JP7072569B2 - アシルスルホンアミドNaV1.7阻害剤 - Google Patents
アシルスルホンアミドNaV1.7阻害剤 Download PDFInfo
- Publication number
- JP7072569B2 JP7072569B2 JP2019523090A JP2019523090A JP7072569B2 JP 7072569 B2 JP7072569 B2 JP 7072569B2 JP 2019523090 A JP2019523090 A JP 2019523090A JP 2019523090 A JP2019523090 A JP 2019523090A JP 7072569 B2 JP7072569 B2 JP 7072569B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- chloro
- benzenesulfonamide
- fluoro
- thiazole
- 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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Classifications
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- 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
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
-
- 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- 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
- C07D285/06—1,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
-
- 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
-
- 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
-
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662413555P | 2016-10-27 | 2016-10-27 | |
| US62/413,555 | 2016-10-27 | ||
| PCT/US2017/058472 WO2018081384A1 (en) | 2016-10-27 | 2017-10-26 | Acyl sulfonamide nav1.7 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019536764A JP2019536764A (ja) | 2019-12-19 |
| JP2019536764A5 JP2019536764A5 (enExample) | 2020-11-19 |
| JP7072569B2 true JP7072569B2 (ja) | 2022-05-20 |
Family
ID=60245256
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019523090A Active JP7072569B2 (ja) | 2016-10-27 | 2017-10-26 | アシルスルホンアミドNaV1.7阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10836758B2 (enExample) |
| EP (1) | EP3532462B1 (enExample) |
| JP (1) | JP7072569B2 (enExample) |
| KR (1) | KR102561076B1 (enExample) |
| CN (1) | CN110088093B (enExample) |
| ES (1) | ES2897998T3 (enExample) |
| MA (1) | MA46615A (enExample) |
| WO (1) | WO2018081384A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018106284A1 (en) | 2016-12-09 | 2018-06-14 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| CA3103600A1 (en) | 2018-06-13 | 2019-12-19 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| WO2020117626A1 (en) | 2018-12-05 | 2020-06-11 | Merck Sharp & Dohme Corp. | 4-amino or 4-alkoxy-substituted aryl sulfonamide compounds with selective activity in voltage-gated sodium channels |
| 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 |
| WO2020199683A1 (zh) * | 2019-04-04 | 2020-10-08 | 上海海雁医药科技有限公司 | 氮杂环取代的磺酰基苯甲酰胺衍生物、其制法与医药上的用途 |
| WO2020248123A1 (en) | 2019-06-11 | 2020-12-17 | Merck Sharp & Dohme Corp. | Hydroxypyrrolidine-substituted arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| JP2024534364A (ja) | 2021-09-15 | 2024-09-20 | リヒター ゲデオン ニュイルヴァーノシャン ミューコェデー レースヴェーニュタールシャシャーグ | (1r,4r)-4-置換シクロヘキサン-1-アミンを生成する方法 |
| TW202530205A (zh) * | 2023-10-31 | 2025-08-01 | 加拿大商再諾製藥公司 | 經取代之芳基磺醯胺及其組合物及用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013118854A1 (ja) | 2012-02-09 | 2013-08-15 | 第一三共株式会社 | シクロアルカン誘導体 |
| JP2014532640A (ja) | 2011-10-31 | 2014-12-08 | ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. | ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用 |
| WO2015080988A1 (en) | 2013-11-29 | 2015-06-04 | Merck Sharp & Dohme Corp. | Bicycloamine-substituted-n-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels |
| WO2017106409A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| WO2017106226A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2598481B1 (en) * | 2010-07-26 | 2016-08-31 | Bristol-Myers Squibb Company | Sulfonamide compounds useful as cyp17 inhibitors |
| CA2944115A1 (en) * | 2014-03-29 | 2015-10-08 | Lupin Limited | Sulfonamide compounds as voltage gated sodium channel modulators |
| TW201718629A (zh) * | 2015-09-25 | 2017-06-01 | 韓美藥品股份有限公司 | 包含多個生理多肽及免疫球蛋白Fc區之蛋白質接合物 |
| GB201518888D0 (en) * | 2015-10-24 | 2015-12-09 | Smiths Medical Int Ltd | Medico-surgical tubes and their manufacture |
-
2017
- 2017-10-26 WO PCT/US2017/058472 patent/WO2018081384A1/en not_active Ceased
- 2017-10-26 KR KR1020197014690A patent/KR102561076B1/ko active Active
- 2017-10-26 US US16/344,414 patent/US10836758B2/en active Active
- 2017-10-26 ES ES17794203T patent/ES2897998T3/es active Active
- 2017-10-26 EP EP17794203.4A patent/EP3532462B1/en active Active
- 2017-10-26 JP JP2019523090A patent/JP7072569B2/ja active Active
- 2017-10-26 CN CN201780079199.3A patent/CN110088093B/zh active Active
- 2017-10-26 MA MA046615A patent/MA46615A/fr unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014532640A (ja) | 2011-10-31 | 2014-12-08 | ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. | ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用 |
| WO2013118854A1 (ja) | 2012-02-09 | 2013-08-15 | 第一三共株式会社 | シクロアルカン誘導体 |
| WO2015080988A1 (en) | 2013-11-29 | 2015-06-04 | Merck Sharp & Dohme Corp. | Bicycloamine-substituted-n-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels |
| WO2017106409A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| WO2017106226A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
Non-Patent Citations (1)
| Title |
|---|
| REGISTRY(STN)[online],2015年,CAS 登録番号:1798132-99-6 ほか19化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN110088093A (zh) | 2019-08-02 |
| JP2019536764A (ja) | 2019-12-19 |
| KR102561076B1 (ko) | 2023-07-28 |
| MA46615A (fr) | 2019-09-04 |
| CN110088093B (zh) | 2023-06-13 |
| US10836758B2 (en) | 2020-11-17 |
| US20200048240A1 (en) | 2020-02-13 |
| KR20190067895A (ko) | 2019-06-17 |
| EP3532462B1 (en) | 2021-10-13 |
| EP3532462A1 (en) | 2019-09-04 |
| WO2018081384A1 (en) | 2018-05-03 |
| ES2897998T3 (es) | 2022-03-03 |
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