JP2014526500A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014526500A5 JP2014526500A5 JP2014530370A JP2014530370A JP2014526500A5 JP 2014526500 A5 JP2014526500 A5 JP 2014526500A5 JP 2014530370 A JP2014530370 A JP 2014530370A JP 2014530370 A JP2014530370 A JP 2014530370A JP 2014526500 A5 JP2014526500 A5 JP 2014526500A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- trifluoromethyl
- oxadiazol
- halogen atoms
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 32
- 125000005843 halogen group Chemical group 0.000 claims 31
- 229910052799 carbon Inorganic materials 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 5
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 4
- -1 R 14 Chemical compound 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- HNMSYIKEBOLQKV-UHFFFAOYSA-N 2-[5-[3-amino-5,6-bis(trifluoromethyl)pyrazin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C(C(O)(C)C(F)(F)F)=NN=C1C1=NC(C(F)(F)F)=C(C(F)(F)F)N=C1N HNMSYIKEBOLQKV-UHFFFAOYSA-N 0.000 claims 2
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 230000036571 hydration Effects 0.000 claims 2
- 238000006703 hydration reaction Methods 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 102000008371 intracellularly ATP-gated chloride channel activity proteins Human genes 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- GESXZHFWDCTRHG-SNVBAGLBSA-N (2r)-2-[5-[3-amino-4-chloro-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound ClC1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@@](C)(O)C(F)(F)F)=C1N GESXZHFWDCTRHG-SNVBAGLBSA-N 0.000 claims 1
- HNMSYIKEBOLQKV-MRVPVSSYSA-N (2r)-2-[5-[3-amino-5,6-bis(trifluoromethyl)pyrazin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C([C@](O)(C)C(F)(F)F)=NN=C1C1=NC(C(F)(F)F)=C(C(F)(F)F)N=C1N HNMSYIKEBOLQKV-MRVPVSSYSA-N 0.000 claims 1
- GJICZLZFKWSSBD-SECBINFHSA-N (2r)-2-[5-[3-amino-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C([C@](O)(C)C(F)(F)F)=NN=C1C1=NC=C(C(F)(F)F)C=C1N GJICZLZFKWSSBD-SECBINFHSA-N 0.000 claims 1
- HMXVTLCFBUROJI-SNVBAGLBSA-N (2r)-2-[5-[3-amino-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound C1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@@](C)(O)C(F)(F)F)=C1N HMXVTLCFBUROJI-SNVBAGLBSA-N 0.000 claims 1
- GESXZHFWDCTRHG-JTQLQIEISA-N (2s)-2-[5-[3-amino-4-chloro-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound ClC1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@](C)(O)C(F)(F)F)=C1N GESXZHFWDCTRHG-JTQLQIEISA-N 0.000 claims 1
- CTRQIOYBLMEECE-LBPRGKRZSA-N (2s)-2-[5-[3-amino-4-ethyl-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound COC1=C(C(F)(F)F)C(CC)=C(N)C(C=2OC(=NN=2)[C@](C)(O)C(F)(F)F)=N1 CTRQIOYBLMEECE-LBPRGKRZSA-N 0.000 claims 1
- HNMSYIKEBOLQKV-QMMMGPOBSA-N (2s)-2-[5-[3-amino-5,6-bis(trifluoromethyl)pyrazin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C([C@@](O)(C)C(F)(F)F)=NN=C1C1=NC(C(F)(F)F)=C(C(F)(F)F)N=C1N HNMSYIKEBOLQKV-QMMMGPOBSA-N 0.000 claims 1
- GJICZLZFKWSSBD-VIFPVBQESA-N (2s)-2-[5-[3-amino-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C([C@@](O)(C)C(F)(F)F)=NN=C1C1=NC=C(C(F)(F)F)C=C1N GJICZLZFKWSSBD-VIFPVBQESA-N 0.000 claims 1
- AIEPIMYPVPRVOQ-INIZCTEOSA-N (2s)-2-[5-[3-amino-6-methoxy-4-phenyl-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound NC=1C(C=2C=CC=CC=2)=C(C(F)(F)F)C(OC)=NC=1C1=NN=C([C@](C)(O)C(F)(F)F)O1 AIEPIMYPVPRVOQ-INIZCTEOSA-N 0.000 claims 1
- IPXOIMMPOYXWFR-ZDUSSCGKSA-N (2s)-2-[5-[3-amino-6-methoxy-4-prop-1-en-2-yl-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound CC(=C)C1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@](C)(O)C(F)(F)F)=C1N IPXOIMMPOYXWFR-ZDUSSCGKSA-N 0.000 claims 1
