JP2016529312A5 - - Google Patents
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- JP2016529312A5 JP2016529312A5 JP2016540387A JP2016540387A JP2016529312A5 JP 2016529312 A5 JP2016529312 A5 JP 2016529312A5 JP 2016540387 A JP2016540387 A JP 2016540387A JP 2016540387 A JP2016540387 A JP 2016540387A JP 2016529312 A5 JP2016529312 A5 JP 2016529312A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- carbocyclyl
- heterocyclyl
- alkynyl
- alkenyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims description 134
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 128
- 125000000623 heterocyclic group Chemical group 0.000 claims description 93
- 125000005843 halogen group Chemical group 0.000 claims description 66
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 61
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 60
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 57
- 229910052739 hydrogen Inorganic materials 0.000 claims description 51
- 150000001875 compounds Chemical class 0.000 claims description 35
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 34
- 229940127089 cytotoxic agent Drugs 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 29
- 125000000304 alkynyl group Chemical group 0.000 claims description 27
- 125000004043 oxo group Chemical group O=* 0.000 claims description 27
- 125000003342 alkenyl group Chemical group 0.000 claims description 26
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 23
- -1 amino, hydroxyl Chemical group 0.000 claims description 20
- 239000002254 cytotoxic agent Substances 0.000 claims description 20
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 20
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 19
- 125000002252 acyl group Chemical group 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 17
- 206010028980 Neoplasm Diseases 0.000 claims description 16
- 125000004429 atom Chemical group 0.000 claims description 16
- 201000011510 cancer Diseases 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000002883 imidazolyl group Chemical group 0.000 claims description 13
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 13
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims description 13
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 13
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 11
- 125000004423 acyloxy group Chemical group 0.000 claims description 11
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 9
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
- 239000001257 hydrogen Substances 0.000 claims description 7
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 claims description 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 3
- 230000000069 prophylactic effect Effects 0.000 claims description 3
- 230000001225 therapeutic effect Effects 0.000 claims description 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 230000005855 radiation Effects 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 238000000034 method Methods 0.000 description 30
- 239000003112 inhibitor Substances 0.000 description 18
- 239000002246 antineoplastic agent Substances 0.000 description 14
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 description 8
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 6
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical group [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 description 6
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 description 4
- 0 CCC(*(C)C)=C*=C(*)[*@]1*=CC(C(C=**2C(C(CC)=C3C)=O)=C2*3=C)=C1 Chemical compound CCC(*(C)C)=C*=C(*)[*@]1*=CC(C(C=**2C(C(CC)=C3C)=O)=C2*3=C)=C1 0.000 description 4
- 229940123237 Taxane Drugs 0.000 description 4
- 208000035475 disorder Diseases 0.000 description 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical group C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- 229910052697 platinum Inorganic materials 0.000 description 4
- 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 description 4
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 description 3
- 206010006187 Breast cancer Diseases 0.000 description 3
- 208000026310 Breast neoplasm Diseases 0.000 description 3
- 206010009944 Colon cancer Diseases 0.000 description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 3
- 229940122558 EGFR antagonist Drugs 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 201000005202 lung cancer Diseases 0.000 description 3
