KR101933843B1 - 피라졸릴 퀴녹살린 키나제 억제제 - Google Patents
피라졸릴 퀴녹살린 키나제 억제제 Download PDFInfo
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- KR101933843B1 KR101933843B1 KR1020187023217A KR20187023217A KR101933843B1 KR 101933843 B1 KR101933843 B1 KR 101933843B1 KR 1020187023217 A KR1020187023217 A KR 1020187023217A KR 20187023217 A KR20187023217 A KR 20187023217A KR 101933843 B1 KR101933843 B1 KR 101933843B1
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- South Korea
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- alkoxy
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- 0 *N(c1ccccc1)c(cc1)cc2c1ncc(-c1c[n](*)nc1)n2 Chemical compound *N(c1ccccc1)c(cc1)cc2c1ncc(-c1c[n](*)nc1)n2 0.000 description 13
- JSUQGYCISCKCSF-UHFFFAOYSA-N Clc1nc(cc(cc2)Nc3ccccc3)c2nc1 Chemical compound Clc1nc(cc(cc2)Nc3ccccc3)c2nc1 JSUQGYCISCKCSF-UHFFFAOYSA-N 0.000 description 3
- YUDQIUJRJBBJTI-UHFFFAOYSA-N CC(C)C(COC(C1)C(C)c(c(OC)cc(OC)c2)c2N1c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)O Chemical compound CC(C)C(COC(C1)C(C)c(c(OC)cc(OC)c2)c2N1c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)O YUDQIUJRJBBJTI-UHFFFAOYSA-N 0.000 description 2
- YYKVKXQIRJYYTQ-UHFFFAOYSA-N CC(C)(C)OC(CNCCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1)=O Chemical compound CC(C)(C)OC(CNCCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1)=O YYKVKXQIRJYYTQ-UHFFFAOYSA-N 0.000 description 1
- LGZCGNQXVVZYCD-UHFFFAOYSA-N CC(C)(C)OC(N(CCCOS(C)(=O)=O)CC(F)(F)F)=O Chemical compound CC(C)(C)OC(N(CCCOS(C)(=O)=O)CC(F)(F)F)=O LGZCGNQXVVZYCD-UHFFFAOYSA-N 0.000 description 1
- UZIQZYKQNQGCGV-UHFFFAOYSA-N CC(C)(C)OC(N(CCC[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(OC)c4)c3nc2)c1)C(OC(C)(C)C)=O)=O Chemical compound CC(C)(C)OC(N(CCC[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(OC)c4)c3nc2)c1)C(OC(C)(C)C)=O)=O UZIQZYKQNQGCGV-UHFFFAOYSA-N 0.000 description 1
- NCUXFZFOUYDOGS-UHFFFAOYSA-N CC(C)(C)OC(NCCC[n]1ncc(-c2nc(cc(cc3)N(CCO)c4cc(OC)cc(OC)c4)c3nc2)c1)=O Chemical compound CC(C)(C)OC(NCCC[n]1ncc(-c2nc(cc(cc3)N(CCO)c4cc(OC)cc(OC)c4)c3nc2)c1)=O NCUXFZFOUYDOGS-UHFFFAOYSA-N 0.000 description 1
- ODWHUOXCJXLMPI-UHFFFAOYSA-N CC(C)(C)OC(NCCC[n]1ncc(-c2nc(cc(cc3)N(CCO[Si](C)(C)C(C)(C)C)c4cc(OC)cc(OC)c4)c3nc2)c1)=O Chemical compound CC(C)(C)OC(NCCC[n]1ncc(-c2nc(cc(cc3)N(CCO[Si](C)(C)C(C)(C)C)c4cc(OC)cc(OC)c4)c3nc2)c1)=O ODWHUOXCJXLMPI-UHFFFAOYSA-N 0.000 description 1
- YYNSVJSIHCPECJ-UHFFFAOYSA-N CC(C)(C)[Si](C)(C)OCc1cc(Nc(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)cc(OC)c1 Chemical compound CC(C)(C)[Si](C)(C)OCc1cc(Nc(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)cc(OC)c1 YYNSVJSIHCPECJ-UHFFFAOYSA-N 0.000 description 1
- LUDGMVDSCQQOMP-UHFFFAOYSA-N CC(C)CN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1 Chemical compound CC(C)CN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1 LUDGMVDSCQQOMP-UHFFFAOYSA-N 0.000 description 1
- WRLWYPHGUGGAFD-UHFFFAOYSA-N CC(C)N(CCOC1CN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)C1=O Chemical compound CC(C)N(CCOC1CN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)C1=O WRLWYPHGUGGAFD-UHFFFAOYSA-N 0.000 description 1
- VSIZOFOKNLADGC-UHFFFAOYSA-N CC(C)NCCN(c(cc1)cc2c1ncc(-c1c[n](CCS(C)(=O)=O)nc1)n2)c1cc(OC)cc(OC)c1 Chemical compound CC(C)NCCN(c(cc1)cc2c1ncc(-c1c[n](CCS(C)(=O)=O)nc1)n2)c1cc(OC)cc(OC)c1 VSIZOFOKNLADGC-UHFFFAOYSA-N 0.000 description 1
- ZAWBYXATEBIOBQ-UHFFFAOYSA-N CC1(C)NC(CN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)COC1 Chemical compound CC1(C)NC(CN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)COC1 ZAWBYXATEBIOBQ-UHFFFAOYSA-N 0.000 description 1
- IRQQWKLISVHOTL-OPBFZPCWSA-N CCC(C)(C)OC[C@@H](C)[C@@H](C/C=C(\CC)/OC)CCl Chemical compound CCC(C)(C)OC[C@@H](C)[C@@H](C/C=C(\CC)/OC)CCl IRQQWKLISVHOTL-OPBFZPCWSA-N 0.000 description 1
- MRGCIZUVAAEOML-UHFFFAOYSA-N CCC(CN(C)C)N(C)N=C Chemical compound CCC(CN(C)C)N(C)N=C MRGCIZUVAAEOML-UHFFFAOYSA-N 0.000 description 1
