[go: up one dir, main page]

ES2626555T3 - Pyridone amides como moduladores de canales de sodio - Google Patents

Pyridone amides como moduladores de canales de sodio Download PDF

Info

Publication number
ES2626555T3
ES2626555T3 ES14704053T ES14704053T ES2626555T3 ES 2626555 T3 ES2626555 T3 ES 2626555T3 ES 14704053 T ES14704053 T ES 14704053T ES 14704053 T ES14704053 T ES 14704053T ES 2626555 T3 ES2626555 T3 ES 2626555T3
Authority
ES
Spain
Prior art keywords
alkyl
halogen
substituted
units
adjacent
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.)
Active
Application number
ES14704053T
Other languages
English (en)
Inventor
Sara Sabina Hadida-Ruah
Corey Anderson
Vijayalaksmi Arumugam
Iuliana Luci ASGIAN
Brian Richard Bear
Andreas P. Termin
James Philip Johnson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2626555T3 publication Critical patent/ES2626555T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • 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
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/04—Monocyclic monocarboxylic acids
    • C07C63/06—Benzoic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
    • C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Ink Jet (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Un compuesto de fórmula I o I' ++Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que, independientemente para cada caso: G es **Fórmula** X es un enlace o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno, en donde hasta 35 dos unidades CH2 no adyacentes de dicho C1-C6 alquilo pueden estar reemplazadas con -O-; Rx está ausente, H, o C3-C8 cicloalifático, en la que hasta dos unidades CH2 no adyacentes de dicho C3-C8 cicloalifático pueden estar sustituidas con -O- y dicho C3-C8 cicloalifático está sustituido con 0-3 sustituyentes seleccionados de halógeno y C1-C4 alquilo; R1 es H, halógeno, CN, o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno y en la que hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo puede estar reemplazado con -O-; R2 es H, halógeno, CN, o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno, en donde hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo pueden estar sustituidas con -O-; R3 es H, halógeno, CN, o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno, en donde hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo puede estar reemplazado con -O-; R4 es H, halógeno, CN, o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno, en donde hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo pueden estar sustituidas con -O-; R5 es H, halógeno, CN, o -X-Rx; R5' es H, halógeno, CN, o -X-Rx; R6 es H, halógeno, CN, o -X-Rx; R6' es H, halógeno, CN, o -X-Rx; R7 es H, halógeno, CN, o -X-Rx; R8 es halógeno, o C1-C6 alquilo en el que dicho C1-C6 alquilo está sustituido con 0-6 halógeno, en donde hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo pueden estar sustituidas con -O-; p es un número entero de 0 a 3 inclusive; y R9 es H, o C1-C6 alquilo en el que hasta dos unidades CH2 no adyacentes de dicho C1-C6 alquilo pueden estar sustituidas con -O-.
ES14704053T 2013-01-31 2014-01-29 Pyridone amides como moduladores de canales de sodio Active ES2626555T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361759059P 2013-01-31 2013-01-31
PCT/US2014/013652 WO2014120808A1 (en) 2013-01-31 2014-01-29 Pyridone amides as modulators of sodium channels

Publications (1)

Publication Number Publication Date
ES2626555T3 true ES2626555T3 (es) 2017-07-25

Family

ID=50073531

Family Applications (2)

Application Number Title Priority Date Filing Date
ES17152492T Active ES2857687T3 (es) 2013-01-31 2014-01-29 Piridona amidas como moduladores de los canales de sodio
ES14704053T Active ES2626555T3 (es) 2013-01-31 2014-01-29 Pyridone amides como moduladores de canales de sodio

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES17152492T Active ES2857687T3 (es) 2013-01-31 2014-01-29 Piridona amidas como moduladores de los canales de sodio

Country Status (34)