- 208000020816 lung neoplasm Diseases 0.000 description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 3
- 201000001441 melanoma Diseases 0.000 description 3
- 201000002528 pancreatic cancer Diseases 0.000 description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 2
- 229940125431 BRAF inhibitor Drugs 0.000 description 2
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 description 2
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 description 2
- 102100034671 L-lactate dehydrogenase A chain Human genes 0.000 description 2
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 2
- 108010088350 Lactate Dehydrogenase 5 Proteins 0.000 description 2
- 101100523539 Mus musculus Raf1 gene Proteins 0.000 description 2
- 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 description 2
- 239000012828 PI3K inhibitor Substances 0.000 description 2
- 229930012538 Paclitaxel Natural products 0.000 description 2
- 229940079156 Proteasome inhibitor Drugs 0.000 description 2
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 description 2
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 description 2
- 239000002168 alkylating agent Substances 0.000 description 2
- 229940100198 alkylating agent Drugs 0.000 description 2
- 239000004037 angiogenesis inhibitor Substances 0.000 description 2
- 229940121369 angiogenesis inhibitor Drugs 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 230000000340 anti-metabolite Effects 0.000 description 2
- 229940044684 anti-microtubule agent Drugs 0.000 description 2
- 229940100197 antimetabolite Drugs 0.000 description 2
- 239000002256 antimetabolite Substances 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000022131 cell cycle Effects 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 229960003668 docetaxel Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229960001433 erlotinib Drugs 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000003668 hormone analog Substances 0.000 description 2
- 150000002431 hydrogen Chemical class 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 229960001592 paclitaxel Drugs 0.000 description 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 description 2
- 239000003207 proteasome inhibitor Substances 0.000 description 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 2
- 230000035945 sensitivity Effects 0.000 description 2
- 230000019491 signal transduction Effects 0.000 description 2
- 230000011664 signaling Effects 0.000 description 2
- 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 description 2
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical group 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 description 2
- 229960003862 vemurafenib Drugs 0.000 description 2
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 description 1
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 0.000 description 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 description 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 description 1
- CSLJXILIWIMLTL-UHFFFAOYSA-N CC(C)c1c[n](-c(nc2)ncc2N(C)C)nc1 Chemical compound CC(C)c1c[n](-c(nc2)ncc2N(C)C)nc1 CSLJXILIWIMLTL-UHFFFAOYSA-N 0.000 description 1
- ZAZCIHKBUVQXKV-UHFFFAOYSA-N CC(Nc([n](C1=O)nc2)c2-c2c[n](-c3ccccn3)nc2)=C1Cl Chemical compound CC(Nc([n](C1=O)nc2)c2-c2c[n](-c3ccccn3)nc2)=C1Cl ZAZCIHKBUVQXKV-UHFFFAOYSA-N 0.000 description 1
- XCJHHYWFOXAYBC-UHFFFAOYSA-N CC(c1c[n](-c2ccncn2)nc1)=C Chemical compound CC(c1c[n](-c2ccncn2)nc1)=C XCJHHYWFOXAYBC-UHFFFAOYSA-N 0.000 description 1
- VVAMRKQTTRRZBC-LSDHQDQOSA-N CC/C(/[n]1cnc(-c2ccccn2)c1)=C(/NC(c1ccccc1)=C(CC)C1=O)\N1N Chemical compound CC/C(/[n]1cnc(-c2ccccn2)c1)=C(/NC(c1ccccc1)=C(CC)C1=O)\N1N VVAMRKQTTRRZBC-LSDHQDQOSA-N 0.000 description 1
- LPLZTGZNKNRTLL-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-[n]1cnc(-c2ccccn2)c1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-[n]1cnc(-c2ccccn2)c1 LPLZTGZNKNRTLL-UHFFFAOYSA-N 0.000 description 1
- UTTNHAMRKOCBMO-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-[n]1cnc(-c2cccnc2)c1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-[n]1cnc(-c2cccnc2)c1 UTTNHAMRKOCBMO-UHFFFAOYSA-N 0.000 description 1
- WWYNJDQPWNRJLC-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2cc(N(C)C)ccn2)nc1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2cc(N(C)C)ccn2)nc1 WWYNJDQPWNRJLC-UHFFFAOYSA-N 0.000 description 1
