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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- amino
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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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841 | 2011-12-15 | ||
| EP11193841.1 | 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)
Families Citing this family (48)
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| US10388493B2 (en) | 2011-09-16 | 2019-08-20 | Lam Research Corporation | Component of a substrate support assembly producing localized magnetic fields |
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| WO2015008844A1 (ja) | 2013-07-18 | 2015-01-22 | 大鵬薬品工業株式会社 | Ｆｇｆｒ阻害剤耐性癌の治療薬 |
| TR201907147T4 (tr) | 2013-07-18 | 2019-06-21 | Taiho Pharmaceutical Co Ltd | Fgfr inhibitörünün aralıklı uygulanmasına yönelik anti-tümör ilaç. |
| MY184561A (en) * | 2013-10-21 | 2021-04-03 | Genosco | Substituted pyrimidine compounds and their use as syk inhibitors |
| EP3229800A2 (en) * | 2014-12-11 | 2017-10-18 | Bayer Pharma Aktiengesellschaft | Use of pan fgfr inhibitors and method of identifying patients with cancer eligible for treatment with a pan fgfr inhibitor |
| JP6867295B2 (ja) | 2015-03-09 | 2021-04-28 | バイエル ファーマ アクチエンゲゼルシャフト | 置換２，３−ジヒドロイミダゾ［１，２−ｃ］キナゾリンを含んでいる組合せ |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| 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 |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| 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 |
| SG10201911076QA (en) | 2016-12-16 | 2020-01-30 | Cystic Fibrosis Found | Bycyclic heteroaryl derivatives as cftr potentiators |
| JP7514005B2 (ja) | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| 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 |
| SI3687996T1 (sl) | 2017-09-27 | 2022-04-29 | Incyte Corporation | Soli pirolotriazinskih derivatov, ki so uporabne kot zaviralci TAM |
| JOP20200090A1 (ar) * | 2017-10-25 | 2020-05-03 | Bayer Pharma AG | عملية لتحضير بنزوثيوفين-2 يل بورونات |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| SG11202008435SA (en) | 2018-03-19 | 2020-10-29 | Taiho Pharmaceutical Co Ltd | Pharmaceutical composition including sodium alkyl sulfate |
| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| JP2022519081A (ja) * | 2019-01-31 | 2022-03-18 | バイエル アクチェンゲゼルシャフト | ロガラチニブ塩酸塩の一水和物およびその固体状態 |
| EP3925960B1 (en) * | 2019-02-15 | 2023-07-26 | CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | Fgfr inhibitor compound in solid form and preparation method therefor |
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| CN109928976A (zh) * | 2019-02-26 | 2019-06-25 | 泰州亿腾景昂药业有限公司 | 一种工业化生产eoc317的方法 |
| US10829493B2 (en) | 2019-04-12 | 2020-11-10 | Blueprint Medicines Corporation | Compositions and methods for treating KIT- and PDGFRA-mediated diseases |
| AU2020274083B9 (en) | 2019-05-13 | 2025-05-01 | D.E. Shaw Research, Llc | FGFR inhibitors and methods of use thereof |
| 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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| WO2000071129A1 (en) | 1999-05-21 | 2000-11-30 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
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| WO2000071129A1 (en) | 1999-05-21 | 2000-11-30 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
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