KR102057444B1 - 이치환된 벤조티에닐-피롤로트리아진 및 fgfr 키나제 억제제로서의 그의 용도 - Google Patents
이치환된 벤조티에닐-피롤로트리아진 및 fgfr 키나제 억제제로서의 그의 용도 Download PDFInfo
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- KR102057444B1 KR102057444B1 KR1020147019406A KR20147019406A KR102057444B1 KR 102057444 B1 KR102057444 B1 KR 102057444B1 KR 1020147019406 A KR1020147019406 A KR 1020147019406A KR 20147019406 A KR20147019406 A KR 20147019406A KR 102057444 B1 KR102057444 B1 KR 102057444B1
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- alkyl
- hydrogen
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- amino
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- Expired - Fee Related
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- 0 *OCc(cc12)c[n]1ncnc2N Chemical compound *OCc(cc12)c[n]1ncnc2N 0.000 description 9
- DQZDJICDOWNODJ-UHFFFAOYSA-N CC(C)(C)OC(N1CCN(Cc2c(C)c(-c3cc4cc(C)cc(OC)c4[s]3)c3[n]2ncnc3N)CC1)=O Chemical compound CC(C)(C)OC(N1CCN(Cc2c(C)c(-c3cc4cc(C)cc(OC)c4[s]3)c3[n]2ncnc3N)CC1)=O DQZDJICDOWNODJ-UHFFFAOYSA-N 0.000 description 1
- FTQGVCCIRGLDQX-UHFFFAOYSA-N CC(C)(C)[Si](C)(C)OCc(c([Br]=C)c12)c(C#N)[n]1ncnc2N Chemical compound CC(C)(C)[Si](C)(C)OCc(c([Br]=C)c12)c(C#N)[n]1ncnc2N FTQGVCCIRGLDQX-UHFFFAOYSA-N 0.000 description 1
- HNXJXOXKHKFGNB-UHFFFAOYSA-N CC(N1CCN(Cc2c(CN(CCN3)CC3=O)c(-c3cc(cc(C)cc4OC)c4[s]3)c3[n]2ncnc3N)CC1)=O Chemical compound CC(N1CCN(Cc2c(CN(CCN3)CC3=O)c(-c3cc(cc(C)cc4OC)c4[s]3)c3[n]2ncnc3N)CC1)=O HNXJXOXKHKFGNB-UHFFFAOYSA-N 0.000 description 1
- PGYHNFZYLXOCCZ-UHFFFAOYSA-N CC(NCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN(CC3)CCN3C=O)[n]1ncnc2N)=O Chemical compound CC(NCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN(CC3)CCN3C=O)[n]1ncnc2N)=O PGYHNFZYLXOCCZ-UHFFFAOYSA-N 0.000 description 1
- JPESTLPEBJPKGA-UHFFFAOYSA-N CC(NCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN3CCNCC3)[n]1ncnc2N)=O Chemical compound CC(NCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN3CCNCC3)[n]1ncnc2N)=O JPESTLPEBJPKGA-UHFFFAOYSA-N 0.000 description 1
- IGLSLLWKILRJQQ-UHFFFAOYSA-N CCCOCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN3CCNCC3)[n]1ncnc2N Chemical compound CCCOCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(CN3CCNCC3)[n]1ncnc2N IGLSLLWKILRJQQ-UHFFFAOYSA-N 0.000 description 1
- SPVHAGRWFNXBCU-UHFFFAOYSA-N CCOC(CSc(ccc(C)c1)c1OC)OCC Chemical compound CCOC(CSc(ccc(C)c1)c1OC)OCC SPVHAGRWFNXBCU-UHFFFAOYSA-N 0.000 description 1
- BHJUBKASSJEGOB-UHFFFAOYSA-N CCOCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(C(C3CC3)O)[n]1ncnc2N Chemical compound CCOCc(c(-c1cc2cc(C)cc(OC)c2[s]1)c12)c(C(C3CC3)O)[n]1ncnc2N BHJUBKASSJEGOB-UHFFFAOYSA-N 0.000 description 1
- PAPZVKMUDMAAAR-UHFFFAOYSA-N COCc(cc12)c(C=O)[n]1ncnc2N Chemical compound COCc(cc12)c(C=O)[n]1ncnc2N PAPZVKMUDMAAAR-UHFFFAOYSA-N 0.000 description 1
- KMYLVMKQGNHPIB-UHFFFAOYSA-N Cc1cc(OC)c2[s]c(-c(c(CN(CCN3)CC3=O)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 Chemical compound Cc1cc(OC)c2[s]c(-c(c(CN(CCN3)CC3=O)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 KMYLVMKQGNHPIB-UHFFFAOYSA-N 0.000 description 1
- JFRMAVZKDFQNCB-UHFFFAOYSA-N Cc1cc(OC)c2[s]c(-c(c(CNC3CC3)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 Chemical compound Cc1cc(OC)c2[s]c(-c(c(CNC3CC3)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 JFRMAVZKDFQNCB-UHFFFAOYSA-N 0.000 description 1
- OPYADQWBIKESKM-UHFFFAOYSA-N Cc1cc(OC)c2[s]c(-c(c(CO)c3C#N)c4[n]3ncnc4N)cc2c1 Chemical compound Cc1cc(OC)c2[s]c(-c(c(CO)c3C#N)c4[n]3ncnc4N)cc2c1 OPYADQWBIKESKM-UHFFFAOYSA-N 0.000 description 1
