RU2014120792A - Способ лечения стромальных опухолей желудочно-кишечного тракта - Google Patents
Способ лечения стромальных опухолей желудочно-кишечного тракта Download PDFInfo
- Publication number
- RU2014120792A RU2014120792A RU2014120792/15A RU2014120792A RU2014120792A RU 2014120792 A RU2014120792 A RU 2014120792A RU 2014120792/15 A RU2014120792/15 A RU 2014120792/15A RU 2014120792 A RU2014120792 A RU 2014120792A RU 2014120792 A RU2014120792 A RU 2014120792A
- Authority
- RU
- Russia
- Prior art keywords
- gist
- combination
- inhibitor
- imatinib
- pharmaceutically acceptable
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract 13
- 206010028980 Neoplasm Diseases 0.000 title 1
- 210000001035 gastrointestinal tract Anatomy 0.000 title 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims abstract 10
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims abstract 8
- 229960002411 imatinib Drugs 0.000 claims abstract 8
- 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 abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 8
- 229940124204 C-kit inhibitor Drugs 0.000 claims abstract 6
- 239000012828 PI3K inhibitor Substances 0.000 claims abstract 4
- 229940125829 fibroblast growth factor receptor inhibitor Drugs 0.000 claims abstract 4
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims abstract 4
- 238000002560 therapeutic procedure Methods 0.000 claims abstract 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 abstract 2
- IHGVAVLSTPCCJP-UHFFFAOYSA-N 4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-amine Chemical compound N1=C(N)SC(C=2C=C(N=CC=2)C(C)(C)C(F)(F)F)=C1C IHGVAVLSTPCCJP-UHFFFAOYSA-N 0.000 claims abstract 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 abstract 2
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims abstract 2
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims abstract 2
- 239000002139 L01XE22 - Masitinib Substances 0.000 claims abstract 2
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound 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 abstract 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 abstract 2
- 229960004655 masitinib Drugs 0.000 claims abstract 2
- 229960001346 nilotinib Drugs 0.000 claims abstract 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 abstract 2
- 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 abstract 2
- 229960001796 sunitinib Drugs 0.000 claims abstract 2
Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| RU2014120792A true RU2014120792A (ru) | 2015-12-10 |
Family
ID=47116505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014120792/15A RU2014120792A (ru) | 2011-10-28 | 2012-10-24 | Способ лечения стромальных опухолей желудочно-кишечного тракта |
Country Status (18)
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 |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| AU2013289175A1 (en) * | 2012-07-11 | 2015-01-22 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2014191938A1 (en) * | 2013-05-31 | 2014-12-04 | Novartis Ag | Combination therapy containing a pi3k-alpha inhibitor and fgfr kinase inhibitor for treating cancer |
| JP6445573B2 (ja) | 2013-10-17 | 2018-12-26 | サルタル セラピューティクス エルティーディＳａｒｔａｒ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｔｄ | ヒト患者の固形腫瘍の治療に用いるためのホスホジエステラーゼ阻害剤含有組成物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2017086332A1 (ja) * | 2015-11-19 | 2017-05-26 | 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 |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020102095A1 (en) * | 2018-11-12 | 2020-05-22 | Blueprint Medicines Corporation | Avapritinib resistance of kit mutants |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| 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 |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
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 |
| UA98141C2 (ru) * | 2007-04-11 | 2012-04-25 | Экселиксис, Инк. | Способы лечения с применением хинаксолиновых ингибиторов pi3k-альфа |
| AU2009248774B2 (en) | 2008-05-23 | 2012-05-31 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| JP5248677B2 (ja) * | 2008-07-01 | 2013-07-31 | イカノス テクノロジー リミテッド | メモリ削減されたベクトル化されたｄｓｌ |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
-
2012
- 2012-10-24 RU RU2014120792/15A patent/RU2014120792A/ru not_active Application Discontinuation
- 2012-10-24 WO PCT/US2012/061532 patent/WO2013063000A1/en not_active Ceased
- 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 AU AU2012328979A patent/AU2012328979B2/en not_active Expired - Fee Related
- 2012-10-24 MX MX2014005130A patent/MX2014005130A/es not_active Application Discontinuation
- 2012-10-24 CA CA2853095A patent/CA2853095A1/en not_active Abandoned
- 2012-10-24 JP JP2014538891A patent/JP2014532647A/ja active Pending
- 2012-10-24 US US14/353,186 patent/US20140288073A1/en not_active Abandoned
- 2012-10-24 SG SG11201400543TA patent/SG11201400543TA/en unknown
- 2012-10-24 BR BR112014009993A patent/BR112014009993A2/pt not_active IP Right Cessation
- 2012-10-24 EP EP12780391.4A patent/EP2770999A1/en not_active Withdrawn
- 2012-10-24 PH PH1/2014/500897A patent/PH12014500897A1/en unknown
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| PH12014500897A1 (en) | 2019-10-07 |
| AU2012328979B2 (en) | 2016-04-21 |
| AU2012328979A1 (en) | 2014-05-15 |
| JP2014532647A (ja) | 2014-12-08 |
| SG11201400543TA (en) | 2014-08-28 |
| CL2014001062A1 (es) | 2014-10-10 |
| CN103889422A (zh) | 2014-06-25 |
| IL231943A0 (en) | 2014-05-28 |
| WO2013063000A1 (en) | 2013-05-02 |
| EP2770999A1 (en) | 2014-09-03 |
| US20140288073A1 (en) | 2014-09-25 |
| BR112014009993A2 (pt) | 2017-04-25 |
| CA2853095A1 (en) | 2013-05-02 |
| TN2014000093A1 (en) | 2015-07-01 |
| NZ622155A (en) | 2015-12-24 |
| ZA201401622B (en) | 2015-12-23 |
| TW201332550A (zh) | 2013-08-16 |
| KR20140096035A (ko) | 2014-08-04 |
| MX2014005130A (es) | 2014-08-27 |
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