JP2020504742A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020504742A5 JP2020504742A5 JP2019534303A JP2019534303A JP2020504742A5 JP 2020504742 A5 JP2020504742 A5 JP 2020504742A5 JP 2019534303 A JP2019534303 A JP 2019534303A JP 2019534303 A JP2019534303 A JP 2019534303A JP 2020504742 A5 JP2020504742 A5 JP 2020504742A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- cycloalkyl
- aryl
- heterocyclyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 93
- 125000003118 aryl group Chemical group 0.000 claims 61
- 125000000623 heterocyclic group Chemical group 0.000 claims 47
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 36
- 125000001072 heteroaryl group Chemical group 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 30
- 239000001257 hydrogen Substances 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 29
- 125000001424 substituent group Chemical group 0.000 claims 29
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 26
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 26
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 24
- 239000003112 inhibitor Substances 0.000 claims 23
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 14
- 125000005842 heteroatom Chemical group 0.000 claims 12
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 11
- 239000013543 active substance Substances 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 229940126271 SOS1 inhibitor Drugs 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 229940123237 Taxane Drugs 0.000 claims 3
- -1 and C 1- 6- alkyl Chemical group 0.000 claims 3
- 230000000340 anti-metabolite Effects 0.000 claims 3
- 229940100197 antimetabolite Drugs 0.000 claims 3
- 239000002256 antimetabolite Substances 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 229960001592 paclitaxel Drugs 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 3
- 101100404726 Arabidopsis thaliana NHX7 gene Proteins 0.000 claims 2
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 2
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 2
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 2
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 2
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 2
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims 2
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 108700022176 SOS1 Proteins 0.000 claims 2
- 101100197320 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) RPL35A gene Proteins 0.000 claims 2
- 102100032929 Son of sevenless homolog 1 Human genes 0.000 claims 2
- 101150100839 Sos1 gene Proteins 0.000 claims 2
- 229950001573 abemaciclib Drugs 0.000 claims 2
- 229960001686 afatinib Drugs 0.000 claims 2
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims 2
- 208000014104 capillary malformation-arteriovenous malformation syndrome Diseases 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 2
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- UZWDCWONPYILKI-UHFFFAOYSA-N n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims 2
- 229960002621 pembrolizumab Drugs 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 102200006538 rs121913530 Human genes 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 229960004066 trametinib Drugs 0.000 claims 2
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 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 1
- 108010058566 130-nm albumin-bound paclitaxel Proteins 0.000 claims 1
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims 1
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims 1
- 101150019464 ARAF gene Proteins 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 1
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims 1
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 1
- 101150029707 ERBB2 gene Proteins 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 208000006334 Gingival Fibromatosis Diseases 0.000 claims 1
