AU2014212431B2 - Amides as modulators of sodium channels - Google Patents
Amides as modulators of sodium channels Download PDFInfo
- Publication number
- AU2014212431B2 AU2014212431B2 AU2014212431A AU2014212431A AU2014212431B2 AU 2014212431 B2 AU2014212431 B2 AU 2014212431B2 AU 2014212431 A AU2014212431 A AU 2014212431A AU 2014212431 A AU2014212431 A AU 2014212431A AU 2014212431 B2 AU2014212431 B2 AU 2014212431B2
- Authority
- AU
- Australia
- Prior art keywords
- alkyl
- another embodiment
- halogen
- benzamido
- pain
- 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.)
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- 0 COc1c(*)ccc(F)c1 Chemical compound COc1c(*)ccc(F)c1 0.000 description 4
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- SXBQMPXVMASFTE-UHFFFAOYSA-N Cc(c(Cl)c1)cc(Oc(ccc(OC)c2)c2Cl)c1C(Nc1ccc(C(O)=O)nc1)=O Chemical compound Cc(c(Cl)c1)cc(Oc(ccc(OC)c2)c2Cl)c1C(Nc1ccc(C(O)=O)nc1)=O SXBQMPXVMASFTE-UHFFFAOYSA-N 0.000 description 1
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- HNQLMBJUMVLFCF-UHFFFAOYSA-N Cc(cc1)c(C)cc1Cl Chemical compound Cc(cc1)c(C)cc1Cl HNQLMBJUMVLFCF-UHFFFAOYSA-N 0.000 description 1
- XGYLSRFSXKAYCR-UHFFFAOYSA-N Cc(cc1)cc(Cl)c1N Chemical compound Cc(cc1)cc(Cl)c1N XGYLSRFSXKAYCR-UHFFFAOYSA-N 0.000 description 1
- LVDHTYMXUHPTOP-UHFFFAOYSA-N Cc(cc1)cc(OC)c1I Chemical compound Cc(cc1)cc(OC)c1I LVDHTYMXUHPTOP-UHFFFAOYSA-N 0.000 description 1
- MPXDAIBTYWGBSL-UHFFFAOYSA-N Cc(ccc(F)c1)c1F Chemical compound Cc(ccc(F)c1)c1F MPXDAIBTYWGBSL-UHFFFAOYSA-N 0.000 description 1
- OSNMRWURXNWCGA-UHFFFAOYSA-N Cc(ccc(OC)c1)c1OC Chemical compound Cc(ccc(OC)c1)c1OC OSNMRWURXNWCGA-UHFFFAOYSA-N 0.000 description 1
- KRZCOLNOCZKSDF-UHFFFAOYSA-N Nc(cc1)ccc1F Chemical compound Nc(cc1)ccc1F KRZCOLNOCZKSDF-UHFFFAOYSA-N 0.000 description 1
- KTHRLYGNINDXBX-UHFFFAOYSA-N OC(c(nc1)ccc1NC(c(c(C(F)(F)F)ccc1)c1Oc(c(Cl)c1)ccc1F)=O)=O Chemical compound OC(c(nc1)ccc1NC(c(c(C(F)(F)F)ccc1)c1Oc(c(Cl)c1)ccc1F)=O)=O KTHRLYGNINDXBX-UHFFFAOYSA-N 0.000 description 1
- KGZXPYSTVRCFHV-UHFFFAOYSA-N OC(c(nc1)ccc1NC(c(c(Oc(cc1)ccc1OCC(F)(F)F)c1)cc(Cl)c1Cl)=O)=O Chemical compound OC(c(nc1)ccc1NC(c(c(Oc(cc1)ccc1OCC(F)(F)F)c1)cc(Cl)c1Cl)=O)=O KGZXPYSTVRCFHV-UHFFFAOYSA-N 0.000 description 1
- ZJDFLPLEPVWDIP-UHFFFAOYSA-N OC(c(nc1)ccc1NC(c1cc(C(F)(F)F)ccc1Oc(ccc(F)c1)c1Cl)=O)=O Chemical compound OC(c(nc1)ccc1NC(c1cc(C(F)(F)F)ccc1Oc(ccc(F)c1)c1Cl)=O)=O ZJDFLPLEPVWDIP-UHFFFAOYSA-N 0.000 description 1
- QPVZBOZWYRYQOY-UHFFFAOYSA-N OC(c(nc1)ccc1NC(c1cc(C(F)(F)F)ccc1Oc(cccc1)c1Cl)=O)=O Chemical compound OC(c(nc1)ccc1NC(c1cc(C(F)(F)F)ccc1Oc(cccc1)c1Cl)=O)=O QPVZBOZWYRYQOY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/64—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361759062P | 2013-01-31 | 2013-01-31 | |
| US61/759,062 | 2013-01-31 | ||
| PCT/US2014/013667 WO2014120820A1 (en) | 2013-01-31 | 2014-01-29 | Amides as modulators of sodium channels |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2014212431A1 AU2014212431A1 (en) | 2015-08-06 |
| AU2014212431B2 true AU2014212431B2 (en) | 2018-04-05 |
Family
ID=50114569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014212431A Active AU2014212431B2 (en) | 2013-01-31 | 2014-01-29 | Amides as modulators of sodium channels |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9108903B2 (enExample) |
| EP (1) | EP2951155B1 (enExample) |
| JP (1) | JP6346622B2 (enExample) |
| KR (1) | KR102226588B1 (enExample) |
| CN (1) | CN104968647B (enExample) |
| AR (1) | AR094668A1 (enExample) |
| AU (1) | AU2014212431B2 (enExample) |
| BR (1) | BR112015018284B1 (enExample) |
| CA (1) | CA2898653C (enExample) |
| IL (1) | IL240196B (enExample) |
| MX (1) | MX359882B (enExample) |
| RU (1) | RU2658920C2 (enExample) |
| SG (1) | SG11201505954RA (enExample) |
| TW (1) | TWI659945B (enExample) |
| WO (1) | WO2014120820A1 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT201700256T1 (it) | 2013-01-31 | 2017-09-07 | Vertex Pharma | Piridone ammidi come modulatori di canali del sodio |
