-11 | 2022-12-23 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| JP2023530351A (ja) | 2020-06-18 | 2023-07-14 | レヴォリューション・メディスンズ，インコーポレイテッド | Ｒａｓ阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法 |
| WO2021259077A1 (zh) * | 2020-06-22 | 2021-12-30 | 四川科伦博泰生物医药股份有限公司 | 取代吡嗪类化合物，包含其的药物组合物及其用途 |
| CN115916786B (zh) | 2020-07-08 | 2025-10-17 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物的制造 |
| KR20230081726A (ko) | 2020-09-03 | 2023-06-07 | 레볼루션 메디슨즈, 인크. | Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도 |
| KR20230067635A (ko) | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | 암의 치료에서 ras 억제제로서 인돌 유도체 |
| WO2022089389A1 (zh) * | 2020-10-30 | 2022-05-05 | 赣江新区博瑞创新医药有限公司 | 杂环化合物及其制备方法、药物组合物和应用 |
| CN112194652B (zh) * | 2020-11-30 | 2021-03-05 | 北京华氏开元医药科技有限公司 | 4-羟甲基-1h-吲哚类化合物、制备方法及应用 |
| CN112402385B (zh) * | 2020-11-30 | 2022-04-01 | 北京华氏开元医药科技有限公司 | 4-羟甲基-1h-吲哚类化合物药物制剂及其制备方法 |
| WO2022140427A1 (en) | 2020-12-22 | 2022-06-30 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| CA3217393A1 (en) | 2021-05-05 | 2022-11-10 | Elena S. Koltun | Ras inhibitors |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2022235817A1 (en) | 2021-05-05 | 2022-11-10 | Huabio International, Llc | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
| MX2023012929A (es) * | 2021-05-05 | 2023-11-13 | Huyabio Int Llc | Terapias de combinacion que comprenden inhibidores de shp2 e inhibidores de tirosina cinasa egfr. |
| CN118852330A (zh) | 2021-05-05 | 2024-10-29 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| EP4333850A4 (en) | 2021-05-05 | 2025-04-09 | Huyabio International, LLC | SHP2 INHIBITOR MONOTHERAPY AND ITS USES |
| 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 |
| WO2023280237A1 (zh) * | 2021-07-07 | 2023-01-12 | 海创药业股份有限公司 | 一种磷酸酶降解剂的合成和应用 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| KR20230106506A (ko) * | 2022-01-03 | 2023-07-13 | 한국생명공학연구원 | Cda 억제제를 포함하는 alk 저해제 내성 비소세포폐암 치료용 조성물 |
| TW202342040A (zh) * | 2022-02-21 | 2023-11-01 | 瑞士商諾華公司 | 藥物配製物 |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| TW202446388A (zh) | 2023-04-14 | 2024-12-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑之結晶形式、含有其之組合物及其使用方法 |
| 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 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025137507A1 (en) | 2023-12-22 | 2025-06-26 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| CN120227378A (zh) * | 2023-12-28 | 2025-07-01 | 轩竹生物科技股份有限公司 | 间变性淋巴瘤激酶抑制剂的药物组合物及其制备方法 |
| 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 |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2567518B1 (fr) | 1984-07-11 | 1987-11-13 | Sanofi Sa | Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent |
| US4959368A (en) | 1986-02-24 | 1990-09-25 | Mitsui Petrochemical Industries Ltd. | Therapeutic agent for neurological diseases |
| DK169008B1 (da) | 1990-06-01 | 1994-07-25 | Holec Lk A S | Fremgangsmåde og skærm til afskærmning af en strømtransformer samt strømtransformer med en sådan afskærmning |
| GB9012316D0 (en) | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
| CA2369945A1 (en) | 1999-04-06 | 2000-10-12 | James L. Kelley | Neurotrophic thio substituted pyrimidines |
| JP4272338B2 (ja) | 2000-09-22 | 2009-06-03 | バイエル アクチェンゲゼルシャフト | ピリジン誘導体 |
| EP2090571B1 (de) | 2001-10-17 | 2012-05-16 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung |
| GB0300783D0 (en) | 2003-01-14 | 2003-02-12 | Btg Int Ltd | Treatment of neurodegenerative conditions |
| JP4978192B2 (ja) | 2004-04-01 | 2012-07-18 | アステラス製薬株式会社 | ピラジン誘導体およびその医薬的使用 |
| AU2005249380C1 (en) | 2004-04-23 | 2012-09-20 | Exelixis, Inc. | Kinase modulators and methods of use |