- 208000030839 Hereditary gingival fibromatosis Diseases 0.000 claims 1
- 102100035108 High affinity nerve growth factor receptor Human genes 0.000 claims 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims 1
- 101000596894 Homo sapiens High affinity nerve growth factor receptor Proteins 0.000 claims 1
- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 claims 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims 1
- 101001130509 Homo sapiens Ras GTPase-activating protein 1 Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 102100037852 Insulin-like growth factor I Human genes 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 229940083338 MDM2 inhibitor Drugs 0.000 claims 1
- 239000012819 MDM2-Inhibitor Substances 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims 1
- 102100031426 Ras GTPase-activating protein 1 Human genes 0.000 claims 1
- 102100022122 Ras-related C3 botulinum toxin substrate 1 Human genes 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229960003852 atezolizumab Drugs 0.000 claims 1
- 229950002916 avelumab Drugs 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 229950003054 binimetinib Drugs 0.000 claims 1
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims 1
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 1
- 229960004117 capecitabine Drugs 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 229960002271 cobimetinib Drugs 0.000 claims 1
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 229960000684 cytarabine Drugs 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229950009791 durvalumab Drugs 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 229960000961 floxuridine Drugs 0.000 claims 1
- ODKNJVUHOIMIIZ-RRKCRQDMSA-N floxuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ODKNJVUHOIMIIZ-RRKCRQDMSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000000062 kidney sarcoma Diseases 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000394 mitotic effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
- IOMMMLWIABWRKL-WUTDNEBXSA-N nazartinib Chemical compound C1N(C(=O)/C=C/CN(C)C)CCCC[C@H]1N1C2=C(Cl)C=CC=C2N=C1NC(=O)C1=CC=NC(C)=C1 IOMMMLWIABWRKL-WUTDNEBXSA-N 0.000 claims 1
- 229960004378 nintedanib Drugs 0.000 claims 1
- XZXHXSATPCNXJR-ZIADKAODSA-N nintedanib Chemical compound O=C1NC2=CC(C(=O)OC)=CC=C2\C1=C(C=1C=CC=CC=1)\NC(C=C1)=CC=C1N(C)C(=O)CN1CCN(C)CC1 XZXHXSATPCNXJR-ZIADKAODSA-N 0.000 claims 1
- 229960003301 nivolumab Drugs 0.000 claims 1
- 229960003278 osimertinib Drugs 0.000 claims 1
- DUYJMQONPNNFPI-UHFFFAOYSA-N osimertinib Chemical compound COC1=CC(N(C)CCN(C)C)=C(NC(=O)C=C)C=C1NC1=NC=CC(C=2C3=CC=CC=C3N(C)C=2)=N1 DUYJMQONPNNFPI-UHFFFAOYSA-N 0.000 claims 1
- 229960004390 palbociclib Drugs 0.000 claims 1
- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 229910052697 platinum Inorganic materials 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 108010062302 rac1 GTP Binding Protein Proteins 0.000 claims 1
- 102000016914 ras Proteins Human genes 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 229950008933 refametinib Drugs 0.000 claims 1
- 229950003687 ribociclib Drugs 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- QQHMKNYGKVVGCZ-UHFFFAOYSA-N tipiracil Chemical compound N1C(=O)NC(=O)C(Cl)=C1CN1C(=N)CCC1 QQHMKNYGKVVGCZ-UHFFFAOYSA-N 0.000 claims 1
- 229960002952 tipiracil Drugs 0.000 claims 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 1
- VSQQQLOSPVPRAZ-RRKCRQDMSA-N trifluridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(C(F)(F)F)=C1 VSQQQLOSPVPRAZ-RRKCRQDMSA-N 0.000 claims 1
- 229960003962 trifluridine Drugs 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16206422 | 2016-12-22 | ||
| EP16206422.4 | 2016-12-22 | ||
| PCT/EP2017/084265 WO2018115380A1 (en) | 2016-12-22 | 2017-12-21 | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020504742A JP2020504742A (ja) | 2020-02-13 |
| JP2020504742A5 true JP2020504742A5 (https=) | 2021-02-04 |