- PSRCAUFYXJRQBZ-UHFFFAOYSA-N Cc1cc(OC)c2[s]c(-c(c(COCC(F)(F)F)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 Chemical compound Cc1cc(OC)c2[s]c(-c(c(COCC(F)(F)F)c3CN4CCNCC4)c4[n]3ncnc4N)cc2c1 PSRCAUFYXJRQBZ-UHFFFAOYSA-N 0.000 description 1
- NSDFGGPKCWFCSL-UHFFFAOYSA-N Nc1ncn[n]2c(Br)c(CO)c(Br)c12 Chemical compound Nc1ncn[n]2c(Br)c(CO)c(Br)c12 NSDFGGPKCWFCSL-UHFFFAOYSA-N 0.000 description 1
- UGJUWEUTGDVUDV-UHFFFAOYSA-N Nc1ncn[n]2c(Br)c(CO)cc12 Chemical compound Nc1ncn[n]2c(Br)c(CO)cc12 UGJUWEUTGDVUDV-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/5355—Non-condensed oxazines 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
- A61K31/535—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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841.1 | 2011-12-15 | ||
| EP11193841 | 2011-12-15 | ||
| PCT/EP2012/074977 WO2013087578A1 (en) | 2011-12-15 | 2012-12-10 | Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20140103328A KR20140103328A (ko) | 2014-08-26 |
| KR102057444B1 true KR102057444B1 (ko) | 2019-12-19 |
Family
ID=47326168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147019406A Expired - Fee Related KR102057444B1 (ko) | 2011-12-15 | 2012-12-10 | 이치환된 벤조티에닐-피롤로트리아진 및 fgfr 키나제 억제제로서의 그의 용도 |
Country Status (42)
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| KR20170090431A (ko) * | 2014-12-11 | 2017-08-07 | 바이엘 파마 악티엔게젤샤프트 | 범 ｆｇｆｒ 억제제의 용도 및 범 ｆｇｆｒ 억제제를 사용하는 치료에 대하여 적격인 암 환자를 확인하는 방법 |
| WO2016142312A1 (en) * | 2015-03-09 | 2016-09-15 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations |
| SG11201804901WA (en) | 2015-12-22 | 2018-07-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| EP3424505A4 (en) | 2016-03-04 | 2019-10-16 | Taiho Pharmaceutical Co., Ltd. | PREPARATION AND COMPOSITION FOR THE TREATMENT OF MALIGNANT TUMORS |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| KR102483020B1 (ko) | 2016-03-28 | 2023-01-04 | 인사이트 코포레이션 | Tam 저해제로서의 피롤로트리아진 화합물 |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| AU2017362350B2 (en) | 2016-11-18 | 2021-12-23 | Cystic Fibrosis Foundation | Pyrrolopyrimidines as CFTR potentiators |
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| WO2019034076A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr抑制剂及其医药用途 |
| WO2019034075A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr和egfr抑制剂 |
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| PE20211268A1 (es) * | 2017-10-25 | 2021-07-19 | Bayer Pharma AG | Proceso para preparar el benzotiofen-2-il boronato |
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| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| AR117600A1 (es) | 2018-06-29 | 2021-08-18 | Incyte Corp | Formulaciones de un inhibidor de axl / mer |
| US12391705B2 (en) | 2018-12-19 | 2025-08-19 | Shy Therapeutics, Llc | Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| JOP20210204A1 (ar) * | 2019-01-31 | 2023-01-30 | Bayer Ag | أحادي هيدرات هيدروكلوريد روجاراتينيب وأشكال صلبة منه |
| AU2020220512B2 (en) * | 2019-02-15 | 2023-08-24 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | FGFR inhibitor compound in solid form and preparation method therefor |
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| CN114641293B (zh) * | 2019-11-08 | 2024-05-31 | 石药集团中奇制药技术（石家庄）有限公司 | 一种fgfr抑制剂的用途 |
| CN111004234A (zh) * | 2019-11-28 | 2020-04-14 | 湖南农业大学 | 一种2-苯基咪唑并[1,2-α]吡啶类化合物的C3位卤化方法 |
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