AR082152A1 - Derivados de n-(metilsulfonil)benzamida, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de nav1.7 - Google Patents
Derivados de n-(metilsulfonil)benzamida, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de nav1.7Info
- Publication number
- AR082152A1 AR082152A1 ARP110102489A ARP110102489A AR082152A1 AR 082152 A1 AR082152 A1 AR 082152A1 AR P110102489 A ARP110102489 A AR P110102489A AR P110102489 A ARP110102489 A AR P110102489A AR 082152 A1 AR082152 A1 AR 082152A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- independently
- cycloalkyl
- alkyl
- het1
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 title 2
- 101000654386 Homo sapiens Sodium channel protein type 9 subunit alpha Proteins 0.000 title 1
- 102100031367 Sodium channel protein type 9 subunit alpha Human genes 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 229940124777 Nav1.7 inhibitor Drugs 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- 150000003456 sulfonamides Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
- C07C311/51—Y being a hydrogen or a carbon atom
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Derivados de sulfonamida, su uso en medicina, composiciones que los contienen. Los inhibidores de Nav1.7. se utilizan en el tratamiento de un amplio rango de trastornos, en particular, del dolor.Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una sal de este farmacéuticamente aceptable, en donde X es O, S, NH o CH2; Ar1 es (i) naftilo; o (ii) naftilo o fenilo, cada uno de los cuales se sustituye, independientemente, con 1 a 3 Y; Y es F; Cl; CN; alquilo C1-8, opcionalmente sustituido con cicloalquilo C3-8 y/o, si lo permite la valencia, con 1 a 8 F; cicloalquilo C3-8, opcionalmente sustituido, si lo permite la valencia, con 1 a 8 F; NR7R8, alquiloxi C1-8, opcionalmente sustituido, de forma independiente, con 1 a 3 R9, o si lo permite la valencia, con 1 a 8 F; cicloalquiloxi C3-8; fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R10; Het1 y Het2; en donde cicloalquiloxi C3-8 puede fusionarse opcionalmente a un anillo de fenilo o puede sustituirse, en forma independiente, con 1 a 3 R10; R1 es alquilo C1-6 o cicloalquilo C3-8, cada uno de los cuales se sustituye opcionalmente, si lo permite la valencia, con 1 a 8 F; R2, R3, R4 son, independientemente, H, F, Cl u -OCH3; R5 es H, CN, F, Cl o R6; R6 es un grupo seleccionado de alquilo C1-6 y alquiloxi C1-6, en donde cada grupo se sustituye, opcionalmente, si lo permite la valencia, con 1 a 8 F; R7 y R8 son, independientemente, H; alquilo C1-8, opcionalmente sustituido, en forma independiente, con 1 a 3 R11; cicloalquilo C3-8; o Het1 “unido a C”; en donde cicloalquilo C3-8 puede fusionarse opcionalmente a un anillo de fenilo o puede sustituirse, en forma independiente, con 1 a 3 R10; o R7 y R8, junto con el átomo de nitrógeno al que están unidos, forman un anillo de 7 a 9 miembros en puente, saturado; R9 es alquiloxi C1-6; cicloalquilo C3-8, opcionalmente sustituido, si lo permite la valencia, con 1 a 8 F; Het1 o fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R6; R10 es F, Cl o R6; R11 es F; alquiloxi C1-6; cicloalquilo C3-8, opcionalmente sustituido, silo permite la valencia, con 1 a 8 F; Het1 “unido a C”; o fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R6; Het1 es un monoheterocicloalquilo saturado de 3 a 8 miembros que comprende 1 ó 2 miembros del anillo seleccionados de -NR12- y -O-, en donde dicho monoheterocicloalquilo se sustituye, opcionalmente, en un átomo de carbono del anillo con 1 a 3 sustituyentes seleccionados, independientemente, de F, alquilo C1-6, alquiloxi C1-4-alquileno C0-4 y cicloalquilo C3-8; Het2 es un heteroarilo de 5 ó 6 miembros que comprende de 1 a 3 átomos de nitrógeno, en donde dicho heteroarilo se sustituye, opcionalmente, con 1 a 3 sustituyentes seleccionados de F, Cl, CN y R6; y R12 es H, alquilo C1-6 o cicloalquilo C3-8, en donde alquilo C1-6 y cicloalquilo C3-8 se sustituye, opcionalmente, si lo permite la valencia, con 1 a 8 F; o, cuando Het1 está “unido a N”, está ausente.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36335510P | 2010-07-12 | 2010-07-12 | |
| US201161473287P | 2011-04-08 | 2011-04-08 | |
| US201161488972P | 2011-05-23 | 2011-05-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082152A1 true AR082152A1 (es) | 2012-11-14 |
Family
ID=45439021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110102489A AR082152A1 (es) | 2010-07-12 | 2011-07-11 | Derivados de n-(metilsulfonil)benzamida, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de nav1.7 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8685977B2 (es) |
| EP (1) | EP2593427B1 (es) |
| JP (1) | JP2013536165A (es) |
| AR (1) | AR082152A1 (es) |
| CA (1) | CA2804877A1 (es) |
| ES (1) | ES2532357T3 (es) |
| TW (1) | TW201216956A (es) |
| UY (1) | UY33500A (es) |
| WO (1) | WO2012007883A1 (es) |
Families Citing this family (33)