| WO2006065946A1 (en) | 2004-12-16 | 2006-06-22 | Vertex Pharmaceuticals Incorporated | Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases |
| AU2006290715A1 (en) | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 2-aminopyrimidine derivatives as modulators of the histamine H4 receptor activity |
| WO2007112368A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Preparation of (r)-3-aminopiperidine dihydrochloride |
| US7515405B2 (en) | 2006-07-25 | 2009-04-07 | Hewlett-Packard Development Company, L.P. | Anti-rotation mechanism for an electronic device |
| US20090137549A1 (en) | 2006-11-09 | 2009-05-28 | Paul John Edward | Novel compounds useful for the treatment of degenerative & inflamatory diseases |
| ME00811B (me) | 2006-12-08 | 2012-03-20 | Novartis Ag | JEDINJENJA l KOMPOZICIJE KAO INHIBITORI PROTEIN KINAZE |
| JP2010518083A (ja) | 2007-02-12 | 2010-05-27 | メルク・シャープ・エンド・ドーム・コーポレイション | ピペリジン誘導体 |
| DK2137162T3 (en) | 2007-03-15 | 2018-11-26 | Novartis Ag | Organic compounds and their applications |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2310381A1 (en) | 2008-06-13 | 2011-04-20 | Novartis AG | 2,4'-bipyridinyl compounds as protein kinase d inhibitors useful for the treatment of ia heart failure and cancer |
| BRPI0914891A2 (pt) | 2008-06-20 | 2015-11-24 | Metabolex Inc | agonistas de aril gpr119 e usos dos mesmos |
| NZ624345A (en) | 2008-06-27 | 2016-07-29 | Celgene Avilomics Res Inc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| WO2010011666A2 (en) | 2008-07-21 | 2010-01-28 | University Of South Florida | Indoline scaffold shp-2 inhibitors and cancer treatment method |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| US20110306606A1 (en) | 2008-12-10 | 2011-12-15 | Jei Man Ryu | Novel 2,6-substituted-3-nitropyridine derivative, method for preparing same, and pharmaceutical composition including same |
| FR2941696B1 (fr) | 2009-02-05 | 2011-04-15 | Sanofi Aventis | Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| US9567318B2 (en) | 2009-08-17 | 2017-02-14 | Memorial Sloan-Kettering Cancer Center | Substituted pyrimidine compounds and uses thereof |
| US8673913B2 (en) | 2009-11-13 | 2014-03-18 | Case Western Reserve University | SHP-2 phosphatase inhibitor |
| WO2011078143A1 (ja) | 2009-12-22 | 2011-06-30 | 塩野義製薬株式会社 | ピリミジン誘導体およびそれらを含有する医薬組成物 |
| MY177250A (en) | 2010-06-30 | 2020-09-10 | Fujifilm Corp | Novel nicotinamide derivative or salt thereof |
| WO2012009217A1 (en) | 2010-07-13 | 2012-01-19 | Merck Sharp & Dohme Corp. | Spirocyclic compounds |
| CA2806341C (en) | 2010-07-29 | 2020-03-24 | Rigel Pharmaceuticals, Inc. | Ampk-activating heterocyclic compounds and methods for using the same |
| WO2012027495A1 (en) | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| WO2012052948A1 (en) | 2010-10-20 | 2012-04-26 | Pfizer Inc. | Pyridine- 2- derivatives as smoothened receptor modulators |
| JP6082011B2 (ja) | 2011-09-12 | 2017-02-15 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体 |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| PL3290414T3 (pl) | 2012-05-23 | 2020-01-31 | Nerviano Medical Sciences S.R.L. | Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu |
| CA2874546A1 (en) | 2012-06-07 | 2013-12-12 | F. Hoffmann-La Roche Ag | Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase |
| EP2903985A1 (en) | 2012-10-03 | 2015-08-12 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| US9499522B2 (en) | 2013-03-15 | 2016-11-22 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2015050344A1 (ko) | 2013-10-01 | 2015-04-09 | 주식회사 엘지화학 | 도전성 적층체 |