- FDJPJZNPKVAQDQ-ZDUSSCGKSA-N (2s)-2-[5-[3-amino-6-methoxy-4-propan-2-yl-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound CC(C)C1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@](C)(O)C(F)(F)F)=C1N FDJPJZNPKVAQDQ-ZDUSSCGKSA-N 0.000 claims 1
- HMXVTLCFBUROJI-JTQLQIEISA-N (2s)-2-[5-[3-amino-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound C1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)[C@](C)(O)C(F)(F)F)=C1N HMXVTLCFBUROJI-JTQLQIEISA-N 0.000 claims 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- ZCPYJTVACTXCQN-UHFFFAOYSA-N 2-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-bromo-5-(trifluoromethyl)pyridin-3-amine Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(O1)=NN=C1CC1=CC=CC=C1 ZCPYJTVACTXCQN-UHFFFAOYSA-N 0.000 claims 1
- QOFCKRKVCJKVJW-SNVBAGLBSA-N 2-[5-[(r)-amino(phenyl)methyl]-1,3,4-oxadiazol-2-yl]-6-bromo-5-(trifluoromethyl)pyridin-3-amine Chemical compound O1C([C@H](N)C=2C=CC=CC=2)=NN=C1C1=NC(Br)=C(C(F)(F)F)C=C1N QOFCKRKVCJKVJW-SNVBAGLBSA-N 0.000 claims 1
- GJICZLZFKWSSBD-UHFFFAOYSA-N 2-[5-[3-amino-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C(C(O)(C)C(F)(F)F)=NN=C1C1=NC=C(C(F)(F)F)C=C1N GJICZLZFKWSSBD-UHFFFAOYSA-N 0.000 claims 1
- SLYMSJFTGUGSPB-UHFFFAOYSA-N 2-[5-[3-amino-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-thiadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound S1C(C(O)(C)C(F)(F)F)=NN=C1C1=NC=C(C(F)(F)F)C=C1N SLYMSJFTGUGSPB-UHFFFAOYSA-N 0.000 claims 1
- OBYGNKZCTZZYRW-UHFFFAOYSA-N 2-[5-[3-amino-6-bromo-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C(C(O)(C)C(F)(F)F)=NN=C1C1=NC(Br)=C(C(F)(F)F)C=C1N OBYGNKZCTZZYRW-UHFFFAOYSA-N 0.000 claims 1
- GXAUSGXVGWVBKQ-UHFFFAOYSA-N 2-[5-[3-amino-6-bromo-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]propan-2-ol Chemical compound O1C(C(C)(O)C)=NN=C1C1=NC(Br)=C(C(F)(F)F)C=C1N GXAUSGXVGWVBKQ-UHFFFAOYSA-N 0.000 claims 1
- GILUBKYXXVYQHQ-UHFFFAOYSA-N 2-[5-[3-amino-6-cyclopropyl-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound O1C(C(O)(C)C(F)(F)F)=NN=C1C1=NC(C2CC2)=C(C(F)(F)F)C=C1N GILUBKYXXVYQHQ-UHFFFAOYSA-N 0.000 claims 1
- HMXVTLCFBUROJI-UHFFFAOYSA-N 2-[5-[3-amino-6-methoxy-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound C1=C(C(F)(F)F)C(OC)=NC(C=2OC(=NN=2)C(C)(O)C(F)(F)F)=C1N HMXVTLCFBUROJI-UHFFFAOYSA-N 0.000 claims 1
- WIQHUQHSUZPFOM-UHFFFAOYSA-N 2-[5-[3-amino-6-methyl-5-(trifluoromethyl)pyridin-2-yl]-1,3,4-oxadiazol-2-yl]-1,1,1-trifluoropropan-2-ol Chemical compound C1=C(C(F)(F)F)C(C)=NC(C=2OC(=NN=2)C(C)(O)C(F)(F)F)=C1N WIQHUQHSUZPFOM-UHFFFAOYSA-N 0.000 claims 1
- BGYUULQTVSRSJN-UHFFFAOYSA-N 3-(5-benzyl-1,3,4-oxadiazol-2-yl)-5-bromo-6-(trifluoromethyl)pyrazin-2-amine Chemical compound NC1=NC(C(F)(F)F)=C(Br)N=C1C(O1)=NN=C1CC1=CC=CC=C1 BGYUULQTVSRSJN-UHFFFAOYSA-N 0.000 claims 1
- 102000016911 Deoxyribonucleases Human genes 0.000 claims 1
- 108010053770 Deoxyribonucleases Proteins 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- AVTAXIOQVRBSRX-UHFFFAOYSA-N [5-[3-amino-6-bromo-5-(trifluoromethyl)pyrazin-2-yl]-1,3,4-oxadiazol-2-yl]-phenylmethanone Chemical compound NC1=NC(C(F)(F)F)=C(Br)N=C1C1=NN=C(C(=O)C=2C=CC=CC=2)O1 AVTAXIOQVRBSRX-UHFFFAOYSA-N 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000003434 antitussive agent Substances 0.000 claims 1
- 229940124584 antitussives Drugs 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- 239000002713 epithelial sodium channel blocking agent Substances 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 230000003204 osmotic effect Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161535560P | 2011-09-16 | 2011-09-16 | |
