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 |
| AU2013348018A1 (en) | 2012-11-20 | 2015-06-04 | Discoverybiomed, Inc. | Small molecule CFTR correctors |
| EP2922853A4 (en) | 2012-11-20 | 2016-11-23 | Discoverybiomed Inc | SMALL MOLECULE BICYCLIC AND TRICYCLIC CFTR CORRECTING DEVICES |
| US9815825B2 (en) | 2013-03-15 | 2017-11-14 | Discoverybiomed, Inc. | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
| MX379292B (es) | 2013-03-15 | 2025-03-11 | Discoverybiomed Inc | Derivados de cumarina y metodos de uso en el tratamiento de enfermedades hiperproliferativas. |
| CA2952862A1 (en) | 2014-06-19 | 2015-12-23 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| TWI735416B (zh) | 2014-10-06 | 2021-08-11 | 美商維泰克斯製藥公司 | 囊腫纖維化症跨膜傳導調節蛋白之調節劑 |
| CA2971850A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylthiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| WO2016105468A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-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 |
| MA42488A (fr) | 2015-07-24 | 2018-05-30 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| BR112018070747B1 (pt) | 2016-04-07 | 2024-01-09 | Proteostasis Therapeutics, Inc | Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos |
| MA45397A (fr) | 2016-06-21 | 2019-04-24 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| WO2018081381A1 (en) | 2016-10-26 | 2018-05-03 | 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 |
| WO2018081378A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| 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 |
| US20190210973A1 (en) | 2018-01-05 | 2019-07-11 | The Curators Of The University Of Missouri | Compounds and methods for treatment of cystic fibrosis |
| UA129188C2 (uk) | 2018-09-09 | 2025-02-05 | Канатфарма Аг | Застосування модуляторів cftr для лікування цереброваскулярних станів |
| 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 |
| DE10133665A1 (de) | 2001-07-11 | 2003-01-30 | Boehringer Ingelheim Pharma | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Herstellung |
| 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 |
| 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 |
| CN101076332A (zh) | 2004-10-13 | 2007-11-21 | Ptc医疗公司 | 吡唑或三唑化合物及其用于制备治疗体细胞突变相关疾病的药物的用途 |
| EP2402323A3 (en) * | 2004-10-13 | 2012-05-30 | PTC Therapeutics, Inc. | Pyrazole or triazole compounds and their use for the manufacture of a medicament for treating somatic mutation-related diseases |
| JP2008515986A (ja) * | 2004-10-13 | 2008-05-15 | ワイス | Ｎ−ベンゼンスルホニル置換アニリノ−ピリミジン類似物 |
| 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 |
| EP2581451B1 (en) * | 2007-12-13 | 2016-03-09 | Indiana University Research and Technology Corporation | Compounds 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 |
| US9815825B2 (en) | 2013-03-15 | 2017-11-14 | Discoverybiomed, Inc. | Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders |
| MX379292B (es) | 2013-03-15 | 2025-03-11 | Discoverybiomed Inc | Derivados de cumarina y metodos de uso en el tratamiento de enfermedades hiperproliferativas. |
-
2014
- 2014-03-14 US US14/775,010 patent/US9815825B2/en not_active Expired - Fee Related
- 2014-03-14 CN CN201480009649.8A patent/CN105121437B/zh not_active Expired - Fee Related
- 2014-03-14 WO PCT/US2014/027079 patent/WO2014152213A2/en not_active Ceased
- 2014-03-14 MX MX2015013173A patent/MX372775B/es active IP Right Grant
- 2014-03-14 JP JP2016502329A patent/JP6514680B2/ja not_active Expired - Fee Related
- 2014-03-14 AU AU2014240026A patent/AU2014240026B2/en not_active Ceased
- 2014-03-14 KR KR1020157029643A patent/KR20150131309A/ko not_active Ceased
- 2014-03-14 CA CA2903103A patent/CA2903103C/en active Active
- 2014-03-14 EP EP14767955.9A patent/EP2970248B1/en not_active Not-in-force