| JP7219218B2 JP7219218B2 (ja) | 2023-02-07 |
Family
ID=57777432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019534303A Active JP7219218B2 (ja) | 2016-12-22 | 2017-12-21 | 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10898487B2 (https=) |
| EP (2) | EP3878850A1 (https=) |
| JP (1) | JP7219218B2 (https=) |
| CN (1) | CN110167928A (https=) |
| WO (1) | WO2018115380A1 (https=) |
Families Citing this family (189)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7039489B2 (ja) | 2016-05-18 | 2022-03-22 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| JP7219218B2 (ja) | 2016-12-22 | 2023-02-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体 |
| WO2018126192A1 (en) * | 2016-12-30 | 2018-07-05 | Children's Medical Center Corporation | Map2k1 (mek1) as a therapeutic target for arteriovenous malformations and associated disorders |
| CA3056970A1 (en) * | 2017-03-21 | 2018-09-27 | Bayer Pharma Aktiengesellschaft | 2-methyl-quinazolines |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| HRP20230377T1 (hr) | 2017-11-15 | 2023-06-23 | Mirati Therapeutics, Inc. | Inhibitori mutacije kras g12c |
| RS64167B1 (sr) | 2017-12-21 | 2023-05-31 | Boehringer Ingelheim Int | Benzilamino supstituisani piridopirimidinoni i derivati kao sos1 inhibitori |
| CN111615514B (zh) | 2018-01-18 | 2022-10-11 | 奥瑞生物药品公司 | 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3097231A1 (en) * | 2018-04-18 | 2019-10-24 | Bayer Pharma Aktiengesellschaft | 2-methyl-aza-quinazolines |
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| WO2020023502A1 (en) | 2018-07-23 | 2020-01-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| SMT202500028T1 (it) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2020180768A1 (en) * | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| CN113727758A (zh) * | 2019-03-01 | 2021-11-30 | 锐新医药公司 | 双环杂环基化合物及其用途 |
| BR112021022099A2 (pt) | 2019-05-31 | 2021-12-28 | Chiesi Farm Spa | Derivados de amino quinazolina como inibidores de p2x3 |
| AU2020296914A1 (en) * | 2019-06-19 | 2021-12-23 | Boehringer Ingelheim International Gmbh | Anticancer combination therapy |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和失調症之化合物 |
| WO2021041671A1 (en) | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| UA128683C2 (uk) | 2019-10-22 | 2024-09-25 | Люпін Лімітед | Фармацевтична комбінація на основі інгібіторів prmt5 |
| 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 |
| AU2020388848A1 (en) | 2019-11-18 | 2022-05-26 | Inxmed (Nanjing) Co., Ltd. | Use of FAK inhibitor in preparation of drug for treating tumors having NRAS mutation |
| CA3154914A1 (en) | 2019-11-29 | 2021-06-03 | Lupin Limited | Substituted tricyclic compounds |
| PH12022551513A1 (en) * | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| KR20220132543A (ko) * | 2019-12-27 | 2022-09-30 | 루핀 리미티드 | 치환된 삼환 화합물 |
| WO2023205701A1 (en) * | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| WO2021203768A1 (zh) * | 2020-04-08 | 2021-10-14 | 江苏恒瑞医药股份有限公司 | 嘧啶并二环类衍生物、其制备方法及其在医药上的应用 |
| EP3903581A1 (en) | 2020-04-28 | 2021-11-03 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors i |
| EP3903582A1 (en) | 2020-04-28 | 2021-11-03 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors ii |
| EP3903583A1 (en) | 2020-04-28 | 2021-11-03 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors iii |
| CA3172204A1 (en) | 2020-04-28 | 2021-11-04 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors ii |
| EP3903584A1 (en) | 2020-04-28 | 2021-11-03 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors iv |
| ES3050733T3 (en) | 2020-04-28 | 2025-12-22 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors (iv) |
| KR20230005260A (ko) | 2020-04-28 | 2023-01-09 | 바스프 에스이 | Qo 억제제 I 에 대한 내성을 부여하는 미토콘드리아 시토크롬 b 단백질 내에 아미노산 치환 F129L 을 함유하는 식물병원성 진균의 퇴치를 위한 스트로빌루린 유형 화합물의 용도 |
