JP2022514253A - Ｎ－（ピリジン－２－イルスルホニル）シクロプロパンカルボキサミド誘導体及びｃｆｔｒ媒介疾患の処置におけるその使用 - Google Patents
Ｎ－（ピリジン－２－イルスルホニル）シクロプロパンカルボキサミド誘導体及びｃｆｔｒ媒介疾患の処置におけるその使用 Download PDFInfo
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- JP2022514253A JP2022514253A JP2021534200A JP2021534200A JP2022514253A JP 2022514253 A JP2022514253 A JP 2022514253A JP 2021534200 A JP2021534200 A JP 2021534200A JP 2021534200 A JP2021534200 A JP 2021534200A JP 2022514253 A JP2022514253 A JP 2022514253A
- Authority
- JP
- Japan
- Prior art keywords
- sulfonyl
- pyridin
- methylphenoxy
- alkyl
- carboxamide
- 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.)
- Pending
Links
- 0 C1C2CCC1*2 Chemical compound C1C2CCC1*2 0.000 description 44
- PCQDDLZQZKGTOL-UHFFFAOYSA-N C=CC[C-](C1=CC(C2)C2C(F)=N1)O Chemical compound C=CC[C-](C1=CC(C2)C2C(F)=N1)O PCQDDLZQZKGTOL-UHFFFAOYSA-N 0.000 description 1
- QLHAHSGJZGOCBT-UHFFFAOYSA-N C=S(c1nc(F)ccc1)(N)=O Chemical compound C=S(c1nc(F)ccc1)(N)=O QLHAHSGJZGOCBT-UHFFFAOYSA-N 0.000 description 1
- SFCIMLAQFAVMAZ-UHFFFAOYSA-N CC(C)(C([O]=C)=O)Oc1c(C2CC2)ccc(C)c1 Chemical compound CC(C)(C([O]=C)=O)Oc1c(C2CC2)ccc(C)c1 SFCIMLAQFAVMAZ-UHFFFAOYSA-N 0.000 description 1
- NZCXINWGLSIWRY-LSDHHAIUSA-N CC(C)(C)OC(C1(CC1)Nc1c([C@H](C2)[C@@H]2C(F)(F)[I]=C)ccc(C)c1)=O Chemical compound CC(C)(C)OC(C1(CC1)Nc1c([C@H](C2)[C@@H]2C(F)(F)[I]=C)ccc(C)c1)=O NZCXINWGLSIWRY-LSDHHAIUSA-N 0.000 description 1
- DKOSEJCDDHIWQW-UHFFFAOYSA-N CC(C1)C1(C)OC(CN(C)CC(O)=O)O Chemical compound CC(C1)C1(C)OC(CN(C)CC(O)=O)O DKOSEJCDDHIWQW-UHFFFAOYSA-N 0.000 description 1
- AABYTTSGNZMXJH-UHFFFAOYSA-N CC(COCC1)N1c1nc(SO)ccc1 Chemical compound CC(COCC1)N1c1nc(SO)ccc1 AABYTTSGNZMXJH-UHFFFAOYSA-N 0.000 description 1
- SFWWGMKXCYLZEG-UHFFFAOYSA-N CC1NCCOC1 Chemical compound CC1NCCOC1 SFWWGMKXCYLZEG-UHFFFAOYSA-N 0.000 description 1
- AVRIREUHDGOEJX-MTLKNEJZSA-N C[C@H](C1C(C2)[C@@H]2C(CNC(C2=CC=CC(C3F)C3=CC2)=O)N)C1(/C=C\C(Cl)=C)N1CCC(C)(C)CC1 Chemical compound C[C@H](C1C(C2)[C@@H]2C(CNC(C2=CC=CC(C3F)C3=CC2)=O)N)C1(/C=C\C(Cl)=C)N1CCC(C)(C)CC1 AVRIREUHDGOEJX-MTLKNEJZSA-N 0.000 description 1
- UIPUUXIIXCWXCX-IMXWASOLSA-N C[C@H](C[C@@H](C1[BrH+])OC2(CC2)C=C)C2C1=C2 Chemical compound C[C@H](C[C@@H](C1[BrH+])OC2(CC2)C=C)C2C1=C2 UIPUUXIIXCWXCX-IMXWASOLSA-N 0.000 description 1
- JYZDNIJNMOMBBW-PHUNFMHTSA-N C[S@](C1NC(F)=CC=C1)=O Chemical compound C[S@](C1NC(F)=CC=C1)=O JYZDNIJNMOMBBW-PHUNFMHTSA-N 0.000 description 1
- YUZHZMIQNQUNQY-UHFFFAOYSA-N Cc(ccc(N)c1)c1[O]=C Chemical compound Cc(ccc(N)c1)c1[O]=C YUZHZMIQNQUNQY-UHFFFAOYSA-N 0.000 description 1
- AFCKRAXZACOVNJ-UHFFFAOYSA-N Cc1cc(OC2(CC2)C(O)=C)c(C)cc1 Chemical compound Cc1cc(OC2(CC2)C(O)=C)c(C)cc1 AFCKRAXZACOVNJ-UHFFFAOYSA-N 0.000 description 1
- BSKHPKMHTQYZBB-UHFFFAOYSA-N Cc1ncccc1 Chemical compound Cc1ncccc1 BSKHPKMHTQYZBB-UHFFFAOYSA-N 0.000 description 1
- MBTGBRYMJKYYOE-UHFFFAOYSA-N Fc1nc(F)ccc1 Chemical compound Fc1nc(F)ccc1 MBTGBRYMJKYYOE-UHFFFAOYSA-N 0.000 description 1
- ZVVCFLDVNRICKQ-UHFFFAOYSA-N O=CCC(C=CC=C1)N=C1F Chemical compound O=CCC(C=CC=C1)N=C1F ZVVCFLDVNRICKQ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- 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
- C07D487/10—Spiro-condensed systems
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862781139P | 2018-12-18 | 2018-12-18 | |
| US62/781,139 | 2018-12-18 | ||
