JP2017502017A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017502017A5 JP2017502017A5 JP2016540575A JP2016540575A JP2017502017A5 JP 2017502017 A5 JP2017502017 A5 JP 2017502017A5 JP 2016540575 A JP2016540575 A JP 2016540575A JP 2016540575 A JP2016540575 A JP 2016540575A JP 2017502017 A5 JP2017502017 A5 JP 2017502017A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- delta
- cas number
- intellikine
- therapeutics
- 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.)
- Granted
Links
- 239000003112 inhibitor Substances 0.000 claims description 366
- 239000003814 drug Substances 0.000 claims description 309
- 230000037361 pathway Effects 0.000 claims description 204
- 239000002246 antineoplastic agent Substances 0.000 claims description 112
- 229940126656 GS-4224 Drugs 0.000 claims description 90
- 206010028980 Neoplasm Diseases 0.000 claims description 90
- 201000011510 cancer Diseases 0.000 claims description 90
- 150000003839 salts Chemical group 0.000 claims description 84
- 229940118166 PI3 kinase delta inhibitor Drugs 0.000 claims description 72
- 102000038030 PI3Ks Human genes 0.000 claims description 72
- 108091007960 PI3Ks Proteins 0.000 claims description 72
- 239000003795 chemical substances by application Substances 0.000 claims description 69
- 229940124597 therapeutic agent Drugs 0.000 claims description 54
- 229940116355 PI3 kinase inhibitor Drugs 0.000 claims description 50
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims description 50
- 241000124008 Mammalia Species 0.000 claims description 46
- 230000000694 effects Effects 0.000 claims description 39
- -1 radionuclides Substances 0.000 claims description 38
- 239000008194 pharmaceutical composition Substances 0.000 claims description 37
- SRLVNYDXMUGOFI-XBXARRHUSA-N (5e)-5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione Chemical compound C1=C2OC(F)(F)OC2=CC=C1\C=C1\SC(=O)NC1=O SRLVNYDXMUGOFI-XBXARRHUSA-N 0.000 claims description 36
- LFWGZXMTCUOPFI-UHFFFAOYSA-N 2,3-diphenyl-6-quinoxalinecarboxylic acid Chemical compound C=1C=CC=CC=1C1=NC2=CC(C(=O)O)=CC=C2N=C1C1=CC=CC=C1 LFWGZXMTCUOPFI-UHFFFAOYSA-N 0.000 claims description 36
- KGPGFQWBCSZGEL-ZDUSSCGKSA-N GSK690693 Chemical compound C=12N(CC)C(C=3C(=NON=3)N)=NC2=C(C#CC(C)(C)O)N=CC=1OC[C@H]1CCCNC1 KGPGFQWBCSZGEL-ZDUSSCGKSA-N 0.000 claims description 36
- ZHEHVZXPFVXKEY-RUAOOFDTSA-N KT 5720 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@](C(=O)OCCCCCC)(O)[C@@]4(C)O1 ZHEHVZXPFVXKEY-RUAOOFDTSA-N 0.000 claims description 36
- 241001465754 Metazoa Species 0.000 claims description 36
- 229960003445 idelalisib Drugs 0.000 claims description 36
- YKLIKGKUANLGSB-HNNXBMFYSA-N idelalisib Chemical compound C1([C@@H](NC=2[C]3N=CN=C3N=CN=2)CC)=NC2=CC=CC(F)=C2C(=O)N1C1=CC=CC=C1 YKLIKGKUANLGSB-HNNXBMFYSA-N 0.000 claims description 36
- LBTVHXHERHESKG-UHFFFAOYSA-N tetrahydrocurcumin Chemical compound C1=C(O)C(OC)=CC(CCC(=O)CC(=O)CCC=2C=C(OC)C(O)=CC=2)=C1 LBTVHXHERHESKG-UHFFFAOYSA-N 0.000 claims description 36
