KR20190035870A - Fgfr 저해제로서 헤테로시클릭 화합물 - Google Patents
Fgfr 저해제로서 헤테로시클릭 화합물 Download PDFInfo
- Publication number
- KR20190035870A KR20190035870A KR1020197006637A KR20197006637A KR20190035870A KR 20190035870 A KR20190035870 A KR 20190035870A KR 1020197006637 A KR1020197006637 A KR 1020197006637A KR 20197006637 A KR20197006637 A KR 20197006637A KR 20190035870 A KR20190035870 A KR 20190035870A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- group
- cycloalkyl
- heterocyclyl
- independently selected
- 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.)
- Ceased
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- 150000002391 heterocyclic compounds Chemical class 0.000 title abstract 3
- 229940125829 fibroblast growth factor receptor inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 15
- 239000000651 prodrug Substances 0.000 claims abstract 9
- 229940002612 prodrug Drugs 0.000 claims abstract 9
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 108091008794 FGF receptors Proteins 0.000 claims abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 201000010099 disease Diseases 0.000 claims abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 4
- 230000001404 mediated effect Effects 0.000 claims abstract 4
- 206010028980 Neoplasm Diseases 0.000 claims abstract 3
- 238000000034 method Methods 0.000 claims abstract 3
- 201000011510 cancer Diseases 0.000 claims abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- -1 C 1 -C 6 alkyl Chemical class 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 102000044168 Fibroblast Growth Factor Receptor Human genes 0.000 abstract 3
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 0 ***(C=C1)C=Cc2c1nc[o]2 Chemical compound ***(C=C1)C=Cc2c1nc[o]2 0.000 description 5
- GFHZIJLRLXZEDG-LAQIPUCWSA-N C/C=C/C(N(CC1)C[C@@H]1c1nc(C#Cc2cc(OC)cc(OC)c2)c2[n]1ccnc2N)=O Chemical compound C/C=C/C(N(CC1)C[C@@H]1c1nc(C#Cc2cc(OC)cc(OC)c2)c2[n]1ccnc2N)=O GFHZIJLRLXZEDG-LAQIPUCWSA-N 0.000 description 1
- UHPPFIOSYWGDJO-QGZVFWFLSA-N CC#CC(N(CC1)C[C@@H]1c1nc(C#Cc2cc(OC)cc(OC)c2)c2[n]1ccnc2N)=O Chemical compound CC#CC(N(CC1)C[C@@H]1c1nc(C#Cc2cc(OC)cc(OC)c2)c2[n]1ccnc2N)=O UHPPFIOSYWGDJO-QGZVFWFLSA-N 0.000 description 1
- PSLHUNJMSLYTMJ-UHFFFAOYSA-N COc1cc(C#CC(C23)N=C(C(CC4)CN4C(C=C)=O)N2C=CN=C3N)cc(OC)c1 Chemical compound COc1cc(C#CC(C23)N=C(C(CC4)CN4C(C=C)=O)N2C=CN=C3N)cc(OC)c1 PSLHUNJMSLYTMJ-UHFFFAOYSA-N 0.000 description 1
- JYGFTBXVXVMTGB-UHFFFAOYSA-N O=C(C1)Nc2c1cccc2 Chemical compound O=C(C1)Nc2c1cccc2 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 description 1
- ZYGHJZDHTFUPRJ-UHFFFAOYSA-N O=C1Oc(cccc2)c2C=C1 Chemical compound O=C1Oc(cccc2)c2C=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 description 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N c1c[nH]c2ccccc12 Chemical compound c1c[nH]c2ccccc12 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N c1n[nH]c2c1cccc2 Chemical compound c1n[nH]c2c1cccc2 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 1
- IOJUPLGTWVMSFF-UHFFFAOYSA-N c1nc(cccc2)c2[s]1 Chemical compound c1nc(cccc2)c2[s]1 IOJUPLGTWVMSFF-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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610647295.0A CN107698593A (zh) | 2016-08-09 | 2016-08-09 | 作为fgfr抑制剂的杂环化合物 |
| CN201610647295.0 | 2016-08-09 | ||
| PCT/CN2017/094620 WO2018028438A1 (zh) | 2016-08-09 | 2017-07-27 | 作为fgfr抑制剂的杂环化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20190035870A true KR20190035870A (ko) | 2019-04-03 |
Family
ID=61162708
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197006637A Ceased KR20190035870A (ko) | 2016-08-09 | 2017-07-27 | Fgfr 저해제로서 헤테로시클릭 화합물 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10752631B2 (enExample) |
| EP (1) | EP3498706A4 (enExample) |
| JP (1) | JP6959663B2 (enExample) |
| KR (1) | KR20190035870A (enExample) |
| CN (2) | CN107698593A (enExample) |
