JP2014509859A - １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤 - Google Patents

１７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤 Download PDF

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JP2014509859A
JP2014509859A JP2013558223A JP2013558223A JP2014509859A JP 2014509859 A JP2014509859 A JP 2014509859A JP 2013558223 A JP2013558223 A JP 2013558223A JP 2013558223 A JP2013558223 A JP 2013558223A JP 2014509859 A JP2014509859 A JP 2014509859A
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methyl
composition
amino acid
arginine
residues
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JP2014509859A5 (enExample
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マレー，ジヤステイン・ケイ
ミランダ，レスリー・ピー
マツクドノー，ステフアン・アイ
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アムジエン・インコーポレーテツド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/43504—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates
    • C07K14/43513—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates from arachnidae
    • C07K14/43518—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates from arachnidae from spiders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/44—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere, e.g. haptens, metals, DNA, RNA, amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/30—Immunoglobulins specific features characterized by aspects of specificity or valency
    • C07K2317/35—Valency
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Insects & Arthropods (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2013558223A 2011-03-16 2012-03-16 １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤 Pending JP2014509859A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161453492P 2011-03-16 2011-03-16
US61/453,492 2011-03-16
US201261608088P 2012-03-07 2012-03-07
US61/608,088 2012-03-07
PCT/US2012/029537 WO2012125973A2 (en) 2011-03-16 2012-03-16 Potent and selective inhibitors of nav1.3 and nav1.7

Related Child Applications (1)

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JP2016161682A Division JP2017031157A (ja) 2011-03-16 2016-08-22 １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤

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JP2014509859A true JP2014509859A (ja) 2014-04-24
JP2014509859A5 JP2014509859A5 (enExample) 2015-04-30

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JP2013558223A Pending JP2014509859A (ja) 2011-03-16 2012-03-16 １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤
JP2016161682A Pending JP2017031157A (ja) 2011-03-16 2016-08-22 １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤

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JP2016161682A Pending JP2017031157A (ja) 2011-03-16 2016-08-22 １７ｎａｖ１．３およびｎａｖ１．７の強力かつ選択的阻害剤

Country Status (24)

Country Link
US (2) US9340590B2 (enExample)
EP (1) EP2686340A2 (enExample)
JP (2) JP2014509859A (enExample)
KR (1) KR20140145947A (enExample)
CN (1) CN103930437A (enExample)
AP (1) AP2013007173A0 (enExample)
AR (1) AR088413A1 (enExample)
AU (1) AU2012228990B2 (enExample)
BR (1) BR112013023674A2 (enExample)
CA (1) CA2830065A1 (enExample)
CL (1) CL2013002673A1 (enExample)
CO (1) CO6821886A2 (enExample)
CR (1) CR20130533A (enExample)
EA (1) EA201391331A1 (enExample)
HK (1) HK1198173A1 (enExample)
MA (1) MA35385B1 (enExample)
MX (1) MX2013010497A (enExample)
PE (1) PE20140593A1 (enExample)
PH (1) PH12013501865A1 (enExample)
SG (2) SG10201601789TA (enExample)
TW (1) TW201300407A (enExample)
UY (1) UY33959A (enExample)
WO (1) WO2012125973A2 (enExample)
ZA (1) ZA201306920B (enExample)

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AR096927A1 (es) 2013-03-12 2016-02-10 Amgen Inc INHIBIDORES POTENTES Y SELECTIVOS DE NaV1.7
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MX2016016449A (es) * 2014-06-12 2017-08-24 Ra Pharmaceuticals Inc Modulacion de la actividad del complemento.
CN105348392B (zh) * 2015-11-18 2019-08-02 北京华金瑞清生物医药技术有限公司 一种Nav1.7抑制剂及其改造方法
WO2017147147A1 (en) * 2016-02-23 2017-08-31 PixarBio Corporation Compositions comprising nav1.7 selective inhibitors for treating acute, post-operative, or chronic pain and methods of using the same
US20190218255A1 (en) * 2016-09-16 2019-07-18 Olipass Corporation Scn9a antisense oligonucleotides
JP7241019B2 (ja) * 2017-01-24 2023-03-16 オリパス コーポレーション Ｓｃｎ９ａアンチセンス鎮痛剤
CN109517041B (zh) * 2018-11-14 2019-09-17 青海芬陀利华生物科技有限公司 Gptx-1毒素及其应用
AU2021320360B2 (en) * 2020-08-05 2025-07-10 National Institute Of Advanced Industrial Science And Technology Method for screening for polypeptide that acts on target protein
US20230374084A1 (en) 2020-09-23 2023-11-23 Aldevron, Llc Potent and selective inhibitors of nav1.7
CN113429463B (zh) * 2021-05-18 2022-08-23 湖南百尔泰克生物医药有限公司 一种具有镇痛作用的多肽及其应用
CN114805492B (zh) * 2022-03-15 2025-07-22 上海元炘执药科技有限公司 一种用于抑制电压门控钠离子通道1.4的芋螺毒素kiiia突变体及其制备方法和应用
CN114805491B (zh) * 2022-03-15 2025-10-03 青岛海洋生物医药研究院 一种芋螺毒素kiiia突变体及其制备方法和应用
CN114917324B (zh) * 2022-04-22 2025-05-30 江苏好上医生物医药有限公司 一种含虎纹毒素-iv的药物组合物及其应用
US20250388543A1 (en) 2022-04-22 2025-12-25 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
CA3256604A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
CA3257285A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
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
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
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
US20250163168A1 (en) 2023-11-17 2025-05-22 Pfizer Inc. Novel antibodies and antibody conjugates for the treatment of metabolic disorders
US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating pain
TR2024005209A2 (tr) * 2024-04-30 2024-05-21 Vsy Bi̇yoteknoloji̇ Ve İlaç Sanayi̇ Anoni̇m Şi̇rketi̇ Bi̇lhassa i̇ntersti̇syel si̇sti̇t hastaliğinin tedavi̇si̇ i̇çi̇n bi̇r formülasyon
US20260001877A1 (en) 2024-06-28 2026-01-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain

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