| IL297583A (en) | 2020-04-28 | 2022-12-01 | Basf Se | Use of strobilurin type compounds to control phytopathogenic fungi containing amino acid transformation f129l in mitochondrial cytochrome b protein conferring resistance to ii qo inhibitors |
| CA3182745A1 (en) * | 2020-05-09 | 2021-11-18 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Sos1 inhibitor containing phosphorus |
| WO2021245055A1 (en) | 2020-06-02 | 2021-12-09 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2021250521A1 (en) | 2020-06-09 | 2021-12-16 | Array Biopharma Inc. | 4-oxo-3,4-dihydroquinazolinon compounds for the treatment of braf-associated diseases and disorders |
| WO2021249475A1 (zh) * | 2020-06-10 | 2021-12-16 | 江苏恒瑞医药股份有限公司 | 稠合喹唑啉类衍生物、其制备方法及其在医药上的应用 |
| CN113801114B (zh) * | 2020-06-11 | 2022-11-18 | 江苏恒瑞医药股份有限公司 | 稠合二环杂芳基类衍生物、其制备方法及其在医药上的应用 |
| TW202214639A (zh) * | 2020-06-11 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 吡啶酮并嘧啶類衍生物、其製備方法及其在醫藥上的應用 |
| EP4171570A1 (en) * | 2020-06-24 | 2023-05-03 | Boehringer Ingelheim International GmbH | Anticancer combination therapy comprising a sos1 inhibitor and a kras g12c inhibitor |
| CN113912608B (zh) * | 2020-07-10 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用 |
| TW202214608A (zh) * | 2020-07-20 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合噠嗪類衍生物、其製備方法及其在醫藥上的應用 |
| US12552787B2 (en) | 2020-07-24 | 2026-02-17 | Medshine Discovery Inc. | Quinazoline compound |
| CN116194446A (zh) * | 2020-08-06 | 2023-05-30 | 北京泰德制药股份有限公司 | Sos1抑制剂、包含其的药物组合物及其用途 |
| EP4195928B1 (en) | 2020-08-11 | 2025-06-18 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors viii |
| EP3970494A1 (en) | 2020-09-21 | 2022-03-23 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors viii |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| WO2022056307A1 (en) | 2020-09-11 | 2022-03-17 | Mirati Therapeutics, Inc. | Crystalline forms of a kras g12c inhibitor |
| MX2023003060A (es) | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
| WO2022061348A1 (en) * | 2020-09-16 | 2022-03-24 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| EP4214204A1 (en) * | 2020-09-18 | 2023-07-26 | Bayer Aktiengesellschaft | Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors |
| CN114907324A (zh) * | 2021-02-09 | 2022-08-16 | 苏州泽璟生物制药股份有限公司 | 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用 |
| EP4234548A4 (en) * | 2020-10-20 | 2024-10-23 | Suzhou Zelgen Biopharmaceutical Co., Ltd. | SUBSTITUTED BENZO OR PYRIDOPYRIMIDINE AMINE INHIBITOR, ITS PREPARATION METHOD AND ITS APPLICATION |
| CN112174891B (zh) * | 2020-11-02 | 2022-02-01 | 浙江省农业科学院 | 一种氟唑菌苯胺代谢物的制备方法 |
| US20240025935A1 (en) * | 2020-11-18 | 2024-01-25 | Modernatx, Inc. | Ribonucleic acid purification |
| CN114524810B (zh) * | 2020-11-21 | 2023-12-01 | 上海凌达生物医药有限公司 | 一类嘧啶并杂环类化合物、制备方法和用途 |
| CN114539245A (zh) * | 2020-11-26 | 2022-05-27 | 上海翰森生物医药科技有限公司 | 含嘧啶并环类衍生物调节剂、其制备方法和应用 |
| WO2022121813A1 (zh) * | 2020-12-07 | 2022-06-16 | 北京泰德制药股份有限公司 | Sos1抑制剂、包含其的药物组合物及其用途 |
| CN114621231B (zh) * | 2020-12-14 | 2025-09-12 | 杭州中美华东制药有限公司 | 一种靶向降解/抑制活性的嵌合化合物及其制备方法和用途 |
| WO2022132200A1 (en) | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| US20240051956A1 (en) | 2020-12-22 | 2024-02-15 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| WO2022139304A1 (ko) * | 2020-12-22 | 2022-06-30 | 한미약품 주식회사 | Sos1 억제제로서의 신규한 퀴나졸린 유도체 화합물 및 이의 용도 |
| CN114685531B (zh) * | 2020-12-25 | 2024-10-22 | 武汉誉祥医药科技有限公司 | 四并环化合物及其药物组合物和应用 |
| WO2022135590A1 (zh) * | 2020-12-27 | 2022-06-30 | 上海凌达生物医药有限公司 | 一类嘧啶并杂环类化合物、制备方法和用途 |
| WO2022143533A1 (zh) * | 2020-12-30 | 2022-07-07 | 成都百裕制药股份有限公司 | 喹唑啉衍生物及其在医药上的应用 |
| CN114685488A (zh) * | 2020-12-31 | 2022-07-01 | 南京圣和药业股份有限公司 | 作为sos1抑制剂的化合物及其应用 |
| WO2022148442A1 (zh) * | 2021-01-07 | 2022-07-14 | 武汉人福创新药物研发中心有限公司 | 6-取代磷酰基喹唑啉类衍生物及其制备方法和用途 |
| MX2023008460A (es) | 2021-01-19 | 2023-09-12 | Lupin Ltd | Combinaciones farmacéuticas de inhibidores de sos1 para el tratamiento y/o prevención del cáncer. |