| CA (1) | CA3032921A1 (enExample) |
| WO (1) | WO2018028438A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3062591A1 (en) | 2017-05-08 | 2018-11-15 | Gritstone Oncology, Inc. | Alphavirus neoantigen vectors |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| JP2022533939A (ja) * | 2019-05-17 | 2022-07-27 | キネート バイオファーマ インク． | 線維芽細胞増殖因子受容体キナーゼの阻害剤 |
| MX2021014525A (es) | 2019-05-30 | 2022-03-17 | Gritstone Bio Inc | Adenovirus modificados. |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2021285974A1 (en) * | 2020-06-05 | 2023-01-19 | Kinnate Biopharma Inc. | Inhibitors of fibroblast growth factor receptor kinases |
| TW202210472A (zh) | 2020-06-05 | 2022-03-16 | 美商奇奈特生物製藥公司 | 纖維母細胞生長因子受體激酶之抑制劑 |
| CA3187258A1 (en) | 2020-08-06 | 2022-02-10 | Karin Jooss | Multiepitope vaccine cassettes |
| CN112480109B (zh) * | 2020-11-16 | 2022-04-01 | 浙江大学 | 吡啶并[2,3-b]吡嗪-3(4H)-酮类衍生物及其用途 |
| AU2022206989A1 (en) * | 2021-01-12 | 2023-08-24 | Beijing Innocare Pharma Tech Co., Ltd. | Process for preparing (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl) ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide |
| CN114853739B (zh) * | 2021-02-03 | 2023-09-22 | 药雅科技(上海)有限公司 | 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途 |
| CN115043832B (zh) * | 2021-03-08 | 2023-08-22 | 药雅科技(上海)有限公司 | 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途 |
| CN120051471A (zh) * | 2022-10-18 | 2025-05-27 | 首药控股(北京)股份有限公司 | 一种新型杂环化合物 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7659274B2 (en) * | 2006-01-25 | 2010-02-09 | Osi Pharmaceuticals, Inc. | Unsaturated mTOR inhibitors |
| CN103958512B (zh) * | 2012-01-19 | 2016-01-20 | 大鹏药品工业株式会社 | 3,5-双取代炔基苯化合物及其盐 |
| AU2014243869A1 (en) * | 2013-03-13 | 2015-09-24 | Boston Biomedical, Inc. | 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer |
| US10124003B2 (en) * | 2013-07-18 | 2018-11-13 | Taiho Pharmaceutical Co., Ltd. | Therapeutic agent for FGFR inhibitor-resistant cancer |
| KR101974254B1 (ko) * | 2013-07-18 | 2019-04-30 | 다이호야쿠힌고교 가부시키가이샤 | Fgfr 저해제의 간헐 투여용 항종양제 |
| CN104341425B (zh) * | 2013-08-08 | 2018-11-02 | 上海医药集团股份有限公司 | 氘代乙炔衍生物、其药物组合物及应用 |
| WO2015048662A2 (en) * | 2013-09-30 | 2015-04-02 | X-Rx Discovery, Inc. | Substituted nicotinimide inhibitors of btk and their preparation and use in the treatment of cancer, inflammation and autoimmune disease |
| KR102022866B1 (ko) * | 2014-08-19 | 2019-09-19 | 상하이 하이헤 파마수티컬 컴퍼니 리미티드 | 섬유 아세포 성장 인자 수용체 키나아제 억제제인 인다졸계 화합물 및 이의 제조와 응용 |
-
2016
- 2016-08-09 CN CN201610647295.0A patent/CN107698593A/zh active Pending
-
2017
- 2017-07-27 JP JP2019529309A patent/JP6959663B2/ja not_active Expired - Fee Related
- 2017-07-27 CA CA3032921A patent/CA3032921A1/en active Pending
- 2017-07-27 CN CN201780045675.XA patent/CN109715626B/zh active Active
- 2017-07-27 WO PCT/CN2017/094620 patent/WO2018028438A1/zh not_active Ceased
- 2017-07-27 KR KR1020197006637A patent/KR20190035870A/ko not_active Ceased
- 2017-07-27 US US16/324,189 patent/US10752631B2/en not_active Expired - Fee Related
- 2017-07-27 EP EP17838568.8A patent/EP3498706A4/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CN109715626B (zh) | 2022-04-26 |
| EP3498706A4 (en) | 2020-02-26 |
| CA3032921A1 (en) | 2018-02-15 |
| US10752631B2 (en) | 2020-08-25 |
| CN109715626A (zh) | 2019-05-03 |
| US20190177333A1 (en) | 2019-06-13 |
| CN107698593A (zh) | 2018-02-16 |
| WO2018028438A1 (zh) | 2018-02-15 |
| JP2019524883A (ja) | 2019-09-05 |
| EP3498706A1 (en) | 2019-06-19 |
| JP6959663B2 (ja) | 2021-11-02 |
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Patent event date: 20190306 Patent event code: PA01051R01D Comment text: International Patent Application |
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Patent event code: PA02012R01D Patent event date: 20200527 Comment text: Request for Examination of Application |
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