Country Link
US (6) US9051270B2 (es)
EP (3) EP3239134B1 (es)
JP (4) JP6389194B2 (es)
KR (2) KR102295748B1 (es)
CN (2) CN108164457B (es)
AP (1) AP2015008633A0 (es)
AR (1) AR094667A1 (es)
AU (3) AU2014212509B2 (es)
BR (1) BR112015018289A2 (es)
CA (1) CA2898866C (es)
CL (1) CL2015002147A1 (es)
CY (1) CY1119163T1 (es)
DK (2) DK3239134T3 (es)
ES (2) ES2857687T3 (es)
GE (2) GEP20207177B (es)
HR (2) HRP20170787T1 (es)
HU (2) HUE033370T2 (es)
IL (2) IL269964B1 (es)
LT (2) LT2953931T (es)
MX (2) MX2021003687A (es)
NZ (2) NZ710270A (es)
PE (2) PE20151781A1 (es)
PH (1) PH12015501661B1 (es)
PL (2) PL2953931T3 (es)
PT (2) PT2953931T (es)
RS (2) RS61503B1 (es)
RU (1) RU2662223C2 (es)
SG (2) SG11201505953TA (es)
SI (2) SI2953931T1 (es)
SM (2) SMT201700256T1 (es)
TW (2) TWI655187B (es)
UA (1) UA120589C2 (es)
UY (1) UY35288A (es)
WO (1) WO2014120808A1 (es)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8933236B2 (en) 2012-05-22 2015-01-13 Xenon Pharmaceuticals Inc. N-substituted benzamides and methods of use thereof
JP6014154B2 (ja) 2011-10-31 2016-10-25 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
WO2013064984A1 (en) 2011-10-31 2013-05-10 Xenon Pharmaceuticals Inc. Biaryl ether sulfonamides and their use as therapeutic agents
BR112015000187A2 (pt) 2012-07-06 2017-06-27 Genentech Inc benzamidas substituídas com n e métodos de uso das mesmas
BR112015017997B1 (pt) 2013-01-31 2023-03-07 Vertex Pharmaceuticals Incorporated Amidas de quinolina e quinoxalina como moduladores de canais de sódio, seus usos, e composição farmacêutica
ES2857687T3 (es) 2013-01-31 2021-09-29 Vertex Pharma Piridona amidas como moduladores de los canales de sodio
KR20150131233A (ko) 2013-03-14 2015-11-24 제넨테크, 인크. 치환된 트리아졸로피리딘 및 이의 사용 방법
US9493429B2 (en) 2013-03-15 2016-11-15 Genentech, Inc. Substituted benzoxazoles and methods of use thereof
BR112016000825B1 (pt) 2013-07-19 2023-04-25 Vertex Pharmaceuticals Incorporated Compostos moduladores de sulfonamidas dos canais de sódio, composição farmacêutica, e uso dos mesmos
CR20160296A (es) 2013-11-27 2016-09-20 Genentech Inc Benzamidas sustituidas y métodos para usarlas
US9163042B2 (en) 2013-12-13 2015-10-20 Vertex Pharmaceuticals Incorporated Prodrugs of pyridone amides useful as modulators of sodium channels
WO2016007534A1 (en) 2014-07-07 2016-01-14 Genentech, Inc. Therapeutic compounds and methods of use thereof
EP3297989A1 (en) 2015-05-22 2018-03-28 Genentech, Inc. Substituted benzamides and methods of use thereof
CN108137477A (zh) 2015-08-27 2018-06-08 基因泰克公司 治疗化合物及其使用方法
CN108290881B (zh) 2015-09-28 2021-12-07 健泰科生物技术公司 治疗性化合物和其使用方法
EP3380466A1 (en) 2015-11-25 2018-10-03 Genentech, Inc. Substituted benzamides useful as sodium channel blockers
MX2018009870A (es) 2016-02-15 2018-11-29 Cemm Forschungszentrum Fuer Molekulare Medizin Gmbh Inhibidores de taf1 para la terapia del cancer.
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
MX388175B (es) 2016-10-17 2025-03-19 Genentech Inc Compuestos terapéuticos y métodos para utilizarlos
EP3601273B1 (en) 2017-03-24 2021-12-01 Genentech, Inc. 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors
AU2018271110A1 (en) 2017-05-16 2019-12-05 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
CN111065383A (zh) 2017-07-11 2020-04-24 沃泰克斯药物股份有限公司 用作钠通道调节剂的羧酰胺
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain
CN112041313A (zh) 2018-02-26 2020-12-04 基因泰克公司 吡啶-磺酰胺化合物及其针对疼痛和相关疾患的用途
JP2021519788A (ja) 2018-03-30 2021-08-12 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ナトリウムチャネル阻害剤としての縮合環ヒドロピリド化合物
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
CN113272293B (zh) 2018-11-02 2024-06-14 默沙东有限责任公司 作为nav1.8抑制剂的2-胺基-n-杂芳基-烟酰胺
EP3873468A4 (en) 2018-11-02 2022-10-26 Merck Sharp & Dohme LLC 2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
MX2021007970A (es) * 2019-01-04 2021-08-16 Jiangsu Hengrui Medicine Co Derivado de 6-oxo-1,6-dihidropiridazina, metodo de preparacion del mismo y uso medico del mismo.
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
CN112996774B (zh) * 2019-01-25 2022-11-22 江苏恒瑞医药股份有限公司 2-氧代-1,2-二氢吡啶类衍生物、其制备方法及其在医药上的应用
TW202102480A (zh) * 2019-02-20 2021-01-16 大陸商江蘇恆瑞醫藥股份有限公司 ６－側氧基－１，６－二氫噠嗪類前藥衍生物、其製備方法及其在醫藥上的應用
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
WO2021018165A1 (zh) * 2019-07-30 2021-02-04 江苏恒瑞医药股份有限公司 吡啶苯甲酰胺类衍生物、其制备方法及其在医药上的应用
CN112390745B (zh) * 2019-08-19 2022-10-21 江苏恒瑞医药股份有限公司 吡啶烟酰胺类衍生物、其制备方法及其在医药上的应用
WO2021032074A1 (zh) * 2019-08-19 2021-02-25 江苏恒瑞医药股份有限公司 苯甲酰胺稠芳环类衍生物、其制备方法及其在医药上的应用
PH12022550584A1 (en) * 2019-09-12 2024-03-04 Orion Corp Pyridine oxynitride, preparation method therefor and use thereof
LT4069691T (lt) 2019-12-06 2024-12-10 Vertex Pharmaceuticals Incorporated Pakeistieji tetrahidrofuranai kaip natrio kanalų moduliatoriai
CN113045487B (zh) * 2019-12-27 2025-01-17 明慧医药（上海）有限公司 一种选择性钠通道调节剂及其制备和应用
CN114437062B (zh) * 2020-04-30 2024-05-17 成都海博为药业有限公司 一种可作为钠通道调节剂的化合物及其用途
CA3182633A1 (en) 2020-06-17 2021-12-23 Ashok Arasappan 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors
CN113880771B (zh) * 2020-07-03 2023-09-19 福建盛迪医药有限公司 一种选择性Nav抑制剂的结晶形式及其制备方法
CN111808019B (zh) * 2020-09-08 2020-11-27 上海济煜医药科技有限公司 一种并环化合物及其应用
CN114031518B (zh) 2020-12-08 2023-08-18 成都海博为药业有限公司 一种苄胺或苄醇衍生物及其用途
GEP20257795B (en) 2021-05-07 2025-09-25 Merck Sharp & Dohme Llc Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors
EP4347032A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
CN117858875A (zh) 2021-06-04 2024-04-09 沃泰克斯药物股份有限公司 羟基和(卤代)烷氧基取代的四氢呋喃作为钠通道调节剂
CN117794919A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N-(羟烷基(杂)芳基)四氢呋喃甲酰胺类似物作为钠通道调节剂
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
EP4346818B1 (en) 2021-06-04 2025-12-03 Vertex Pharmaceuticals Incorporated Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide
UY39882A (es) 2021-08-02 2023-06-15 Eurofarma Laboratorios S A COMPUESTOS NACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS
UY39881A (es) 2021-08-02 2023-06-15 Eurofarma Laboratorios S A “COMPUESTOS N-ACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS”
WO2023160509A1 (zh) * 2022-02-25 2023-08-31 中国科学院上海药物研究所 脒类衍生化合物及其制备方法和用途
CN119487003A (zh) 2022-04-22 2025-02-18 沃泰克斯药物股份有限公司 用于治疗疼痛的杂芳基化合物
WO2023205778A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CR20240513A (es) 2022-04-22 2025-04-30 Vertex Pharma Compuestos de heteroarilo para el tratamiento del dolor