- PQCIOURXCUVAEZ-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2nccc(Cl)c2)nc1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2nccc(Cl)c2)nc1 PQCIOURXCUVAEZ-UHFFFAOYSA-N 0.000 description 1
- RTWAURZQZXFUNZ-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2nccc(OC)c2)nc1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2nccc(OC)c2)nc1 RTWAURZQZXFUNZ-UHFFFAOYSA-N 0.000 description 1
- RMLRQNYPXZAZLZ-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2ncccn2)nc1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1c[n](-c2ncccn2)nc1 RMLRQNYPXZAZLZ-UHFFFAOYSA-N 0.000 description 1
- ANRQHYNHPUYMMB-UHFFFAOYSA-N CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1cnc(-c2ccccn2)[nH]1 Chemical compound CCC(C([n]1nc2)=O)=C(C)Nc1c2-c1cnc(-c2ccccn2)[nH]1 ANRQHYNHPUYMMB-UHFFFAOYSA-N 0.000 description 1
- JPEUQZVNSKXPHA-UHFFFAOYSA-N CNc1c[n](-c2nc(N(C)C)ccn2)nc1 Chemical compound CNc1c[n](-c2nc(N(C)C)ccn2)nc1 JPEUQZVNSKXPHA-UHFFFAOYSA-N 0.000 description 1
- ZTDDWLMWLULANI-UHFFFAOYSA-N Cc1ccnc(-[n]2ncc(N)c2)n1 Chemical compound Cc1ccnc(-[n]2ncc(N)c2)n1 ZTDDWLMWLULANI-UHFFFAOYSA-N 0.000 description 1
- XHRMXJNKNQKYRQ-UHFFFAOYSA-N O=C1[n]2ncc(-c3c[n](-c4ccccn4)nc3)c2NC2=C1CCC2 Chemical compound O=C1[n]2ncc(-c3c[n](-c4ccccn4)nc3)c2NC2=C1CCC2 XHRMXJNKNQKYRQ-UHFFFAOYSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000012830 cancer therapeutic Substances 0.000 description 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 description 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 description 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000002955 immunomodulating agent Substances 0.000 description 1
- 238000009169 immunotherapy Methods 0.000 description 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 description 1
- 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 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 1
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000011272 standard treatment Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361874310P | 2013-09-05 | 2013-09-05 | |
| US61/874,310 | 2013-09-05 | ||
| PCT/US2014/054114 WO2015035062A1 (en) | 2013-09-05 | 2014-09-04 | Antiproliferative compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016529312A JP2016529312A (ja) | 2016-09-23 |
| JP2016529312A5 true JP2016529312A5 (enExample) | 2017-09-07 |
| JP6336598B2 JP6336598B2 (ja) | 2018-06-06 |
Family
ID=51541384
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540387A Active JP6336598B2 (ja) | 2013-09-05 | 2014-09-04 | 抗増殖性化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9505767B2 (enExample) |
| EP (1) | EP3041474B1 (enExample) |
| JP (1) | JP6336598B2 (enExample) |
| KR (1) | KR20160049003A (enExample) |
| CN (1) | CN105611933B (enExample) |
| CA (1) | CA2922925A1 (enExample) |
| MX (1) | MX2016002794A (enExample) |
| RU (1) | RU2016112568A (enExample) |
| WO (1) | WO2015035062A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150203453A1 (en) | 2012-10-02 | 2015-07-23 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| JP6514117B2 (ja) | 2013-02-27 | 2019-05-15 | エピセラピューティクス アーペーエス | ヒストン脱メチル化酵素の阻害剤 |
| CN105980386B (zh) | 2013-03-13 | 2021-08-13 | 基因泰克公司 | 吡唑并化合物及其用途 |
| CA2957947A1 (en) | 2014-08-27 | 2016-03-03 | Gilead Sciences, Inc. | Compounds and methods for inhibiting histone demethylases |
| CN107001358A (zh) | 2014-10-29 | 2017-08-01 | 东亚St株式会社 | 调节组蛋白赖氨酸脱甲基酶(kdm)催化活性的新型吡啶并嘧啶酮化合物 |
| WO2016186949A1 (en) * | 2015-05-15 | 2016-11-24 | Whetstine Johnathan R | Methods relating to the prevention and treatment of drug resistance |
| IL265115B (en) | 2016-08-31 | 2022-07-01 | Agios Pharmaceuticals Inc | Inhibitors of metabolic processes in the cell |
| EP3525785B1 (en) * | 2016-10-12 | 2025-08-27 | Merck Sharp & Dohme LLC | Kdm5 inhibitors |
| US20200048259A1 (en) * | 2016-10-12 | 2020-02-13 | Merck Sharp & Dohme Corp. | Kdm5 inhibitors |
| WO2018160356A1 (en) | 2017-02-28 | 2018-09-07 | University Of Massachusetts | Genetic and pharmacological transcriptional upregulation of the repressed fxn gene as a therapeutic strategy for friedreich ataxia |
| CN108947985A (zh) * | 2017-05-22 | 2018-12-07 | 苏州偶领生物医药有限公司 | 用作自噬调节剂的化合物及其制备方法和用途 |
| KR20200134203A (ko) | 2017-08-21 | 2020-12-01 | 나비젠, 인코포레이티드 | Ａｒｆ6 억제제 및 관련 방법 |
| JP2020533376A (ja) | 2017-09-15 | 2020-11-19 | アドゥロ バイオテック，インク． | ピラゾロピリミジノン化合物およびその使用 |
