CA2917364C - Heterocyclic compounds and uses thereof - Google Patents

Heterocyclic compounds and uses thereof Download PDF

Info

Publication number
CA2917364C
CA2917364C CA2917364A CA2917364A CA2917364C CA 2917364 C CA2917364 C CA 2917364C CA 2917364 A CA2917364 A CA 2917364A CA 2917364 A CA2917364 A CA 2917364A CA 2917364 C CA2917364 C CA 2917364C
Authority
CA
Canada
Prior art keywords
alkyl
compound
optionally substituted
substituted
cyclic ring
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
CA2917364A
Other languages
English (en)
French (fr)
Other versions
CA2917364A1 (en
Inventor
Xiao Xu
Xiaobo Wang
Long Mao
Li Zhao
Biao Xi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Acea Biosciences Inc
Original Assignee
Acea Biosciences Inc
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 Acea Biosciences Inc filed Critical Acea Biosciences Inc
Publication of CA2917364A1 publication Critical patent/CA2917364A1/en
Application granted granted Critical
Publication of CA2917364C publication Critical patent/CA2917364C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • C07D239/49Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two 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
    • C07D239/553Two 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2917364A 2013-07-11 2014-07-11 Heterocyclic compounds and uses thereof Active CA2917364C (en)

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 (2)

Publication Number Publication Date
CA2917364A1 CA2917364A1 (en) 2015-01-15
CA2917364C true CA2917364C (en) 2020-09-29

Family

ID=51298956

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2917364A Active CA2917364C (en) 2013-07-11 2014-07-11 Heterocyclic compounds and uses thereof

Country Status (16)

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

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
CA2861010A1 (en) 2012-01-13 2013-07-18 Xiao Xu Heterocyclic compounds and uses as anticancer agents
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
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
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
NZ715687A (en) 2013-07-11 2019-04-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
AU2014308616B2 (en) 2013-08-23 2018-12-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN117069700B (zh) * 2014-10-11 2026-01-30 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2015371251B2 (en) 2014-12-23 2020-06-11 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
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
HK1246645A1 (zh) * 2015-03-27 2018-09-14 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
CN108137559B (zh) * 2015-07-09 2021-11-02 默克专利有限公司 用作btk抑制剂的嘧啶衍生物及其用途
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
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
CN108137544B (zh) * 2015-12-10 2022-01-04 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
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Bmpシグナル阻害化合物
WO2018139883A1 (ko) * 2017-01-26 2018-08-02 부광약품 주식회사 다중 표적 키나아제 저해제로서 융합피리미딘 유도체
CN110072865B (zh) * 2017-02-08 2022-02-11 中国医药研究开发中心有限公司 吡咯并芳杂环类化合物及其制备方法和医药用途
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
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
JP7675647B2 (ja) * 2018-08-09 2025-05-13 エイシア セラピューティクス, インコーポレイテッド (s)-n-(3-((2-((4-((1-アセチルピロリジン-3-イル)(メチル)アミノ)フェニル)アミノ)-5-メトキシピリミジン-4-イル)オキシ)フェニル)アクリルアミドの製造のためのプロセスおよびその製剤
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
JP7660063B2 (ja) 2018-12-28 2025-04-10 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼ7のインヒビターおよびそれらの使用
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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020385513A1 (en) * 2019-11-22 2022-07-14 Medshine Discovery Inc. Pyrimidopyrrole spiro compounds and derivatives thereof as DNA-PK inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 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
WO2021146424A1 (en) 2020-01-15 2021-07-22 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
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
CA3238851A1 (en) * 2021-12-21 2023-06-29 Yuli Xie Compound as fak inhibitor and use thereof
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
EP1230225A2 (en) 1999-11-01 2002-08-14 Eli Lilly And Company Pharmaceutically active 4-substituted pyrimidine derivatives
EP1369418B1 (en) 2001-02-21 2010-07-28 Mitsubishi Tanabe Pharma Corporation Quinazoline derivatives
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
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
US7192752B2 (en) 2002-12-20 2007-03-20 Acea Biosciences Real time electronic cell sensing systems and applications for cell-based assays
US7732127B2 (en) 2002-12-20 2010-06-08 Acea Biosciences, Inc. Dynamic monitoring of cell adhesion and spreading using the RT-CES system
US7470533B2 (en) 2002-12-20 2008-12-30 Acea Biosciences Impedance based devices and methods for use in assays
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
WO2004010102A2 (en) 2002-07-20 2004-01-29 Acea Biosciences, Inc. Impedance based apparatuses and methods for analyzing cells and particles
AU2003265636A1 (en) 2002-09-06 2004-03-29 Smithkline Beecham Corporation Pyrrolo(2, 3-d)pyrimidine-4-yl and purin-6-yl urea compounds
TW200416034A (en) 2002-11-15 2004-09-01 Mitsubishi Pharma Corp Medicinal composition
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
NZ546058A (en) 2004-01-12 2010-09-30 Ym Biosciences Australia Pty Benzimidazole and other fused ring derivatives as selective janus kinase inhibitors
JP2007526339A (ja) 2004-03-02 2007-09-13 ニューロジェン・コーポレーション アリール置換プリン類縁体
CA2570817A1 (en) 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
CA2572331A1 (en) 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
BRPI0617167B8 (pt) 2005-09-21 2021-05-25 Nycomed Gmbh sulfonilpirróis como inibidores de hdac's, seu uso, composição farmacêutica e combinação
WO2007042298A1 (en) 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
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
CA2644494A1 (en) 2006-03-03 2007-09-13 Aveo Pharmaceuticals, Inc. Processes for synthesizing 7-alkynyl-4-aminoquinazolines and a related intermediate
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
WO2008039359A2 (en) 2006-09-25 2008-04-03 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
BRPI0720264B1 (pt) 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
CN101622001A (zh) 2007-01-26 2010-01-06 Irm责任有限公司 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物
US8846704B2 (en) 2007-01-31 2014-09-30 YM Biosciences Austraila 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
US7981903B2 (en) 2007-08-08 2011-07-19 Glaxosmithkline Llc 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
CN105367503A (zh) 2007-10-19 2016-03-02 阿维拉制药公司 杂芳基化合物和其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TWI546290B (zh) * 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
WO2010045451A1 (en) 2008-10-16 2010-04-22 Glaxosmithkline Llc Pyrrolopyrimidine compounds
US20100204221A1 (en) 2009-02-09 2010-08-12 Hariprasad Vankayalapati Pyrrolopyrimidinyl axl kinase inhibitors
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
WO2011047739A1 (en) * 2009-10-22 2011-04-28 Marcel Peter Gerard Maes Signaling system having improved contrast ratio
US20110207736A1 (en) * 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, 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
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
PT2585470T (pt) * 2010-06-23 2017-03-06 Hanmi Science Co Ltd Novos derivados fundidos de pirimidina para inibição da actividade da tirosina cinase
EP2635285B1 (en) * 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
MX382354B (es) * 2010-11-01 2025-03-13 Celgene Car Llc Compuestos heterocíclicos y usos de los mismos.
JP5957003B2 (ja) * 2010-11-10 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 変異体選択的egfr阻害剤およびその使用
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
JP2014511391A (ja) 2011-03-07 2014-05-15 フォンダッツィオーネ・テレソン Tfebリン酸化阻害剤およびその使用
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
US9834518B2 (en) * 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
CA2836449C (en) * 2011-05-17 2021-04-27 The Regents Of The University Of California Kinase inhibitors
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
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
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
BR112015002709B1 (pt) * 2012-08-06 2022-09-20 Acea Biosciences Inc Compostos, composição farmacêutica, uso dos mesmos e uso de uma combinação de composto ou composição farmacêutica e um segundo agente profilático ou agente terapêutico
NZ715687A (en) 2013-07-11 2019-04-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
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
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
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