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
JP2025516005A (ja) 2022-04-25 2025-05-23 サイトワン セラピューティクス インコーポレイテッド 疼痛の処置のためのｎａｖ１．８の二環式複素環アミド阻害剤
WO2023207949A1 (zh) * 2022-04-25 2023-11-02 中国科学院上海药物研究所 并环类化合物及其应用
CN120603815A (zh) 2022-12-06 2025-09-05 沃泰克斯药物股份有限公司 钠通道的取代四氢呋喃调节剂的合成方法
AR131658A1 (es) 2023-01-30 2025-04-16 Eurofarma Laboratorios S A Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y sus kits
WO2024159287A1 (pt) 2023-01-30 2024-08-08 Eurofarma Laboratórios S.A. Hidroxamatos bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits
EP4660182A1 (en) 2023-01-30 2025-12-10 Eurofarma Laboratórios S.A. Nav1.7- and/or nav1.8-inhibiting aryl pyridine compounds, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits
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
AR131715A1 (es) 2023-01-30 2025-04-23 Eurofarma Laboratorios S A AMIDAS BLOQUEADORAS DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y KITS
WO2024217344A1 (zh) 2023-04-19 2024-10-24 中国科学院上海药物研究所 Nav1.8抑制剂及其制备方法和用途
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
TW202535867A (zh) 2023-10-23 2025-09-16 美商維泰克斯製藥公司 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法
TW202523313A (zh) 2023-10-23 2025-06-16 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating pain
WO2025160286A1 (en) 2024-01-24 2025-07-31 Siteone Therapeutics, Inc. 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH598252A5 (es) * 1974-01-04 1978-04-28 Hoffmann La Roche
GB1447583A (en) * 1974-02-04 1976-08-25 Ici Ltd Xanthene derivatives
US4086350A (en) * 1974-11-06 1978-04-25 Smithkline Corporation Pharmaceutical compositions and method of producing anti-psychotic activity without extrapyramidal symptoms
GB1543964A (en) * 1976-04-08 1979-04-11 Ici Ltd Method of antagonising herbicides on soyabean and cotton
US5281620A (en) * 1986-12-23 1994-01-25 Cancer Research Campaign Technology Limited Compounds having antitumor and antibacterial properties
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
JP3285391B2 (ja) * 1992-09-01 2002-05-27 日本化学工業株式会社 ２−フェノキシ安息香酸の製造法
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
WO2001021652A1 (en) 1999-09-24 2001-03-29 The Johns Hopkins University School Of Medicine Methods for identifying an agent that corrects defective protein folding
JP2003034671A (ja) * 2001-05-17 2003-02-07 Nippon Nohyaku Co Ltd ベンズアミド誘導体及び農園芸用薬剤並びにその使用方法
SI1490064T1 (sl) * 2002-02-14 2010-01-29 Pharmacia Corp Substituirani piridinoni kot modulatorji p38 MAP kinaze
CA2539227A1 (en) * 2003-08-08 2005-02-17 Vertex Pharmaceuticals Incorporated Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
WO2005021508A1 (en) * 2003-09-03 2005-03-10 Pfizer Inc. Phenyl or pyridyl amide compounds as prostaglandin e2 antagonists
WO2006011050A2 (en) 2004-07-23 2006-02-02 Pfizer Limited Pyridine derivatives
CA2611731A1 (en) 2005-06-09 2006-12-14 Vertex Pharmaceuticals Incorporated Indane derivatives as modulators of ion channels
NZ567132A (en) 2005-09-09 2011-12-22 Vertex Pharma Bicyclic derivatives as modulators of voltage gated ion channels
AU2006304283B2 (en) 2005-10-12 2012-01-19 Vertex Pharmaceuticals Incorporated Biphenyl derivatives as modulators of voltage gated ion channels
