PE20241726A1 - Compuestos n-acilhidrazonicos inhibidores de nav 1.7 y/o nav 1.8, sus procesos de obtencion, composiciones, usos, metodos de tratamiento de estos y kits - Google Patents
Compuestos n-acilhidrazonicos inhibidores de nav 1.7 y/o nav 1.8, sus procesos de obtencion, composiciones, usos, metodos de tratamiento de estos y kitsInfo
- Publication number
- PE20241726A1 PE20241726A1 PE2024000187A PE2024000187A PE20241726A1 PE 20241726 A1 PE20241726 A1 PE 20241726A1 PE 2024000187 A PE2024000187 A PE 2024000187A PE 2024000187 A PE2024000187 A PE 2024000187A PE 20241726 A1 PE20241726 A1 PE 20241726A1
- Authority
- PE
- Peru
- Prior art keywords
- nav
- branched
- alkyl
- linear
- compound
- Prior art date
Links
Classifications
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- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
- A61K31/175—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine having the group, >N—C(O)—N=N— or, e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazones; Thioanalogues 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- 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]
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
- C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
- C07D241/30—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms in which said hetero-bound carbon atoms are part of a substructure —C(=X)—X—C(=X)—X— in which X is an oxygen or sulphur atom or an imino radical, e.g. imidoylguanidines
- C07D241/32—(Amino-pyrazinoyl) guanidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Liquid Crystal Substances (AREA)
Abstract
Se refiere a compuestos n-acilhidrazonicos de formula I, o una sal, hidrato, solvato, y un isomero del mismo farmaceuticamente aceptable, donde R1 es H, halogeno, alquilo C1-6 ramificado o recto, entre otros; R2 y R3 se selecciona independientemente de H, halogeno, alquilo C1-C6 lineal o ramificado, entre otros; R4 es H, halogeno, alquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, entre otros; R5 y R6 se seleccionan independientemente entre H y alquilo C1-6 lineal o ramificado. Un compuesto seleccionado es 6-(4-clorofenil)-N'-[(E)-(3,5-dimetoxifenil)metilideno]pirazina-2-carbohidrazida (Compuesto 1). Estos compuestos son inhibidores selectivos de canales de sodio dependientes de voltaje Nav 1.7 y/o Nav 1.8. Tambien se refiere a procedimientos de obtencion, a una composicion farmaceutica que comprende dicho compuesto, y su uso para tratar o prevenir patologias relacionadas con el dolor.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163228472P | 2021-08-02 | 2021-08-02 | |
| PCT/BR2022/050303 WO2023010191A1 (pt) | 2021-08-02 | 2022-08-02 | Compostos n-acilidrazônicos inibidores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20241726A1 true PE20241726A1 (es) | 2024-08-19 |
Family
ID=85153925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2024000187A PE20241726A1 (es) | 2021-08-02 | 2022-08-02 | Compuestos n-acilhidrazonicos inhibidores de nav 1.7 y/o nav 1.8, sus procesos de obtencion, composiciones, usos, metodos de tratamiento de estos y kits |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20240335442A1 (es) |
| EP (1) | EP4382100A1 (es) |
| JP (1) | JP2024528214A (es) |
| KR (1) | KR20240105362A (es) |
| CN (1) | CN118076348A (es) |
| AR (1) | AR126669A1 (es) |
| BR (1) | BR112024002228A2 (es) |
| CA (1) | CA3227730A1 (es) |
| CO (1) | CO2024002075A2 (es) |
| IL (1) | IL310568A (es) |
| MX (1) | MX2024001692A (es) |
| PE (1) | PE20241726A1 (es) |
| UY (1) | UY39881A (es) |
| WO (1) | WO2023010191A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR131690A1 (es) * | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS |
| WO2024159285A1 (pt) * | 2023-01-30 | 2024-08-08 | Eurofarma Laboratórios S.A. | Compostos aril piridinas bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3573306A (en) * | 1969-03-05 | 1971-03-30 | Merck & Co Inc | Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides |
| WO2003103665A1 (ja) * | 2002-06-06 | 2003-12-18 | 株式会社医薬分子設計研究所 | 抗アレルギー薬 |
| KR20060019558A (ko) * | 2003-05-27 | 2006-03-03 | 바스프 악티엔게젤샤프트 | 유해 곤충류 및 거미류의 방제를 위한 히드라존 유도체 |
| US7928107B2 (en) | 2004-09-02 | 2011-04-19 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7786139B2 (en) * | 2006-11-21 | 2010-08-31 | Omeros Corporation | PDE10 inhibitors and related compositions and methods |
