JP6564771B2 - キナーゼ阻害剤としてのピリミジン誘導体 - Google Patents

キナーゼ阻害剤としてのピリミジン誘導体 Download PDF

Info

Publication number
JP6564771B2
JP6564771B2 JP2016525833A JP2016525833A JP6564771B2 JP 6564771 B2 JP6564771 B2 JP 6564771B2 JP 2016525833 A JP2016525833 A JP 2016525833A JP 2016525833 A JP2016525833 A JP 2016525833A JP 6564771 B2 JP6564771 B2 JP 6564771B2
Authority
JP
Japan
Prior art keywords
alkyl
halo
substituted
compound
alkoxy
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.)
Active
Application number
JP2016525833A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016528209A5 (enExample
JP2016528209A (ja
Inventor
シャオ スー，
シャオ スー，
シャオボ ワン，
シャオボ ワン，
ロン マオ，
ロン マオ，
リ ジャオ，
リ ジャオ，
ビアオ シ，
ビアオ シ，
Original Assignee
エイシア バイオサイエンシーズ インコーポレイテッド
エイシア バイオサイエンシーズ インコーポレイテッド
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by エイシア バイオサイエンシーズ インコーポレイテッド, エイシア バイオサイエンシーズ インコーポレイテッド filed Critical エイシア バイオサイエンシーズ インコーポレイテッド
Publication of JP2016528209A publication Critical patent/JP2016528209A/ja
Publication of JP2016528209A5 publication Critical patent/JP2016528209A5/ja
Application granted granted Critical
Publication of JP6564771B2 publication Critical patent/JP6564771B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • 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
    • C07D403/12—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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2016525833A 2013-07-11 2014-07-11 キナーゼ阻害剤としてのピリミジン誘導体 Active JP6564771B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361845342P 2013-07-11 2013-07-11
US61/845,342 2013-07-11
US201461923179P 2014-01-02 2014-01-02
US61/923,179 2014-01-02
PCT/US2014/046442 WO2015006754A2 (en) 2013-07-11 2014-07-11 Heterocyclic compounds and uses thereof

Publications (3)

Publication Number Publication Date
JP2016528209A JP2016528209A (ja) 2016-09-15
JP2016528209A5 JP2016528209A5 (enExample) 2017-08-17
JP6564771B2 true JP6564771B2 (ja) 2019-08-21

Family

ID=51298956

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016525833A Active JP6564771B2 (ja) 2013-07-11 2014-07-11 キナーゼ阻害剤としてのピリミジン誘導体

Country Status (16)

Country Link
US (1) US10562918B2 (enExample)
EP (1) EP3019496B1 (enExample)
JP (1) JP6564771B2 (enExample)
KR (1) KR102173433B1 (enExample)
CN (3) CN112592334B (enExample)
AU (1) AU2014287016B2 (enExample)
BR (1) BR112016000195A8 (enExample)
CA (1) CA2917364C (enExample)
DK (1) DK3019496T3 (enExample)
ES (1) ES2761572T3 (enExample)
IL (1) IL243420A0 (enExample)
MX (1) MX368491B (enExample)
NZ (1) NZ715687A (enExample)
RU (1) RU2677653C2 (enExample)
SG (1) SG11201600062RA (enExample)
WO (1) WO2015006754A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11007197B2 (en) 2012-08-06 2021-05-18 ACEA Therapeutics, Inc. EGFR modulators and uses thereof