| US61/535,560 | 2011-09-16 | ||
| PCT/IB2012/054826 WO2013038386A1 (en) | 2011-09-16 | 2012-09-14 | Heterocyclic compounds for the treatment of cystic fibrosis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014526500A JP2014526500A (ja) | 2014-10-06 |
| JP2014526500A5 true JP2014526500A5 (enExample) | 2014-12-11 |
| JP5886433B2 JP5886433B2 (ja) | 2016-03-16 |
Family
ID=47143988
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014530370A Expired - Fee Related JP5886433B2 (ja) | 2011-09-16 | 2012-09-14 | 嚢胞性線維症処置のためのヘテロ環式化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9034879B2 (enExample) |
| EP (1) | EP2755967B1 (enExample) |
| JP (1) | JP5886433B2 (enExample) |
| CN (1) | CN103946221B (enExample) |
| ES (1) | ES2558457T3 (enExample) |
| WO (1) | WO2013038386A1 (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| CN105130948A (zh) | 2010-04-22 | 2015-12-09 | 弗特克斯药品有限公司 | 制备环烷基甲酰胺基-吲哚化合物的方法 |
| ES2882807T3 (es) | 2011-09-16 | 2021-12-02 | Novartis Ag | Heterociclil carboxamidas N-sustituidas |
| JP6543268B2 (ja) | 2014-04-15 | 2019-07-10 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 嚢胞性線維症膜コンダクタンス調節因子が媒介する疾患を処置するための医薬組成物 |
| EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| RS60906B1 (sr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulatori regulatora transmembranske provodljivosti za cističnu fibrozu |
| US9567322B2 (en) | 2014-10-31 | 2017-02-14 | Abbvie S.Á.R.L. | Substituted tetrahydropyrans and method of use |
| 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 |
| 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 |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| KR20180029204A (ko) | 2015-06-02 | 2018-03-20 | 애브비 에스.에이.알.엘. | 치환된 피리딘 및 사용 방법 |
| US9840513B2 (en) | 2015-07-16 | 2017-12-12 | Abbvie S.Á.R.L. | Substituted tricyclics and method of use |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| WO2017062581A1 (en) | 2015-10-06 | 2017-04-13 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| WO2017060879A1 (en) | 2015-10-09 | 2017-04-13 | AbbVie S.à.r.l. | Novel compounds for treatment of cystic fibrosis |
| PL3359541T3 (pl) | 2015-10-09 | 2021-01-11 | AbbVie Overseas S.à r.l. | N-SULFONYLOWANE PIRAZOLO[3,4-b]PIRYDYNO-6-KARBOKSAMIDY I SPOSÓB ZASTOSOWANIA |
| EP3359539A1 (en) | 2015-10-09 | 2018-08-15 | AbbVie S.À.R.L. | Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use |
| US10662207B2 (en) | 2016-04-07 | 2020-05-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating CFTR |
| AU2017256172A1 (en) | 2016-04-26 | 2018-09-06 | AbbVie S.à.r.l. | Modulators of cystic fibrosis transmembrane conductance regulator protein |
| US10138227B2 (en) | 2016-06-03 | 2018-11-27 | Abbvie S.Á.R.L. | Heteroaryl substituted pyridines and methods of use |
| US10899751B2 (en) | 2016-06-21 | 2021-01-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
| US10399940B2 (en) | 2016-10-07 | 2019-09-03 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
| US9981910B2 (en) | 2016-10-07 | 2018-05-29 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
| US20190256474A1 (en) | 2016-10-26 | 2019-08-22 | 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 |
| EP3532467A1 (en) | 2016-10-26 | 2019-09-04 | Proteostasis Therapeutics, Inc. | Pyridazine derivatives, compositions and methods for modulating cftr |
| PT3551622T (pt) | 2016-12-09 | 2020-11-12 | Vertex Pharma | Modulador do regulador da condutância transmembrana da fibrose quística, composições farmacêuticas, métodos de tratamento e processo de fabrico do modulador |
| ES2891527T3 (es) | 2016-12-19 | 2022-01-28 | Novartis Ag | Nuevos derivados de ácido picolínico y su uso como intermedios |
| WO2018116185A1 (en) | 2016-12-20 | 2018-06-28 | AbbVie S.à.r.l. | Deuterated cftr modulators and methods of use |
| TW201831471A (zh) | 2017-02-24 | 2018-09-01 | 盧森堡商艾伯維公司 | 囊腫纖化症跨膜傳導調節蛋白的調節劑及其使用方法 |
| US20200055844A1 (en) | 2017-04-28 | 2020-02-20 | Proteostasis Therapeutics, Inc. | 4-sulfonylaminocarbonylquinoline derivatives for increasing cftr activity |
| WO2019018395A1 (en) | 2017-07-17 | 2019-01-24 | Vertex Pharmaceuticals Incorporated | METHODS OF TREATING CYSTIC FIBROSIS |
| US10988454B2 (en) | 2017-09-14 | 2021-04-27 | Abbvie Overseas S.À.R.L. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
| AU2018346602B2 (en) | 2017-10-06 | 2024-10-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing CFTR activity |
| CA3085006A1 (en) | 2017-12-08 | 2019-06-13 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| US20190210973A1 (en) | 2018-01-05 | 2019-07-11 | The Curators Of The University Of Missouri | Compounds and methods for treatment of cystic fibrosis |
| CA3088577A1 (en) * | 2018-02-15 | 2019-08-22 | Vertex Pharmaceuticals Incorporated | Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them |
| WO2019193062A1 (en) | 2018-04-03 | 2019-10-10 | Abbvie S.Á.R.L | Substituted pyrrolidines and their use |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| US11345691B2 (en) | 2019-06-03 | 2022-05-31 | AbbVie Global Enterprises Ltd. | Prodrug modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
| WO2021011327A1 (en) | 2019-07-12 | 2021-01-21 | Orphomed, Inc. | Compound for treating cystic fibrosis |
| TWI899097B (zh) | 2019-08-14 | 2025-10-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| US11873300B2 (en) | 2019-08-14 | 2024-01-16 | Vertex Pharmaceuticals Incorporated | Crystalline forms of CFTR modulators |
| CA3157798A1 (en) | 2019-11-12 | 2021-05-20 | Zhongli Gao | 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity |
| WO2021113806A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
| WO2021113809A1 (en) | 2019-12-05 | 2021-06-10 | Genzyme Corporation | Arylamides and methods of use thereof |
| CR20230120A (es) * | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| WO2022036060A1 (en) | 2020-08-13 | 2022-02-17 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| US12612416B2 (en) | 2020-10-07 | 2026-04-28 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CR20230260A (es) * | 2020-11-18 | 2023-10-05 | Vertex Pharma | Macrociclos que contienen un anillo de 1,3,4-oxadiazol para su uso como moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| US12324802B2 (en) * | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| IL303519A (en) | 2020-12-10 | 2023-08-01 | Vertex Pharma | Cystic fibrosis treatment methods |
| WO2022150173A1 (en) | 2021-01-06 | 2022-07-14 | AbbVie Global Enterprises Ltd. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
| EP4274828A1 (en) | 2021-01-06 | 2023-11-15 | AbbVie Global Enterprises Ltd. | Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use |
| WO2023034946A1 (en) | 2021-09-03 | 2023-03-09 | Genzyme Corporation | Indole compounds and uses thereof in the treatement of cystic fibrosis |
| EP4396179A1 (en) | 2021-09-03 | 2024-07-10 | Genzyme Corporation | Indole compounds and methods of use |
| CA3249378A1 (en) * | 2022-02-03 | 2023-08-10 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS FOR CYSTIC FIBROSIS |
| IL314691A (en) * | 2022-02-03 | 2024-10-01 | Vertex Pharma | PREPARATION METHODS AND CRYSTALLINE FORMS OF (6A,12A)-17-AMINO-12-METHYL-6,15-BIS(TRIFLUOROMETHYL)-13,19-DIOXA-3,4,18-TRIAZATRICYCLO[ 12.3.112.3.1. NONADECA-1(18),2,4,14,16-PENTAEN-6-OL |
