CN104011025B - 作为fgfr激酶调节剂的喹啉 - Google Patents
作为fgfr激酶调节剂的喹啉 Download PDFInfo
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- CN104011025B CN104011025B CN201280065182.XA CN201280065182A CN104011025B CN 104011025 B CN104011025 B CN 104011025B CN 201280065182 A CN201280065182 A CN 201280065182A CN 104011025 B CN104011025 B CN 104011025B
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- alkyl
- substituted
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- cancer
- compound
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- 0 NC1*C*C1 Chemical compound NC1*C*C1 0.000 description 15
- HXZNNKORIOLRJX-KQQZHBGOSA-N CC(C)NCCN(/C(/C=C/OC)=C/C(OC)=C)C1=CC=CN=CC(c2c[n](CC[S+]=O)nc2)=CC=C1 Chemical compound CC(C)NCCN(/C(/C=C/OC)=C/C(OC)=C)C1=CC=CN=CC(c2c[n](CC[S+]=O)nc2)=CC=C1 HXZNNKORIOLRJX-KQQZHBGOSA-N 0.000 description 1
- KWTCOFQIPVEJAR-UHFFFAOYSA-N CN(C)S([n]1c(CN(c2ccc3ncc(N4CCOCC4)cc3c2)c2cc(OC)cc(OC)c2)ncc1)(=O)=O Chemical compound CN(C)S([n]1c(CN(c2ccc3ncc(N4CCOCC4)cc3c2)c2cc(OC)cc(OC)c2)ncc1)(=O)=O KWTCOFQIPVEJAR-UHFFFAOYSA-N 0.000 description 1
- IKMMMIRHKSZNQE-PYXUHFBKSA-N CN/C=C(\C=N)/c1cc2cc(N(CC(CC3)NC3=O)c3cc(OC)cc(OC)c3)ccc2nc1 Chemical compound CN/C=C(\C=N)/c1cc2cc(N(CC(CC3)NC3=O)c3cc(OC)cc(OC)c3)ccc2nc1 IKMMMIRHKSZNQE-PYXUHFBKSA-N 0.000 description 1
- RIESQIKYZJWIQR-UHFFFAOYSA-N CNCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)c2)c(c(F)c(cc1OC)OC)c1F Chemical compound CNCCN(c(cc1)cc2c1ncc(-c1c[n](C)nc1)c2)c(c(F)c(cc1OC)OC)c1F RIESQIKYZJWIQR-UHFFFAOYSA-N 0.000 description 1
- VHHYFVJYVWXBEM-IDVUZJLFSA-N Cc1cc(O)cc(N(CCCNCC(F)(F)F)c2ccc3ncc(/C(/C=N)=C/NC)cc3c2)c1 Chemical compound Cc1cc(O)cc(N(CCCNCC(F)(F)F)c2ccc3ncc(/C(/C=N)=C/NC)cc3c2)c1 VHHYFVJYVWXBEM-IDVUZJLFSA-N 0.000 description 1
Classifications
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- 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
- A61K31/4709—Non-condensed quinolines 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
- A61K31/435—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
-
- 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
- A61K31/535—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
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552880P | 2011-10-28 | 2011-10-28 | |
| US61/552880 | 2011-10-28 | ||
| GBGB1118652.5A GB201118652D0 (en) | 2011-10-28 | 2011-10-28 | New compounds |
| GB1118652.5 | 2011-10-28 | ||
| PCT/GB2012/052666 WO2013061074A1 (en) | 2011-10-28 | 2012-10-26 | Quinolines as fgfr kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104011025A CN104011025A (zh) | 2014-08-27 |
| CN104011025B true CN104011025B (zh) | 2017-04-05 |
Family
ID=45373580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280065182.XA Active CN104011025B (zh) | 2011-10-28 | 2012-10-26 | 作为fgfr激酶调节剂的喹啉 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9439896B2 (enExample) |
| EP (1) | EP2776397B1 (enExample) |
| JP (1) | JP6067725B2 (enExample) |
| KR (1) | KR102072869B1 (enExample) |
| CN (1) | CN104011025B (enExample) |
| AU (1) | AU2012328164B2 (enExample) |
| BR (1) | BR112014010177B1 (enExample) |
| CA (1) | CA2853366C (enExample) |
| DK (1) | DK2776397T3 (enExample) |
| ES (1) | ES2661003T3 (enExample) |
| GB (1) | GB201118652D0 (enExample) |
| HU (1) | HUE037458T2 (enExample) |
| IN (1) | IN2014MN00988A (enExample) |