| WO2022156792A1 (en) * | 2021-01-25 | 2022-07-28 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Heterocyclic compounds as sos1 inhibitors |
| CN116546985A (zh) * | 2021-01-28 | 2023-08-04 | 浙江海正药业股份有限公司 | 吡啶并嘧啶类衍生物及其制备方法和用途 |
| WO2022161461A1 (zh) * | 2021-01-29 | 2022-08-04 | 江苏先声药业有限公司 | Sos1抑制剂及其制备方法和应用 |
| CN114436976B (zh) * | 2021-01-29 | 2023-07-11 | 石药集团中奇制药技术（石家庄）有限公司 | 一种新型喹唑啉类衍生物及其制备和应用 |
| CN114835719A (zh) * | 2021-02-01 | 2022-08-02 | 苏州泽璟生物制药股份有限公司 | 取代双环并芳杂环胺类抑制剂及其制备方法和应用 |
| CN114835703A (zh) * | 2021-02-02 | 2022-08-02 | 苏州泽璟生物制药股份有限公司 | 取代嘧啶并吡啶酮类抑制剂及其制备方法和应用 |
| CN114853812A (zh) * | 2021-02-04 | 2022-08-05 | 四川科伦博泰生物医药股份有限公司 | 含氧化膦基团的化合物、其制备方法及其在医药上的应用 |
| KR20230144065A (ko) * | 2021-02-08 | 2023-10-13 | 우한 휴먼웰 이노베이티브 드러그 리서치 앤드 디벨롭먼트 센터 리미티드 컴퍼니 | 피리도피리미디논계 유도체 및 이의 제조 방법과 용도 |
| CN116669738B (zh) * | 2021-02-09 | 2026-04-03 | 苏州阿尔脉生物科技有限公司 | 一种作为sos1抑制剂的嘧啶并吡啶酮类衍生物、其制备方法及用途 |
| WO2022170917A1 (zh) * | 2021-02-09 | 2022-08-18 | 苏州阿尔脉生物科技有限公司 | 一种作为sos1抑制剂的多环嘧啶类衍生物、其制备方法及用途 |
| WO2022171018A1 (zh) * | 2021-02-09 | 2022-08-18 | 苏州泽璟生物制药股份有限公司 | 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用 |
| CN114907284B (zh) * | 2021-02-10 | 2023-11-03 | 石药集团中奇制药技术（石家庄）有限公司 | 一种具有抗肿瘤活性的化合物及其用途 |
| CN113200981A (zh) * | 2021-02-10 | 2021-08-03 | 杭州英创医药科技有限公司 | 作为sos1抑制剂的杂环化合物 |
| US11648254B2 (en) | 2021-03-02 | 2023-05-16 | Kumquat Biosciences Inc. | Substituted pyrido[2,3-d]pyrimidines as inhibitors of Ras pathway signaling |
| US20240109887A1 (en) * | 2021-03-02 | 2024-04-04 | Viva Star Biosciences (Suzhou) Co., Ltd. | Novel substituted bicyclic aza-heterocycles as sos1 inhibitors |
| WO2022184116A1 (zh) * | 2021-03-05 | 2022-09-09 | 江苏先声药业有限公司 | 新型sos1抑制剂及其制备方法和应用 |
| CN115028644A (zh) * | 2021-03-08 | 2022-09-09 | 首药控股(北京)股份有限公司 | Sos1抑制剂杂环化合物 |
| CN115043817A (zh) * | 2021-03-09 | 2022-09-13 | 苏州泽璟生物制药股份有限公司 | Sos1蛋白水解调节剂及其制备方法和应用 |
| WO2022197862A1 (en) * | 2021-03-17 | 2022-09-22 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022199635A1 (zh) * | 2021-03-25 | 2022-09-29 | 南京明德新药研发有限公司 | 苄氨基喹唑啉类衍生物 |
| US20240208945A1 (en) * | 2021-03-26 | 2024-06-27 | Medshine Discovery Inc. | 6-carbamate substituted heteroaryl ring derivatives |
| GB202104609D0 (en) | 2021-03-31 | 2021-05-12 | Sevenless Therapeutics Ltd | New Treatments for Pain |
| US20220324862A1 (en) * | 2021-03-31 | 2022-10-13 | Acerand Therapeutics (Usa) Limited | Pyridopyrimidinone compounds |
| EP4313151A1 (en) | 2021-03-31 | 2024-02-07 | Sevenless Therapeutics Limited | Sos1 inhibitors and ras inhibitors for use in the treatment of pain |
| TW202304452A (zh) * | 2021-04-09 | 2023-02-01 | 美商銳新醫藥公司 | Ｓｏｓ１抑制劑與ｒａｓ抑制劑於治療癌症之用途 |
| WO2022214594A1 (en) | 2021-04-09 | 2022-10-13 | Boehringer Ingelheim International Gmbh | Anticancer therapy |
| EP4323356A1 (en) | 2021-04-13 | 2024-02-21 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| CN115215847B (zh) * | 2021-04-16 | 2025-05-13 | 中国科学院上海药物研究所 | 一类kras-sos1抑制剂、其制备方法及其应用 |
| CN115215884A (zh) * | 2021-04-19 | 2022-10-21 | 昆药集团股份有限公司 | 苯并嘧啶三环类衍生物及其制备方法和应用 |
| TWI807787B (zh) * | 2021-04-19 | 2023-07-01 | 大陸商昆藥集團股份有限公司 | 苯並嘧啶三環衍生物及製備方法和應用 |
| CN115232114B (zh) * | 2021-04-23 | 2023-12-19 | 上海领泰生物医药科技有限公司 | Sos1降解剂及其制备方法和应用 |
| EP4346826A4 (en) * | 2021-05-27 | 2025-04-30 | Mirati Therapeutics, Inc. | COMBINATION THERAPIES |
| WO2022258057A1 (en) * | 2021-06-11 | 2022-12-15 | Jingrui Biopharma Co., Ltd. | Compounds as anticancer agents |
| AU2022292649A1 (en) * | 2021-06-16 | 2024-01-04 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022262691A1 (en) * | 2021-06-17 | 2022-12-22 | Beijing Innocare Pharma Tech Co., Ltd. | Heterocyclic compounds as sos1 inhibitors |
| US20250059182A1 (en) | 2021-06-21 | 2025-02-20 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| WO2022268209A1 (zh) * | 2021-06-24 | 2022-12-29 | 四川汇宇制药股份有限公司 | 一种嘧啶并环结构衍生物及其用途 |
| CN115677699B (zh) * | 2021-07-23 | 2024-11-22 | 武汉誉祥医药科技有限公司 | 三并环化合物及其药物组合物和应用 |