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| ES2526675T3 (es) | 2010-07-09 | 2015-01-14 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje |
| JP5872552B2 (ja) | 2010-07-09 | 2016-03-01 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化学化合物 |
| WO2012004743A1 (en) | 2010-07-09 | 2012-01-12 | Pfizer Limited | Benzenesulfonamides useful as sodium channel inhibitors |
| EP2593431B1 (en) | 2010-07-12 | 2014-11-19 | Pfizer Limited | N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels |
| EP2593428B1 (en) | 2010-07-12 | 2014-11-19 | Pfizer Limited | N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels |
| CA2804351A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Chemical compounds |
| JP2013532184A (ja) * | 2010-07-12 | 2013-08-15 | ファイザー・リミテッド | 電位開口型ナトリウムチャネル阻害剤として有用なｎ−スルホニルベンズアミド誘導体 |
| MX2014005304A (es) | 2011-10-31 | 2015-03-20 | Xenon Pharmaceuticals Inc | Biaril eter sulfonamidas y su uso como agentes terapeuticos. |
| ES2586213T3 (es) | 2011-10-31 | 2016-10-13 | Xenon Pharmaceuticals Inc. | Compuestos de bencenosulfonamida y su uso como agentes terapéuticos |
| CA2860553C (en) * | 2012-01-04 | 2016-08-23 | Pfizer Limited | N-aminosulfonyl benzamides |
| CA2874621A1 (en) | 2012-05-22 | 2013-11-28 | Genentech, Inc. | N-substituted benzamides and their use in the treatment of pain |
| US10071957B2 (en) | 2012-07-06 | 2018-09-11 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
| AU2013334664A1 (en) | 2012-10-26 | 2015-05-07 | Merck Sharp & Dohme Corp. | N-substituted indazole sulfonamide compounds with selective activity in voltage-gated sodium channels |
| CN105263490B (zh) | 2013-03-14 | 2018-05-22 | 基因泰克公司 | 取代的三唑并吡啶及其使用方法 |
| CA2898680A1 (en) | 2013-03-15 | 2014-09-18 | Genentech,Inc. | Substituted benzoxazoles and methods of use thereof |
| US10179781B2 (en) * | 2013-03-15 | 2019-01-15 | Chromocell Corporation | Sodium channel modulators for the treatment of pain |
| CN105611923B (zh) | 2013-09-10 | 2019-08-23 | 卓莫赛尔公司 | 用于治疗疼痛和糖尿病的钠通道调节剂 |
| JP6383418B2 (ja) | 2013-11-27 | 2018-08-29 | ジェネンテック， インコーポレイテッド | 置換ベンズアミド及びその使用方法 |
| CN106715418A (zh) | 2014-07-07 | 2017-05-24 | 基因泰克公司 | 治疗化合物及其使用方法 |
| WO2016145032A1 (en) * | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Compositions for use in treating pulmonary arterial hypertension |
| MA42118A (fr) | 2015-05-22 | 2018-03-28 | Genentech Inc | Benzamides substitués et leurs méthodes d'utilisation |
| WO2017035271A1 (en) | 2015-08-27 | 2017-03-02 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| JP6987746B2 (ja) | 2015-09-28 | 2022-01-05 | ジェネンテック， インコーポレイテッド | 治療用化合物及びその使用方法 |
| US10899732B2 (en) | 2015-11-25 | 2021-01-26 | Genentech, Inc. | Substituted benzamides useful as sodium channel blockers |
| US20170239183A1 (en) * | 2016-02-23 | 2017-08-24 | PixarBio Corporation | COMPOSITIONS COMPRISING NAv1.7 SELECTIVE INHIBITORS FOR TREATING ACUTE, POST-OPERATIVE, OR CHRONIC PAIN AND METHODS OF USING THE SAME |
| US10766858B2 (en) | 2016-03-30 | 2020-09-08 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| BR112019007763A2 (pt) | 2016-10-17 | 2019-07-02 | Genentech Inc | composto de fórmula, composição farmacêutica, métodos para tratar uma doença ou condição, para tratar dores, para diminuir o fluxo de íons e para tratar prurido, uso de um composto e invenção |
| EP3601273B1 (en) | 2017-03-24 | 2021-12-01 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| AR114263A1 (es) | 2018-02-26 | 2020-08-12 | Genentech Inc | Compuestos terapéuticos y métodos para utilizarlos |
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| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| US12533341B2 (en) | 2019-12-11 | 2026-01-27 | Duke University | Small molecule inhibitors of voltage-gated sodium channel 1.7 and methods of using same |
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-
2011
- 2011-07-07 EP EP11748997.1A patent/EP2593427B1/en not_active Not-in-force
- 2011-07-07 ES ES11748997.1T patent/ES2532357T3/es active Active
- 2011-07-07 CA CA2804877A patent/CA2804877A1/en not_active Abandoned
- 2011-07-07 JP JP2013519195A patent/JP2013536165A/ja not_active Withdrawn
- 2011-07-07 WO PCT/IB2011/053030 patent/WO2012007883A1/en not_active Ceased
- 2011-07-11 UY UY0001033500A patent/UY33500A/es not_active Application Discontinuation
- 2011-07-11 US US13/179,585 patent/US8685977B2/en not_active Expired - Fee Related
- 2011-07-11 AR ARP110102489A patent/AR082152A1/es not_active Application Discontinuation
- 2011-07-11 TW TW100124486A patent/TW201216956A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8685977B2 (en) | 2014-04-01 |
| UY33500A (es) | 2012-02-29 |
| US20120010207A1 (en) | 2012-01-12 |
| EP2593427A1 (en) | 2013-05-22 |
| CA2804877A1 (en) | 2012-01-19 |
| WO2012007883A1 (en) | 2012-01-19 |
| JP2013536165A (ja) | 2013-09-19 |
| ES2532357T3 (es) | 2015-03-26 |
| TW201216956A (en) | 2012-05-01 |
| EP2593427B1 (en) | 2014-12-24 |
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