TWI669300B - 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途 - Google Patents
嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途 Download PDFInfo
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- TWI669300B TWI669300B TW106116657A TW106116657A TWI669300B TW I669300 B TWI669300 B TW I669300B TW 106116657 A TW106116657 A TW 106116657A TW 106116657 A TW106116657 A TW 106116657A TW I669300 B TWI669300 B TW I669300B
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- 0 CC(C=C)N(CC1)CC11CN(*)CC1 Chemical compound CC(C=C)N(CC1)CC11CN(*)CC1 0.000 description 5
- XJVZSZODRVBVGV-UHFFFAOYSA-N CCN(CC1)C2(CC2)CN1c(cc1)cc(NC(C=C)=O)c1Nc1ncnc(N(C)C(Nc(c(Cl)c(cc2OC)OC)c2Cl)=O)c1 Chemical compound CCN(CC1)C2(CC2)CN1c(cc1)cc(NC(C=C)=O)c1Nc1ncnc(N(C)C(Nc(c(Cl)c(cc2OC)OC)c2Cl)=O)c1 XJVZSZODRVBVGV-UHFFFAOYSA-N 0.000 description 1
- PCUWIJVPOXEWJH-UHFFFAOYSA-N CN(C(NC(C(Cl)=C(CC1OC)OC)=C1Cl)=O)C1=NCNC(Nc(ccc(N2CC3(CC3)NCC2)c2)c2NC(C=C)=O)=C1 Chemical compound CN(C(NC(C(Cl)=C(CC1OC)OC)=C1Cl)=O)C1=NCNC(Nc(ccc(N2CC3(CC3)NCC2)c2)c2NC(C=C)=O)=C1 PCUWIJVPOXEWJH-UHFFFAOYSA-N 0.000 description 1
- RMBOTBYLWKFONE-UHFFFAOYSA-N CN(C(Nc(c(Cl)c(cc1OC)OC)c1Cl)=O)c1cc(Nc(c(NC(C=C)=O)c2)ccc2N(C2)CC22CCNCC2)ncn1 Chemical compound CN(C(Nc(c(Cl)c(cc1OC)OC)c1Cl)=O)c1cc(Nc(c(NC(C=C)=O)c2)ccc2N(C2)CC22CCNCC2)ncn1 RMBOTBYLWKFONE-UHFFFAOYSA-N 0.000 description 1
- XCGAGBWTJLMLSN-UHFFFAOYSA-N CN(CC1)CC11CCN(C)CC1 Chemical compound CN(CC1)CC11CCN(C)CC1 XCGAGBWTJLMLSN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D403/14—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 three or more hetero 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- 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
- C07D487/10—Spiro-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610341444 | 2016-05-20 | ||
| ??CN201610341444.0 | 2016-05-20 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201741303A TW201741303A (zh) | 2017-12-01 |
| TWI669300B true TWI669300B (zh) | 2019-08-21 |
Family
ID=60324797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW106116657A TWI669300B (zh) | 2016-05-20 | 2017-05-19 | 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途 |
Country Status (7)
| Country | Link |
|---|---|
| US (4) | US10654836B2 (enExample) |
| EP (1) | EP3459952B1 (enExample) |
| JP (1) | JP6667014B2 (enExample) |
| CN (1) | CN108884097B (enExample) |
| CA (1) | CA3024532C (enExample) |
| TW (1) | TWI669300B (enExample) |
| WO (1) | WO2017198221A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201602069WA (en) | 2013-10-18 | 2016-04-28 | Eisai R&D Man Co Ltd | Pyrimidine fgfr4 inhibitors |
| CN107660200B (zh) | 2015-04-14 | 2022-01-11 | 卫材R&D管理有限公司 | 结晶fgfr4抑制剂化合物和其用途 |
| JP7372740B2 (ja) | 2016-05-10 | 2023-11-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 細胞生存性及び／又は細胞増殖を低減するための薬物の組み合わせ |