| CN117769556A (zh) * | 2021-07-23 | 2024-03-26 | 浙江海正药业股份有限公司 | 嘧啶并环类衍生物及其制备方法和用途 |
| CN115677824B (zh) * | 2021-07-26 | 2026-02-03 | 中国科学院上海药物研究所 | 可诱导sos1蛋白质降解的化合物、制备方法和用途 |
| CN115677601B (zh) * | 2021-07-29 | 2025-06-03 | 石药集团中奇制药技术（石家庄）有限公司 | 一种具有抗肿瘤活性的化合物及其用途 |
| EP4375284A1 (en) * | 2021-08-03 | 2024-05-29 | Evopoint Biosciences Co., Ltd. | Fused ring compound, pharmaceutical composition, and application thereof |
| US20240382475A1 (en) * | 2021-08-30 | 2024-11-21 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Quinazoline Derivative, Or Preparation Method Therefor And Use Thereof |
| CN115417868B (zh) * | 2021-09-13 | 2024-04-02 | 石药集团中奇制药技术（石家庄）有限公司 | 一种具有抗肿瘤活性的杂环化合物及其用途 |
| CN115246841B (zh) * | 2021-09-14 | 2024-02-09 | 北京福元医药股份有限公司 | 苄氨基取代的嘧啶并吡喃酮衍生物及其组合物、制剂和用途 |
| WO2023041049A1 (zh) | 2021-09-17 | 2023-03-23 | 江苏先声药业有限公司 | 作为sos1抑制剂的杂环化合物及其用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| US20240425501A1 (en) * | 2021-10-21 | 2024-12-26 | Sanjita Sasmal | Novel bicyclic heteroaryl derivatives as sos1:kras proteinprotein interaction inhibitors |
| WO2023072670A1 (en) | 2021-10-28 | 2023-05-04 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors x |
| WO2023072671A1 (en) | 2021-10-28 | 2023-05-04 | Basf Se | Use of strobilurin type compounds for combating phytopathogenic fungi containing an amino acid substitution f129l in the mitochondrial cytochrome b protein conferring resistance to qo inhibitors ix |
| CN120923498A (zh) * | 2021-11-04 | 2025-11-11 | 北京福元医药股份有限公司 | 苄氨基取代的杂多环化合物及其组合物、制剂和用途 |
| CN116143708A (zh) * | 2021-11-21 | 2023-05-23 | 四川汇宇制药股份有限公司 | 一种多取代苯并氮杂芳基衍生物及其用途 |
| US20250145608A1 (en) | 2021-12-01 | 2025-05-08 | Boehringer Ingelheim Int'l GmbH Corp. | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| WO2023099624A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US20250313553A1 (en) | 2021-12-01 | 2025-10-09 | Boehringer Ingelheim Int'l GmbH Corp. | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| JP2024543982A (ja) | 2021-12-01 | 2024-11-26 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | がんの処置のための縮環２－アミノ－３－シアノチオフェン及び誘導体 |
| US20250129096A1 (en) | 2021-12-01 | 2025-04-24 | Boehringer Ingelheim Int'l GmbH Corp. | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023098825A1 (zh) * | 2021-12-02 | 2023-06-08 | 勤浩医药（苏州）有限公司 | Sos1抑制剂、包含其的药物组合物及其用途 |
| EP4444710A1 (en) | 2021-12-08 | 2024-10-16 | Array BioPharma Inc. | Crystalline form of n-(2-chloro-3-((5-chloro-3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)-4-fluorophenyl)-3-fluoroazetidine-1-sulfonamide |
| TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
| CA3240780A1 (en) | 2021-12-17 | 2023-06-22 | Zhenyu Wang | Heterocyclic compound having anti-tumor activity and use thereof |
| EP4463454A1 (en) | 2022-01-14 | 2024-11-20 | Jazz Pharmaceuticals Ireland Limited | Novel amine-substituted phthalazines and derivatives as sos1 inhibitors |
| CN118696042A (zh) * | 2022-01-21 | 2024-09-24 | 南京明德新药研发有限公司 | 含烯丙基的甲基吡啶并嘧啶化合物的晶型 |
| CN118574830A (zh) * | 2022-01-28 | 2024-08-30 | 中山优理生物医药有限公司 | 一种哒嗪并吡啶酮类化合物、其药物组合物及应用 |
| KR20230121208A (ko) | 2022-02-10 | 2023-08-18 | (주)파로스아이바이오 | Sos1 억제제 및 이의 유도체 |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| CN116768858B (zh) * | 2022-03-15 | 2025-09-12 | 杭州中美华东制药有限公司 | 具有kras-sos1抑制或降解活性的嵌合化合物及其用途 |
| US12419962B2 (en) | 2022-03-16 | 2025-09-23 | Biotheryx, Inc. | Quinazolines, pharmaceutical compositions, and therapeutic applications |
| GB202203976D0 (en) | 2022-03-22 | 2022-05-04 | Jazz Pharmaceuticals Ireland Ltd | Tricyclic phthalazines and derivatives as sos1 inhibitors |
| US20250177406A1 (en) | 2022-03-31 | 2025-06-05 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumors |
| CN118973580A (zh) * | 2022-04-08 | 2024-11-15 | 米拉蒂治疗股份有限公司 | 包含sos1抑制剂和mek抑制剂的组合疗法 |
| US20250177410A1 (en) * | 2022-04-08 | 2025-06-05 | Mirati Therapeutics, Inc. | Combination therapies comprising a sos1 inhibitor and an egfr inhibitor |