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CA2861010A1 (en) 2012-01-13 2013-07-18 Xiao Xu Heterocyclic compounds and uses as anticancer agents
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
BR112016000195A8 (pt) 2013-07-11 2019-12-31 Acea Biosciences Inc compostos heterocíclicos, composição farmacêutica, combinação, seu uso, e método para inibir uma atividade da tirosina quinase btk ou jak, egfr, alk, pdgfr, blk, bmx/etk, flt3(d835y), itk, tec, txk, e suas respectivas vias
ES3069593T3 (en) 2013-08-23 2026-06-09 Neupharma Inc Quinazolin-8-yl derivatives for use in methods of treating melanoma, non-small cell lung cancer, thyroid cancer, ovarian cancer, or colon cancer
EP3205650B1 (en) * 2014-10-11 2021-08-04 Shanghai Hansoh Biomedical Co., Ltd. Egfr inhibitor, and preparation and application thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN105884695B (zh) * 2015-02-13 2019-02-26 山东轩竹医药科技有限公司 杂环衍生物类酪氨酸激酶抑制剂
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CN107427521B (zh) * 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
CN106146515B (zh) * 2015-04-17 2020-09-04 常州隆赛医药科技有限公司 新型激酶抑制剂的制备及应用
KR101778004B1 (ko) * 2015-06-22 2017-09-15 (주) 에빅스젠 이마티닙을 유효성분으로 포함하는 안구 건조 질환 예방 및 치료용 약학 조성물
JP6853234B2 (ja) * 2015-07-09 2021-03-31 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのピリミジン誘導体及びその使用
EP3359159B1 (en) 2015-10-09 2023-06-07 ACEA Therapeutics, Inc. Pharmaceutical compositions of a pyrrolopyrimidine kinase inhibitor, and methods of making same
CN106608868A (zh) * 2015-10-21 2017-05-03 复旦大学 5-(硫醚基)嘧啶类化合物及其药用组合物和应用
KR20170050453A (ko) * 2015-10-30 2017-05-11 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 이에 사용되는 중간체
WO2017097113A1 (zh) * 2015-12-10 2017-06-15 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
RU2714206C1 (ru) * 2016-06-30 2020-02-13 Даевунг Фармасьютикал Ко., Лтд. Пиразолопиримидиновые производные в качестве ингибитора киназы
CN109843858B (zh) 2016-08-15 2023-05-05 润新生物公司 某些化学实体、组合物及方法
CN106749042B (zh) * 2016-11-16 2019-01-22 大连医科大学 磺酰胺基嘧啶类化合物，组合物及用途
KR20180075228A (ko) * 2016-12-26 2018-07-04 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 중간체
EP3564232B1 (en) 2016-12-27 2022-01-26 Riken Bmp-signal-inhibiting compound
WO2018139883A1 (ko) * 2017-01-26 2018-08-02 부광약품 주식회사 다중 표적 키나아제 저해제로서 융합피리미딘 유도체
US11608334B2 (en) * 2017-02-08 2023-03-21 The National Institutes of Pharmaceutical R&D Co., Ltd. Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof
AU2017408099A1 (en) * 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
CN112752750B (zh) * 2018-08-09 2025-11-28 艾森医药公司 N-(嘧啶基苯基)-丙烯酰胺化合物的固体形式及其用途
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021098813A1 (zh) * 2019-11-22 2021-05-27 南京明德新药研发有限公司 作为dna-pk抑制剂的嘧啶并吡咯类螺环化合物及其衍生物
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN111018842B (zh) * 2019-12-04 2021-02-12 宜春市人民医院 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN111848631B (zh) * 2020-08-28 2022-04-19 四川大学华西医院 一种靶向EGFR突变的吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
CN114184671B (zh) * 2021-12-09 2024-02-06 中国石油大学(北京) 用于确定表面活性剂在岩石表面的吸附层数的方法
CN118525015A (zh) * 2021-12-21 2024-08-20 微境生物医药科技(上海)有限公司 作为fak抑制剂的化合物及其用途
WO2024092047A1 (en) * 2022-10-26 2024-05-02 Sorrento Therapeutics, Inc. Administration of pyrrolopyrimidine-based kinase inhibitors for treatment of psoriasis
CN117586235B (zh) * 2023-11-27 2025-08-22 广东省人民医院 增强线粒体自噬的嵌合分子及其应用