| NZ710111A (en) | 2013-01-31 | 2020-08-28 | Vertex Pharma | Quinoline and quinoxaline amides as modulators of sodium channels |
| JP6337109B2 (ja) | 2013-07-19 | 2018-06-06 | 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 | ナトリウムチャネルの調節剤としてのスルホンアミド |
| JP6463580B2 (ja) | 2013-12-13 | 2019-02-06 | 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 | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
| BR112019024016A2 (pt) | 2017-05-16 | 2020-06-09 | Vertex Pharma | amidas de piridona deuteradas e profármacos das mesmas como moduladores de canais de sódio |
| CA3069720A1 (en) | 2017-07-11 | 2019-01-17 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| EP3752152A1 (en) | 2018-02-12 | 2020-12-23 | Vertex Pharmaceuticals Incorporated | A method of treating pain |
| EP3873893A1 (en) | 2018-11-02 | 2021-09-08 | Merck Sharp & Dohme Corp. | 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors |
| US12344595B2 (en) | 2018-11-02 | 2025-07-01 | Merck Sharp & Dohme Llc | 2-amino-n-phenyl-nicotinamides as NAV1.8 inhibitors |
| EP3907218A4 (en) * | 2019-01-04 | 2022-09-21 | Jiangsu Hengrui Medicine Co., Ltd. | 6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, METHOD FOR PREPARATION AND MEDICAL USE |
| US12441703B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| CN112996776B (zh) * | 2019-02-20 | 2024-03-15 | 福建盛迪医药有限公司 | 6-氧代-1,6-二氢哒嗪类前药衍生物、其制备方法及其在医药上的应用 |
| WO2020176763A1 (en) | 2019-02-27 | 2020-09-03 | Vertex Pharmaceuticals Incorporated | Dosage form comprising prodrug of na 1.8 sodium channel inhibitor |
| WO2020219867A1 (en) | 2019-04-25 | 2020-10-29 | Vertex Pharmaceuticals Incorporated | Pyridone amide co-crystal compositions for the treatment of pain |
| AU2020346951A1 (en) * | 2019-09-12 | 2022-04-28 | Shanghai Jeyou Pharmaceutical Co., Ltd. | Pyridine oxynitride, preparation method therefor and use thereof |
| DK4069691T3 (da) | 2019-12-06 | 2024-10-28 | Vertex Pharma | Substituerede tetrahydrofuraner som modulatorer af natriumkanaler |
| CN114437062B (zh) * | 2020-04-30 | 2024-05-17 | 成都海博为药业有限公司 | 一种可作为钠通道调节剂的化合物及其用途 |
| IL299180A (en) | 2020-06-17 | 2023-02-01 | Merck Sharp & Dohme Llc | 2-OXOIMIDAZOLIDINE-4-CARBOXAMIDES AS NAV1.8 INHIBITORS |
| JP2023530319A (ja) | 2020-06-17 | 2023-07-14 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｎａｖ１．８阻害剤としての２－オキソ－オキサゾリジン－５－カルボキサミド |
| CN113880771B (zh) * | 2020-07-03 | 2023-09-19 | 福建盛迪医药有限公司 | 一种选择性Nav抑制剂的结晶形式及其制备方法 |
| CN114031518B (zh) * | 2020-12-08 | 2023-08-18 | 成都海博为药业有限公司 | 一种苄胺或苄醇衍生物及其用途 |
| CN112225695B (zh) * | 2020-12-15 | 2021-03-02 | 上海济煜医药科技有限公司 | 一种氮氧化合物及其制备方法和用途 |
| TW202300147A (zh) * | 2021-03-11 | 2023-01-01 | 大陸商上海濟煜醫藥科技有限公司 | 吡啶氮氧化合物晶型及其應用 |
| CA3217565A1 (en) | 2021-05-07 | 2022-11-10 | Ashok Arasappan | Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors |
| JP2024520649A (ja) | 2021-06-04 | 2024-05-24 | 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 | （２ｒ，３ｓ，４ｓ，５ｒ）－４－［［３－（３，４－ジフルオロ－２－メトキシ－フェニル）－４，５－ジメチル－５－（トリフルオロメチル）テトラヒドロフラン－２－カルボニル］アミノ］ピリジン－２－カルボキサミドを含む固体剤形及び投与レジメン |
| JP2024520648A (ja) | 2021-06-04 | 2024-05-24 | 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 | ナトリウムチャネルの調節因子としての置換テトラヒドロフラン－２－カルボキサミド |
| CA3221939A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| CN117794918A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | 经取代的四氢呋喃类似物作为钠通道调节剂 |
| EP4347033A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| MA64853B1 (fr) | 2021-06-04 | 2025-11-28 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hétéro)aryl) tétrahydrofuran carboxamides utilisés en tant que modulateurs de canaux sodiques |
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| WO2014120820A1 (en) | 2014-08-07 |
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| WO2014120820A9 (en) | 2015-07-02 |
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| BR112015018284B1 (pt) | 2023-03-07 |
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| RU2658920C2 (ru) | 2018-06-26 |
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