- UHTLKZSSOZYNMP-UHFFFAOYSA-N CCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1 Chemical compound CCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)c1cc(OC)cc(OC)c1 UHTLKZSSOZYNMP-UHFFFAOYSA-N 0.000 description 1
- QPXCBVHAGGPGCX-UHFFFAOYSA-N CCNC(c1cc(N)cc(OC)c1)=O Chemical compound CCNC(c1cc(N)cc(OC)c1)=O QPXCBVHAGGPGCX-UHFFFAOYSA-N 0.000 description 1
- JMNBRXGZUGRIPY-UHFFFAOYSA-N CCOc1cc(F)cc(N(CCN)c(cc2)cc3c2ncc(-c2c[n](C4OCCCC4)nc2)n3)c1 Chemical compound CCOc1cc(F)cc(N(CCN)c(cc2)cc3c2ncc(-c2c[n](C4OCCCC4)nc2)n3)c1 JMNBRXGZUGRIPY-UHFFFAOYSA-N 0.000 description 1
- CPLYQZKEYHJUJZ-UHFFFAOYSA-N CN(C)Cc([n](C)nc1)c1-c1nc(cc(cc2)N(CCO)c3cc(OC)cc(OC)c3)c2nc1 Chemical compound CN(C)Cc([n](C)nc1)c1-c1nc(cc(cc2)N(CCO)c3cc(OC)cc(OC)c3)c2nc1 CPLYQZKEYHJUJZ-UHFFFAOYSA-N 0.000 description 1
- XTDKZSUYCXHXJM-UHFFFAOYSA-N COC1OCCCC1 Chemical compound COC1OCCCC1 XTDKZSUYCXHXJM-UHFFFAOYSA-N 0.000 description 1
- QAQJMSZWWPFNJB-UHFFFAOYSA-N COc(cc1OC)cc(N)c1Cl Chemical compound COc(cc1OC)cc(N)c1Cl QAQJMSZWWPFNJB-UHFFFAOYSA-N 0.000 description 1
- BXBWZDDZLDSYQH-UHFFFAOYSA-N COc1cc(N(CC2CC2)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OCCO)c1 Chemical compound COc1cc(N(CC2CC2)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OCCO)c1 BXBWZDDZLDSYQH-UHFFFAOYSA-N 0.000 description 1
- PIOVDHZNDKMBCX-UHFFFAOYSA-N COc1cc(N(CCCN(CC2)CC2(F)F)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OC)c1 Chemical compound COc1cc(N(CCCN(CC2)CC2(F)F)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OC)c1 PIOVDHZNDKMBCX-UHFFFAOYSA-N 0.000 description 1
- NOCCEPOVUSRFDS-UHFFFAOYSA-N COc1cc(N(CCO)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OC)c1 Chemical compound COc1cc(N(CCO)c(cc2)cc3c2ncc(-c2c[nH]nc2)n3)cc(OC)c1 NOCCEPOVUSRFDS-UHFFFAOYSA-N 0.000 description 1
- ZLIXAXDZDFQVBX-UHFFFAOYSA-N COc1cc(OC)cc(N(CC2CC2)c(cc2)cc3c2ncc(-c2c[n](CCN)nc2)n3)c1 Chemical compound COc1cc(OC)cc(N(CC2CC2)c(cc2)cc3c2ncc(-c2c[n](CCN)nc2)n3)c1 ZLIXAXDZDFQVBX-UHFFFAOYSA-N 0.000 description 1
- FVUYKZNGSHSNBI-UHFFFAOYSA-N C[n]1ncc(-c2cnc(ccc(N(CCP(O)(O)=O)c3cc(OC)cc(OC)c3)c3)c3n2)c1 Chemical compound C[n]1ncc(-c2cnc(ccc(N(CCP(O)(O)=O)c3cc(OC)cc(OC)c3)c3)c3n2)c1 FVUYKZNGSHSNBI-UHFFFAOYSA-N 0.000 description 1
- JRZBGTIYYHVJEO-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CC(CN)O)c4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CC(CN)O)c4cc(OC)cc(OC)c4)c3nc2)c1 JRZBGTIYYHVJEO-UHFFFAOYSA-N 0.000 description 1
- BHKNJNBAQCANQS-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CC(CN4)OC4=O)c4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CC(CN4)OC4=O)c4cc(OC)cc(OC)c4)c3nc2)c1 BHKNJNBAQCANQS-UHFFFAOYSA-N 0.000 description 1
- WMYLESPXATZBNH-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CC4CC4)c4cc(C#N)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CC4CC4)c4cc(C#N)cc(OC)c4)c3nc2)c1 WMYLESPXATZBNH-UHFFFAOYSA-N 0.000 description 1
- ZGLQPPJENDKPPE-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CC4NCCNC4)c4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CC4NCCNC4)c4cc(OC)cc(OC)c4)c3nc2)c1 ZGLQPPJENDKPPE-UHFFFAOYSA-N 0.000 description 1
- XFQQPBXZMOROTB-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CCN4CCC(CN)CC4)c4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CCN4CCC(CN)CC4)c4cc(OC)cc(OC)c4)c3nc2)c1 XFQQPBXZMOROTB-UHFFFAOYSA-N 0.000 description 1
- RTJRHBHZFYFHCT-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CCNOC)c4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CCNOC)c4cc(OC)cc(OC)c4)c3nc2)c1 RTJRHBHZFYFHCT-UHFFFAOYSA-N 0.000 description 1
- JLJYYWKYPUAYPA-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)N(CCOS(C)(=O)=O)c4cc(OC)cc(OCOCCOC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)N(CCOS(C)(=O)=O)c4cc(OC)cc(OCOCCOC)c4)c3nc2)c1 JLJYYWKYPUAYPA-UHFFFAOYSA-N 0.000 description 1
- HQIZTGGWMNWYTQ-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(CO)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(CO)c4)c3nc2)c1 HQIZTGGWMNWYTQ-UHFFFAOYSA-N 0.000 description 1