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974277A (en) 1974-09-06 1976-08-10 Diamond Shamrock Corporation 2-[2-(5-Nitro-2-furyl)vinyl]-4-(anilino)quinazolines as growth promotants and feed efficiency enhancing agents
SV2002000205A (es) 1999-11-01 2002-06-07 Lilly Co Eli Compuestos farmaceuticos ref. x-01095
JP4285996B2 (ja) 2001-02-21 2009-06-24 田辺三菱製薬株式会社 キナゾリン誘導体
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
WO2003026665A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
US7470533B2 (en) 2002-12-20 2008-12-30 Acea Biosciences Impedance based devices and methods for use in assays
CN100577811C (zh) 2002-07-20 2010-01-06 美国艾森生物科学公司 基于阻抗分析细胞和颗粒的装置和方法
US7560269B2 (en) 2002-12-20 2009-07-14 Acea Biosciences, Inc. Real time electronic cell sensing system and applications for cytotoxicity profiling and compound assays
US7732127B2 (en) 2002-12-20 2010-06-08 Acea Biosciences, Inc. Dynamic monitoring of cell adhesion and spreading using the RT-CES system
US7468255B2 (en) 2002-12-20 2008-12-23 Acea Biosciences Method for assaying for natural killer, cytotoxic T-lymphocyte and neutrophil-mediated killing of target cells using real-time microelectronic cell sensing technology
WO2004021979A2 (en) 2002-09-06 2004-03-18 Smithkline Beecham Corporation PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS
AU2003280799A1 (en) 2002-11-15 2004-06-15 Mitsubishi Pharma Corporation Medicinal composition
CA2550274A1 (en) 2003-11-12 2005-05-26 Acea Biosciences, Inc. Real time electronic cell sensing systems and applications for cell-based assays
JP5138938B2 (ja) 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Ｒｅｔ調節剤の開発のための化合物および方法
ES2389203T3 (es) 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Inhibidores de quinasa selectivos
AU2005218655A1 (en) 2004-03-02 2005-09-15 Neurogen Corporation Aryl substituted purine analogues
TW200616632A (en) 2004-06-17 2006-06-01 Plexxikon Inc Compounds modulating c-kit activity and uses therefor
CA2572331A1 (en) 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
KR101256846B1 (ko) 2005-09-21 2013-04-24 4에스체 악티엔게젤샤프트 Ｈｄａｃ의 억제제로서의 신규한 설포닐피롤
JP2009511527A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Ｓｙｋ阻害物質としてのピロロピリミジン誘導体
KR100832593B1 (ko) 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
GB0526246D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
US20100048898A1 (en) 2006-03-03 2010-02-25 Jacobsen Eric N Process for Synthesizing 7-Alkynyl-4- Aminoquinazolines and a Related Intermediate
US20100273776A1 (en) 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
US8314234B2 (en) 2006-09-25 2012-11-20 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
JP5208123B2 (ja) 2006-12-08 2013-06-12 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
CA2676138A1 (en) 2007-01-26 2008-08-07 Irm Llc Compounds and compositions as kinase inhibitors
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
TWI377944B (en) 2007-06-05 2012-12-01 Hanmi Holdings Co Ltd Novel amide derivative for inhibiting the growth of cancer cells
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
EP2188292B1 (en) 2007-08-08 2013-05-29 GlaxoSmithKline Intellectual Property Development Limited 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d]pyrimidin-4-yl) amino]benzamide derivatives as igf-1r inhibitors for the treatment of cancer
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
JP5600063B2 (ja) 2007-10-19 2014-10-01 セルジーン アビロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
BRPI0910668A2 (pt) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009262068C1 (en) * 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
WO2010045451A1 (en) 2008-10-16 2010-04-22 Glaxosmithkline Llc Pyrrolopyrimidine compounds
SG172857A1 (en) 2009-02-09 2011-08-29 Supergen Inc Pyrrolopyrimidinyl axl kinase inhibitors
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
US9966510B2 (en) * 2009-10-22 2018-05-08 Marcel Peter Gerard Maes Signaling system having improved contrast ration
WO2011079231A1 (en) * 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN102639936B (zh) 2009-12-28 2016-05-04 巴西石油公司 高性能燃烧设备和用于生产轻石蜡的流体催化裂化工艺
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
ES2622138T3 (es) * 2010-06-23 2017-07-05 Hanmi Science Co., Ltd. Nuevos derivados de pirimidina condensados para la inhibición de la actividad tirosina quinasa
JP5956999B2 (ja) * 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
BR112013010564B1 (pt) * 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
EP2637502B1 (en) * 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CN102583089B (zh) 2011-01-11 2015-11-25 山东新北洋信息技术股份有限公司 薄片类介质处理装置
KR20130131461A (ko) 2011-03-07 2013-12-03 폰다지오네 텔레톤 Tfeb 변종 및 그의 용도
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
AU2012250517B2 (en) * 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
DK2710007T3 (da) * 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
CA2861010A1 (en) 2012-01-13 2013-07-18 Xiao Xu Heterocyclic compounds and uses as anticancer agents
HRP20170311T1 (hr) 2012-08-06 2017-04-21 Acea Biosciences Inc. Novi spojevi pirolopirimidina kao inhibitori protein kinaza
BR112016000195A8 (pt) 2013-07-11 2019-12-31 Acea Biosciences Inc compostos heterocíclicos, composição farmacêutica, combinação, seu uso, e método para inibir uma atividade da tirosina quinase btk ou jak, egfr, alk, pdgfr, blk, bmx/etk, flt3(d835y), itk, tec, txk, e suas respectivas vias
CN104306348B (zh) 2014-09-30 2017-05-31 地奥集团成都药业股份有限公司 一种辛伐他汀片及其制备方法
EP3359159B1 (en) 2015-10-09 2023-06-07 ACEA Therapeutics, Inc. Pharmaceutical compositions of a pyrrolopyrimidine kinase inhibitor, and methods of making same
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11007197B2 (en) 2012-08-06 2021-05-18 ACEA Therapeutics, Inc. EGFR modulators and uses thereof