| WO2015092819A2 (en) | 2013-12-21 | 2015-06-25 | Nektar Therapeutics (India) Pvt. Ltd. | Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine |
| CN105848682A (zh) * | 2013-12-23 | 2016-08-10 | 诺华股份有限公司 | 药物组合 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| WO2015107493A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| ES2699354T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2 |
| SG11201609033TA (en) | 2014-05-01 | 2016-11-29 | Celgene Quanticel Res Inc | Inhibitors of lysine specific demethylase-1 |
| US10174032B2 (en) | 2014-05-05 | 2019-01-08 | Signalrx Pharmaceuticals, Inc. | Heterocyclic compound classes for signaling modulation |
| CN107207524B (zh) | 2014-08-15 | 2020-02-07 | 贵州省中国科学院天然产物化学重点实验室 | 双苄基异喹啉衍生物、其制备方法及其在肝病的治疗与预防中的用途 |
| EP3185866A1 (en) * | 2014-08-25 | 2017-07-05 | Pfizer Inc. | Combination of a pd-1 antagonist and an alk inhibitor for treating cancer |
| US9296721B1 (en) * | 2015-02-13 | 2016-03-29 | Yong Xu | Method for preparing ALK inhibitor ceritinib |
| 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 |
| WO2016203404A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| JP6878316B2 (ja) | 2015-06-19 | 2021-05-26 | ノバルティス アーゲー | Ｓｈｐ２の活性を阻害するための化合物および組成物 |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| RU2744988C2 (ru) | 2016-06-14 | 2021-03-17 | Новартис Аг | Соединения и композиции для подавления активности shp2 |
| EP3515916B1 (en) * | 2016-09-22 | 2023-06-07 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| TWI848901B (zh) * | 2016-10-24 | 2024-07-21 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
-
2018
- 2018-01-08 CA CA3048340A patent/CA3048340A1/en active Pending
- 2018-01-08 CN CN201880006104.XA patent/CN110730678B/zh active Active
- 2018-01-08 EP EP18701574.8A patent/EP3568204B1/en active Active
- 2018-01-08 RU RU2019120986A patent/RU2769132C2/ru active
- 2018-01-08 AU AU2018207464A patent/AU2018207464B2/en not_active Ceased
- 2018-01-08 ES ES18701574T patent/ES2964956T3/es active Active
- 2018-01-08 KR KR1020197019305A patent/KR102571130B1/ko active Active
- 2018-01-08 US US16/475,982 patent/US20190343836A1/en not_active Abandoned
- 2018-01-08 WO PCT/IB2018/050111 patent/WO2018130928A1/en not_active Ceased
- 2018-01-08 JP JP2019536863A patent/JP7503380B2/ja active Active
-
2019
- 2019-06-24 IL IL267617A patent/IL267617A/en unknown
-
2022
- 2022-04-06 US US17/714,996 patent/US12053470B2/en active Active
- 2022-09-07 JP JP2022142153A patent/JP2022184886A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022184886A5 (enExample) | ||
| JP2020504136A5 (enExample) | ||
| JP7503380B2 (ja) | Ａｌｋ阻害剤およびｓｈｐ２阻害剤を含む組合せ医薬 | |
| JP2024517695A (ja) | 複素環式化合物及び使用方法 | |
| JP2024532733A (ja) | 複素環式化合物及び使用方法 | |
| JP7654071B2 (ja) | 複素環スピロ化合物及び使用方法 | |
| JP2025508702A (ja) | キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 | |
| US9926324B2 (en) | Heteroaromatic compounds as PI3 kinase modulators and methods of use | |
| JP6695353B2 (ja) | Ｆｇｆｒ４阻害剤としてのホルミル化ｎ−複素環式誘導体 | |
| TWI682930B (zh) | 治療性雜環化合物 | |
| JP2018529731A5 (enExample) | ||
| JP2016538316A5 (enExample) | ||
| HRP20192151T1 (hr) | Derivati izokromena kao inhibitori fosfoinozitid 3-kinaza | |
| WO2022093856A1 (en) | Heterocyclic spiro compounds and methods of use | |
| JP2011511034A5 (enExample) | ||
| JP2016537384A5 (enExample) | ||
| JP2025535046A (ja) | Ｋｒａｓ ｇ１２ｃ変異タンパク質の複素環阻害剤及びその使用 | |
| US20230203062A1 (en) | Therapeutic compounds and methods of use | |
| JPWO2023046117A5 (enExample) | ||
| MX2008000897A (es) | Combinacion de una pirimidil-amino-benzamida y un inhibidor de cinasa mtor. | |
| CN117561063A (zh) | 杂环化合物及使用方法 | |
| HK40019993A (en) | Therapeutic heterocyclic compounds |