JP2016515131A5 - - Google Patents
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- Publication number
- JP2016515131A5 JP2016515131A5 JP2016502329A JP2016502329A JP2016515131A5 JP 2016515131 A5 JP2016515131 A5 JP 2016515131A5 JP 2016502329 A JP2016502329 A JP 2016502329A JP 2016502329 A JP2016502329 A JP 2016502329A JP 2016515131 A5 JP2016515131 A5 JP 2016515131A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- pharmaceutically acceptable
- prodrug
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 46
- 229940002612 prodrug Drugs 0.000 claims description 29
- 239000000651 prodrug Substances 0.000 claims description 29
- 150000003839 salts Chemical class 0.000 claims description 29
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 20
- 210000004027 cell Anatomy 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 230000035772 mutation Effects 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 208000007153 proteostasis deficiencies Diseases 0.000 claims description 6
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 claims description 4
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims description 4
- 150000004820 halides Chemical class 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 108010062745 Chloride Channels Proteins 0.000 claims description 2
- 102000011045 Chloride Channels Human genes 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 claims description 2
- 210000001552 airway epithelial cell Anatomy 0.000 claims description 2
- KWEDUNSJJZVRKR-UHFFFAOYSA-N carbononitridic azide Chemical compound [N-]=[N+]=NC#N KWEDUNSJJZVRKR-UHFFFAOYSA-N 0.000 claims description 2
- 150000001805 chlorine compounds Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 230000007547 defect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 210000002919 epithelial cell Anatomy 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- 238000001727 in vivo Methods 0.000 claims description 2
- 230000003834 intracellular effect Effects 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 2
- 229940124530 sulfonamide Drugs 0.000 claims description 2
- 150000003456 sulfonamides Chemical class 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000004950 trifluoroalkyl group Chemical group 0.000 claims description 2
- 238000000034 method Methods 0.000 description 22
- 0 *c(c(*)c1*)c(*)c(*)c1NIC1=Cc(cccc2Cl)c2OC1=O Chemical compound *c(c(*)c1*)c(*)c(*)c1NIC1=Cc(cccc2Cl)c2OC1=O 0.000 description 6
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361788353P | 2013-03-15 | 2013-03-15 | |
| US61/788,353 | 2013-03-15 | ||
| PCT/US2014/027079 WO2014152213A2 (en) | 2013-03-15 | 2014-03-14 | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016515131A JP2016515131A (ja) | 2016-05-26 |
| JP2016515131A5 true JP2016515131A5 (https=) | 2017-04-20 |
| JP6514680B2 JP6514680B2 (ja) | 2019-05-15 |
Family
ID=51581684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016502329A Expired - Fee Related JP6514680B2 (ja) | 2013-03-15 | 2014-03-14 | クマリン誘導体、ならびに嚢胞性線維症、慢性閉塞性肺疾患、及びミスフォールドタンパク質障害の治療における使用方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9815825B2 (https=) |
| EP (1) | EP2970248B1 (https=) |
| JP (1) | JP6514680B2 (https=) |
| KR (1) | KR20150131309A (https=) |
| CN (1) | CN105121437B (https=) |
| AU (1) | AU2014240026B2 (https=) |
| CA (1) | CA2903103C (https=) |
| MX (1) | MX372775B (https=) |
| WO (1) | WO2014152213A2 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012158913A2 (en) | 2011-05-17 | 2012-11-22 | Discoverybiomed Inc. | Treating protein folding disorders with small molecule cftr correctors |
| EP2922852A4 (en) | 2012-11-20 | 2016-05-25 | Discoverybiomed Inc | SMALL MOLECULAR CFTR CORRECTORS |
| US9546176B2 (en) | 2012-11-20 | 2017-01-17 | Discoverybiomed, Inc. | Small molecule bicyclic and tricyclic CFTR correctors |
| KR20150132483A (ko) * | 2013-03-15 | 2015-11-25 | 디스커버리바이오메드 인코포레이티드 | 쿠마린 유도체 및 과증식성 질환의 치료에서의 사용 방법 |
| CA2903103C (en) | 2013-03-15 | 2020-06-09 | Discoverybiomed, Inc. | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
| EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| MA41051B1 (fr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose |
| US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US10344023B2 (en) | 2014-12-23 | 2019-07-09 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| MA43775A (fr) | 2016-04-07 | 2021-05-05 | Proteostasis Therapeutics Inc | Analogues du ivacaftor conentant des atomes de silicium |
| MA45397A (fr) | 2016-06-21 | 2019-04-24 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| WO2018081378A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| AU2017348186A1 (en) | 2016-10-26 | 2019-05-16 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating CFTR |
| CA3041675A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | N-phenyl-2-(3-phenyl-6-oxo-1,6-dihydropyridazin-1-yl)acetamide derivatives for treating cystic fibrosis |
| MA49061A (fr) | 2017-04-28 | 2021-04-21 | Proteostasis Therapeutics Inc | Dérivés 4-sulfonylaminocarbonylquinoline pour augmenter l'activité cftr |
| AU2018346602B2 (en) | 2017-10-06 | 2024-10-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing CFTR activity |
| WO2019136314A1 (en) | 2018-01-05 | 2019-07-11 | The Curators Of The University Of Missouri | Compounds and methods for treatment of cystic fibrosis |
| AU2019334684B2 (en) | 2018-09-09 | 2025-03-06 | Qanatpharma Ag | Use of CFTR modulators for treating cerebrovascular conditions |
| CN110156761B (zh) * | 2019-06-18 | 2022-08-09 | 郑州大学 | 含香豆素-联苯骨架化合物、制备方法及其应用 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5566580A (en) * | 1978-11-11 | 1980-05-20 | Kaken Pharmaceut Co Ltd | Coumarin derivative, its preparation and antiallergic agent containing the same as effective component |
| US20030055263A1 (en) | 2001-07-11 | 2003-03-20 | Boehringer Ingelheim Pharma Kg | Carboxylic acid derivatives, medicaments comprising these compounds, their use and processes for their production |
| DE10133665A1 (de) | 2001-07-11 | 2003-01-30 | Boehringer Ingelheim Pharma | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Herstellung |
| US6822097B1 (en) * | 2002-02-07 | 2004-11-23 | Amgen, Inc. | Compounds and methods of uses |
| AU2003245935A1 (en) | 2002-06-13 | 2003-12-31 | Novuspharma S.P.A. | Derivatives of chromen-2-one as inhibitors of vegf production in mammalian cells |
| CN101076703A (zh) * | 2004-10-13 | 2007-11-21 | Ptc医疗公司 | 用于无义抑制的化合物及其使用方法 |
| MX2007004488A (es) * | 2004-10-13 | 2007-09-11 | Wyeth Corp | Analogos de anilino-pirimidina n-bencenosulfonilo sustituidos. |
| EP1799659A1 (en) * | 2004-10-13 | 2007-06-27 | PTC Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
| CN101351208A (zh) * | 2005-11-01 | 2009-01-21 | 康乃尔研究基金会有限公司 | 减少细胞胆固醇水平和/或治疗或预防磷脂质病 |
| US20090012148A1 (en) * | 2005-11-01 | 2009-01-08 | Maxfield Frederick R | Reducing cellular cholesterol levels and/or treating or preventing phospholipidosis |
| WO2009076665A1 (en) * | 2007-12-13 | 2009-06-18 | Indiana University Research And Technology Corporation | Materials and methods for inhibiting mammalian s-nitrosoglutathione reductase |
| WO2010111713A2 (en) * | 2009-03-27 | 2010-09-30 | Zacharon Pharmaceuticals, Inc. | N-linked glycan biosynthesis modulators |
| ITMI20111068A1 (it) * | 2011-06-14 | 2012-12-15 | Azienda Ospedaliera Universitaria I Ntegrata Di Ve | Trimetilangelicina come correttore di cftr in cellule dell'epitelio bronchiale |
| CA2903103C (en) | 2013-03-15 | 2020-06-09 | Discoverybiomed, Inc. | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
| KR20150132483A (ko) | 2013-03-15 | 2015-11-25 | 디스커버리바이오메드 인코포레이티드 | 쿠마린 유도체 및 과증식성 질환의 치료에서의 사용 방법 |
-
2014
- 2014-03-14 CA CA2903103A patent/CA2903103C/en active Active
- 2014-03-14 JP JP2016502329A patent/JP6514680B2/ja not_active Expired - Fee Related
- 2014-03-14 US US14/775,010 patent/US9815825B2/en not_active Expired - Fee Related
- 2014-03-14 MX MX2015013173A patent/MX372775B/es active IP Right Grant
- 2014-03-14 CN CN201480009649.8A patent/CN105121437B/zh not_active Expired - Fee Related
- 2014-03-14 KR KR1020157029643A patent/KR20150131309A/ko not_active Ceased
- 2014-03-14 WO PCT/US2014/027079 patent/WO2014152213A2/en not_active Ceased
- 2014-03-14 EP EP14767955.9A patent/EP2970248B1/en not_active Not-in-force
- 2014-03-14 AU AU2014240026A patent/AU2014240026B2/en not_active Ceased
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