KR20080109918A (ko) 2006-04-11 2008-12-17 버텍스 파마슈티칼스 인코포레이티드 전압 개폐 나트륨 채널의 억제제로서 유용한 조성물
CA2684105C (en) * 2007-05-03 2011-09-06 Pfizer Limited Pyridine derivatives
EP2158183A2 (en) 2007-05-25 2010-03-03 Vertex Pharmaceuticals Incorporated Ion channel modulators and methods of use
JP5436434B2 (ja) * 2007-10-11 2014-03-05 バーテックス ファーマシューティカルズ インコーポレイテッド 電位開口型ナトリウムチャネルの阻害剤として有用なアミド
KR20100075631A (ko) * 2007-10-11 2010-07-02 버텍스 파마슈티칼스 인코포레이티드 전압­개폐 나트륨 채널의 억제제로서 유용한 아릴 아미드
AU2008310660A1 (en) * 2007-10-11 2009-04-16 Vertex Pharmaceuticals Incorporated Heteroaryl amides useful as inhibitors of voltage-gated sodium channels
CA2703915C (en) * 2007-10-31 2015-02-24 Merck Sharp & Dohme Corp. P2x3 receptor antagonists for treatment of pain
KR101370185B1 (ko) 2008-12-23 2014-03-05 에프. 호프만-라 로슈 아게 Ｐ２ｘ7 조절제로서의 디히드로피리돈 아미드
JP5685203B2 (ja) * 2009-05-29 2015-03-18 ラクオリア創薬株式会社 カルシウムチャネル遮断薬またはナトリウムチャネル遮断薬としてのアリール置換カルボキサミド誘導体
TW201103904A (en) * 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
US8883782B2 (en) * 2010-03-15 2014-11-11 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
US8999967B2 (en) * 2010-09-29 2015-04-07 Presidio Pharmaceuticals, Inc. Tricyclic fused ring inhibitors of hepatitis C
TW201604196A (zh) 2011-02-02 2016-02-01 維泰克斯製藥公司 作為離子通道調節劑之吡咯并吡－螺環哌啶醯胺
EP2675810A1 (en) * 2011-02-15 2013-12-25 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
MX2013009393A (es) 2011-02-18 2013-08-29 Vertex Pharma Piperidinamidas cromano-espirociclicas como moduladores de canales de iones.
EP2686325B1 (en) 2011-03-14 2016-12-14 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
WO2012122716A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Tetracyclic xanthene derivatives and methods of use thereof for treatment of viral diseases
US20120252852A1 (en) * 2011-03-29 2012-10-04 Sanofi Otamixaban formulations with improved stability
WO2013021535A1 (ja) 2011-08-10 2013-02-14 三菱電機株式会社 誘導加熱調理器及びそのプログラム
CN102584774B (zh) * 2011-12-22 2014-08-06 合肥工业大学 一种呫吨酮类衍生物及其用途
GEP201606560B (en) 2012-03-06 2016-10-25 Pfizer Macrocyclic derivatives for the treatment of proliferative diseases
CN102659628B (zh) * 2012-04-26 2014-07-02 四川大学 含芳酰胺的邻苯二甲腈单体及其合成方法和用其固化制备的聚邻苯二甲腈树脂
CA2898653C (en) 2013-01-31 2021-09-28 Vertex Pharmaceuticals Incorporated Amides as modulators of sodium channels
BR112015017997B1 (pt) 2013-01-31 2023-03-07 Vertex Pharmaceuticals Incorporated Amidas de quinolina e quinoxalina como moduladores de canais de sódio, seus usos, e composição farmacêutica
TWI606048B (zh) 2013-01-31 2017-11-21 帝人製藥股份有限公司 唑苯衍生物
ES2857687T3 (es) 2013-01-31 2021-09-29 Vertex Pharma Piridona amidas como moduladores de los canales de sodio
BR112016000825B1 (pt) 2013-07-19 2023-04-25 Vertex Pharmaceuticals Incorporated Compostos moduladores de sulfonamidas dos canais de sódio, composição farmacêutica, e uso dos mesmos
US9163042B2 (en) 2013-12-13 2015-10-20 Vertex Pharmaceuticals Incorporated Prodrugs of pyridone amides useful as modulators of sodium channels
CN111065383A (zh) 2017-07-11 2020-04-24 沃泰克斯药物股份有限公司 用作钠通道调节剂的羧酰胺
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain

Also Published As

Publication number Publication date
MX383688B (es) 2025-03-14
JP2016506963A (ja) 2016-03-07
EP3239134B1 (en) 2020-12-23
US9758483B2 (en) 2017-09-12
EP2953931B1 (en) 2017-03-01
JP6741704B2 (ja) 2020-08-19
US20140213616A1 (en) 2014-07-31
CN105026373A (zh) 2015-11-04
RU2018126184A3 (es) 2021-07-26
AR094667A1 (es) 2015-08-19
JP6389194B2 (ja) 2018-09-12
RU2662223C2 (ru) 2018-07-25
US20170037009A1 (en) 2017-02-09
PT3239134T (pt) 2021-01-28
AP2015008633A0 (en) 2015-07-31
UA120589C2 (uk) 2020-01-10
KR20150112031A (ko) 2015-10-06
US10087143B2 (en) 2018-10-02
MX2015009602A (es) 2015-11-25
RU2015136795A (ru) 2017-03-10
JP2019089861A (ja) 2019-06-13
HRP20210349T1 (hr) 2021-04-16
PE20191495A1 (es) 2019-10-21
IL240195B (en) 2019-10-31
HK1217693A1 (en) 2017-01-20
CA2898866C (en) 2023-03-07
SI3239134T1 (sl) 2021-03-31
US10738009B2 (en) 2020-08-11
UY35288A (es) 2014-08-29
HK1244269A1 (en) 2018-08-03
SMT201700256T1 (it) 2017-09-07
AU2014212509B2 (en) 2018-05-10
TW201943701A (zh) 2019-11-16
ES2857687T3 (es) 2021-09-29
IL269964B1 (en) 2025-09-01
CN105026373B (zh) 2018-03-30
GEAP201414909A (es) 2020-07-10
CA2898866A1 (en) 2014-08-07
PL2953931T3 (pl) 2017-09-29
US11673864B2 (en) 2023-06-13
WO2014120808A8 (en) 2015-09-11
IL240195A0 (en) 2015-09-24
CN108164457B (zh) 2021-07-09
PH12015501661B1 (en) 2020-10-16
US20180016235A1 (en) 2018-01-18
PL3239134T3 (pl) 2021-06-14
KR102295748B1 (ko) 2021-09-01
AU2014212509A1 (en) 2015-08-06
JP2021001232A (ja) 2021-01-07
KR20210029848A (ko) 2021-03-16
HUE033370T2 (en) 2017-11-28
SG11201505953TA (en) 2015-08-28
RS56015B1 (sr) 2017-09-29
US9393235B2 (en) 2016-07-19
PH12015501661A1 (en) 2015-10-19
SI2953931T1 (sl) 2017-08-31
WO2014120808A1 (en) 2014-08-07
MX2021003687A (es) 2023-01-25
CL2015002147A1 (es) 2016-06-03
CY1119163T1 (el) 2018-02-14
AU2020204425A1 (en) 2020-07-23
GEP20217286B (en) 2021-08-25
DK2953931T3 (en) 2017-06-06
HUE053448T2 (hu) 2021-06-28
RU2018126184A (ru) 2019-03-12
EP3865475A1 (en) 2021-08-18
EP3239134A1 (en) 2017-11-01
CN108164457A (zh) 2018-06-15
GEP20207177B (en) 2020-11-10
AU2018214105A1 (en) 2018-08-30
US20190248745A1 (en) 2019-08-15
US9051270B2 (en) 2015-06-09
LT2953931T (lt) 2017-07-25
JP2018104453A (ja) 2018-07-05
EP2953931A1 (en) 2015-12-16
NZ750187A (en) 2020-09-25
RS61503B1 (sr) 2021-03-31
AU2018214105B9 (en) 2020-04-23
AU2018214105B2 (en) 2020-04-02
PE20151781A1 (es) 2015-12-02
LT3239134T (lt) 2021-02-25
DK3239134T3 (da) 2021-02-22
WO2014120808A9 (en) 2015-05-14
SMT202100030T1 (it) 2021-03-15
IL269964A (en) 2019-11-28
TW201443019A (zh) 2014-11-16
NZ710270A (en) 2020-09-25
HRP20170787T1 (hr) 2017-08-11
KR102227592B1 (ko) 2021-03-15
TWI655187B (zh) 2019-04-01
TWI714967B (zh) 2021-01-01
SG10201706206PA (en) 2017-08-30
US20210047271A1 (en) 2021-02-18
BR112015018289A2 (pt) 2017-07-18
PT2953931T (pt) 2017-06-14
US20150246028A1 (en) 2015-09-03