- BHFGEPMLMSSSSI-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(OC)c4)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)Nc4cc(OC)cc(OC)c4)c3nc2)c1 BHFGEPMLMSSSSI-UHFFFAOYSA-N 0.000 description 1
- WOSVNYMVLJXSBE-VWLOTQADSA-N C[n]1ncc(-c2nc3cc(N(CCCN4S[C@H](CCl)CCC4)c4cc(OC)cc(OC)c4)ccc3nc2)c1 Chemical compound C[n]1ncc(-c2nc3cc(N(CCCN4S[C@H](CCl)CCC4)c4cc(OC)cc(OC)c4)ccc3nc2)c1 WOSVNYMVLJXSBE-VWLOTQADSA-N 0.000 description 1
- XNCGHPSDJDLXOW-UHFFFAOYSA-N Cc(c(N)cc(OC)c1)c1OC Chemical compound Cc(c(N)cc(OC)c1)c1OC XNCGHPSDJDLXOW-UHFFFAOYSA-N 0.000 description 1
- YPTPHGKUZUTKPO-UHFFFAOYSA-N Cc(nc1CO)c[n]1S(N(C)C)(=O)=O Chemical compound Cc(nc1CO)c[n]1S(N(C)C)(=O)=O YPTPHGKUZUTKPO-UHFFFAOYSA-N 0.000 description 1
- QBEFGIIZODSORK-UHFFFAOYSA-N Cc1cc(CCCN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)ncc1 Chemical compound Cc1cc(CCCN(c(cc2)cc3c2ncc(-c2c[n](C)nc2)n3)c2cc(OC)cc(OC)c2)ncc1 QBEFGIIZODSORK-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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Families Citing this family (103)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| KR101913109B1 (ko) | 2009-03-18 | 2018-10-31 | 리스버로직스 코퍼레이션 | 신규한 소염제 |
| US9757368B2 (en) | 2009-04-22 | 2017-09-12 | Resverlogix Corp. | Anti-inflammatory agents |
| GB201007286D0 (en) * | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| WO2013059740A1 (en) | 2011-10-21 | 2013-04-25 | Foundation Medicine, Inc. | Novel alk and ntrk1 fusion molecules and uses thereof |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
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| GB201209609D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori fgfr |
| SG11201500125QA (en) | 2012-07-11 | 2015-02-27 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| PT2906531T (pt) * | 2012-10-15 | 2018-02-06 | Resverlogix Corp | Compostos úteis na síntese de compostos de benzamida |
| EP2914621B1 (en) | 2012-11-05 | 2023-06-07 | Foundation Medicine, Inc. | Novel ntrk1 fusion molecules and uses thereof |
| US11230589B2 (en) | 2012-11-05 | 2022-01-25 | Foundation Medicine, Inc. | Fusion molecules and uses thereof |
| WO2014085486A2 (en) | 2012-11-30 | 2014-06-05 | Waters Technologies Corporation | Methods and apparatus for the analysis of vitamin d metabolites |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CA3150658A1 (en) | 2013-01-18 | 2014-07-24 | Foundation Medicine, Inc. | Methods of treating cholangiocarcinoma |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| CN105307657B (zh) * | 2013-03-15 | 2020-07-10 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| GB201307577D0 (en) * | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| CN104163794A (zh) * | 2013-10-17 | 2014-11-26 | 中国药科大学 | 2-氨基芳环类血管内皮生长因子受体(vegfr)抑制剂及其制备方法和用途 |
| RS63405B1 (sr) | 2013-10-25 | 2022-08-31 | Blueprint Medicines Corp | Inhibitori receptora faktora rasta fibroblasta |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| RU2715236C2 (ru) * | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| HRP20210319T1 (hr) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | Kombinacije inhibitora fgfr i inhibitora igf1r |
| CN105017227B (zh) * | 2014-07-08 | 2018-03-09 | 四川百利药业有限责任公司 | N‑(1h‑吡唑‑5‑基)喹唑啉‑4‑胺类化合物 |
| KR102344105B1 (ko) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
| KR102470456B1 (ko) * | 2014-09-26 | 2022-11-23 | 얀센 파마슈티카 엔.브이. | Fgfr 억제제를 사용한 치료에 반응할 암 환자를 확인하는 데 있어서 fgfr 돌연변이 유전자 패널의 사용 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| TWI695837B (zh) | 2014-12-04 | 2020-06-11 | 比利時商健生藥品公司 | 作為激酶調節劑之三唑並嗒 |
| TWI719960B (zh) * | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| TWI712601B (zh) | 2015-02-20 | 2020-12-11 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
| EP3275442B1 (en) | 2015-03-25 | 2021-07-28 | National Cancer Center | Therapeutic agent for bile duct cancer |