| AU2020307544A1 (en) * | 2019-06-24 | 2021-11-18 | Dana-Farber Cancer Institute, Inc. | E3 ligase binders and uses thereof |
| WO2021010492A1 (en) * | 2019-07-17 | 2021-01-21 | Ono Pharmaceutical Co., Ltd. | Compound having kdm5 inhibitory activity and pharmaceutical use thereof |
| JOP20220125A1 (ar) | 2019-11-25 | 2023-01-30 | Amgen Inc | مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها |
| CN116425757B (zh) * | 2022-01-13 | 2025-05-20 | 浙江同源康医药股份有限公司 | 多环类化合物及其用途 |
| EP4615431A1 (en) | 2022-11-11 | 2025-09-17 | Astrazeneca AB | Combination therapies for the treatment of cancer |
| WO2025194015A1 (en) * | 2024-03-15 | 2025-09-18 | Dem Biopharma, Inc. | Heteroaryl modulators of gpr84 and uses thereof |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| US4943533A (en) | 1984-03-01 | 1990-07-24 | The Regents Of The University Of California | Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor |
| DE69025946T2 (de) | 1989-09-08 | 1996-10-17 | Univ Duke | Modifikationen der struktur des egf-rezeptor-gens in menschlichen glioma |
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| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
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| ATE207366T1 (de) | 1993-12-24 | 2001-11-15 | Merck Patent Gmbh | Immunokonjugate |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| US5654307A (en) | 1994-01-25 | 1997-08-05 | Warner-Lambert Company | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| ATE176910T1 (de) | 1994-07-21 | 1999-03-15 | Akzo Nobel Nv | Zyklische keton peroxyde zubereitungen |
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| ATE212993T1 (de) | 1995-07-06 | 2002-02-15 | Novartis Erfind Verwalt Gmbh | Pyrolopyrimidine und verfahren zu ihrer herstellung |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
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| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
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| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6235883B1 (en) | 1997-05-05 | 2001-05-22 | Abgenix, Inc. | Human monoclonal antibodies to epidermal growth factor receptor |
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| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| CN1278176A (zh) | 1997-11-06 | 2000-12-27 | 美国氰胺公司 | 喹唑啉衍生物作为用于治疗结肠息肉的酪氨酸激酶抑制剂的应用 |
| EA003786B1 (ru) | 1998-11-19 | 2003-10-30 | Варнер Ламберт Компани | N-[4-(3-хлор-4-фторфениламино)-7-(3-морфолин-4-илпропокси)хиназолин-6-ил]акриламид - необратимый ингибитор тирозинкиназ |
| TWI271406B (en) | 1999-12-13 | 2007-01-21 | Eisai Co Ltd | Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same |
| JP4100865B2 (ja) * | 1999-12-13 | 2008-06-11 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 三環式縮合異項環化合物、その製造法およびその医薬 |
| EP1511751B1 (en) | 2002-06-04 | 2008-03-19 | Neogenesis Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine compounds as antiviral agents |
| US7605155B2 (en) * | 2002-09-04 | 2009-10-20 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| WO2007149907A2 (en) * | 2006-06-20 | 2007-12-27 | Abbott Laboratories | Pyrazoloquinazolinones as parp inhibitors |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| CN101906105B (zh) | 2009-06-08 | 2013-01-16 | 河北医科大学 | 吡唑并[1，5-a]嘧啶酮衍生物及其药物组合物以及其用途 |
| US10953012B2 (en) * | 2011-04-26 | 2021-03-23 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of pask |
| WO2014066795A1 (en) * | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| EP2961741B1 (en) * | 2013-03-01 | 2017-04-05 | Fundacion para la Investigacion Medica Aplicada | Novel compounds as dual inhibitors of phosphodiesterases and histone deacetylases |
| CN105980386B (zh) | 2013-03-13 | 2021-08-13 | 基因泰克公司 | 吡唑并化合物及其用途 |
-
2014
- 2014-09-04 US US14/477,566 patent/US9505767B2/en active Active
- 2014-09-04 CA CA2922925A patent/CA2922925A1/en not_active Abandoned
- 2014-09-04 EP EP14766355.3A patent/EP3041474B1/en active Active
- 2014-09-04 JP JP2016540387A patent/JP6336598B2/ja active Active
- 2014-09-04 WO PCT/US2014/054114 patent/WO2015035062A1/en not_active Ceased
- 2014-09-04 MX MX2016002794A patent/MX2016002794A/es unknown
- 2014-09-04 CN CN201480055129.0A patent/CN105611933B/zh active Active
- 2014-09-04 KR KR1020167008823A patent/KR20160049003A/ko not_active Withdrawn
- 2014-09-04 RU RU2016112568A patent/RU2016112568A/ru not_active Application Discontinuation
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