| US20100035932A1 (en) * | 2008-08-07 | 2010-02-11 | Schepetkin Igor A | Novel formyl peptide receptor like 1 agonists that induce macrophage tumor necrosis factor alpha and computational structure-activity relationship analysis of thereof |
| CA2771472A1 (en) | 2009-09-04 | 2011-03-10 | Zalicus Pharmaceuticals Ltd. | Oxopiperazine derivatives for the treatment of pain and epilepsy |
| US8518968B2 (en) * | 2009-12-04 | 2013-08-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Hydrazone and diacyl hydrazine compounds and methods of use |
| EP2593434A1 (en) | 2010-07-16 | 2013-05-22 | Purdue Pharma LP | Pyridine compounds as sodium channel blockers |
| WO2013123071A1 (en) * | 2012-02-13 | 2013-08-22 | Cleave Biosciences, Inc. | Methods and compositions for jamm protease inhibition |
| CN103880707B (zh) * | 2012-12-19 | 2016-04-13 | 上海交通大学医学院 | Stat3小分子抑制剂及其应用 |
| AU2014212509B2 (en) | 2013-01-31 | 2018-05-10 | Vertex Pharmaceuticals Incorporated | Pyridone amides as modulators of sodium channels |
| EP2951168B1 (en) | 2013-01-31 | 2017-01-04 | Vertex Pharmaceuticals Incorporated | Quinoline and quinoxaline amides as modulators of sodium channels |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| SG11201600082VA (en) | 2013-07-10 | 2016-02-26 | Vertex Pharma | Fused piperidine amides as modulators of ion channels |
| US9163042B2 (en) | 2013-12-13 | 2015-10-20 | Vertex Pharmaceuticals Incorporated | Prodrugs of pyridone amides useful as modulators of sodium channels |
| CN105481765A (zh) * | 2015-04-15 | 2016-04-13 | 江苏艾凡生物医药有限公司 | 一类用于治疗心力衰竭的酰腙类衍生物 |
| JP2017001991A (ja) | 2015-06-11 | 2017-01-05 | 大日本住友製薬株式会社 | 新規ベンズオキサゾロン化合物 |
| JP2019514879A (ja) | 2016-04-20 | 2019-06-06 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | アシルスルホンアミドNaV1.7阻害剤 |
| KR102714561B1 (ko) | 2017-05-16 | 2024-10-10 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 중수소화 피리돈 아미드 및 이의 프로드럭 |
| MX393803B (es) | 2017-06-20 | 2025-03-24 | Raqualia Pharma Inc | Derivados de amida como bloqueadores de nav1.7 y nav1.8 |
| TW201920081A (zh) | 2017-07-11 | 2019-06-01 | 美商維泰克斯製藥公司 | 作為鈉通道調節劑的羧醯胺 |
| WO2020023802A1 (en) * | 2018-07-25 | 2020-01-30 | City Of Hope | Parg inhibitors and method of use thereof |
| GEP20237568B (en) | 2018-11-02 | 2023-11-27 | Merck Sharp & Dohme Llc | 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors |
| EP3894392A4 (en) * | 2018-12-11 | 2022-08-24 | Duke University | COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER |
| CN110128343A (zh) * | 2019-06-18 | 2019-08-16 | 四川省人民医院 | 一种酰肼类化合物 |
| BR112021026395A2 (pt) | 2019-06-27 | 2022-02-08 | Glaxosmithkline Ip Dev Ltd | Compostos de 2,3-di-hidroquinazolina como inibidores de nav1.8 |
-
2022
- 2022-08-01 AR ARP220102052A patent/AR126669A1/es not_active Application Discontinuation
- 2022-08-01 UY UY0001039881A patent/UY39881A/es unknown
- 2022-08-02 IL IL310568A patent/IL310568A/en unknown
- 2022-08-02 PE PE2024000187A patent/PE20241726A1/es unknown
- 2022-08-02 WO PCT/BR2022/050303 patent/WO2023010191A1/pt not_active Ceased
- 2022-08-02 JP JP2024506677A patent/JP2024528214A/ja active Pending
- 2022-08-02 BR BR112024002228A patent/BR112024002228A2/pt unknown
- 2022-08-02 US US18/294,976 patent/US20240335442A1/en active Pending
- 2022-08-02 MX MX2024001692A patent/MX2024001692A/es unknown
- 2022-08-02 EP EP22851497.2A patent/EP4382100A1/en not_active Withdrawn
- 2022-08-02 KR KR1020247007069A patent/KR20240105362A/ko active Pending
- 2022-08-02 CA CA3227730A patent/CA3227730A1/en active Pending
- 2022-08-02 CN CN202280065832.4A patent/CN118076348A/zh active Pending
-
2024
- 2024-02-23 CO CONC2024/0002075A patent/CO2024002075A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2024001692A (es) | 2024-04-30 |
| US20240335442A1 (en) | 2024-10-10 |
| EP4382100A1 (en) | 2024-06-12 |
| JP2024528214A (ja) | 2024-07-26 |
| KR20240105362A (ko) | 2024-07-05 |
| BR112024002228A2 (pt) | 2024-04-30 |
| CN118076348A (zh) | 2024-05-24 |
| CA3227730A1 (en) | 2023-02-09 |
| UY39881A (es) | 2023-06-15 |
| CO2024002075A2 (es) | 2024-05-30 |
| WO2023010191A1 (pt) | 2023-02-09 |
| IL310568A (en) | 2024-03-01 |
| AR126669A1 (es) | 2023-11-01 |
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