| TWI703984B (zh) * | 2015-04-03 | 2020-09-11 | 英商阿斯特克斯治療有限公司 | 用於癌症治療之fgfr/pd-1組合療法 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| US11155555B2 (en) | 2015-09-23 | 2021-10-26 | Janssen Pharmaceutica Nv | Compounds |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| CN105596330B (zh) * | 2015-12-11 | 2018-10-16 | 深圳市坤健创新药物研究院 | 虚拟筛选化合物在制备激酶抑制剂中的应用和药物 |
| CN108367000A (zh) | 2015-12-17 | 2018-08-03 | 卫材R&D管理有限公司 | 用于乳腺癌的治疗剂 |
| CN107459519A (zh) | 2016-06-06 | 2017-12-12 | 上海艾力斯医药科技有限公司 | 稠合嘧啶哌啶环衍生物及其制备方法和应用 |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| US10689362B2 (en) * | 2016-10-10 | 2020-06-23 | Development Center For Biotechnology | Quinoxaline compounds as type III receptor tyrosine kinase inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| JOP20190280A1 (ar) | 2017-06-02 | 2019-12-02 | Janssen Pharmaceutica Nv | مثبطات fgfr2 لعلاج سرطان الأوعية الصفراوية |
| US10717703B2 (en) | 2017-08-21 | 2020-07-21 | Celgene Corporation | Processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate |
| US11661411B2 (en) | 2017-12-01 | 2023-05-30 | Board Of Regents Of The University Of Nebraska | Quinoxaline compounds and uses thereof |
| US11219619B2 (en) | 2018-03-28 | 2022-01-11 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| JP7491510B2 (ja) * | 2018-04-26 | 2024-05-28 | メディシナル バイオコンバージェンス リサーチ センター | mTOR阻害剤としての新規化合物及びその用途 |
| AU2019262579B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Salts of an FGFR inhibitor |
| HRP20241288T1 (hr) | 2018-05-04 | 2024-12-06 | Incyte Corporation | Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju |
| WO2020058432A1 (en) | 2018-09-21 | 2020-03-26 | Janssen Pharmaceutica Nv | Treatment of cholangiocarcinoma |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| MA55486A (fr) | 2019-03-29 | 2022-02-09 | Janssen Pharmaceutica Nv | Inhibiteurs de la tyrosine kinase fgfr pour le traitement du carcinome urothélial |
| PH12021552342A1 (en) | 2019-03-29 | 2022-08-22 | Janssen Pharmaceutica Nv | Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma |
| WO2020208592A1 (en) * | 2019-04-12 | 2020-10-15 | Dr. Reddy’S Laboratories Limited | Process for preparation of erdafitinib, its purification and amorphous solid dispersion |
| CN111909044A (zh) * | 2019-05-09 | 2020-11-10 | 南京爱德程医药科技有限公司 | 2-(烷基氨基)乙基苯甲酸酯类化合物的合成方法 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI759829B (zh) * | 2019-08-23 | 2022-04-01 | 財團法人生物技術開發中心 | 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物 |
| EP4034118A1 (en) | 2019-09-26 | 2022-08-03 | Janssen Pharmaceutica NV | Use of fgfr inhibitors in fgfr-genetically altered cancers to enhance patient response to immune checkpoint inhibitors in sequential treatment settings |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN110790677B (zh) * | 2019-11-05 | 2022-04-29 | 浙江工业大学 | 一种金刚烷甲酰胺类化合物及其制备方法和应用 |
| AU2020391161A1 (en) | 2019-11-25 | 2022-06-09 | Amgen Inc. | Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| JP7832891B2 (ja) | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Fgfr阻害剤の誘導体 |
| CN113024518A (zh) * | 2019-12-09 | 2021-06-25 | 武汉九州钰民医药科技有限公司 | 一种厄达替尼的制备方法 |
| CN113024517A (zh) * | 2019-12-09 | 2021-06-25 | 武汉九州钰民医药科技有限公司 | 一种制备厄达替尼的方法 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2023512482A (ja) * | 2020-01-17 | 2023-03-27 | ベータ・ファーマ・インコーポレイテッド | Fgfrキナーゼ阻害剤としてのピリダジンおよび1,2,4-トリアジン誘導体 |
| CN115103678A (zh) | 2020-02-12 | 2022-09-23 | 詹森药业有限公司 | 用于治疗高风险非肌层浸润性膀胱癌的fgfr酪氨酸激酶抑制剂 |
| TWI900527B (zh) | 2020-02-12 | 2025-10-11 | 比利時商健生藥品公司 | 用於治療尿路上皮癌的fgfr酪胺酸激酶抑制劑和抗pd1藥劑 |
| US20240010632A1 (en) | 2020-08-17 | 2024-01-11 | Teva Pharmaceuticals International Gmbh | Solid state forms of erdafitinib salts and processes for preparation of erdafitinib |
| CN112920167B (zh) * | 2020-08-19 | 2022-08-26 | 四川大学华西医院 | 靶向fgfr和hdac的双靶点抑制剂及其制备方法和应用、药物组合物及药剂 |
