KR101811938B1 - FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체 - Google Patents

FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체 Download PDF

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KR101811938B1
KR101811938B1 KR1020157037254A KR20157037254A KR101811938B1 KR 101811938 B1 KR101811938 B1 KR 101811938B1 KR 1020157037254 A KR1020157037254 A KR 1020157037254A KR 20157037254 A KR20157037254 A KR 20157037254A KR 101811938 B1 KR101811938 B1 KR 101811938B1
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mmol
optionally substituted
grams
compound
pyrrolo
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KR20160007677A (ko
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뎅밍 샤오
량 쳉
시지에 리우
유안동 후
신허 수
지화 리우
리펑 장
웨이 우
수룽 왕
유 셴
젠 리
인 왕
셩 자오
충룽 리
지아 탕
홍하오 유
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켄타우루스 바이오파마 컴퍼니 리미티드
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • A61K31/495—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
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings

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  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020157037254A 2011-01-07 2012-01-07 FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체 Expired - Fee Related KR101811938B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201110002776.3 2011-01-07
CN201110002776.3A CN102093364B (zh) 2011-01-07 2011-01-07 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
US201161457217P 2011-02-02 2011-02-02
US61/457,217 2011-02-02
PCT/CN2012/070122 WO2012092880A1 (en) 2011-01-07 2012-01-07 2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE DERIVATIVES AS FAK/Pyk2 INHIBITORS

Related Parent Applications (1)

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KR1020137020933A Division KR20130122778A (ko) 2011-01-07 2012-01-07 FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체

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KR20160007677A KR20160007677A (ko) 2016-01-20
KR101811938B1 true KR101811938B1 (ko) 2017-12-22

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KR1020157037254A Expired - Fee Related KR101811938B1 (ko) 2011-01-07 2012-01-07 FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체
KR1020137020933A Ceased KR20130122778A (ko) 2011-01-07 2012-01-07 FAK/Pyk2 억제제인 2,4-디아미노-6,7-디히드로-5H-피롤로[2,3]피리미딘 유도체

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US (1) US9428508B2 (enExample)
EP (1) EP2661437B1 (enExample)
JP (1) JP5961628B2 (enExample)
KR (2) KR101811938B1 (enExample)
CN (1) CN102093364B (enExample)
AU (1) AU2012204982B2 (enExample)
CA (1) CA2823969C (enExample)
WO (1) WO2012092880A1 (enExample)

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CN102093364B (zh) * 2011-01-07 2015-01-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
CN103476776B (zh) * 2011-01-07 2016-09-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
CN108558842B (zh) * 2014-03-06 2021-06-04 山东轩竹医药科技有限公司 嘧啶衍生物类间变性淋巴瘤激酶抑制剂
CN107108586B (zh) * 2014-09-29 2020-07-10 山东轩竹医药科技有限公司 多环类间变性淋巴瘤激酶抑制剂
JP6975514B2 (ja) * 2016-07-08 2021-12-01 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 縮合ピリミジン誘導体
EP3484884B1 (en) 2016-07-14 2021-01-27 Hoffmann-La Roche AG Fused pyrimidine derivatives
US10633375B2 (en) 2016-08-31 2020-04-28 Jinagsu Hengrui Medicine Co., Ltd Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof
CN107936024B (zh) * 2016-10-12 2021-04-30 北京赛林泰医药技术有限公司 一种间变性淋巴瘤激酶抑制剂及其制备方法和用途
CN108276410B (zh) * 2017-01-06 2021-12-10 首药控股(北京)股份有限公司 一种间变性淋巴瘤激酶抑制剂及其制备方法和用途
CN108456210A (zh) * 2017-02-22 2018-08-28 北京赛林泰医药技术有限公司 一种alk酪氨酸激酶抑制剂的多晶型物及其制备方法
SI3612531T1 (sl) 2017-04-18 2022-11-30 Shanghai Fochon Pharmaceutical Co., Ltd. Sredstva, ki sprožajo apoptozo
KR101992621B1 (ko) * 2017-12-07 2019-09-27 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
CN110526915B (zh) * 2018-05-25 2022-02-01 首药控股(北京)股份有限公司 一种间变性淋巴瘤激酶抑制剂的制备方法
KR102377007B1 (ko) 2018-09-20 2022-03-22 한미약품 주식회사 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체
EP3842435A4 (en) * 2018-09-20 2022-05-11 Hanmi Pharm. Co., Ltd. NEW SULFONAMIDE DERIVATIVE PRESENTING A FUSED PYRIMIDINE SKELETON, HAVING AN INHIBITOR EFFECT OF EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION
CN113087709A (zh) * 2020-01-09 2021-07-09 沈阳药科大学 吡咯并嘧啶类衍生物及其制备方法和应用
MX2023013065A (es) * 2021-05-04 2024-01-03 Enalare Therapeutics Inc Moduladores de canales de potasio de gran conductancia, composiciones de estos, métodos para su fabricación y métodos para su uso.
CN115368364B (zh) * 2021-05-19 2024-07-16 四川大学 7H-吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途

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US20100160356A1 (en) 2006-04-07 2010-06-24 Timo Heinrich Novel cyclobutyl compounds as kinase inhibitors

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CN102093364B (zh) * 2011-01-07 2015-01-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物

Patent Citations (2)

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WO2005080393A1 (en) 2004-02-14 2005-09-01 Irm Llc Compounds and compositions as protein kinase inhibitors
US20100160356A1 (en) 2006-04-07 2010-06-24 Timo Heinrich Novel cyclobutyl compounds as kinase inhibitors

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AU2012204982A1 (en) 2012-07-12
WO2012092880A1 (en) 2012-07-12
KR20160007677A (ko) 2016-01-20
EP2661437A1 (en) 2013-11-13
JP5961628B2 (ja) 2016-08-02
US20130281438A1 (en) 2013-10-24
AU2012204982A8 (en) 2013-08-29
EP2661437B1 (en) 2018-11-07
CN102093364A (zh) 2011-06-15
CA2823969C (en) 2017-11-28
CA2823969A1 (en) 2012-07-12
CN102093364B (zh) 2015-01-28
EP2661437A4 (en) 2014-07-02
KR20130122778A (ko) 2013-11-08
JP2014501766A (ja) 2014-01-23
AU2012204982B2 (en) 2017-02-23
US9428508B2 (en) 2016-08-30

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