- 210000004027 cell Anatomy 0.000 claims description 34
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims description 33
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims description 33
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 claims description 32
- KSERXGMCDHOLSS-LJQANCHMSA-N n-[(1s)-1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-chloro-2-(propan-2-ylamino)pyridin-4-yl]-1h-pyrrole-2-carboxamide Chemical compound C1=NC(NC(C)C)=CC(C=2C=C(NC=2)C(=O)N[C@H](CO)C=2C=C(Cl)C=CC=2)=C1Cl KSERXGMCDHOLSS-LJQANCHMSA-N 0.000 claims description 22
- ZKZXNDJNWUTGDK-NSCUHMNNSA-N (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide Chemical compound C1=CC(Br)=CC=C1\C=C\CNCCNS(=O)(=O)C1=CC=CC2=CN=CC=C12 ZKZXNDJNWUTGDK-NSCUHMNNSA-N 0.000 claims description 20
- IUGRBTCJEYEDIY-VZUCSPMQSA-N (e)-2-(3,4-dihydroxybenzoyl)-3-(2-oxo-3h-1,3-benzoxazol-5-yl)prop-2-enenitrile Chemical compound C1=C(O)C(O)=CC=C1C(=O)C(\C#N)=C\C1=CC=C(OC(=O)N2)C2=C1 IUGRBTCJEYEDIY-VZUCSPMQSA-N 0.000 claims description 18
- SCSSXJVRZMQUKA-UHFFFAOYSA-N 2-(9h-fluoren-9-ylmethoxycarbonylamino)-3-pyridin-4-ylpropanoic acid Chemical compound C12=CC=CC=C2C2=CC=CC=C2C1COC(=O)NC(C(=O)O)CC1=CC=NC=C1 SCSSXJVRZMQUKA-UHFFFAOYSA-N 0.000 claims description 18
- PUYVJBBSBPUKBT-AWEZNQCLSA-N 2-[(1s)-1-[(2-amino-7h-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one Chemical compound C1([C@@H](NC=2C=3NC=NC=3N=C(N)N=2)C)=NC2=CC=CC(C)=C2C(=O)N1C1=CC=CC=C1C PUYVJBBSBPUKBT-AWEZNQCLSA-N 0.000 claims description 18
- RZIDZIGAXXNODG-UHFFFAOYSA-N 4-[(4-chlorophenyl)methyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine Chemical compound C1CN(C=2C=3C=CNC=3N=CN=2)CCC1(N)CC1=CC=C(Cl)C=C1 RZIDZIGAXXNODG-UHFFFAOYSA-N 0.000 claims description 18
- BYWWNRBKPCPJMG-UHFFFAOYSA-N 4-dodecyl-n-(1,3,4-thiadiazol-2-yl)benzenesulfonamide Chemical compound C1=CC(CCCCCCCCCCCC)=CC=C1S(=O)(=O)NC1=NN=CS1 BYWWNRBKPCPJMG-UHFFFAOYSA-N 0.000 claims description 18
- SDGWAUUPHUBJNQ-UHFFFAOYSA-N 5-(1,3-benzodioxol-5-ylmethylidene)-1,3-thiazolidine-2,4-dione Chemical compound S1C(=O)NC(=O)C1=CC1=CC=C(OCO2)C2=C1 SDGWAUUPHUBJNQ-UHFFFAOYSA-N 0.000 claims description 18
- DOCINCLJNAXZQF-LBPRGKRZSA-N 6-fluoro-3-phenyl-2-[(1s)-1-(7h-purin-6-ylamino)ethyl]quinazolin-4-one Chemical compound C1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)=NC2=CC=C(F)C=C2C(=O)N1C1=CC=CC=C1 DOCINCLJNAXZQF-LBPRGKRZSA-N 0.000 claims description 18
- HWUHTJIKQZZBRA-UHFFFAOYSA-N 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2h-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride Chemical compound Cl.Cl.C=1C=C(C=2C(=CC=3C=4N(C(NN=4)=O)C=CC=3N=2)C=2C=CC=CC=2)C=CC=1C1(N)CCC1 HWUHTJIKQZZBRA-UHFFFAOYSA-N 0.000 claims description 18
- SJVQHLPISAIATJ-ZDUSSCGKSA-N 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]-1-isoquinolinone Chemical compound C1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)=CC2=CC=CC(Cl)=C2C(=O)N1C1=CC=CC=C1 SJVQHLPISAIATJ-ZDUSSCGKSA-N 0.000 claims description 18
