AR112187A1 - 2-OXO-BENZO [D] OXAZOL-6-SULFONAMIDE COMPOSITION, INCLUDING PHARMACEUTICAL COMPOSITION AND ITS USE IN THE MANUFACTURE OF A MEDICINAL - Google Patents
2-OXO-BENZO [D] OXAZOL-6-SULFONAMIDE COMPOSITION, INCLUDING PHARMACEUTICAL COMPOSITION AND ITS USE IN THE MANUFACTURE OF A MEDICINALInfo
- Publication number
- AR112187A1 AR112187A1 ARP180101214A AR112187A1 AR 112187 A1 AR112187 A1 AR 112187A1 AR P180101214 A ARP180101214 A AR P180101214A AR 112187 A1 AR112187 A1 AR 112187A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- substituted
- halo
- optionally substituted
- alkyl
- Prior art date
Links
Classifications
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- 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
- C07D417/14—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 three or more hetero 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Una composición farmacéutica que lo comprende: junto con al menos un excipiente farmacéuticamente aceptable. Uso del compuesto o de una sal farmacéuticamente aceptable del mismo o de la composición farmacéutica para la fabricación de un medicamento para su uso en el tratamiento del dolor. El compuesto descrito inhibe la actividad de Nav1,7, siendo de utilidad para su uso en terapia para el tratamiento de enfermedades mediadas por la actividad de Nav1,7. Reivindicación 1: Un compuesto de 2-oxo-benzo[d]oxazol-6-sulfonamida caracterizado porque es de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde, R¹ se selecciona entre el grupo que consiste en: i) ciclopropilo sustituido con piperidinilo o alquilo C₁₋₃; donde: el alquilo C₁₋₃, está sustituido con piperidinilo o NH₂; ii) fenilo sustituido con (CH₂)ₘNRˣRʸ; donde: m es 1 ó 2, Rˣ es H o metilo; Rʸ es H, metilo, CH₂CH₂OH, CH₂COOH o CH₂CH₂NH₂; iii) fenilo sustituido con metilo; donde: el metilo está sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo que consiste en OH, halo, CH₂NH₂ y morfolinilo; iv) fenilo sustituido con heterocicloalquilo de 4 a 6 miembros; donde: el heterocicloalquilo está opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en metilo, halo y metoxi; v) fenilo sustituido con dos sustituyentes seleccionados independientemente entre el grupo que consiste en halo y alquilo C₁₋₃; donde: el alquilo C₁₋₃ está opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en NH₂, N(CH₃)₂ y NHCH₂(C=O)NH₂; vi) fenilo sustituido con tetrahidropiridinilo; donde: el tetrahidropiridinilo está opcionalmente sustituido con metilo; vii) tetrahidroisoquinolinilo; donde: el tetrahidroisoquinolinilo está opcionalmente sustituido con metilo; viii) tetrahidronaftalenilo; donde: el tetrahidronaftalenilo; está opcionalmente sustituido con NH₂ u OH; R² es H o halo y R³ es H o halo; donde: uno de R² y R³ es H y el otro es halo; R⁴ es metilo o H; y Het es heteroarilo de 5 ó 6 miembros que comprende de 1 a 3 heteroátomos seleccionados entre N, S y O; y donde: el heteroarilo está opcionalmente sustituido con un sustituyente seleccionado entre halógeno, alquilo C₁₋₃ y CN.A pharmaceutical composition comprising it: together with at least one pharmaceutically acceptable excipient. Use of the compound or of a pharmaceutically acceptable salt thereof or of the pharmaceutical composition for the manufacture of a medicament for use in the treatment of pain. The described compound inhibits the activity of Nav1.7, being useful for use in therapy for the treatment of diseases mediated by the activity of Nav1.7. Claim 1: A 2-oxo-benzo [d] oxazole-6-sulfonamide compound characterized in that it is of formula (1) or a pharmaceutically acceptable salt thereof, wherein, R¹ is selected from the group consisting of: i ) cyclopropyl substituted with piperidinyl or C₁₋₃ alkyl; where: C₁₋₃ alkyl, is substituted