Also Published As

Publication number Publication date
DK3019496T3 (da) 2019-12-09
HK1223351A1 (en) 2017-07-28
CN105916851A (zh) 2016-08-31
RU2016104388A3 (https=) 2018-04-27
RU2016104388A (ru) 2017-08-16
IL243420A0 (en) 2016-02-29
KR20160037929A (ko) 2016-04-06
CN117486865A (zh) 2024-02-02
EP3019496A2 (en) 2016-05-18
MX368491B (es) 2019-10-04
MX2016000261A (es) 2016-12-09
ES2761572T3 (es) 2020-05-20
CA2917364A1 (en) 2015-01-15
KR102173433B1 (ko) 2020-11-04
EP3019496B1 (en) 2019-09-11
US10562918B2 (en) 2020-02-18
NZ715687A (en) 2019-04-26
JP6564771B2 (ja) 2019-08-21
JP2016528209A (ja) 2016-09-15
SG11201600062RA (en) 2016-02-26
AU2014287016A1 (en) 2016-02-04
WO2015006754A2 (en) 2015-01-15
AU2014287016B2 (en) 2018-11-01
CN112592334B (zh) 2023-10-27
WO2015006754A3 (en) 2015-03-12
BR112016000195A8 (pt) 2019-12-31
US20180251475A1 (en) 2018-09-06
RU2677653C2 (ru) 2019-01-18
CN112592334A (zh) 2021-04-02

Similar Documents

Publication Publication Date Title
CA2917364C (en) Heterocyclic compounds and uses thereof
US9920074B2 (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
US9938264B2 (en) Proteolysis targeting chimera compounds and methods of preparing and using same
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
CN106456580A (zh) 作为蛋白质脱乙酰酶抑制剂和蛋白质脱乙酰酶‑蛋白质激酶双重抑制剂的杂环异羟肟酸及其使用方法
CN101184758A (zh) 新的化合物
CN108368060B (zh) 一类嘧啶类衍生物激酶抑制剂
CN107428762B (zh) 酞嗪酮衍生物、其制备方法及用途
HK1223351B (en) Pyrimidine derivatives as kinase inhibitors
CA3225475A1 (en) Heterocyclic compounds and uses thereof
HK1229722A1 (en) Heterocyclic hydroxamic acids as protein deacetylase inhibitors and dual protein deacetylase-protein kinase inhibitors and methods of use thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180622

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 10TH ANNIV.) - STANDARD

Year of fee payment: 10

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241231

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241231

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20241231

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-4-4-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20251210

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-4-4-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20251211

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 11TH ANNIV.) - STANDARD

Year of fee payment: 11

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20260106

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20260106

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-4-4-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20260326