- 229960005531 AMG 319 Drugs 0.000 claims description 18
- BYTORXDZJWWIKR-UHFFFAOYSA-N Hinokiol Natural products CC(C)c1cc2CCC3C(C)(CO)C(O)CCC3(C)c2cc1O BYTORXDZJWWIKR-UHFFFAOYSA-N 0.000 claims description 18
- 241000282412 Homo Species 0.000 claims description 18
- 101150093335 KIN1 gene Proteins 0.000 claims description 18
- 108091054455 MAP kinase family Proteins 0.000 claims description 18
- 102000043136 MAP kinase family Human genes 0.000 claims description 18
- 241000288906 Primates Species 0.000 claims description 18
- 239000004037 angiogenesis inhibitor Substances 0.000 claims description 18
- 239000002254 cytotoxic agent Substances 0.000 claims description 18
- 229940127089 cytotoxic agent Drugs 0.000 claims description 18
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 18
- 239000012634 fragment Substances 0.000 claims description 18
- FVYXIJYOAGAUQK-UHFFFAOYSA-N honokiol Chemical compound C1=C(CC=C)C(O)=CC=C1C1=CC(CC=C)=CC=C1O FVYXIJYOAGAUQK-UHFFFAOYSA-N 0.000 claims description 18
- VVOAZFWZEDHOOU-UHFFFAOYSA-N honokiol Natural products OC1=CC=C(CC=C)C=C1C1=CC(CC=C)=CC=C1O VVOAZFWZEDHOOU-UHFFFAOYSA-N 0.000 claims description 18
- 239000005556 hormone Substances 0.000 claims description 18
- 229940088597 hormone Drugs 0.000 claims description 18
- 239000002955 immunomodulating agent Substances 0.000 claims description 18
- 229940121354 immunomodulator Drugs 0.000 claims description 18
- 229960003775 miltefosine Drugs 0.000 claims description 18
- 230000035772 mutation Effects 0.000 claims description 18
- KWRYMZHCQIOOEB-LBPRGKRZSA-N n-[(1s)-1-(7-fluoro-2-pyridin-2-ylquinolin-3-yl)ethyl]-7h-purin-6-amine Chemical compound C1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)=CC2=CC=C(F)C=C2N=C1C1=CC=CC=N1 KWRYMZHCQIOOEB-LBPRGKRZSA-N 0.000 claims description 18
- SZFPYBIJACMNJV-UHFFFAOYSA-N perifosine Chemical compound CCCCCCCCCCCCCCCCCCOP([O-])(=O)OC1CC[N+](C)(C)CC1 SZFPYBIJACMNJV-UHFFFAOYSA-N 0.000 claims description 18
- 229950010632 perifosine Drugs 0.000 claims description 18
- 239000003053 toxin Substances 0.000 claims description 18
- 231100000765 toxin Toxicity 0.000 claims description 18
- 108700012359 toxins Proteins 0.000 claims description 18
- NGFFVZQXSRKHBM-FKBYEOEOSA-N 5-[[(1r,1as,6br)-1-[6-(trifluoromethyl)-1h-benzimidazol-2-yl]-1a,6b-dihydro-1h-cyclopropa[b][1]benzofuran-5-yl]oxy]-3,4-dihydro-1h-1,8-naphthyridin-2-one Chemical compound N1C(=O)CCC2=C1N=CC=C2OC(C=C1[C@@H]23)=CC=C1O[C@@H]3[C@H]2C1=NC2=CC=C(C(F)(F)F)C=C2N1 NGFFVZQXSRKHBM-FKBYEOEOSA-N 0.000 claims description 16
- 108020004459 Small interfering RNA Proteins 0.000 claims description 16
- PQLXHQMOHUQAKB-UHFFFAOYSA-N miltefosine Chemical compound CCCCCCCCCCCCCCCCOP([O-])(=O)OCC[N+](C)(C)C PQLXHQMOHUQAKB-UHFFFAOYSA-N 0.000 claims description 16
- 230000000392 somatic effect Effects 0.000 claims description 16
