CN102695510A - 囊性纤维化跨膜传导调节蛋白的嘧啶并-吡咯并-喹喔啉二酮抑制剂及其用途 - Google Patents

囊性纤维化跨膜传导调节蛋白的嘧啶并-吡咯并-喹喔啉二酮抑制剂及其用途 Download PDF

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Publication number
CN102695510A
CN102695510A CN2010800427350A CN201080042735A CN102695510A CN 102695510 A CN102695510 A CN 102695510A CN 2010800427350 A CN2010800427350 A CN 2010800427350A CN 201080042735 A CN201080042735 A CN 201080042735A CN 102695510 A CN102695510 A CN 102695510A
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China
Prior art keywords
pyrimido
dione
quinoxaline
dihydro
dimethyl
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Pending
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CN2010800427350A
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English (en)
Chinese (zh)
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艾伦·S·韦克曼
鲁克曼尼·特拉特兰迪普
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University of California San Diego UCSD
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University of California San Diego UCSD
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Publication of CN102695510A publication Critical patent/CN102695510A/zh
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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • 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
    • 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
    • A61P1/12Antidiarrhoeals
    • 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
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2010800427350A 2009-08-10 2010-08-10 囊性纤维化跨膜传导调节蛋白的嘧啶并-吡咯并-喹喔啉二酮抑制剂及其用途 Pending CN102695510A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23274109P 2009-08-10 2009-08-10
US61/232,741 2009-08-10
PCT/US2010/045052 WO2011019737A1 (en) 2009-08-10 2010-08-10 Pyrimido-pyrrolo-quinoxalinedione inhibitors of cystic fibrosis transmembrane conductance regulator protein and uses therefor

Publications (1)

Publication Number Publication Date
CN102695510A true CN102695510A (zh) 2012-09-26

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CN2010800427350A Pending CN102695510A (zh) 2009-08-10 2010-08-10 囊性纤维化跨膜传导调节蛋白的嘧啶并-吡咯并-喹喔啉二酮抑制剂及其用途

Country Status (6)

Country Link
US (1) US8609661B2 (https=)
EP (1) EP2464354B1 (https=)
CN (1) CN102695510A (https=)
CA (1) CA2769847C (https=)
IN (1) IN2012DN00719A (https=)
WO (1) WO2011019737A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105008370A (zh) * 2012-12-19 2015-10-28 诺华股份有限公司 作为cftr抑制剂的三环化合物
CN105143230A (zh) * 2012-12-19 2015-12-09 诺华股份有限公司 用于抑制cftr通道的三环化合物
CN113727711A (zh) * 2019-04-24 2021-11-30 加拉帕戈斯股份有限公司 用于治疗肾脏疾病的新化合物及其药物组合物
CN115998763A (zh) * 2023-01-17 2023-04-25 暨南大学 氯离子及靶向氯离子通道的化合物在调控铁死亡中的应用

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012166658A1 (en) * 2011-05-27 2012-12-06 The Regents Of The University Of California Pyrimido-pyrrolo-oxazine-dione compound inhibitors of the cystic fibrosis transmembrane conductance regulator protein and uses therefor
CN114948966B (zh) * 2022-04-27 2023-06-20 南京鼓楼医院 一种小分子抑制剂在制备治疗多发性硬化和脓毒症的药物中的应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998005642A1 (fr) * 1996-08-01 1998-02-12 Centre National De La Recherche Scientifique Composes activateurs du canal cftr, et compositions pharmaceutiques les contenant
CN1246119A (zh) * 1996-12-21 2000-03-01 英国阿斯特拉药品有限公司 吡咯并[3,4-d]-嘧啶酮衍生物及其作为药物的用途
WO2004111014A1 (en) * 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
WO2005039589A2 (fr) * 2003-10-23 2005-05-06 Universite Joseph Fourier Modulateurs des canaux cftr
US20060160815A1 (en) * 2004-12-20 2006-07-20 Wyeth Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents
US20080269206A1 (en) * 2007-04-02 2008-10-30 Institute For Oneworld Health Cftr inhibitor compounds and uses thereof
WO2009076593A1 (en) * 2007-12-13 2009-06-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7235573B2 (en) 2002-09-30 2007-06-26 The Regents Of The University Of California Methods of treating secretory diarrhea using cystic fibrosis transmembrane conductance regulator protein inhibitors
EP1740532A4 (en) 2004-03-30 2009-06-10 Univ California CFTR INHIBITOR COMPOUNDS CONTAINING HYDRAZIDS AND USES THEREOF
AU2009228307A1 (en) 2008-03-25 2009-10-01 The Regents Of The University Of California Water soluble small molecule inhibitors of the cystic fibrosis transmembrane conductance regulator
WO2009146144A2 (en) 2008-04-04 2009-12-03 The Regents Of The University Of California Divalent hydrazide compound conjugates for inhibiting cystic fibrosis transmembrane conductance regulator
WO2012166658A1 (en) 2011-05-27 2012-12-06 The Regents Of The University Of California Pyrimido-pyrrolo-oxazine-dione compound inhibitors of the cystic fibrosis transmembrane conductance regulator protein and uses therefor

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998005642A1 (fr) * 1996-08-01 1998-02-12 Centre National De La Recherche Scientifique Composes activateurs du canal cftr, et compositions pharmaceutiques les contenant
CN1246119A (zh) * 1996-12-21 2000-03-01 英国阿斯特拉药品有限公司 吡咯并[3,4-d]-嘧啶酮衍生物及其作为药物的用途
WO2004111014A1 (en) * 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
WO2005039589A2 (fr) * 2003-10-23 2005-05-06 Universite Joseph Fourier Modulateurs des canaux cftr
US20060160815A1 (en) * 2004-12-20 2006-07-20 Wyeth Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents
US20080269206A1 (en) * 2007-04-02 2008-10-30 Institute For Oneworld Health Cftr inhibitor compounds and uses thereof
WO2009076593A1 (en) * 2007-12-13 2009-06-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105008370A (zh) * 2012-12-19 2015-10-28 诺华股份有限公司 作为cftr抑制剂的三环化合物
CN105143230A (zh) * 2012-12-19 2015-12-09 诺华股份有限公司 用于抑制cftr通道的三环化合物
CN105143230B (zh) * 2012-12-19 2017-06-09 诺华股份有限公司 用于抑制cftr通道的三环化合物
CN105008370B (zh) * 2012-12-19 2017-06-09 诺华股份有限公司 作为cftr抑制剂的三环化合物
CN113727711A (zh) * 2019-04-24 2021-11-30 加拉帕戈斯股份有限公司 用于治疗肾脏疾病的新化合物及其药物组合物
CN115998763A (zh) * 2023-01-17 2023-04-25 暨南大学 氯离子及靶向氯离子通道的化合物在调控铁死亡中的应用

Also Published As

Publication number Publication date
IN2012DN00719A (https=) 2015-06-19
CA2769847C (en) 2019-01-08
US20120208822A1 (en) 2012-08-16
WO2011019737A1 (en) 2011-02-17
EP2464354B1 (en) 2015-04-01
EP2464354A4 (en) 2013-03-27
US8609661B2 (en) 2013-12-17
EP2464354A1 (en) 2012-06-20
CA2769847A1 (en) 2011-02-17

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Application publication date: 20120926