CN105143230B - 用于抑制cftr通道的三环化合物 - Google Patents

用于抑制cftr通道的三环化合物 Download PDF

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Publication number
CN105143230B
CN105143230B CN201380073218.3A CN201380073218A CN105143230B CN 105143230 B CN105143230 B CN 105143230B CN 201380073218 A CN201380073218 A CN 201380073218A CN 105143230 B CN105143230 B CN 105143230B
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dimethyl
bases
diketone
alkyl
pyrrolo
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CN105143230A (zh
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M·艾哈迈德
A·阿什尔-凯利
L·古尔特兹
J·麦肯纳
S·姆顿
R·帕尔马
J·谢坡德
P·赖特
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—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
    • A61K31/495—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
    • A61K31/54—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
    • A61K31/542—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 ortho- or peri-condensed with 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • C07D487/22—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 four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380073218.3A 2012-12-19 2013-12-17 用于抑制cftr通道的三环化合物 Expired - Fee Related CN105143230B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261739335P 2012-12-19 2012-12-19
US61/739,335 2012-12-19
US201361906141P 2013-11-19 2013-11-19
US61/906,141 2013-11-19
PCT/IB2013/061043 WO2014097148A1 (en) 2012-12-19 2013-12-17 Tricyclic compounds for inhibiting the cftr channel

Publications (2)

Publication Number Publication Date
CN105143230A CN105143230A (zh) 2015-12-09
CN105143230B true CN105143230B (zh) 2017-06-09

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CN201380073218.3A Expired - Fee Related CN105143230B (zh) 2012-12-19 2013-12-17 用于抑制cftr通道的三环化合物

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US (2) US20140171417A1 (https=)
EP (1) EP2935278B1 (https=)
JP (1) JP6284546B2 (https=)
KR (1) KR20150097660A (https=)
CN (1) CN105143230B (https=)
AP (1) AP2015008539A0 (https=)
AR (1) AR094122A1 (https=)
AU (1) AU2013365739A1 (https=)
BR (1) BR112015014292A2 (https=)
CA (1) CA2895660A1 (https=)
CL (1) CL2015001730A1 (https=)
CR (1) CR20150325A (https=)
CU (1) CU20150066A7 (https=)
EA (1) EA201591177A1 (https=)
ES (1) ES2628369T3 (https=)
HK (1) HK1209741A1 (https=)
IL (1) IL239389A0 (https=)
MX (1) MX2015007939A (https=)
PE (1) PE20151055A1 (https=)
PH (1) PH12015501386A1 (https=)
SG (1) SG11201504594QA (https=)
TN (1) TN2015000279A1 (https=)
TW (1) TW201429974A (https=)
UY (1) UY35211A (https=)
WO (1) WO2014097148A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9056867B2 (en) 2011-09-16 2015-06-16 Novartis Ag N-substituted heterocyclyl carboxamides
AU2013365827A1 (en) 2012-12-19 2015-07-09 Novartis Ag Tricyclic compounds as CFTR inhibitors
EA201591177A1 (ru) 2012-12-19 2015-11-30 Новартис Аг Трициклические соединения для ингибирования канала cftr
TWI686429B (zh) 2014-09-19 2020-03-01 美商摩曼帝夫特性材料公司 用於經控制之矽氧烷交聯的鉑(ii)二烯錯合物
HUE054399T2 (hu) * 2015-04-23 2021-09-28 Trevi Therapeutics Inc Vegyületek viszketéses állapotok kezelésére
CN106478558B (zh) * 2016-10-17 2019-03-29 天津雅奥科技发展有限公司 一种4-羟甲基-二氢-呋喃-2(3h)-酮的合成方法
US12319686B2 (en) 2019-01-17 2025-06-03 Hoffmann-La Roche Inc. Process for the preparation of tetrahydropyridopyrimidines
BR112021025048A2 (pt) * 2019-06-12 2022-02-01 Univ California Métodos de tratamento de diarreia por ácido biliar
EP4329815A1 (en) 2021-04-29 2024-03-06 Novartis AG Deubiquitinase-targeting chimeras and related methods
CN117654560B (zh) * 2023-12-01 2024-06-04 安徽泽升科技股份有限公司 一种通过氧化氨基连续化制备硝基化合物的方法

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WO2009042270A2 (en) * 2007-07-05 2009-04-02 Trustees Of Boston University Reca inhibitors and their uses as microbial inhibitors or potentiators of antibiotic activity
CN102695510A (zh) * 2009-08-10 2012-09-26 加利福尼亚大学董事会 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
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

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EP1207161B1 (en) 1999-08-25 2006-01-18 Banyu Pharmaceutical Co., Ltd. Novel isoindole derivatives
JP2002255967A (ja) 2001-02-27 2002-09-11 Banyu Pharmaceut Co Ltd イソインドール誘導体を有効成分とする糖尿病の治療剤、糖尿病の慢性合併症の予防剤又は肥満の治療剤。
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AU2007332754A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
AU2013365827A1 (en) 2012-12-19 2015-07-09 Novartis Ag Tricyclic compounds as CFTR inhibitors
EA201591177A1 (ru) 2012-12-19 2015-11-30 Новартис Аг Трициклические соединения для ингибирования канала cftr

Patent Citations (3)

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WO2009042270A2 (en) * 2007-07-05 2009-04-02 Trustees Of Boston University Reca inhibitors and their uses as microbial inhibitors or potentiators of antibiotic activity
CN102695510A (zh) * 2009-08-10 2012-09-26 加利福尼亚大学董事会 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
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

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"Nanomolar Potency Pyrimido-pyrrolo-quinoxalinedione CFTR Inhibitor Reduces Cyst Size in a Polycystic Kidney Disease Model";Lukmanee Tradtrantip et al.;《Journal of Medicinal Chemistry》;20090928;第52卷;第6447–6455页 *
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Also Published As

Publication number Publication date
CR20150325A (es) 2015-08-10
JP2016509579A (ja) 2016-03-31
WO2014097148A9 (en) 2015-02-19
MX2015007939A (es) 2016-03-11
CU20150066A7 (es) 2015-11-27
EA201591177A1 (ru) 2015-11-30
CN105143230A (zh) 2015-12-09
JP6284546B2 (ja) 2018-02-28
HK1209741A1 (en) 2016-04-08
US20150336986A1 (en) 2015-11-26
AU2013365739A1 (en) 2015-07-09
AP2015008539A0 (en) 2015-06-30
PE20151055A1 (es) 2015-08-05
TN2015000279A1 (en) 2016-10-03
EP2935278B1 (en) 2017-03-15
BR112015014292A2 (pt) 2017-07-11
PH12015501386A1 (en) 2015-09-02
US9359381B2 (en) 2016-06-07
SG11201504594QA (en) 2015-07-30
CL2015001730A1 (es) 2015-08-28
TW201429974A (zh) 2014-08-01
US20140171417A1 (en) 2014-06-19
WO2014097148A1 (en) 2014-06-26
UY35211A (es) 2014-07-31
KR20150097660A (ko) 2015-08-26
AR094122A1 (es) 2015-07-08
CA2895660A1 (en) 2014-06-26
ES2628369T3 (es) 2017-08-02
EP2935278A1 (en) 2015-10-28
IL239389A0 (en) 2015-07-30

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