- 229950003873 triciribine Drugs 0.000 claims description 16
- HOGVTUZUJGHKPL-HTVVRFAVSA-N triciribine Chemical compound C=12C3=NC=NC=1N(C)N=C(N)C2=CN3[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O HOGVTUZUJGHKPL-HTVVRFAVSA-N 0.000 claims description 16
- 230000002195 synergetic effect Effects 0.000 claims description 15
- VWMJHAFYPMOMGF-ZCFIWIBFSA-N TAK-580 Chemical compound N([C@H](C)C=1SC(=CN=1)C(=O)NC=1N=CC(Cl)=C(C=1)C(F)(F)F)C(=O)C1=NC=NC(N)=C1Cl VWMJHAFYPMOMGF-ZCFIWIBFSA-N 0.000 claims description 14
- 229960002465 dabrafenib Drugs 0.000 claims description 12
- BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical group S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 claims description 12
- 239000002552 dosage form Substances 0.000 claims description 12
- 239000003085 diluting agent Substances 0.000 claims description 10
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims description 9
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims description 9
- CMJCXYNUCSMDBY-ZDUSSCGKSA-N lgx818 Chemical compound COC(=O)N[C@@H](C)CNC1=NC=CC(C=2C(=NN(C=2)C(C)C)C=2C(=C(NS(C)(=O)=O)C=C(Cl)C=2)F)=N1 CMJCXYNUCSMDBY-ZDUSSCGKSA-N 0.000 claims description 9
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical compound N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims description 8
- DEZZLWQELQORIU-RELWKKBWSA-N GDC-0879 Chemical compound N=1N(CCO)C=C(C=2C=C3CCC(/C3=CC=2)=N\O)C=1C1=CC=NC=C1 DEZZLWQELQORIU-RELWKKBWSA-N 0.000 claims description 8
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims description 8
- 239000002138 L01XE21 - Regorafenib Substances 0.000 claims description 8
- YZDJQTHVDDOVHR-UHFFFAOYSA-N PLX-4720 Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(Cl)=CN=C3NC=2)=C1F YZDJQTHVDDOVHR-UHFFFAOYSA-N 0.000 claims description 8
- OJFKUJDRGJSAQB-UHFFFAOYSA-N TAK-632 Chemical compound C1=C(NC(=O)CC=2C=C(C=CC=2)C(F)(F)F)C(F)=CC=C1OC(C(=C1S2)C#N)=CC=C1N=C2NC(=O)C1CC1 OJFKUJDRGJSAQB-UHFFFAOYSA-N 0.000 claims description 8
- 210000003050 axon Anatomy 0.000 claims description 8
- 239000002774 b raf kinase inhibitor Substances 0.000 claims description 8
- HXINDCTZKGGRDE-JPKZNVRTSA-L disodium;[3-[5-[2-[[(3r)-1-(1-methylpyrazol-3-yl)sulfonylpiperidin-3-yl]amino]pyrimidin-4-yl]imidazo[2,1-b][1,3]oxazol-6-yl]phenoxy]methyl phosphate Chemical compound [Na+].[Na+].CN1C=CC(S(=O)(=O)N2C[C@@H](CCC2)NC=2N=C(C=CN=2)C=2N3C=COC3=NC=2C=2C=C(OCOP([O-])([O-])=O)C=CC=2)=N1 HXINDCTZKGGRDE-JPKZNVRTSA-L 0.000 claims description 8
- 229960000639 pazopanib Drugs 0.000 claims description 8
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims description 8
- 229960004836 regorafenib Drugs 0.000 claims description 8
- 150000004934 Regorafenib derivatives Chemical group 0.000 claims description 6
- KDGFLJKFZUIJMX-UHFFFAOYSA-N alectinib Chemical compound CCC1=CC=2C(=O)C(C3=CC=C(C=C3N3)C#N)=C3C(C)(C)C=2C=C1N(CC1)CCC1N1CCOCC1 KDGFLJKFZUIJMX-UHFFFAOYSA-N 0.000 claims description 6