| KR20250004810A (ko) | 2022-04-20 | 2025-01-08 | 컴쿼트 바이오사이언시즈 인크. | 대환식 헤테로환 및 이의 용도 |
| CN117024404A (zh) * | 2022-05-10 | 2023-11-10 | 四川汇宇制药股份有限公司 | 苯并吡啶衍生物及其用途 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN117263950A (zh) * | 2022-06-13 | 2023-12-22 | 上海优理惠生医药有限公司 | 一种哒嗪类化合物、其药物组合物及应用 |
| TW202404605A (zh) * | 2022-07-07 | 2024-02-01 | 大陸商武漢人福創新藥物研發中心有限公司 | 包含ｓｏｓ１抑制劑的藥物組成物 |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| EP4587439A1 (en) | 2022-09-16 | 2025-07-23 | Bayer Aktiengesellschaft | Sulfone-substituted pyrido[3,4-d]pyrimidine derivatives for the treatment of cancer |
| WO2024061353A1 (zh) * | 2022-09-23 | 2024-03-28 | 南京明德新药研发有限公司 | 喹唑啉类化合物的晶型及其制备方法 |
| WO2024074827A1 (en) | 2022-10-05 | 2024-04-11 | Sevenless Therapeutics Limited | New treatments for pain |
| WO2024075070A2 (ko) * | 2022-10-07 | 2024-04-11 | 제일약품주식회사 | 신규한 바이사이클릭 헤테로사이클릴 화합물 및 이의 용도 |
| EP4602049A1 (en) | 2022-10-13 | 2025-08-20 | Bayer Aktiengesellschaft | Sos1 inhibitors |
| CN119907792B (zh) * | 2022-10-21 | 2025-12-09 | 领泰生物医药(绍兴)有限公司 | 苄基或噻吩亚甲基取代的氨基喹唑啉衍生物及其作为sos1降解剂的用途 |
| WO2024119028A1 (en) * | 2022-12-02 | 2024-06-06 | Accutar Biotechnology, Inc. | Substituted quinoline derivatives having sos1 inhibition activities and uses thereof |
| DE102024102431A1 (de) | 2023-02-01 | 2024-08-01 | Deutsche Institute für Textil- und Faserforschung Denkendorf Stiftung des öffentlichen Rechts | Amin-funktionalisiertes Cellulosematerial, Verfahren zu dessen Herstellung und Verwendung als CO2-Adsorber |
| JPWO2024209717A1 (https=) | 2023-04-06 | 2024-10-10 | ||
| 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 |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| EP4719603A1 (en) | 2023-05-30 | 2026-04-08 | Boehringer Ingelheim International GmbH | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| KR20260016493A (ko) | 2023-05-31 | 2026-02-03 | 쓰추안 휘위 파머슈티컬 컴퍼니., 리미티드. | 질소 함유 관능기 치환 피리다지노피리돈 유도체 및 이의 용도 |
| CN116444447B (zh) * | 2023-06-19 | 2023-09-22 | 中国药科大学 | 一种sos1和hdac双靶点喹唑啉羟肟酸化合物及其制法和应用 |
| GB2631397A (en) | 2023-06-28 | 2025-01-08 | Sevenless Therapeutics Ltd | New treatments for pain |
| AU2024307234A1 (en) | 2023-06-30 | 2026-01-29 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| CN121889152A (zh) | 2023-09-11 | 2026-04-17 | 金橘生物科技公司 | 用于治疗费城染色体阳性血癌的sos1抑制剂 |
| GB2633813A (en) | 2023-09-21 | 2025-03-26 | Sevenless Therapeutics Ltd | New treatments for pain |
| 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 |
| WO2025083426A1 (en) | 2023-10-20 | 2025-04-24 | Sevenless Therapeutics Limited | New treatments for pain |
| WO2025090810A1 (en) | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Use of sos1 inhibitors and amivantamab to treat cancer |
| WO2025090808A1 (en) | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Combinations of sos-1 inhibitors with osimertinib and/or met inhibitors to treat cancer |
| WO2025090812A1 (en) * | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Methods of modulating cell proliferation |
| TW202542151A (zh) | 2023-12-22 | 2025-11-01 | 美商銳格醫藥有限公司 | Ｓｏｓ１抑制劑及其用途 |
| WO2025146548A1 (en) | 2024-01-04 | 2025-07-10 | Sevenless Therapeutics Limited | Sos1 inhibitors useful to treat pain and cancer |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025202022A1 (en) | 2024-03-27 | 2025-10-02 | Bayer Aktiengesellschaft | Anticancer macrocyclic quinazoline-based inhibitors of the ineraction between ras and sos1 |
| WO2025210042A1 (en) | 2024-04-03 | 2025-10-09 | Boehringer Ingelheim International Gmbh | Combination of zongertinib with a sos1 inhibitor for use in the treatment of cancer |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5679683A (en) | 1994-01-25 | 1997-10-21 | Warner-Lambert Company | Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| US6174899B1 (en) | 1998-05-14 | 2001-01-16 | Morton Shulman | Orally administered analgesic composition comprising myfadol |
