JP2014532647A5 - - Google Patents
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- Publication number
- JP2014532647A5 JP2014532647A5 JP2014538891A JP2014538891A JP2014532647A5 JP 2014532647 A5 JP2014532647 A5 JP 2014532647A5 JP 2014538891 A JP2014538891 A JP 2014538891A JP 2014538891 A JP2014538891 A JP 2014538891A JP 2014532647 A5 JP2014532647 A5 JP 2014532647A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- pharmaceutically acceptable
- imatinib
- gist
- combination
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 15
- 229960002411 imatinib Drugs 0.000 claims description 15
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 15
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 10
- 238000002560 therapeutic procedure Methods 0.000 claims description 10
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 9
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 9
- 229960001796 sunitinib Drugs 0.000 claims description 9
- 229940124204 C-kit inhibitor Drugs 0.000 claims description 7
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims description 7
- 238000011282 treatment Methods 0.000 claims description 7
- 239000012828 PI3K inhibitor Substances 0.000 claims description 6
- 229940125829 fibroblast growth factor receptor inhibitor Drugs 0.000 claims description 4
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims description 2
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims description 2
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims description 2
- 239000002139 L01XE22 - Masitinib Substances 0.000 claims description 2
- WJEOLQLKVOPQFV-UHFFFAOYSA-N masitinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3SC=C(N=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 WJEOLQLKVOPQFV-UHFFFAOYSA-N 0.000 claims description 2
- 229960004655 masitinib Drugs 0.000 claims description 2
- 229960001346 nilotinib Drugs 0.000 claims description 2
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 5
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical group O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 description 7
- 238000000034 method Methods 0.000 description 6
- 206010061818 Disease progression Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 230000005750 disease progression Effects 0.000 description 2
- 230000001394 metastastic effect Effects 0.000 description 2
- 206010061289 metastatic neoplasm Diseases 0.000 description 2
- GJTNPPUXEYUHCN-UHFFFAOYSA-N 3-methyl-8-quinolin-3-yl-1h-imidazo[4,5-c]quinolin-2-one Chemical compound C1=CC=CC2=CC(C=3C=CC4=NC=C5N(C(NC5=C4C=3)=O)C)=CN=C21 GJTNPPUXEYUHCN-UHFFFAOYSA-N 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552633P | 2011-10-28 | 2011-10-28 | |
| US61/552,633 | 2011-10-28 | ||
| PCT/US2012/061532 WO2013063000A1 (en) | 2011-10-28 | 2012-10-24 | Method of treating gastrointestinal stromal tumors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014532647A JP2014532647A (ja) | 2014-12-08 |
| JP2014532647A5 true JP2014532647A5 (enExample) | 2015-12-03 |
Family
ID=47116505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014538891A Pending JP2014532647A (ja) | 2011-10-28 | 2012-10-24 | 消化管間質腫瘍を治療する方法 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20140288073A1 (enExample) |
| EP (1) | EP2770999A1 (enExample) |
| JP (1) | JP2014532647A (enExample) |
| KR (1) | KR20140096035A (enExample) |
| CN (1) | CN103889422A (enExample) |
| AU (1) | AU2012328979B2 (enExample) |
| BR (1) | BR112014009993A2 (enExample) |
| CA (1) | CA2853095A1 (enExample) |
| CL (1) | CL2014001062A1 (enExample) |
| IL (1) | IL231943A0 (enExample) |
| MX (1) | MX2014005130A (enExample) |
| PH (1) | PH12014500897A1 (enExample) |
| RU (1) | RU2014120792A (enExample) |
| SG (1) | SG11201400543TA (enExample) |
| TN (1) | TN2014000093A1 (enExample) |
| TW (1) | TW201332550A (enExample) |
| WO (1) | WO2013063000A1 (enExample) |