| CN118974059A (zh) * | 2022-02-08 | 2024-11-15 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调控因子的调节剂 |
| CA3253026A1 (en) * | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | TREATMENT METHODS FOR CYSTIC FIBROSIS |
| WO2023224924A1 (en) * | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Solid forms of a macrocyclic compounds as cftr modulators and their preparation |
| AU2023338225A1 (en) | 2022-09-07 | 2025-03-20 | Genzyme Corporation | Macrocyclic compounds, compositions, and methods of using thereof |
| WO2024054845A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocycic compounds, compositions, and methods of using thereof |
| WO2024054851A1 (en) | 2022-09-07 | 2024-03-14 | Sionna Therapeutics | Macrocyclic compounds, compositions and methods of using thereof |
| WO2025132358A1 (en) | 2023-12-21 | 2025-06-26 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of infectious diseases |
Family Cites Families (108)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1219606A (en) | 1968-07-15 | 1971-01-20 | Rech S Et D Applic Scient Soge | Quinuclidinol derivatives and preparation thereof |
| JPS6235216A (ja) | 1985-08-09 | 1987-02-16 | Noritoshi Nakabachi | 不均質物質層の層厚非破壊測定方法および装置 |
| GB8923590D0 (en) | 1989-10-19 | 1989-12-06 | Pfizer Ltd | Antimuscarinic bronchodilators |
| PT100441A (pt) | 1991-05-02 | 1993-09-30 | Smithkline Beecham Corp | Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso |
| WO1993018007A1 (fr) | 1992-03-13 | 1993-09-16 | Tokyo Tanabe Company Limited | Nouveau derive de carbostyrile |
| HU225869B1 (en) | 1992-04-02 | 2007-11-28 | Smithkline Beecham Corp | Compounds with antiallergic and antiinflammatory activity and pharmaceutical compns. contg. them |
| JP3192424B2 (ja) | 1992-04-02 | 2001-07-30 | スミスクライン・ビーチャム・コーポレイション | アレルギーまたは炎症疾患の治療用化合物 |
| US5605923A (en) | 1992-04-02 | 1997-02-25 | Smithkline Beecham Corporation | Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor |
| GB9622386D0 (en) | 1996-10-28 | 1997-01-08 | Sandoz Ltd | Organic compounds |
| US6166037A (en) | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
| AU9281298A (en) | 1997-10-01 | 1999-04-23 | Kyowa Hakko Kogyo Co. Ltd. | Benzodioxole derivatives |
| US6541669B1 (en) | 1998-06-08 | 2003-04-01 | Theravance, Inc. | β2-adrenergic receptor agonists |
| BR9815931A (pt) | 1998-06-30 | 2001-02-20 | Dow Chemical Co | Polióis poliméricos, um processo para sua produção, e espuma de poliuretanoobtida |
| GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| TR200103214T2 (tr) | 1999-05-04 | 2002-03-21 | Schering Corporation | CCR5 antagonistleri olarak yararlì piperazin trevleri. |
| CZ301161B6 (cs) | 1999-05-04 | 2009-11-18 | Schering Corporation | Piperidinopiperidylový derivát užitecný jako CCR5 antagonista, farmaceutický prostredek jej obsahující |
| US6683115B2 (en) | 1999-06-02 | 2004-01-27 | Theravance, Inc. | β2-adrenergic receptor agonists |
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| CA2715683A1 (en) | 1999-08-21 | 2001-03-01 | Nycomed Gmbh | Synergistic combination |
| OA11558A (en) | 1999-12-08 | 2004-06-03 | Advanced Medicine Inc | Beta 2-adrenergic receptor agonists. |
| AU5629301A (en) | 2000-04-27 | 2001-11-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel, slow-acting betamimetics, a method for their production and their use as medicaments |
| AU6610001A (en) | 2000-06-27 | 2002-01-08 | S A L V A T Lab Sa | Carbamates derived from arylalkylamines |