| EP4210702A1 (en) | 2020-09-14 | 2023-07-19 | JANSSEN Pharmaceutica NV | Fgfr inhibitor combination therapies |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| BR112023023935A2 (pt) | 2021-05-19 | 2024-01-30 | Janssen Pharmaceutica Nv | Inibidores de tirosina quinase de fgfr para o tratamento de tumores sólidos avançados |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| CN117858872A (zh) | 2021-06-22 | 2024-04-09 | 缆图药品公司 | 用于治疗癌症的杂环egfr抑制剂 |
| IL312063A (en) | 2021-10-12 | 2024-06-01 | Taris Biomedical Llc | Ardafitinib formulations and systems for intravesical administration |
| AU2022379973A1 (en) | 2021-11-08 | 2024-06-27 | Progentos Therapeutics, Inc. | Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof |
| KR20240145513A (ko) * | 2022-02-18 | 2024-10-07 | 타리스 바이오메디컬 엘엘씨 | 에르다피티닙 제형 및 방광내 투여를 위한 삼투성 시스템 |
| CN115108926B (zh) * | 2022-04-02 | 2023-06-20 | 上海工程技术大学 | 一种用于制备厄达替尼的中间体化合物及制备方法 |
| KR20250143348A (ko) | 2023-02-13 | 2025-10-01 | 타리스 바이오메디컬 엘엘씨 | 방광암 치료에 사용하기 위한 방광내 투여용 에르다피티닙 |
| EP4665341A1 (en) | 2023-02-13 | 2025-12-24 | Janssen Pharmaceutica NV | Fgfr tyrosine kinase inhibitors for the treatment of high-risk non-muscle invasive bladder cancer |
| CN119101036A (zh) * | 2023-06-08 | 2024-12-10 | 广州六顺生物科技有限公司 | 喹喔啉类化合物及其应用 |
| WO2025059602A1 (en) | 2023-09-14 | 2025-03-20 | Taris Biomedical Llc | Methods of treating bladder cancer using intravesical administration of erdafitinib |
| CN119350298A (zh) * | 2024-10-09 | 2025-01-24 | 沈阳药科大学 | 一种厄达替尼的制备方法以及用于该方法的中间体化合物 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005061463A1 (en) | 2003-12-23 | 2005-07-07 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
| WO2008078091A1 (en) | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| WO2008141065A1 (en) | 2007-05-10 | 2008-11-20 | Smithkline Beecham Corporation | Quinoxaline derivatives as p13 kinase inhibitors |
Family Cites Families (125)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2940972A (en) | 1957-06-27 | 1960-06-14 | Thomae Gmbh Dr K | Tri-and tetra-substituted pteridine derivatives |
| US4666828A (en) | 1984-08-15 | 1987-05-19 | The General Hospital Corporation | Test for Huntington's disease |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| US4801531A (en) | 1985-04-17 | 1989-01-31 | Biotechnology Research Partners, Ltd. | Apo AI/CIII genomic polymorphisms predictive of atherosclerosis |
| US5272057A (en) | 1988-10-14 | 1993-12-21 | Georgetown University | Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase |
| US5192659A (en) | 1989-08-25 | 1993-03-09 | Genetype Ag | Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes |
| GB9125001D0 (en) | 1991-11-25 | 1992-01-22 | Ici Plc | Heterocyclic compounds |
| AU6909194A (en) | 1993-05-14 | 1994-12-12 | Board Of Regents, The University Of Texas System | Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole |
| US5700823A (en) | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| US6331555B1 (en) | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
| US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
| EP0951541B1 (en) | 1995-07-31 | 2005-11-30 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
| TW472045B (en) | 1996-09-25 | 2002-01-11 | Astra Ab | Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation |
| SI0991628T1 (en) | 1997-05-28 | 2005-06-30 | Aventis Pharmaceuticals Inc | QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR P56lck TYROSINE KINASES |
| US6235740B1 (en) | 1997-08-25 | 2001-05-22 | Bristol-Myers Squibb Co. | Imidazoquinoxaline protein tyrosine kinase inhibitors |
| UA71555C2 (en) | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| WO2000042026A1 (en) | 1999-01-15 | 2000-07-20 | Novo Nordisk A/S | Non-peptide glp-1 agonists |
| US7169778B2 (en) | 1999-09-15 | 2007-01-30 | Warner-Lambert Company | Pteridinones as kinase inhibitors |
| DE10013318A1 (de) | 2000-03-17 | 2001-09-20 | Merck Patent Gmbh | Formulierung enthaltend Chinoxalinderivate |