Similar Documents

Publication Publication Date Title
ES2626555T3 (es) Pyridone amides como moduladores de canales de sodio
ES2620379T3 (es) Quinolina y quinoxalina amidas como moduladores de canales de sodio
AR094668A1 (es) Amidas como moduladores de canales de sodio
AR082201A1 (es) Bencenosulfonamidas utiles como inhibidores del canal de sodio
AR092538A1 (es) Inhibidores de girasa triciclica
BR112015021983A2 (pt) compostos heterocíclicos e usos dos mesmos
PH12017501326A1 (en) Tgf-� inhibitors
MX351581B (es) Nuevos derivados tienopirimidina, un proceso para su preparación y composiciones farmacéuticas que los contienen.
ECSP16005566A (es) Sulfonamidas como moduladores de canales de sodio
ECSP16025201A (es) Profármacos de amidas de piridona útiles como moduladores de canales de sodio
EA201690247A1 (ru) Аминометилбиарильные производные-ингибиторы фактора d комплемента и их применения
UA109220C2 (uk) Похідні (4-фенілімідазол-2-іл)етиламіну як модулятори натрієвих каналів
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
MX351812B (es) Derivados de piridona.
MX2015012815A (es) Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3-disustituidos y su uso como inhibidores de bromodominio.
EA201492287A1 (ru) Дейтерированные производные руксолитиниба
MD20140136A2 (ro) Inhibitori ai virusului hepatic C
AR093759A1 (es) Dihidropiridona p1 como inhibidores del factor xia
EA201171328A1 (ru) Производное замещенного изохинолина
BR112016011016A8 (pt) derivados de fenoxietila de amina cíclica, seus usos, e composição farmacêutica.
AR094553A1 (es) Formas de oxadiazolpirazina
EA201690072A1 (ru) Состав, содержащий гиполипидемическое средство
AR097894A1 (es) Inhibidores terapéuticos de cdk8 o uso de los mismos
MX2016015467A (es) Derivados de carbonitrilo como moduladores selectivos del receptor de androgenos.
PH12015502429A1 (en) Dicarboxylic acid compound