| GB0015876D0 (en) | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| DE10038639A1 (de) | 2000-07-28 | 2002-02-21 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| EP2067784A3 (en) | 2000-08-05 | 2012-08-22 | Glaxo Group Limited | 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivatives as anti-inflammatory agents |
| GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
| HUP0303529A3 (en) | 2000-12-22 | 2008-03-28 | Almirall Ag | New quinuclidine carbamate derivatives, process for their preparation and pharmaceutical compositions containing them and their use |
| CN1250545C (zh) | 2000-12-28 | 2006-04-12 | 阿尔米雷尔普罗迪斯制药有限公司 | 新的奎宁环衍生物类及含有这类衍生物的药物组合物 |
| GB0103630D0 (en) | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
| JP2004526720A (ja) | 2001-03-08 | 2004-09-02 | グラクソ グループ リミテッド | βアドレナリン受容体のアゴニスト |
| WO2002076933A1 (en) | 2001-03-22 | 2002-10-03 | Glaxo Group Limited | Formailide derivatives as beta2-adrenoreceptor agonists |
| WO2002088167A1 (en) | 2001-04-30 | 2002-11-07 | Glaxo Group Limited | Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha |
| ATE399174T1 (de) | 2001-06-12 | 2008-07-15 | Glaxo Group Ltd | Neue anti inflammatorische 17.alpha.- heterozyklische ester von 17.beta.-carbothioat androstan derivativen |
| EP1578910A4 (en) | 2001-06-21 | 2008-06-04 | Verenium Corp | NITRILASES |
| ATE417606T1 (de) | 2001-09-14 | 2009-01-15 | Glaxo Group Ltd | Phenethanolamin-derivate zur behandlung von erkrankungen der atemwege |
| RU2004110717A (ru) | 2001-10-17 | 2005-10-20 | Юсиби, С.А. (Be) | Производные хинуклидина, способы их получения и их применение в качестве и нгибиторов м2- и/или м3- мускариновых рецепторов |
| GB0125259D0 (en) | 2001-10-20 | 2001-12-12 | Glaxo Group Ltd | Novel compounds |
| AR037517A1 (es) | 2001-11-05 | 2004-11-17 | Novartis Ag | Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria |
| TWI249515B (en) | 2001-11-13 | 2006-02-21 | Theravance Inc | Aryl aniline beta2 adrenergic receptor agonists |
| US6653323B2 (en) | 2001-11-13 | 2003-11-25 | Theravance, Inc. | Aryl aniline β2 adrenergic receptor agonists |
| AU2002356759A1 (en) | 2001-12-01 | 2003-06-17 | Glaxo Group Limited | 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents |
| JP4505227B2 (ja) | 2001-12-20 | 2010-07-21 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | 1−アルキル−1−アゾニアビシクロ[2.2.2]オクタンカルバメート誘導体およびムスカリンレセプターアンタゴニストとしてのそれらの使用 |
| AU2003202044A1 (en) | 2002-01-15 | 2003-09-09 | Glaxo Group Limited | 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents |
| AU2003201693A1 (en) | 2002-01-21 | 2003-09-02 | Glaxo Group Limited | Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents |
| GB0202216D0 (en) | 2002-01-31 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
| GB0204719D0 (en) | 2002-02-28 | 2002-04-17 | Glaxo Group Ltd | Medicinal compounds |
| AU2003230700A1 (en) | 2002-03-26 | 2003-10-13 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| PL373043A1 (en) | 2002-03-26 | 2005-08-08 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| AU2003221706B2 (en) | 2002-04-11 | 2008-02-28 | Merck Sharp & Dohme Corp. | 1H-Benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators |
| ES2206021B1 (es) | 2002-04-16 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de pirrolidinio. |
| ATE381535T1 (de) | 2002-04-25 | 2008-01-15 | Glaxo Group Ltd | Phenethanolaminderivate |
| EP1507754A1 (en) | 2002-05-28 | 2005-02-23 | Theravance, Inc. | Alkoxy aryl beta-2 adrenergic receptor agonists |
| ES2201907B1 (es) | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
| US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| DE10224888A1 (de) | 2002-06-05 | 2003-12-24 | Merck Patent Gmbh | Pyridazinderivate |