| CN108822048A (zh) * | 2018-07-23 | 2018-11-16 | 上海昌肽生物科技有限公司 | 4-(4-乙基-4,7二氮杂螺环[3,3]辛基)-2-硝基苯胺的合成工艺 |
| TWI723480B (zh) | 2018-07-27 | 2021-04-01 | 大陸商北京加科思新藥研發有限公司 | 用作fgfr4抑制劑的稠環衍生物 |
| CN115490670A (zh) * | 2021-06-17 | 2022-12-20 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂的盐及其制备方法和用途 |
| CN115504965A (zh) | 2021-06-23 | 2022-12-23 | 浙江海正药业股份有限公司 | 嘧啶类衍生物的晶型及其制备方法 |
| CN116947825B (zh) * | 2022-04-14 | 2025-11-28 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂化合物的晶型及其制备方法和用途 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015057938A1 (en) * | 2013-10-18 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Pyrimidine fgfr4 inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| CN102250065B (zh) * | 2011-05-20 | 2015-05-13 | 浙江海正药业股份有限公司 | 取代的三嗪苯脲衍生物及其用途 |
| UA114501C2 (uk) * | 2012-02-28 | 2017-06-26 | Астеллас Фарма Інк. | Азотовмісна ароматична гетероциклічна сполука |
| KR20150037207A (ko) * | 2013-09-30 | 2015-04-08 | 한미약품 주식회사 | Fms 키나아제 저해 활성을 갖는 피리미딘 화합물 |
| CN105683188B (zh) | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| CN104860891B (zh) * | 2014-02-25 | 2017-06-30 | 上海海雁医药科技有限公司 | 芳氨基嘧啶类化合物及其应用以及由其制备的药物组合物和药用组合物 |
-
2017
- 2017-05-19 TW TW106116657A patent/TWI669300B/zh active
- 2017-05-19 CN CN201780022674.3A patent/CN108884097B/zh active Active
- 2017-05-19 CA CA3024532A patent/CA3024532C/en active Active
- 2017-05-19 JP JP2018560780A patent/JP6667014B2/ja active Active
- 2017-05-19 EP EP17798784.9A patent/EP3459952B1/en active Active
- 2017-05-19 WO PCT/CN2017/085135 patent/WO2017198221A1/zh not_active Ceased
- 2017-05-19 US US16/302,310 patent/US10654836B2/en active Active
-
2020
- 2020-02-25 US US16/800,057 patent/US11001572B2/en active Active
-
2021
- 2021-03-31 US US17/218,380 patent/US11827625B2/en active Active
-
2023
- 2023-09-14 US US18/368,362 patent/US12358898B2/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015057938A1 (en) * | 2013-10-18 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Pyrimidine fgfr4 inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| US11827625B2 (en) | 2023-11-28 |
| EP3459952B1 (en) | 2022-01-05 |
| US12358898B2 (en) | 2025-07-15 |
| JP6667014B2 (ja) | 2020-03-18 |
| US20190161476A1 (en) | 2019-05-30 |
| CN108884097B (zh) | 2021-05-28 |
| EP3459952A4 (en) | 2020-01-15 |
| WO2017198221A1 (zh) | 2017-11-23 |
| US20240018130A1 (en) | 2024-01-18 |
| US20210221797A1 (en) | 2021-07-22 |
| CA3024532A1 (en) | 2017-11-23 |
| TW201741303A (zh) | 2017-12-01 |
| US10654836B2 (en) | 2020-05-19 |
| US11001572B2 (en) | 2021-05-11 |
| JP2019519512A (ja) | 2019-07-11 |
| US20200207745A1 (en) | 2020-07-02 |
| CN108884097A (zh) | 2018-11-23 |
| EP3459952A1 (en) | 2019-03-27 |
| CA3024532C (en) | 2021-02-09 |
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