| US7291725B2 (en) * | 2002-06-26 | 2007-11-06 | Chiron Corporation | Sos1 inhibitors |
| EP2139895A1 (en) | 2007-03-23 | 2010-01-06 | F. Hoffmann-Roche AG | Aza-pyridopyrimidinone derivatives |
| TWI377944B (en) | 2007-06-05 | 2012-12-01 | Hanmi Holdings Co Ltd | Novel amide derivative for inhibiting the growth of cancer cells |
| US8383635B2 (en) | 2008-08-12 | 2013-02-26 | Glaxosmithkline Llc | Chemical compounds |
| BRPI0924107A2 (pt) | 2008-11-28 | 2019-09-24 | Novartis Ag | inibidores de hsp90 para tratamento terapêutico |
| NZ592151A (en) | 2008-12-12 | 2012-10-26 | Boehringer Ingelheim Int | Anti-igf antibodies |
| SG10201407012XA (en) | 2009-10-29 | 2014-11-27 | Genosco | Kinase inhibitors |
| KR102027596B1 (ko) | 2010-12-06 | 2019-10-01 | 타폰 바이오시스템즈, 인코포레이티드 | 생물학적 산물을 위한 연속 처리 방법 |
| US8846656B2 (en) | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| KR20140138910A (ko) | 2012-03-14 | 2014-12-04 | 루핀 리미티드 | 헤테로사이클릴 화합물 |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| JP6473133B2 (ja) | 2013-03-15 | 2019-02-20 | アラクセス ファーマ エルエルシー | Ｋｒａｓｇ１２ｃの共有結合性阻害剤 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016077793A1 (en) * | 2014-11-14 | 2016-05-19 | Children's Hospital Medical Center | Sos1 inhibitors for cancer treatment |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| JP7219218B2 (ja) | 2016-12-22 | 2023-02-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体 |
| CA3056970A1 (en) | 2017-03-21 | 2018-09-27 | Bayer Pharma Aktiengesellschaft | 2-methyl-quinazolines |
| AU2020296914A1 (en) | 2019-06-19 | 2021-12-23 | Boehringer Ingelheim International Gmbh | Anticancer combination therapy |
-
2017
- 2017-12-21 JP JP2019534303A patent/JP7219218B2/ja active Active
- 2017-12-21 EP EP20216236.8A patent/EP3878850A1/en not_active Withdrawn
- 2017-12-21 WO PCT/EP2017/084265 patent/WO2018115380A1/en not_active Ceased
- 2017-12-21 US US16/472,433 patent/US10898487B2/en active Active
- 2017-12-21 CN CN201780083358.7A patent/CN110167928A/zh active Pending
- 2017-12-21 EP EP17828914.6A patent/EP3558979B1/en active Active
-
2020
- 2020-10-22 US US17/077,232 patent/US12053473B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020504742A5 (https=) | ||
| RU2492864C2 (ru) | Способ лечения рака, несущего мутации egfr | |
| KR20210087440A (ko) | 삼중 음성 유방암의 치료를 위한 병용 요법 | |
| JP2019532051A5 (https=) | ||
| JP5852678B2 (ja) | 抗腫瘍剤の効果増強剤 | |
| Pietanza et al. | Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non–small-cell lung cancer | |
| ES2736030T3 (es) | Politerapia para el tratamiento del cáncer de ovario | |
| Aprile et al. | Regorafenib for gastrointestinal malignancies: from preclinical data to clinical results of a novel multi-target inhibitor | |
| Roy et al. | A novel multiple tyrosine-kinase targeted agent to explore the future perspectives of anti-angiogenic therapy for the treatment of multiple solid tumors: cabozantinib | |
| JP2011522773A5 (https=) | ||
| JP2025024064A (ja) | 癌治療 | |
| JP2017528487A5 (https=) | ||
| JP2012515184A (ja) | 大腸がんの治療方法 | |
| JP2020532556A5 (https=) | ||
| ES2682270T3 (es) | Combinación farmacéutica sinérgica para el tratamiento del carcinoma de células escamosas de cabeza y cuello | |
| CN114728000A (zh) | 治疗癌症的新型药物组合 | |
| Chu et al. | A phase I, dose-escalation trial of continuous-and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors | |
| JP7303205B2 (ja) | 胆道癌を処置するための方法および併用療法 | |
| CN120282786A (zh) | 治疗晚期实体肿瘤的方法 | |
| TW202317126A (zh) | Ｅｇｆｒ抑制劑和ｐｅｒｋ活化劑組合療法 | |
| Shaib et al. | Derazantinib. Fibroblast growth factor receptor (FGFR) inhibitor, Treatment of intrahepatic cholangiocarcinoma | |
| Jin et al. | Systemic Therapy | |
| Sackett et al. | 20 Inhibitors Targeting | |
| Bonetti et al. | Oxaliplatin-based chemotherapy for colon cancer | |
| Takahashi et al. | Phase 1 study on S-1 and oxaliplatin therapy as an adjuvant after hepatectomy for colorectal liver metastases |