Also Published As

Publication number Publication date
CA2917364C (en) 2020-09-29
MX2016000261A (es) 2016-12-09
ES2761572T3 (es) 2020-05-20
US10562918B2 (en) 2020-02-18
EP3019496B1 (en) 2019-09-11
EP3019496A2 (en) 2016-05-18
KR102173433B1 (ko) 2020-11-04
CN112592334B (zh) 2023-10-27
HK1223351A1 (en) 2017-07-28
CN112592334A (zh) 2021-04-02
CN105916851A (zh) 2016-08-31
RU2677653C2 (ru) 2019-01-18
BR112016000195A8 (pt) 2019-12-31
CN117486865A (zh) 2024-02-02
KR20160037929A (ko) 2016-04-06
MX368491B (es) 2019-10-04
RU2016104388A3 (enExample) 2018-04-27
RU2016104388A (ru) 2017-08-16
JP2016528209A (ja) 2016-09-15
DK3019496T3 (da) 2019-12-09
CA2917364A1 (en) 2015-01-15
NZ715687A (en) 2019-04-26
AU2014287016A1 (en) 2016-02-04
WO2015006754A3 (en) 2015-03-12
AU2014287016B2 (en) 2018-11-01
US20180251475A1 (en) 2018-09-06
WO2015006754A2 (en) 2015-01-15
IL243420A0 (en) 2016-02-29
SG11201600062RA (en) 2016-02-26

Similar Documents

Publication Publication Date Title
US10562918B2 (en) Heterocyclic compounds and uses thereof
JP6353788B2 (ja) 抗がん剤としての複素環式化合物およびその使用
CN116528868B (zh) 三环kras g12c抑制剂
US9920074B2 (en) Heterocyclic compounds and uses thereof
JP6035423B2 (ja) 新規な縮合ピリミジン化合物又はその塩
KR20210044822A (ko) 피롤로피리미딘 itk 억제제
JP2011510010A (ja) ３Ｈ−［１，２，３］トリアゾロ［４，５−ｄ］ピリミジン化合物、ｍＴＯＲキナーゼおよびＰＩ３キナーゼ阻害剤としてのそれらの使用、ならびにそれらの合成
JP6431622B2 (ja) 結晶性ｆｇｆｒ４阻害剤化合物およびその使用
JP2017515848A (ja) タンパク質脱アセチル化酵素阻害剤およびタンパク質脱アセチル化酵素−タンパク質キナーゼ二重阻害剤としての複素環式ヒドロキサム酸ならびにその使用方法
JP2022529518A (ja) チロシンキナーゼの複素環式阻害剤
KR20230163335A (ko) 헤테로아릴 유도체 화합물 및 이의 용도
HK1223351B (en) Pyrimidine derivatives as kinase inhibitors
HK40048660A (en) Pyrimidine derivatives as kinase inhibitors
WO2024175998A1 (en) Benzenesulfonamide derivatives and uses thereof
HK40048660B (en) Pyrimidine derivatives as kinase inhibitors

Legal Events

Date Code Title Description
RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20160628

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20160629

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20160628

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170703

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170703

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180711

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180731

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181025

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190312

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190607

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190702

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190729

R150 Certificate of patent or registration of utility model

Ref document number: 6564771

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250