CN103068821B - 作为脯氨酰羟化酶抑制剂的4-氨基喹唑啉-2-基-1-吡唑-4-羧酸化合物 - Google Patents

作为脯氨酰羟化酶抑制剂的4-氨基喹唑啉-2-基-1-吡唑-4-羧酸化合物 Download PDF

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CN103068821B
CN103068821B CN201180039665.8A CN201180039665A CN103068821B CN 103068821 B CN103068821 B CN 103068821B CN 201180039665 A CN201180039665 A CN 201180039665A CN 103068821 B CN103068821 B CN 103068821B
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pyrazole
carboxylic acid
quinazolin
amino
fluoro
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CN103068821A (zh
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M.H.拉比诺维茨
M.D.罗森
K.T.塔兰蒂诺
H.文卡特桑
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Janssen Pharmaceutica NV
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D403/14—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 three or more hetero rings
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    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D417/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180039665.8A 2010-08-13 2011-08-12 作为脯氨酰羟化酶抑制剂的4-氨基喹唑啉-2-基-1-吡唑-4-羧酸化合物 Active CN103068821B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US37366410P 2010-08-13 2010-08-13
US61/373,664 2010-08-13
US61/373664 2010-08-13
PCT/US2011/047626 WO2012021830A1 (en) 2010-08-13 2011-08-12 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors

Publications (2)

Publication Number Publication Date
CN103068821A CN103068821A (zh) 2013-04-24
CN103068821B true CN103068821B (zh) 2015-02-25

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US (5) US8796263B2 (https=)
EP (1) EP2603502B1 (https=)
JP (1) JP5755741B2 (https=)
CN (1) CN103068821B (https=)
AU (1) AU2011289230B2 (https=)
WO (1) WO2012021830A1 (https=)

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US8916574B2 (en) 2009-09-28 2014-12-23 Qilu Pharmaceutical Co., Ltd. 4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors
AU2011289230B2 (en) * 2010-08-13 2014-09-04 Janssen Pharmaceutica Nv 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors
US9273034B2 (en) 2011-10-25 2016-03-01 Janssen Pharmaceutica Nv Meglumine salt formulations of 1-(5,6-dichloro-1H-benzo[D]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid
JP6506390B2 (ja) 2014-09-02 2019-04-24 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． キノリノン系化合物及びその薬物への使用
CA3006300C (en) * 2015-11-25 2024-02-27 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
EP4048261A4 (en) * 2019-10-25 2023-11-22 Merck Sharp & Dohme LLC N-(HETEROARYL)-QUINAZOLINE-2-AMINE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
WO2021216530A1 (en) 2020-04-20 2021-10-28 Akebia Therapeutics, Inc. Treatment of viral infections, of organ injury, and of related conditions using a hif prolyl hydroxylase inhibitor or a hif-alpha stabilizer
TW202206065A (zh) * 2020-04-29 2022-02-16 美商百愛及生物醫藥公司 用以治療老化相關病況之缺氧誘導因子脯胺醯羥化酶抑制劑
CN115943144B (zh) * 2020-08-14 2025-05-13 成都海博为药业有限公司 一种作为pak4激酶抑制剂的化合物及其制备方法和应用
CN114075175A (zh) * 2020-08-14 2022-02-22 成都海博为药业有限公司 一种作为pak4激酶抑制剂的化合物及其制备方法和应用
TWI896831B (zh) * 2020-12-31 2025-09-11 大陸商成都海博為藥業有限公司 一種作為ｐａｋ４激酶抑制劑的化合物及其製備方法和應用
WO2022150623A1 (en) 2021-01-08 2022-07-14 Akebia Therapeutics, Inc. Compounds and composition for the treatment of anemia
CN117999069A (zh) 2021-05-27 2024-05-07 凯克斯生物制药公司 柠檬酸铁的儿科调配物
US20240415878A1 (en) * 2021-10-13 2024-12-19 Board Of Regents, The University Of Texas System Compositions and Methods for Modulating Mitochondrial Function
US20230183356A1 (en) * 2021-12-14 2023-06-15 Brown University HIF-1a MODULATORS AND USES THEREOF
WO2026015819A1 (en) * 2024-07-12 2026-01-15 The General Hospital Corporation Trdmt1 inhibitors

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Publication number Publication date
US20180148435A9 (en) 2018-05-31
US20150197507A1 (en) 2015-07-16
US20170320859A1 (en) 2017-11-09
US10975062B2 (en) 2021-04-13
JP5755741B2 (ja) 2015-07-29
CN103068821A (zh) 2013-04-24
US9573940B2 (en) 2017-02-21
AU2011289230B2 (en) 2014-09-04
US20140309215A1 (en) 2014-10-16
WO2012021830A1 (en) 2012-02-16
US20200095234A1 (en) 2020-03-26
US10246442B2 (en) 2019-04-02
US20130143871A1 (en) 2013-06-06
EP2603502B1 (en) 2014-07-30
US9006251B2 (en) 2015-04-14
AU2011289230A1 (en) 2013-02-21
JP2013536194A (ja) 2013-09-19
EP2603502A1 (en) 2013-06-19
HK1184451A1 (en) 2014-01-24
US8796263B2 (en) 2014-08-05

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