- OMEUGRCNAZNQLN-UHFFFAOYSA-N isis 5132 Chemical compound O=C1NC(=O)C(C)=CN1C1OC(COP(O)(=S)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(S)(=O)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)CO)C(O)C1 OMEUGRCNAZNQLN-UHFFFAOYSA-N 0.000 claims description 6
- 230000004611 cancer cell death Effects 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims description 2
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims description 2
- 239000003183 carcinogenic agent Substances 0.000 claims description 2
- 239000000575 pesticide Substances 0.000 claims description 2
- FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 claims description 2
- FCKJZIRDZMVDEM-UHFFFAOYSA-N N-(7,8-dimethoxy-2,3-dihydro-1H-imidazo[1,2-c]quinazolin-5-ylidene)pyridine-3-carboxamide Chemical compound COC1=C(C2=NC(=NC(=O)C3=CN=CC=C3)N4CCNC4=C2C=C1)OC FCKJZIRDZMVDEM-UHFFFAOYSA-N 0.000 claims 2
- 229960003862 vemurafenib Drugs 0.000 claims 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 48
- AFCLEMNPGSUBDT-UHFFFAOYSA-N CN(c1c(C(N2)=O)[n](Cc(cc3)ccc3Cl)c(S)n1)C2=O Chemical compound CN(c1c(C(N2)=O)[n](Cc(cc3)ccc3Cl)c(S)n1)C2=O AFCLEMNPGSUBDT-UHFFFAOYSA-N 0.000 description 2
- VTFCZAWGUWVLNZ-UHFFFAOYSA-N CN(c1c(C(N2Cc3ccccc3)=O)[n](Cc3ccccc3)c(SCCO)n1)C2=O Chemical compound CN(c1c(C(N2Cc3ccccc3)=O)[n](Cc3ccccc3)c(SCCO)n1)C2=O VTFCZAWGUWVLNZ-UHFFFAOYSA-N 0.000 description 2
- 101000666730 Homo sapiens T-complex protein 1 subunit alpha Proteins 0.000 description 1
- 102100038410 T-complex protein 1 subunit alpha Human genes 0.000 description 1
- 239000003560 cancer drug Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361919347P | 2013-12-20 | 2013-12-20 | |
| US61/919,347 | 2013-12-20 | ||
| PCT/US2014/071715 WO2015095819A2 (en) | 2013-12-20 | 2014-12-19 | Cancer treatment using combinations of erk and raf inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502017A JP2017502017A (ja) | 2017-01-19 |
| JP2017502017A5 true JP2017502017A5 (https=) | 2018-02-08 |
| JP6678585B2 JP6678585B2 (ja) | 2020-04-22 |
Family
ID=53403899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540575A Active JP6678585B2 (ja) | 2013-12-20 | 2014-12-19 | Ｅｒｋ阻害剤およびｒａｆ阻害剤の組み合わせを使用するがん処置 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10668055B2 (https=) |
| EP (3) | EP4043017B1 (https=) |
| JP (1) | JP6678585B2 (https=) |
| CN (1) | CN106211755B (https=) |
| AU (1) | AU2014368906B2 (https=) |
| BR (1) | BR112016014481B1 (https=) |
| CA (4) | CA3240745A1 (https=) |
| ES (2) | ES2909910T3 (https=) |
| MX (2) | MX384721B (https=) |
| RU (1) | RU2722784C2 (https=) |
| WO (1) | WO2015095819A2 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| TWI674262B (zh) | 2011-01-10 | 2019-10-11 | 美商英菲尼提製藥股份有限公司 | 製備異喹啉酮之方法及異喹啉酮之固體形式 |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| EP2914296B2 (en) | 2012-11-01 | 2021-09-29 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| WO2015095842A2 (en) | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2017066664A1 (en) * | 2015-10-16 | 2017-04-20 | Millennium Pharmaceuticals, Inc. | Combination therapy including a raf inhibitor for the treatment of colorectal cancer |