with piperidinyl or NH₂; ii) phenyl substituted with (CH₂) ₘNRˣRʸ; where: m is 1 or 2, Rˣ is H or methyl; Rʸ is H, methyl, CH₂CH₂OH, CH₂COOH or CH₂CH₂NH₂; iii) phenyl substituted with methyl; where: methyl is substituted with one to three substituents independently selected from the group consisting of OH, halo, CH₂NH₂, and morpholinyl; iv) phenyl substituted with 4- to 6-membered heterocycloalkyl; where: the heterocycloalkyl is optionally substituted with a substituent selected from the group consisting of methyl, halo, and methoxy; v) phenyl substituted with two substituents independently selected from the group consisting of halo and C₁₋₃ alkyl; where: the C₁₋₃ alkyl is optionally substituted with a substituent selected from the group consisting of NH₂, N (CH₃) ₂, and NHCH₂ (C = O) NH₂; vi) phenyl substituted with tetrahydropyridinyl; where: tetrahydropyridinyl is optionally substituted with methyl; vii) tetrahydroisoquinolinyl; where: tetrahydroisoquinolinyl is optionally substituted with methyl; viii) tetrahydronaphthalenyl; where: tetrahydronaphthalenyl; is optionally substituted with NH₂ or OH; R² is H or halo and R³ is H or halo; where: one of R² and R³ is H and the other is halo; R⁴ is methyl or H; and Het is 5- or 6-membered heteroaryl comprising 1 to 3 heteroatoms selected from N, S, and O; and where: the heteroaryl is optionally substituted with a substituent selected from halogen, C₁₋₃ alkyl and CN.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017083938 | 2017-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112187A1 true AR112187A1 (en) | 2019-10-02 |
Family
ID=64104337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101214 AR112187A1 (en) | 2017-05-11 | 2018-05-09 | 2-OXO-BENZO [D] OXAZOL-6-SULFONAMIDE COMPOSITION, INCLUDING PHARMACEUTICAL COMPOSITION AND ITS USE IN THE MANUFACTURE OF A MEDICINAL |
Country Status (4)
| Country | Link |
|---|---|
| AR (1) | AR112187A1 (en) |
| TW (1) | TW201908310A (en) |
| UY (1) | UY37729A (en) |
| WO (1) | WO2018205948A1 (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020199683A1 (en) * | 2019-04-04 | 2020-10-08 | 上海海雁医药科技有限公司 | Nitrogen heterocycle substituted sulfonylbenzamide derivative, preparation method therefor and use thereof in medicine |
| AU2020335426A1 (en) | 2019-08-23 | 2022-03-10 | Mochida Pharmaceutical Co., Ltd. | Method for producing heterocyclidene acetamide derivative |
| WO2021039023A1 (en) | 2019-08-23 | 2021-03-04 | 持田製薬株式会社 | Method for producing heterocyclidene acetamide derivatives |
| CN112028816B (en) * | 2020-09-11 | 2022-10-14 | 江阴迈康升华医药科技有限公司 | Synthesis method of substituted isoindoline |
| WO2023028056A1 (en) | 2021-08-24 | 2023-03-02 | Genentech, Inc. | 3-amino piperidyl sodium channel inhibitors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2427441T3 (en) * | 2009-05-04 | 2017-03-20 | Agios Pharmaceuticals Inc | PKM2 Activators for use in the treatment of cancer |
| KR20140095067A (en) * | 2011-10-28 | 2014-07-31 | 머크 샤프 앤드 돔 코포레이션 | Benzoxazolinone compounds with selective activity in voltage-gated sodium channels |
| US9624208B2 (en) * | 2012-10-26 | 2017-04-18 | Merck Sharp & Dohme Corp. | Benzoxazolinone compounds with selective activity in voltage-gated sodium channels |
-
2018
- 2018-05-09 WO PCT/CN2018/086131 patent/WO2018205948A1/en active Application Filing
- 2018-05-09 AR ARP180101214 patent/AR112187A1/en unknown
- 2018-05-09 TW TW107115678A patent/TW201908310A/en unknown
- 2018-05-09 UY UY0001037729A patent/UY37729A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY37729A (en) | 2019-01-02 |
| TW201908310A (en) | 2019-03-01 |
| WO2018205948A1 (en) | 2018-11-15 |
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| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |