CN102245597B - 用于抑制chk1的化合物 - Google Patents

用于抑制chk1的化合物 Download PDF

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Publication number
CN102245597B
CN102245597B CN200980150018.7A CN200980150018A CN102245597B CN 102245597 B CN102245597 B CN 102245597B CN 200980150018 A CN200980150018 A CN 200980150018A CN 102245597 B CN102245597 B CN 102245597B
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China
Prior art keywords
compound
pyrazine
pyrazol
chk1
salt
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CN200980150018.7A
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English (en)
Chinese (zh)
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CN102245597A (zh
Inventor
F·S·法鲁兹
R·C·霍尔库姆
R·卡萨尔
S·S·迈尔斯
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Eli Lilly and Co
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Eli Lilly and Co
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    • 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN200980150018.7A 2008-12-17 2009-12-10 用于抑制chk1的化合物 Active CN102245597B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13817608P 2008-12-17 2008-12-17
US61/138,176 2008-12-17
PCT/US2009/067437 WO2010077758A1 (en) 2008-12-17 2009-12-10 Compounds useful for inhibiting chk1

Publications (2)

Publication Number Publication Date
CN102245597A CN102245597A (zh) 2011-11-16
CN102245597B true CN102245597B (zh) 2014-04-16

Family

ID=42079067

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980150018.7A Active CN102245597B (zh) 2008-12-17 2009-12-10 用于抑制chk1的化合物

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EP (1) EP2379532B1 (enExample)
JP (1) JP5705743B2 (enExample)
KR (1) KR101301777B1 (enExample)
CN (1) CN102245597B (enExample)
AR (1) AR074471A1 (enExample)
AU (1) AU2009333433B2 (enExample)
BR (1) BRPI0922468A2 (enExample)
CA (1) CA2746423C (enExample)
CL (1) CL2011001463A1 (enExample)
CO (1) CO6382122A2 (enExample)
CR (1) CR20110339A (enExample)
CY (1) CY1113930T1 (enExample)
DK (1) DK2379532T3 (enExample)
DO (1) DOP2011000185A (enExample)
EA (1) EA018118B1 (enExample)
EC (1) ECSP11011136A (enExample)
ES (1) ES2401558T3 (enExample)
HN (1) HN2011001446A (enExample)
HR (1) HRP20130167T1 (enExample)
IL (1) IL213160A (enExample)
JO (1) JO2886B1 (enExample)
MA (1) MA32901B1 (enExample)
MX (1) MX2011006603A (enExample)
MY (1) MY156998A (enExample)
NZ (1) NZ593440A (enExample)
PA (1) PA8850801A1 (enExample)
PE (1) PE20120077A1 (enExample)
PL (1) PL2379532T3 (enExample)
PT (1) PT2379532E (enExample)
RS (1) RS52739B (enExample)
SG (1) SG172222A1 (enExample)
SI (1) SI2379532T1 (enExample)
TN (1) TN2011000298A1 (enExample)
TW (1) TWI436996B (enExample)
UA (1) UA101998C2 (enExample)
WO (1) WO2010077758A1 (enExample)
ZA (1) ZA201103946B (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8314108B2 (en) * 2008-12-17 2012-11-20 Eli Lilly And Company 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile, pharmaceutically acceptable salts thereof, or solvate of salts
JO3145B1 (ar) * 2010-11-08 2017-09-20 Lilly Co Eli مركبات مفيدة لتثبيط chk1
GB201402277D0 (en) * 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
TWI725041B (zh) * 2015-07-23 2021-04-21 美商美國禮來大藥廠 用於治療神經母細胞瘤及/或軟組織肉瘤之chk1/2抑制劑
TWI627168B (zh) * 2015-12-07 2018-06-21 美國禮來大藥廠 (s)-乳酸鹽
SG11201803903YA (en) * 2015-12-15 2018-06-28 Lilly Co Eli Combination therapy for cancer
WO2017132928A1 (en) * 2016-02-04 2017-08-10 Pharmaengine, Inc. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications
AU2018243667A1 (en) 2017-03-31 2019-10-17 Seagen Inc. Combinations of Chk1- and Wee1 - inhibitors
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CN112457306A (zh) 2019-09-06 2021-03-09 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用
US11634424B2 (en) 2019-11-29 2023-04-25 Medshine Discovery Inc. Diazaindole derivative and use thereof as CHK1 inhibitor
WO2021119236A1 (en) 2019-12-10 2021-06-17 Seagen Inc. Preparation of a chk1 inhibitor compound
US11564920B2 (en) 2020-11-30 2023-01-31 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
AU2021389190A1 (en) 2020-11-30 2023-06-29 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1h-pyrazol-3-amine derivative
KR20240021188A (ko) * 2021-05-27 2024-02-16 바운드리스 바이오, 인크. 체크포인트 키나제 1(chk1) 억제제 및 그의 용도
GB202107932D0 (en) 2021-06-03 2021-07-21 Sentinel Oncology Ltd Preparation of a CHK1 Inhibitor Compound
GB202107924D0 (en) 2021-06-03 2021-07-21 Sentinel Oncology Ltd A pharmaceutical salt
MX2024007910A (es) 2021-12-24 2024-09-04 Sumitomo Pharma Co Ltd Derivado de 1h-pirazol-3-amina que tiene una estructura principal bicíclica.
EP4534100A1 (en) * 2022-05-27 2025-04-09 Sumitomo Pharma Co., Ltd. Therapeutic for cancer refractory to immune checkpoint inhibitor
JP7546104B2 (ja) * 2022-05-27 2024-09-05 住友ファーマ株式会社 5-ヘテロアリール-1h-ピラゾール-3-アミン誘導体からなる医薬
GB202213792D0 (en) 2022-09-21 2022-11-02 Benevolentai Bio Ltd New compounds and method
GB202403910D0 (en) 2024-03-19 2024-05-01 Benovental Cambridge Ltd New processes and intermediates for pharmaceutical products

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014876A1 (en) * 2002-08-13 2004-02-19 Abbott Laboratories Urea derivatives as kinase inhibitors
WO2005009435A1 (en) * 2003-07-25 2005-02-03 Pfizer Inc. Aminopyrazole compounds and use as chk1 inhibitors
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090270418A1 (en) * 2008-01-09 2009-10-29 Marianne Sloss Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004014876A1 (en) * 2002-08-13 2004-02-19 Abbott Laboratories Urea derivatives as kinase inhibitors
WO2005009435A1 (en) * 2003-07-25 2005-02-03 Pfizer Inc. Aminopyrazole compounds and use as chk1 inhibitors
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer

Also Published As

Publication number Publication date
PE20120077A1 (es) 2012-02-06
NZ593440A (en) 2013-02-22
TN2011000298A1 (en) 2012-12-17
MY156998A (en) 2016-04-15
HRP20130167T1 (hr) 2013-03-31
ZA201103946B (en) 2012-10-31
CN102245597A (zh) 2011-11-16
CA2746423A1 (en) 2010-07-08
EP2379532B1 (en) 2013-02-20
JP2012512249A (ja) 2012-05-31
PL2379532T3 (pl) 2013-07-31
CR20110339A (es) 2011-09-14
MA32901B1 (fr) 2011-12-01
CY1113930T1 (el) 2016-07-27
ECSP11011136A (es) 2011-07-29
AU2009333433A1 (en) 2011-06-30
EA018118B1 (ru) 2013-05-30
RS52739B (sr) 2013-08-30
SG172222A1 (en) 2011-07-28
PT2379532E (pt) 2013-03-25
CL2011001463A1 (es) 2012-01-20
UA101998C2 (ru) 2013-05-27
IL213160A (en) 2013-12-31
TWI436996B (zh) 2014-05-11
TW201029994A (en) 2010-08-16
BRPI0922468A2 (pt) 2020-08-04
AR074471A1 (es) 2011-01-19
KR20110084539A (ko) 2011-07-25
PA8850801A1 (es) 2010-07-27
IL213160A0 (en) 2011-07-31
EA201170834A1 (ru) 2011-12-30
WO2010077758A1 (en) 2010-07-08
ES2401558T3 (es) 2013-04-22
EP2379532A1 (en) 2011-10-26
CA2746423C (en) 2014-01-14
HN2011001446A (es) 2013-08-05
KR101301777B1 (ko) 2013-08-30
DK2379532T3 (da) 2013-03-18
SI2379532T1 (sl) 2013-05-31
DOP2011000185A (es) 2017-12-15
AU2009333433B2 (en) 2012-06-14
HK1160110A1 (en) 2012-08-10
CO6382122A2 (es) 2012-02-15
JP5705743B2 (ja) 2015-04-22
MX2011006603A (es) 2011-09-27
JO2886B1 (en) 2015-03-15

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