| WO2017095826A1 (en) * | 2015-11-30 | 2017-06-08 | The Regents Of The University Of California | Combination therapy for treatment of melanoma |
| WO2017136741A1 (en) * | 2016-02-05 | 2017-08-10 | Evol Science LLC | Combinations to treat cancer |
| WO2017158621A1 (en) * | 2016-03-14 | 2017-09-21 | Sphaera Pharma Pvt. Ltd. | Trigonelline based compounds |
| WO2017165491A1 (en) * | 2016-03-24 | 2017-09-28 | Millennium Pharmaceuticals, Inc. | Use of a pd-1 antagonist and a raf inhibitor in the treatment of cancer |
| RU2754507C2 (ru) | 2016-06-24 | 2021-09-02 | Инфинити Фармасьютикалз, Инк. | Комбинированная терапия |
| AU2017329090B9 (en) | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
| ES2928773T3 (es) | 2017-01-17 | 2022-11-22 | Heparegenix Gmbh | Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos |
| ES2952265T3 (es) | 2017-05-02 | 2023-10-30 | Novartis Ag | Terapia combinada que comprende un inhibidor de Raf y trametinib |
| AU2018269982B2 (en) * | 2017-05-16 | 2024-06-13 | Biomed Valley Discoveries, Inc. | Compositions and methods for treating cancer with atypical BRAF mutations |
| EP3635396A4 (en) | 2017-06-06 | 2021-05-26 | The Johns Hopkins University | INDUCTION OF ARTIFICIAL LETALITY WITH EPIGENETIC THERAPY |
| KR20200037820A (ko) | 2017-08-07 | 2020-04-09 | 에볼 사이언스 엘엘씨 | 암을 치료하기 위한 조합 |
| JP7332589B2 (ja) | 2017-10-12 | 2023-08-23 | ノバルティス アーゲー | 癌を治療するためのｍｄｍ２阻害剤とｅｒｋの阻害剤との組合せ |
| US11426408B2 (en) * | 2017-11-01 | 2022-08-30 | National University Of Singapore | Use of serotonergic drugs to treat virus-induced thrombocytopenia |
| JP7379355B2 (ja) * | 2017-11-20 | 2023-11-14 | トルレモ セラピューティクス アーゲー | 診断方法 |
| WO2019103984A1 (en) * | 2017-11-22 | 2019-05-31 | Memorial Sloan Kettering Cancer Center | Compositions including fatp1, fatp3, fatp4, fatp5, and/or fatp6 inhibitors and uses thereof |
| WO2019195959A1 (en) * | 2018-04-08 | 2019-10-17 | Cothera Biosciences, Inc. | Combination therapy for cancers with braf mutation |
| ES3025633T3 (en) | 2019-05-13 | 2025-06-09 | Novartis Ag | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
| JP7582694B2 (ja) | 2020-01-10 | 2024-11-13 | イミューニヤリング コーポレーション | Ｍｅｋ阻害剤及びその治療的使用 |
| MX2023009642A (es) * | 2021-02-19 | 2023-10-16 | Day One Biopharmaceuticals Inc | Combinacion de inhibidor de raf e inhibidor de mek. |
| CN113018269B (zh) * | 2021-03-14 | 2022-06-03 | 华中科技大学同济医学院附属协和医院 | 复合颗粒物、其制备方法及其应用 |
| KR20240044419A (ko) * | 2021-06-24 | 2024-04-04 | 에라스카, 아이엔씨. | Erk1/2 및 egfr 억제제 조합 요법 |
| IL312248A (en) * | 2021-10-28 | 2024-06-01 | Verastem Inc | Combined treatment for abnormal cell proliferation |
| IL312469A (en) * | 2021-11-02 | 2024-06-01 | Verastem Inc | Methods of treating abnormal cell growth |
