BR112018012327A2 - compostos de diamina-arilsulfonamida substituídos com hidroxialquilamina e hidroxicicloalquilamina com atividade seletiva em canais de sódio ativados por voltagem - Google Patents
compostos de diamina-arilsulfonamida substituídos com hidroxialquilamina e hidroxicicloalquilamina com atividade seletiva em canais de sódio ativados por voltagemInfo
- Publication number
- BR112018012327A2 BR112018012327A2 BR112018012327A BR112018012327A BR112018012327A2 BR 112018012327 A2 BR112018012327 A2 BR 112018012327A2 BR 112018012327 A BR112018012327 A BR 112018012327A BR 112018012327 A BR112018012327 A BR 112018012327A BR 112018012327 A2 BR112018012327 A2 BR 112018012327A2
- Authority
- BR
- Brazil
- Prior art keywords
- hydroxycycloalkylamine
- hydroxyalkylamine
- voltage
- sodium channels
- compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D277/38—Nitrogen atoms
- C07D277/50—Nitrogen atoms bound to hetero atoms
- C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Abstract
são descritos compostos de fórmula a, ou um sal dos mesmos: fórmula (a) em que r1, r2 e e são aqui definidos, cujos compostos têm propriedades para inibir os canais de íons nav 1.7 encontrados nos neurônios periféricos e simpáticos. também são descritas formulações farmacêuticas compreendendo os compostos de fórmula a ou seus sais e métodos de tratamento de distúrbios de dor, tosse e coceira usando os mesmos.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562269327P | 2015-12-18 | 2015-12-18 | |
US201662290235P | 2016-02-02 | 2016-02-02 | |
US201662420956P | 2016-11-11 | 2016-11-11 | |
PCT/US2016/066445 WO2017106226A1 (en) | 2015-12-18 | 2016-12-14 | Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112018012327A2 true BR112018012327A2 (pt) | 2018-12-04 |
Family
ID=57708830
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018012327A BR112018012327A2 (pt) | 2015-12-18 | 2016-12-14 | compostos de diamina-arilsulfonamida substituídos com hidroxialquilamina e hidroxicicloalquilamina com atividade seletiva em canais de sódio ativados por voltagem |
Country Status (27)
Country | Link |
---|---|
US (2) | US10221167B2 (pt) |
EP (1) | EP3390374B1 (pt) |
JP (1) | JP6572392B2 (pt) |
KR (1) | KR20180095598A (pt) |
CN (1) | CN108699015A (pt) |
AR (1) | AR106987A1 (pt) |
AU (1) | AU2016370554B2 (pt) |
BR (1) | BR112018012327A2 (pt) |
CA (1) | CA3008611A1 (pt) |
CL (1) | CL2018001640A1 (pt) |
CO (1) | CO2018006137A2 (pt) |
CR (1) | CR20180322A (pt) |
DO (1) | DOP2018000150A (pt) |
EA (1) | EA201891313A1 (pt) |
EC (1) | ECSP18052850A (pt) |
HK (1) | HK1255027A1 (pt) |
IL (1) | IL260052A (pt) |
MX (1) | MX2018007450A (pt) |
NI (1) | NI201800067A (pt) |
PE (1) | PE20181495A1 (pt) |
PH (1) | PH12018501288A1 (pt) |
SG (1) | SG11201804936UA (pt) |
SV (1) | SV2018005708A (pt) |
TN (1) | TN2018000195A1 (pt) |
TW (1) | TW201726637A (pt) |
WO (1) | WO2017106226A1 (pt) |
ZA (1) | ZA201803591B (pt) |
Families Citing this family (14)
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TWI773657B (zh) | 2015-12-18 | 2022-08-11 | 美商亞德利克斯公司 | 作爲非全身tgr5促效劑之經取代之4-苯基吡啶化合物 |
US10519147B2 (en) * | 2015-12-18 | 2019-12-31 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
JP6572392B2 (ja) * | 2015-12-18 | 2019-09-11 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | 電位作動型ナトリウムチャネルにおいて選択的活性を有する、ヒドロキシアルキルアミンおよびヒドロキシシクロアルキルアミンで置換されたジアミン−アリールスルホンアミド化合物 |
EP3526205A4 (en) | 2016-10-17 | 2020-05-27 | Genentech, Inc. | THERAPEUTIC CONNECTIONS AND METHOD FOR USE THEREOF |
JP7072569B2 (ja) * | 2016-10-27 | 2022-05-20 | ブリストル-マイヤーズ スクイブ カンパニー | アシルスルホンアミドNaV1.7阻害剤 |
WO2018093694A1 (en) * | 2016-11-17 | 2018-05-24 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
US10793550B2 (en) | 2017-03-24 | 2020-10-06 | 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 |
EP3774801A1 (en) | 2018-03-30 | 2021-02-17 | F. Hoffmann-La Roche AG | Fused ring hydro-pyrido compounds as sodium channel inhibitors |