| WO2002076985A1 (en) | 2001-03-23 | 2002-10-03 | Smithkline Beecham Corporation | Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases |
| DE60223720T2 (de) | 2001-12-18 | 2008-10-30 | Merck & Co., Inc. | Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5 |
| WO2003055491A1 (en) | 2001-12-24 | 2003-07-10 | Astrazeneca Ab | Substituted quinazoline derivatives as inhibitors of aurora kinases |
| JP2003213463A (ja) | 2002-01-17 | 2003-07-30 | Sumitomo Chem Co Ltd | 金属腐食防止剤および洗浄液 |
| US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | Inhibitors of Akt activity |
| US7265378B2 (en) | 2002-07-10 | 2007-09-04 | E. I. Du Pont De Nemours And Company | Electronic devices made with electron transport and/or anti-quenching layers |
| US7825132B2 (en) | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| AU2003282726B2 (en) | 2002-10-03 | 2010-10-07 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| AR043059A1 (es) | 2002-11-12 | 2005-07-13 | Bayer Pharmaceuticals Corp | Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos |
| US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| MXPA05007503A (es) | 2003-01-17 | 2005-09-21 | Warner Lambert Co | Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular. |
| EP1620413A2 (en) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| WO2004110350A2 (en) | 2003-05-14 | 2004-12-23 | Torreypines Therapeutics, Inc. | Compouds and uses thereof in modulating amyloid beta |
| PT1636228E (pt) | 2003-05-23 | 2009-02-02 | Aeterna Zentaris Gmbh | Novas piridopirazinas e sua utilização como moduladores de cinases |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| WO2005007099A2 (en) | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| AU2004259000A1 (en) | 2003-07-21 | 2005-02-03 | Bethesda Pharmaceuticals, Inc. | Design and synthesis of optimized ligands for PPAR |
| JP2007501189A (ja) | 2003-08-01 | 2007-01-25 | ジェネラブス テクノロジーズ,インコーポレイテッド | フラビウイルス科に対する二環式イミダゾール誘導体 |
| PL1673092T3 (pl) | 2003-10-17 | 2008-01-31 | 4 Aza Ip Nv | Pochodne pterydyny podstawione heterocyklem i ich zastosowanie w leczeniu |
| US20050209247A1 (en) | 2003-11-07 | 2005-09-22 | Chiron Corporation | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
| BRPI0416206A (pt) | 2003-11-20 | 2006-12-26 | Janssen Pharmaceutica Nv | 2-quinolinonas e 2-quinoxalinonas substituìdas por 6-alquenila e 6-fenilalquila como inibidores de polimerase de poli(adp-ribose) |
| AU2004295050A1 (en) | 2003-11-24 | 2005-06-16 | F.Hoffmann-La Roche Ag | Pyrazolyl and imidazolyl pyrimidines |
| US7205316B2 (en) | 2004-05-12 | 2007-04-17 | Abbott Laboratories | Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands |
| US7098222B2 (en) | 2004-05-12 | 2006-08-29 | Abbott Laboratories | Bicyclic-substituted amines having cyclic-substituted monocyclic substituents |
| CA2577275A1 (en) | 2004-08-31 | 2006-03-09 | Astrazeneca Ab | Quinazolinone derivatives and their use as b-raf inhibitors |
| US7268231B2 (en) | 2004-10-14 | 2007-09-11 | Hoffmann-La Roche Inc. | 1,5-Naphthyridine azolinone |
| MX2007004480A (es) | 2004-10-15 | 2007-05-08 | Astrazeneca Ab | Quinoxalinas como inhibidores b raf. |
| WO2006066361A1 (en) | 2004-12-24 | 2006-06-29 | The University Of Queensland | Method of treatment or prophylaxis |
| AU2006212726C1 (en) | 2005-02-14 | 2013-05-16 | Bionomics Limited | Novel tubulin polymerisation inhibitors |
| WO2006092430A1 (de) | 2005-03-03 | 2006-09-08 | Universität des Saarlandes | Selektive hemmstoffe humaner corticoidsynthasen |
| US20090156617A1 (en) | 2005-05-12 | 2009-06-18 | Northrup Alan B | Tyrosine kinase inhibitors |
| MX2007014258A (es) | 2005-05-18 | 2008-01-22 | Wyeth Corp | Inhibidores de 4,6-diamino-[1,7]naftiridin-3-carbonitrilo de la tpl2 cinasa y metodos de fabricacion y uso de los mismos. |
| GB0513692D0 (en) | 2005-07-04 | 2005-08-10 | Karobio Ab | Novel pharmaceutical compositions |