| PCT/IB2019/060801 WO2020128768A1 (en) | 2018-12-18 | 2019-12-13 | N-(pyridin-2-ylsulfonyl)cyclopropanecarboxamide derivatives and their use in the treatment of a cftr mediated disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022514253A true JP2022514253A (ja) | 2022-02-10 |
| JP2022514253A5 JP2022514253A5 (enExample) | 2022-12-19 |
Family
ID=69143626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021534200A Pending JP2022514253A (ja) | 2018-12-18 | 2019-12-13 | Ｎ－（ピリジン－２－イルスルホニル）シクロプロパンカルボキサミド誘導体及びｃｆｔｒ媒介疾患の処置におけるその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20220033407A1 (enExample) |
| EP (1) | EP3897832B1 (enExample) |
| JP (1) | JP2022514253A (enExample) |
| CN (1) | CN113226464A (enExample) |
| WO (1) | WO2020128768A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY38806A (es) * | 2019-08-01 | 2021-02-26 | Novartis Ag | Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos |
| WO2022194399A1 (en) | 2020-07-13 | 2022-09-22 | Idorsia Pharmaceuticals Ltd | Macrocycles as cftr modulators |
| CN119907667A (zh) | 2022-09-15 | 2025-04-29 | 爱杜西亚药品有限公司 | 大环cftr调节剂与cftr校正剂和/或cftr增效剂的组合 |
| CA3267791A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | CRYSTALLINE FORM OF (3S,7S,10R,13R)-13-BENZYL-20-FLUORO-7-ISOBUTYL-N-(2-(3-METHOXY-1,2,4-OXADIAZOL-5-YL)ETHYL)-6,9-DIMETHYL-1,5,8,11-TETRAOXO-10-(2,2,2-TRIFLUOROETHYL)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-TETRADECAHYDRO-[1]OXA[4,7,10,14]TETRAAZACYCLOHEPTADECINO [16,17-F]QUINOLINE-3-CARBOXAMIDE |
| WO2024056798A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | Macrocyclic cftr modulators |
| CN115616024B (zh) * | 2022-12-19 | 2023-03-21 | 苏州大学 | 一种液晶聚酯的组分分析方法 |
| WO2025087274A1 (zh) | 2023-10-27 | 2025-05-01 | 浙江海正药业股份有限公司 | 氮杂双环类衍生物及其制备方法和用途 |
| WO2025186214A1 (en) | 2024-03-05 | 2025-09-12 | Idorsia Pharmaceuticals Ltd | Macrocyclic cftr modulators |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011506524A (ja) * | 2007-12-19 | 2011-03-03 | エフ．ホフマン−ラ ロシュ アーゲー | スピロインドリノン誘導体 |
| WO2017173274A1 (en) * | 2016-03-31 | 2017-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| JP2017530167A (ja) * | 2014-10-06 | 2017-10-12 | 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 | 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーター |
| WO2018042316A1 (en) * | 2016-08-29 | 2018-03-08 | Novartis Ag | N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
-
2019
- 2019-12-13 CN CN201980083034.2A patent/CN113226464A/zh active Pending
- 2019-12-13 JP JP2021534200A patent/JP2022514253A/ja active Pending
- 2019-12-13 WO PCT/IB2019/060801 patent/WO2020128768A1/en not_active Ceased
- 2019-12-13 US US17/414,672 patent/US20220033407A1/en not_active Abandoned
- 2019-12-13 EP EP19832736.3A patent/EP3897832B1/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011506524A (ja) * | 2007-12-19 | 2011-03-03 | エフ．ホフマン−ラ ロシュ アーゲー | スピロインドリノン誘導体 |
| JP2017530167A (ja) * | 2014-10-06 | 2017-10-12 | 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 | 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーター |
| WO2017173274A1 (en) * | 2016-03-31 | 2017-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2018042316A1 (en) * | 2016-08-29 | 2018-03-08 | Novartis Ag | N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3897832B1 (en) | 2023-10-11 |
| EP3897832A1 (en) | 2021-10-27 |
| CN113226464A (zh) | 2021-08-06 |
| WO2020128768A1 (en) | 2020-06-25 |
| US20220033407A1 (en) | 2022-02-03 |
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