EP3844150A1 (en) | 2018-08-31 | 2021-07-07 | Xenon Pharmaceuticals Inc. | Heteroaryl-substituted sulfonamide compounds and their use as therapeutic agents |
CN111285825B (zh) * | 2018-12-10 | 2023-02-17 | 中国科学院上海药物研究所 | 一类苯磺酰胺取代的衍生物,其制法及其用途 |
WO2020248123A1 (en) * | 2019-06-11 | 2020-12-17 | Merck Sharp & Dohme Corp. | Hydroxypyrrolidine-substituted arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
CN113527281B (zh) * | 2020-04-20 | 2023-12-22 | 昆山彭济凯丰生物科技有限公司 | 杂环化合物及其制备方法和应用 |
CN117362206B (zh) * | 2023-12-08 | 2024-02-20 | 四川大学华西第二医院 | 一类芳基磺酰胺类化合物、合成方法及用途 |
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JP6572392B2 (ja) * | 2015-12-18 | 2019-09-11 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | 電位作動型ナトリウムチャネルにおいて選択的活性を有する、ヒドロキシアルキルアミンおよびヒドロキシシクロアルキルアミンで置換されたジアミン−アリールスルホンアミド化合物 |
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-
2016
- 2016-12-14 JP JP2018531094A patent/JP6572392B2/ja not_active Expired - Fee Related
- 2016-12-14 TN TNP/2018/000195A patent/TN2018000195A1/en unknown
- 2016-12-14 CR CR20180322A patent/CR20180322A/es unknown
- 2016-12-14 KR KR1020187020090A patent/KR20180095598A/ko active IP Right Grant
- 2016-12-14 AR ARP160103829A patent/AR106987A1/es unknown
- 2016-12-14 WO PCT/US2016/066445 patent/WO2017106226A1/en active Application Filing
- 2016-12-14 US US15/378,465 patent/US10221167B2/en active Active
- 2016-12-14 EP EP16820497.2A patent/EP3390374B1/en active Active
- 2016-12-14 TW TW105141337A patent/TW201726637A/zh unknown
- 2016-12-14 PE PE2018001100A patent/PE20181495A1/es unknown
- 2016-12-14 CA CA3008611A patent/CA3008611A1/en not_active Abandoned
- 2016-12-14 BR BR112018012327A patent/BR112018012327A2/pt not_active Application Discontinuation
- 2016-12-14 CN CN201680081234.0A patent/CN108699015A/zh active Pending
- 2016-12-14 EA EA201891313A patent/EA201891313A1/ru unknown
- 2016-12-14 MX MX2018007450A patent/MX2018007450A/es unknown
- 2016-12-14 AU AU2016370554A patent/AU2016370554B2/en not_active Ceased
- 2016-12-14 SG SG11201804936UA patent/SG11201804936UA/en unknown
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2018
- 2018-05-30 ZA ZA2018/03591A patent/ZA201803591B/en unknown
- 2018-06-12 NI NI201800067A patent/NI201800067A/es unknown
- 2018-06-13 SV SV2018005708A patent/SV2018005708A/es unknown
- 2018-06-14 IL IL260052A patent/IL260052A/en unknown
- 2018-06-14 PH PH12018501288A patent/PH12018501288A1/en unknown
- 2018-06-15 CL CL2018001640A patent/CL2018001640A1/es unknown
- 2018-06-15 CO CONC2018/0006137A patent/CO2018006137A2/es unknown
- 2018-06-18 DO DO2018000150A patent/DOP2018000150A/es unknown
- 2018-07-12 EC ECSENADI201852850A patent/ECSP18052850A/es unknown
- 2018-11-06 HK HK18114148.2A patent/HK1255027A1/zh unknown
-
2019
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US20170174674A1 (en) | 2017-06-22 |
PE20181495A1 (es) | 2018-09-18 |
US20190233406A1 (en) | 2019-08-01 |
EP3390374A1 (en) | 2018-10-24 |
TW201726637A (zh) | 2017-08-01 |
AR106987A1 (es) | 2018-03-07 |
ECSP18052850A (es) | 2018-12-31 |
TN2018000195A1 (en) | 2019-10-04 |
KR20180095598A (ko) | 2018-08-27 |
EA201891313A1 (ru) | 2018-11-30 |
EP3390374B1 (en) | 2020-08-26 |
CO2018006137A2 (es) | 2018-07-10 |
WO2017106226A1 (en) | 2017-06-22 |
CN108699015A (zh) | 2018-10-23 |
CR20180322A (es) | 2018-08-21 |
IL260052A (en) | 2018-07-31 |
SG11201804936UA (en) | 2018-07-30 |
SV2018005708A (es) | 2018-12-14 |
NI201800067A (es) | 2018-07-24 |
ZA201803591B (en) | 2019-04-24 |
CL2018001640A1 (es) | 2018-08-03 |
US10221167B2 (en) | 2019-03-05 |
CA3008611A1 (en) | 2017-06-22 |
MX2018007450A (es) | 2018-11-14 |
AU2016370554A1 (en) | 2018-06-14 |
JP6572392B2 (ja) | 2019-09-11 |
AU2016370554B2 (en) | 2018-11-29 |
JP2019502681A (ja) | 2019-01-31 |
DOP2018000150A (es) | 2018-07-31 |
PH12018501288A1 (en) | 2019-01-28 |
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