| US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| DE10225574A1 (de) | 2002-06-10 | 2003-12-18 | Merck Patent Gmbh | Aryloxime |
| DE10227269A1 (de) | 2002-06-19 | 2004-01-08 | Merck Patent Gmbh | Thiazolderivate |
| ATE356808T1 (de) | 2002-06-25 | 2007-04-15 | Merck Frosst Canada Ltd | 8-(biaryl)chinolin-pde4-inhibitoren |
| ES2204295B1 (es) | 2002-07-02 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de quinuclidina-amida. |
| WO2004005258A1 (en) | 2002-07-02 | 2004-01-15 | Merck Frosst Canada & Co. | Di-aryl-substituted-ethane pyridone pde4 inhibitors |
| ES2518940T3 (es) | 2002-07-08 | 2014-11-06 | Pfizer Products Inc. | Moduladores del receptor de glucocorticoides |
| GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
| PE20050130A1 (es) | 2002-08-09 | 2005-03-29 | Novartis Ag | Compuestos organicos |
| HRP20050197A2 (en) | 2002-08-10 | 2006-06-30 | Altana Pharma Ag | Piperidine-n-oxide-derivatives |
| JP2005538140A (ja) | 2002-08-10 | 2005-12-15 | アルタナ ファルマ アクチエンゲゼルシャフト | Pde4インヒビターとしてのピペリジン−ピリダゾン及びフタラゾン |
| CA2494650A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Pyridazinone-derivatives as pde4 inhibitors |
| WO2004018449A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Piperidine-derivatives as pde4 inhibitors |
| PL374014A1 (en) | 2002-08-17 | 2005-09-19 | Altana Pharma Ag | Novel phenanthridines having pde 3/4 inhibiting properties |
| AU2003263216A1 (en) | 2002-08-17 | 2004-03-11 | Nycomed Gmbh | Benzonaphthyridines with PDE 3/4 inhibiting activity |
| SE0202483D0 (sv) | 2002-08-21 | 2002-08-21 | Astrazeneca Ab | Chemical compounds |
| DE60322713D1 (de) | 2002-08-21 | 2008-09-18 | Boehringer Ingelheim Pharma | Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung |
| JP2006501236A (ja) | 2002-08-23 | 2006-01-12 | ランバクシー ラボラトリーズ リミテッド | ムスカリン性レセプター拮抗薬としてのフルオロおよびスルホニルアミノ含有3,6−二置換アザビシクロ(3.1.0)ヘキサン誘導体 |
| AU2003255493B8 (en) | 2002-08-29 | 2009-03-26 | Takeda Gmbh | 2-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors |
| JP4619786B2 (ja) | 2002-08-29 | 2011-01-26 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 炎症性、アレルギー性及び増殖性疾患の治療において糖質コルチコイドミメティックスとして使用するための3−(スルホンアミドエチル)−インドール誘導体 |
| US7423046B2 (en) | 2002-08-29 | 2008-09-09 | Nycomed Gmbh | 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
| GB0220730D0 (en) | 2002-09-06 | 2002-10-16 | Glaxo Group Ltd | Medicinal compounds |
| JP2006096662A (ja) | 2002-09-18 | 2006-04-13 | Sumitomo Pharmaceut Co Ltd | 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| KR20050057408A (ko) | 2002-09-18 | 2005-06-16 | 오노 야꾸힝 고교 가부시키가이샤 | 트리아자스피로[5.5]운데칸 유도체 및 이를 유효 성분으로하는 약제 |
| JP2004107299A (ja) | 2002-09-20 | 2004-04-08 | Japan Energy Corp | 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| CA2499150A1 (en) | 2002-09-20 | 2004-04-01 | Merck & Co., Inc. | Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators |
| DE10246374A1 (de) | 2002-10-04 | 2004-04-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| ES2302938T3 (es) | 2002-10-11 | 2008-08-01 | Pfizer Inc. | Derivados de indol como agonistas beta-2. |
| EP1440966A1 (en) | 2003-01-10 | 2004-07-28 | Pfizer Limited | Indole derivatives useful for the treatment of diseases |
| US20060205790A1 (en) | 2002-10-22 | 2006-09-14 | Coe Diane M | Medicinal arylethanolamine compounds |
| WO2004037805A1 (en) | 2002-10-23 | 2004-05-06 | Glenmark Pharmaceuticals Ltd. | Novel tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them |
| GB0225030D0 (en) | 2002-10-28 | 2002-12-04 | Glaxo Group Ltd | Medicinal compounds |
| US7442839B2 (en) | 2002-10-28 | 2008-10-28 | Glaxo Group Limited | Phenethanolamine derivative for the treatment of respiratory diseases |