| CN115400122B (zh) * | 2022-04-29 | 2023-04-18 | 佛山病原微生物研究院 | 一种tak-632在制备用于抗腺病毒感染的药物中的用途 |
| US11873296B2 (en) | 2022-06-07 | 2024-01-16 | Verastem, Inc. | Solid forms of a dual RAF/MEK inhibitor |
| TW202517624A (zh) * | 2023-07-03 | 2025-05-01 | 美商醫療免疫工程公司 | Mek免疫腫瘤抑制劑醫藥組合物 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE220114T1 (de) | 1993-03-19 | 2002-07-15 | Sequenom Inc | Dns-sequenzbestimmung durch massenspektrometrie auf dem weg des abbaus mit exonuklease |
| US6140053A (en) | 1996-11-06 | 2000-10-31 | Sequenom, Inc. | DNA sequencing by mass spectrometry via exonuclease degradation |
| US7439016B1 (en) | 2000-06-15 | 2008-10-21 | Digene Corporation | Detection of nucleic acids by type-specific hybrid capture method |
| US7601497B2 (en) | 2000-06-15 | 2009-10-13 | Qiagen Gaithersburg, Inc. | Detection of nucleic acids by target-specific hybrid capture method |
| GB0121490D0 (en) * | 2001-09-05 | 2001-10-24 | Smithkline Beecham Plc | Ciompounds |
| GB0320059D0 (en) | 2003-08-27 | 2003-10-01 | Solexa Ltd | A method of sequencing |
| LT3305776T (lt) * | 2004-05-14 | 2020-01-10 | Vertex Pharmaceuticals Incorporated | Pirolo junginiai kaip erk baltymo kinazės inhibitoriai, ir farmacinės kompozicijos su šiais junginiais |
| US7582623B2 (en) | 2004-05-20 | 2009-09-01 | The Regents Of The University Of California | Photoactive metal nitrosyls for blood pressure regulation and cancer therapy |
| US20060228721A1 (en) | 2005-04-12 | 2006-10-12 | Leamon John H | Methods for determining sequence variants using ultra-deep sequencing |
| CA2609387A1 (en) * | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Combination therapy comprising diaryl ureas for treating diseases |
| CN102206216B (zh) * | 2005-06-22 | 2014-11-12 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
| AR068046A1 (es) * | 2007-06-05 | 2009-11-04 | Schering Corp | Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer |
| WO2010062546A1 (en) | 2008-10-27 | 2010-06-03 | Qiagen Gaithersburg Inc. | Fast results hybrid capture assay on an automated platform |
| JO3002B1 (ar) * | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| KR20120046018A (ko) | 2010-10-04 | 2012-05-09 | 삼성테크윈 주식회사 | 단일 뉴클레오티드 다형성의 실시간 ｐｃｒ 검출 |
| WO2012068562A2 (en) * | 2010-11-19 | 2012-05-24 | The Regents Of The University Of California | Compositions and methods for detection and treatment of b-raf inhibitor-resistant melanomas |
| WO2012125848A2 (en) | 2011-03-16 | 2012-09-20 | Baylor College Of Medicine | A method for comprehensive sequence analysis using deep sequencing technology |
| WO2013074594A1 (en) | 2011-11-14 | 2013-05-23 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with braf inhibitors |
-
2014
- 2014-12-19 CA CA3240745A patent/CA3240745A1/en active Pending
- 2014-12-19 EP EP22154150.1A patent/EP4043017B1/en active Active
- 2014-12-19 ES ES14872061T patent/ES2909910T3/es active Active
- 2014-12-19 JP JP2016540575A patent/JP6678585B2/ja active Active