| US8071597B2 (en) | 2005-08-26 | 2011-12-06 | Merck Serono Sa | Pyrazine compounds and uses as PI3K inhibitors |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| WO2007054556A1 (de) | 2005-11-11 | 2007-05-18 | Æterna Zentaris Gmbh | Neue pyridopyrazine und deren verwendung als modulatoren von kinasen |
| HRP20170103T1 (hr) | 2005-12-21 | 2017-03-24 | Janssen Pharmaceutica N.V. | Triazolopiridazini kao modulatori tirozin kinaze |
| CA2651072A1 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| EP2029600B1 (de) | 2006-05-24 | 2012-03-14 | Boehringer Ingelheim International GmbH | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | 諾華公司 | 吡咯并嘧啶化合物及其用途 |
| AU2007271187A1 (en) | 2006-07-03 | 2008-01-10 | Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg | Fused bicyclic compounds interacting with the histamine H4 receptor |
| US8148361B2 (en) | 2006-11-10 | 2012-04-03 | Bristol-Myers Squibb Company | Kinase inhibitors |
| JP2008127446A (ja) | 2006-11-20 | 2008-06-05 | Canon Inc | 1,5−ナフチリジン化合物及び有機発光素子 |
| EP2104501B1 (en) | 2006-12-13 | 2014-03-12 | Merck Sharp & Dohme Corp. | Methods of cancer treatment with igf1r inhibitors |
| JP2010514695A (ja) | 2006-12-21 | 2010-05-06 | プレキシコン,インコーポレーテッド | キナーゼ調節のための化合物および方法およびそのための適応症 |
| JP2010514693A (ja) | 2006-12-22 | 2010-05-06 | ノバルティス アーゲー | Pdk1阻害のためのキナゾリン |
| KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| WO2008150827A1 (en) | 2007-05-29 | 2008-12-11 | Smithkline Beecham Corporation | Naphthyridine, derivatives as p13 kinase inhibitors |
| AR066879A1 (es) | 2007-06-08 | 2009-09-16 | Novartis Ag | Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus |
| RU2462454C2 (ru) | 2007-06-20 | 2012-09-27 | Мицубиси Танабе Фарма Корпорейшн | Новое сульфонамидное производное малоновой кислоты и его фармацевтическое применение |
| EP2170894A1 (en) | 2007-06-21 | 2010-04-07 | Janssen Pharmaceutica N.V. | Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1h-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline |
| EP2173338A1 (en) | 2007-07-06 | 2010-04-14 | OSI Pharmaceuticals, Inc. | Combination anti-cancer therapy |
| ES2424977T3 (es) | 2007-08-08 | 2013-10-10 | Glaxosmithkline Intellectual Property Development Limited | Derivados de 2-[(2-{fenilamino}-1H-pirrolo[2,3-D]pirimidin-4-il)amino]benzamida como inhibidores de IGF-1R para el tratamiento del cáncer |
| EP2173354A4 (en) | 2007-08-09 | 2011-10-05 | Glaxosmithkline Llc | CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS |
| WO2009019518A1 (en) | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
| US20090054304A1 (en) | 2007-08-23 | 2009-02-26 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 for treatment of disease |
| UA104849C2 (uk) * | 2007-11-16 | 2014-03-25 | Інсайт Корпорейшн | 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus |
| US20110129456A1 (en) | 2008-05-05 | 2011-06-02 | Yaolin Wang | Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer |
| ES2554513T3 (es) | 2008-05-23 | 2015-12-21 | Novartis Ag | Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa |
| US8592448B2 (en) | 2008-11-20 | 2013-11-26 | OSI Pharmaceuticals, LLC | Substituted pyrrolo[2,3-b]-pyridines and -pyrazines |
| AU2010206161B2 (en) | 2009-01-21 | 2014-08-07 | Basilea Pharmaceutica Ag | Novel bicyclic antibiotics |
| AU2010208480A1 (en) | 2009-02-02 | 2011-07-28 | Msd K.K. | Inhibitors of Akt activity |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| SI2440547T1 (sl) | 2009-06-12 | 2023-05-31 | Abivax | Nove kemične molekule, ki zavirajo mehanizem spajanja za zdravljenje bolezni, ki so posledica napak pri spajanju |
| AU2010289397B2 (en) | 2009-09-03 | 2016-05-26 | Bioenergenix | Heterocyclic compounds for the inhibition of PASK |
| JP5728683B2 (ja) | 2009-09-04 | 2015-06-03 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン |
| US20110123545A1 (en) | 2009-11-24 | 2011-05-26 | Bristol-Myers Squibb Company | Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases |
| EP2332939A1 (en) | 2009-11-26 | 2011-06-15 | Æterna Zentaris GmbH | Novel Naphthyridine derivatives and the use thereof as kinase inhibitors |