| GB0225287D0 (en) | 2002-10-30 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| DE10253220A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE10253282A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung |
| DE10253426B4 (de) | 2002-11-15 | 2005-09-22 | Elbion Ag | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
| DE10261874A1 (de) | 2002-12-20 | 2004-07-08 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| US7732432B2 (en) | 2003-01-21 | 2010-06-08 | Merck Sharp & Dohme Corp. | 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators |
| PE20040950A1 (es) | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
| CA2514733A1 (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 |
| EP1460064A1 (en) | 2003-03-14 | 2004-09-22 | Pfizer Limited | Indole-2-carboxamide derivatives useful as beta-2 agonists |
| GB0312832D0 (en) | 2003-06-04 | 2003-07-09 | Pfizer Ltd | 2-amino-pyridine derivatives useful for the treatment of diseases |
| JP2007535897A (ja) | 2003-06-10 | 2007-12-13 | エース バイオサイエンシズ エー/エス | 細胞外コウジカビポリペプチド |
| JP2011520831A (ja) * | 2008-05-13 | 2011-07-21 | ノバルティス アーゲー | 3,5−ジアミノ−6−クロロ−ピラジン−2−カルボン酸誘導体および気道疾患処置用上皮性ナトリウムチャネルブロッカーとしてのその使用 |
| JP5702293B2 (ja) * | 2008-11-10 | 2015-04-15 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な化合物 |
| BRPI0924084B1 (pt) * | 2008-12-19 | 2021-12-21 | Vertex Pharmaceuticals Incorporated | Derivados de pirazina e composição farmacêutica que os compreende |
| US20120136003A1 (en) * | 2009-04-20 | 2012-05-31 | Institute For Oneworld Health | Compounds, compositions and methods comprising 1,3,4-oxadiazole derivatives |
| WO2010151747A1 (en) * | 2009-06-26 | 2010-12-29 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimine compounds and methods of making and using same |
| AU2011253025A1 (en) * | 2010-05-12 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| ES2882807T3 (es) | 2011-09-16 | 2021-12-02 | Novartis Ag | Heterociclil carboxamidas N-sustituidas |
-
2012
- 2012-09-14 WO PCT/IB2012/054826 patent/WO2013038386A1/en not_active Ceased
- 2012-09-14 ES ES12783308.5T patent/ES2558457T3/es active Active
- 2012-09-14 US US14/343,861 patent/US9034879B2/en active Active
- 2012-09-14 EP EP12783308.5A patent/EP2755967B1/en not_active Not-in-force
- 2012-09-14 CN CN201280056105.8A patent/CN103946221B/zh not_active Expired - Fee Related
- 2012-09-14 JP JP2014530370A patent/JP5886433B2/ja not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014526501A5 (enExample) | ||
| RU2485131C2 (ru) | Производные пиридина, замещенные гетероциклическим кольцом и фосфоноксиметильной группой и содержащие их противогрибковые средства | |
| JP2012515787A5 (enExample) | ||
| JP2014530900A5 (enExample) | ||
| JP2019513776A5 (enExample) | ||
| JP2015512435A5 (enExample) | ||
| JP2007519649A5 (enExample) | ||
| JP2017528487A5 (enExample) | ||
| JP2009507896A5 (enExample) | ||
| JP2011502958A5 (enExample) | ||
| JP2014511892A5 (enExample) | ||
| JP2005517006A5 (enExample) | ||
| JP2010534647A5 (enExample) | ||
| JP2013529210A5 (enExample) | ||
| JP2014514360A5 (enExample) | ||
| JP2008500992A5 (enExample) | ||
| JP2013532652A5 (enExample) | ||
| JP2014513110A5 (enExample) | ||
| RU2017116196A (ru) | 2-амино-6-(дифторметил)-5,5-дифтор-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1 | |
| JP2014505107A5 (enExample) | ||
| RU2012116877A (ru) | Соединения 2-пиридона, применяемые в качестве ингибиторов нейтрофильной эластазы | |
| JP2012515788A5 (enExample) | ||
| RU2011105151A (ru) | Азольные соединения | |
| JP2014532754A5 (enExample) | ||
| JP2014523400A5 (enExample) |