- 2014-12-19 ES ES22154150T patent/ES3063344T3/es active Active
- 2014-12-19 CA CA3168002A patent/CA3168002C/en active Active
- 2014-12-19 CA CA3300955A patent/CA3300955A1/en active Pending
- 2014-12-19 BR BR112016014481-3A patent/BR112016014481B1/pt active IP Right Grant
- 2014-12-19 EP EP26154129.6A patent/EP4732908A2/en active Pending
- 2014-12-19 WO PCT/US2014/071715 patent/WO2015095819A2/en not_active Ceased
- 2014-12-19 US US15/105,904 patent/US10668055B2/en active Active
- 2014-12-19 CN CN201480074321.4A patent/CN106211755B/zh active Active
- 2014-12-19 RU RU2016129287A patent/RU2722784C2/ru active
- 2014-12-19 MX MX2016008201A patent/MX384721B/es unknown
- 2014-12-19 MX MX2021008610A patent/MX394252B/es unknown
- 2014-12-19 AU AU2014368906A patent/AU2014368906B2/en active Active
- 2014-12-19 EP EP14872061.8A patent/EP3082800B1/en active Active
- 2014-12-19 CA CA2934669A patent/CA2934669C/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017502017A5 (https=) | ||
| RU2016129287A (ru) | Лечение злокачественных опухолей с применением комбинаций ингибиторов erk и raf | |
| JP2017502013A5 (https=) | ||
| Kumar et al. | Current and emerging therapeutic approaches for colorectal cancer: A comprehensive review | |
| JP2017500320A5 (https=) | ||
| JP2017502016A5 (https=) | ||
| JP2017502014A5 (https=) | ||
| JP7405408B2 (ja) | 異型ｂｒａｆ変異を有するがんを処置するための組成物および方法 | |
| JP7788114B2 (ja) | ヒトにおける固形腫瘍の処置のためのＣ．ｎｏｖｙｉ | |
| EP3111937B1 (en) | Medicament for treatment of liver cancer | |
| Buchbinder et al. | Phase 2 study of sunitinib in patients with metastatic mucosal or acral melanoma | |
| JP2020519660A5 (https=) | ||
| CL2018001371A1 (es) | Uso de un inhibidor de b-raf y de un inhibidor de mek 1/2 para el tratamiento de un paciente que padece melanoma (divisional solicitud 201502807) | |
| CN111821306A (zh) | Mdm2抑制剂和其组合 | |
| CA2939464A1 (en) | Use of anti-ccr5 antibodies in graft versus host disease | |
| KR20180129918A (ko) | 암 치료를 위한 Notch 및 CDK4/6 억제제의 조합 요법 | |
| JP2016520057A (ja) | 癌の治療 | |
| EP4520398A3 (en) | Treatment of prostate cancer | |
| Besse et al. | A phase Ib dose-escalation study of everolimus combined with cisplatin and etoposide as first-line therapy in patients with extensive-stage small-cell lung cancer | |
| JP2019530706A5 (https=) | ||
| JP2014523398A5 (https=) | ||
| Raucci et al. | Cyclic Fasting–Mimicking Diet Plus Bortezomib and Rituximab Is an Effective Treatment for Chronic Lymphocytic Leukemia | |
| US20250041293A1 (en) | An igf1r inhibitor and an akt inhibitor for use in the treatment of cancer | |
| Kivitz et al. | THU0109 Lack of efficacy of CCR1 antagonist BMS-817399 in patients with moderate to severe rheumatoid arthritis: results of 12-week proof-of-concept study | |
| Weng et al. | Vemurafenib-associated neutrophilic panniculitis in a patient with metastatic amelanotic melanoma presenting as cancer of unknown primary origin |