| ZA (1) | ZA201401622B (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| LT3495367T (lt) | 2012-06-13 | 2021-02-25 | Incyte Holdings Corporation | Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai |
| RU2015104537A (ru) * | 2012-07-11 | 2016-08-27 | Новартис Аг | Способы лечения стромальных опухолей желудочно-кишечного тракта |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| WO2014191938A1 (en) * | 2013-05-31 | 2014-12-04 | Novartis Ag | Combination therapy containing a pi3k-alpha inhibitor and fgfr kinase inhibitor for treating cancer |
| EP3057581B1 (en) | 2013-10-17 | 2019-09-04 | Sartar Therapeutics Ltd | Compositions comprising phosphodiesterase inhibitors for use in the treatment of a solid tumor in a human patient |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| SG11201706287PA (en) | 2015-02-20 | 2017-09-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| JP6860919B2 (ja) * | 2015-11-19 | 2021-04-21 | 国立大学法人金沢大学 | 間葉系ｋｒａｓ変異型がん治療剤 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| MX2020011718A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas. |
| ES3061844T3 (en) | 2018-05-04 | 2026-04-07 | Incyte Corp | Salts of an fgfr inhibitor |
| US20220010382A1 (en) * | 2018-11-12 | 2022-01-13 | Blueprint Medicines Corporation | Avapritinib resistance of kit mutants |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN112210541B (zh) * | 2020-10-14 | 2022-11-15 | 上海市普陀区利群医院 | 一种胃肠道间质瘤耐药细胞模型及其构建方法和应用 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| GB0202873D0 (en) | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
| GB0209265D0 (en) | 2002-04-23 | 2002-06-05 | Novartis Ag | Organic compounds |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| GT200600315A (es) | 2005-07-20 | 2007-03-19 | Formas cristalinas de 4-metilo-n-[3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo]-3-(4-pyridina-3-ilo-pirimidina-2-iloamino)-benzamida | |
| GT200600316A (es) | 2005-07-20 | 2007-04-02 | Sales de 4-metilo-n-(3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo)-3-(4-piridina-3-ilo-pirimidina-2-iloamino)- benzamida. | |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EP1923053A1 (en) | 2006-09-27 | 2008-05-21 | Novartis AG | Pharmaceutical compositions comprising nilotinib or its salt |
| EA019064B1 (ru) * | 2007-04-11 | 2013-12-30 | Экселиксис, Инк. | Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа |
| JP5351254B2 (ja) | 2008-05-23 | 2013-11-27 | ノバルティス アーゲー | キノキサリン−およびキノリン−カルボキシアミド誘導体 |
| EP2297912A4 (en) * | 2008-07-01 | 2016-11-30 | Ikanos Communications Inc | VECTORED DSL WITH REDUCED MEMORY |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
-
2012
- 2012-10-24 WO PCT/US2012/061532 patent/WO2013063000A1/en not_active Ceased
- 2012-10-24 RU RU2014120792/15A patent/RU2014120792A/ru not_active Application Discontinuation
- 2012-10-24 CN CN201280052892.9A patent/CN103889422A/zh active Pending
- 2012-10-24 KR KR1020147010940A patent/KR20140096035A/ko not_active Withdrawn
- 2012-10-24 SG SG11201400543TA patent/SG11201400543TA/en unknown
- 2012-10-24 AU AU2012328979A patent/AU2012328979B2/en not_active Expired - Fee Related
- 2012-10-24 EP EP12780391.4A patent/EP2770999A1/en not_active Withdrawn
- 2012-10-24 US US14/353,186 patent/US20140288073A1/en not_active Abandoned
- 2012-10-24 CA CA2853095A patent/CA2853095A1/en not_active Abandoned
- 2012-10-24 PH PH1/2014/500897A patent/PH12014500897A1/en unknown
- 2012-10-24 BR BR112014009993A patent/BR112014009993A2/pt not_active IP Right Cessation
- 2012-10-24 JP JP2014538891A patent/JP2014532647A/ja active Pending
- 2012-10-24 MX MX2014005130A patent/MX2014005130A/es not_active Application Discontinuation
- 2012-10-26 TW TW101139801A patent/TW201332550A/zh unknown
-
2014
- 2014-03-04 ZA ZA2014/01622A patent/ZA201401622B/en unknown
- 2014-03-06 TN TNP2014000093A patent/TN2014000093A1/en unknown
- 2014-04-03 IL IL231943A patent/IL231943A0/en unknown
- 2014-04-25 CL CL2014001062A patent/CL2014001062A1/es unknown