| CN102918034B (zh) | 2010-03-30 | 2015-06-03 | 维颂公司 | 多取代芳族化合物作为凝血酶的抑制剂 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| US8513421B2 (en) | 2010-05-19 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| CN103153062B (zh) | 2010-05-24 | 2015-07-15 | 因特利凯有限责任公司 | 杂环化合物及其用途 |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| CN102532141A (zh) | 2010-12-08 | 2012-07-04 | 中国科学院上海药物研究所 | [1,2,4]三唑并[4,3-b][1,2,4]三嗪类化合物、其制备方法和用途 |
| MX343706B (es) | 2011-01-31 | 2016-11-18 | Novartis Ag | Derivados heterocíclicos novedosos. |
| MX2013008833A (es) | 2011-02-02 | 2013-12-06 | Amgen Inc | Metodos y composiciones relacionadas con la inhibicion de receptor del factor de crecimiento similar a la insulina 1 (igf-1r). |
| US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
| WO2012118492A1 (en) | 2011-03-01 | 2012-09-07 | Array Biopharma Inc. | Heterocyclic sulfonamides as raf inhibitors |
| WO2012149014A1 (en) | 2011-04-25 | 2012-11-01 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
| ES2725790T3 (es) | 2011-08-26 | 2019-09-27 | Neupharma Inc | Algunas entidades químicas, composiciones, y métodos |
| CN115403531A (zh) | 2011-09-14 | 2022-11-29 | 润新生物公司 | 作为激酶抑制剂的化学实体、组合物及方法 |
| US9249110B2 (en) | 2011-09-21 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| HK1201065A1 (en) | 2011-10-04 | 2015-08-21 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of pi3k |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| PT2771342T (pt) | 2011-10-28 | 2016-08-17 | Novartis Ag | Derivados de purina e o seu uso no tratamento de doença |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| PL2824181T3 (pl) | 2012-03-08 | 2019-02-28 | Astellas Pharma Inc. | Nowa fuzja fgfr3 |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| US20150203589A1 (en) | 2012-07-24 | 2015-07-23 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| CA3150658A1 (en) | 2013-01-18 | 2014-07-24 | Foundation Medicine, Inc. | Methods of treating cholangiocarcinoma |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| EP3027623A4 (en) | 2013-08-02 | 2017-03-01 | Ignyta, Inc. | METHODS OF TREATING VARIOUS CANCERS USING AN AXL/cMET INHIBITOR ALONE OR IN COMBINATION WITH OTHER AGENTS |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| RU2715236C2 (ru) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| HRP20210319T1 (hr) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | Kombinacije inhibitora fgfr i inhibitora igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| BR112017017700A2 (pt) | 2015-02-19 | 2018-07-31 | Bioclin Therapeutics Inc | métodos, composições e kits para tratamento do câncer |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
-
2010
- 2010-04-30 GB GB201007286A patent/GB201007286D0/en not_active Ceased
-
2011
- 2011-04-19 JO JOP/2011/0133A patent/JO3366B1/ar active
- 2011-04-27 TW TW100114665A patent/TWI545122B/zh active
- 2011-04-28 MY MYPI2012004699A patent/MY189427A/en unknown
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- 2011-04-28 MX MX2015012476A patent/MX365702B/es unknown
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- 2011-04-28 NZ NZ602726A patent/NZ602726A/en unknown
- 2011-04-28 EA EA201291143A patent/EA023222B8/ru unknown
- 2011-04-28 SI SI201131755T patent/SI3178818T1/sl unknown
- 2011-04-28 RS RSP20191045 patent/RS59196B1/sr unknown
- 2011-04-28 LT LTEP11724710.6T patent/LT2563775T/lt unknown
- 2011-04-28 AU AU2011247047A patent/AU2011247047B2/en active Active
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005061463A1 (en) | 2003-12-23 | 2005-07-07 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
| WO2008078091A1 (en) | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| WO2008141065A1 (en) | 2007-05-10 | 2008-11-20 | Smithkline Beecham Corporation | Quinoxaline derivatives as p13 kinase inhibitors |
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