| MX (1) | MX353806B (enExample) |
| RU (1) | RU2625303C2 (enExample) |
| WO (1) | WO2013061074A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| JP6250686B2 (ja) | 2012-10-16 | 2017-12-20 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｒｏｒγｔのヘテロアリール結合させたキノリニルモジュレータ |
| RS56283B1 (sr) | 2012-10-16 | 2017-12-29 | Janssen Pharmaceutica Nv | Metilen vezani hinolinil modulatori ror-gama-t |
| SG11201502935VA (en) | 2012-10-16 | 2015-09-29 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of ror-gamma-t |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| BR112016008258A2 (pt) | 2013-10-15 | 2017-10-10 | Janssen Pharmaceutica Nv | moduladores de ror?t de quinolinila |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| CA2926339A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of roryt |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| CA2926313A1 (en) * | 2013-10-15 | 2015-04-23 | Kristi A. Leonard | Secondary alcohol quinolinyl modulators of roryt |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| MX370099B (es) | 2014-03-26 | 2019-12-02 | Astex Therapeutics Ltd | Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer. |
| MX369646B (es) | 2014-08-18 | 2019-11-15 | Eisai R&D Man Co Ltd | Sal de derivado de piridina monociclico y su cristal. |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| WO2016152907A1 (ja) | 2015-03-25 | 2016-09-29 | 国立研究開発法人国立がん研究センター | 胆管癌治療剤 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| JP6898919B2 (ja) * | 2015-09-23 | 2021-07-07 | ヤンセン ファーマシューティカ エヌ．ベー． | 新規化合物 |
| WO2017050865A1 (en) * | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| CN108367000A (zh) | 2015-12-17 | 2018-08-03 | 卫材R&D管理有限公司 | 用于乳腺癌的治疗剂 |
| CN108264510A (zh) * | 2017-01-02 | 2018-07-10 | 上海喆邺生物科技有限公司 | 一种选择性抑制激酶化合物及其用途 |
| WO2019189241A1 (ja) | 2018-03-28 | 2019-10-03 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 肝細胞癌治療剤 |
| CN113087696A (zh) * | 2019-12-23 | 2021-07-09 | 江苏开元药业有限公司 | 喹啉类化合物及其应用 |
| EP4076449A4 (en) * | 2020-01-17 | 2023-12-06 | Beta Pharma, Inc. | PYRIDAZINE AND 1,2,4-TRIAZINE DERIVATIVES AS FGFR KINASE INHIBITORS |
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| WO2009141386A1 (en) * | 2008-05-23 | 2009-11-26 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
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| AU2012328164A1 (en) | 2014-05-15 |
| IN2014MN00988A (enExample) | 2015-04-24 |
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| EP2776397B1 (en) | 2017-11-29 |
| KR20140093665A (ko) | 2014-07-28 |
| AU2012328164B2 (en) | 2017-08-03 |
| US20170000781A1 (en) | 2017-01-05 |
| ES2661003T3 (es) | 2018-03-27 |
| MX353806B (es) | 2018-01-30 |
| CA2853366C (en) | 2021-04-20 |
| RU2625303C2 (ru) | 2017-07-13 |
| MX2014004857A (es) | 2014-08-26 |
| US10039759B2 (en) | 2018-08-07 |
| CN104011025A (zh) | 2014-08-27 |
| WO2013061074A1 (en) | 2013-05-02 |
| RU2014121494A (ru) | 2015-12-10 |
| EP2776397A1 (en) | 2014-09-17 |
| BR112014010177B1 (pt) | 2023-01-31 |
| US20140296236A1 (en) | 2014-10-02 |
| DK2776397T3 (en) | 2018-02-26 |
| JP2014530896A (ja) | 2014-11-20 |
| CA2853366A1 (en) | 2013-05-02 |
| KR102072869B1 (ko) | 2020-03-02 |
| BR112014010177A2 (pt) | 2017-04-25 |
| US9439896B2 (en) | 2016-09-13 |
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