AU2012204982B2 - 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as FAK/Pyk2 inhibitors - Google Patents

2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as FAK/Pyk2 inhibitors Download PDF

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Publication number
AU2012204982B2
AU2012204982B2 AU2012204982A AU2012204982A AU2012204982B2 AU 2012204982 B2 AU2012204982 B2 AU 2012204982B2 AU 2012204982 A AU2012204982 A AU 2012204982A AU 2012204982 A AU2012204982 A AU 2012204982A AU 2012204982 B2 AU2012204982 B2 AU 2012204982B2
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mmol
additional embodiments
dihydro
compound
optionally substituted
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AU2012204982A8 (en
AU2012204982A1 (en
Inventor
Liang Cheng
Yuandong Hu
Chonglong LI
Gen LI
Xijie Liu
Zhihua Liu
Yu Shen
Jia Tang
Shulong Wang
Yin Wang
Wei Wu
Dengming Xiao
Xinhe XU
Honghao YU
Lipeng ZHANG
Sheng Zhao
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Centaurus Biopharma Co Ltd
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Centaurus Biopharma Co Ltd
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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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/12—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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2012204982A 2011-01-07 2012-01-07 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as FAK/Pyk2 inhibitors Ceased AU2012204982B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
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
CN201110002776.3 2011-01-07
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

Publications (3)

Publication Number Publication Date
AU2012204982A1 AU2012204982A1 (en) 2012-07-12
AU2012204982A8 AU2012204982A8 (en) 2013-08-29
AU2012204982B2 true AU2012204982B2 (en) 2017-02-23

Family

ID=44126650

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AU2012204982A Ceased AU2012204982B2 (en) 2011-01-07 2012-01-07 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as FAK/Pyk2 inhibitors

Country Status (8)

Country Link
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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* Cited by examiner, † Cited by third party
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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
US10011592B2 (en) * 2014-09-29 2018-07-03 Xuanzhu Pharma Co., Ltd. Polycyclic inhibitor of anaplastic lymphoma kinase
EP3481829B1 (en) * 2016-07-08 2021-04-07 H. Hoffnabb-La Roche Ag Fused pyrimidine derivatives
EP3484884B1 (en) 2016-07-14 2021-01-27 Hoffmann-La Roche AG Fused pyrimidine derivatives
CA3031592A1 (en) 2016-08-31 2018-03-08 Jiangsu 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
MX391501B (es) 2017-04-18 2025-03-21 Fochon Pharmaceuticals Ltd Agentes inductores de apoptosis
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
WO2020060268A1 (ko) * 2018-09-20 2020-03-26 한미약품 주식회사 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체
KR102377007B1 (ko) 2018-09-20 2022-03-22 한미약품 주식회사 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체
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
US20240067668A1 (en) * 2020-12-29 2024-02-29 Voronoi Inc. Heteroaryl derivative compound and use thereof
JP2024516730A (ja) * 2021-05-04 2024-04-16 エナラーレ セラピューティクス インコーポレイテッド 大導電性カリウムチャネル調節剤、その組成物、その製造方法、及びその使用方法
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
WO2026086879A1 (zh) * 2024-10-25 2026-04-30 应世生物科技(南京)有限公司 Fak抑制剂

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WO2003000695A1 (en) * 2001-06-23 2003-01-03 Aventis Pharmaceuticals Inc Pyrrolopyrimidines as protein kinase inhibitors
WO2004043367A2 (en) * 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Fused heterocyclic compounds and use thereof
WO2005080393A1 (en) * 2004-02-14 2005-09-01 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2007140222A2 (en) * 2006-05-26 2007-12-06 Novartis Ag Pyrrolopyrimidine compounds and their uses
WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US20100160356A1 (en) * 2006-04-07 2010-06-24 Timo Heinrich Novel cyclobutyl compounds as kinase inhibitors

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JPH0782174A (ja) 1993-09-17 1995-03-28 Takeda Chem Ind Ltd 抗腫瘍剤
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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003000695A1 (en) * 2001-06-23 2003-01-03 Aventis Pharmaceuticals Inc Pyrrolopyrimidines as protein kinase inhibitors
WO2004043367A2 (en) * 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Fused heterocyclic compounds and use thereof
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
WO2007140222A2 (en) * 2006-05-26 2007-12-06 Novartis Ag Pyrrolopyrimidine compounds and their uses
WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases

Also Published As

Publication number Publication date
US20130281438A1 (en) 2013-10-24
AU2012204982A8 (en) 2013-08-29
EP2661437A4 (en) 2014-07-02
CN102093364A (zh) 2011-06-15
AU2012204982A1 (en) 2012-07-12
CN102093364B (zh) 2015-01-28
US9428508B2 (en) 2016-08-30
EP2661437B1 (en) 2018-11-07
CA2823969A1 (en) 2012-07-12
KR20130122778A (ko) 2013-11-08
KR101811938B1 (ko) 2017-12-22
EP2661437A1 (en) 2013-11-13
KR20160007677A (ko) 2016-01-20
JP5961628B2 (ja) 2016-08-02
JP2014501766A (ja) 2014-01-23
CA2823969C (en) 2017-11-28
WO2012092880A1 (en) 2012-07-12

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