AR088413A1 - INHIBIDORES POTENTES Y SELECTIVOS DE NaV1.3 Y NaV1.7 - Google Patents

INHIBIDORES POTENTES Y SELECTIVOS DE NaV1.3 Y NaV1.7

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Publication number
AR088413A1
AR088413A1 ARP120100896A ARP120100896A AR088413A1 AR 088413 A1 AR088413 A1 AR 088413A1 AR P120100896 A ARP120100896 A AR P120100896A AR P120100896 A ARP120100896 A AR P120100896A AR 088413 A1 AR088413 A1 AR 088413A1
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AR
Argentina
Prior art keywords
amino acid
residue
acid residue
basic
secys
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Application number
ARP120100896A
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English (en)
Inventor
K Murray Justin
P Miranda Leslie
I Mdonough Stefan
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Amgen Inc
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Publication of AR088413A1 publication Critical patent/AR088413A1/es

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    • 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
    • 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
    • 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)
  • Insects & Arthropods (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

Se describe una composición, la cual comprende un polipéptido aislado, el cual es un inhibidor de Nav1.7 restringido periféricamente. En algunas realizaciones que se dan a conocer, el polipéptido aislado es un inhibidor de Nav1.7 y/o Nav1.3. Otras realizaciones son realizaciones conjugadas de la composición y composiciones farmacéuticas. Se dan a conocer ácidos nucleicos aislados que codifican algunas realizaciones de polipéptidos y vectores de expresión, así como células huésped recombinantes que los contienen. También se da a conocer un método para tratar o prevenir el dolor. Reivindicación 1: Una composición de la materia, la cual comprende un polipéptido aislado que comprende la secuencia de aminoácidos de fórmula: Xₐₐ¹Xₐₐ²Xₐₐ³Xₐₐ⁴Xₐₐ⁵Xₐₐ⁶Xₐₐ⁷Xₐₐ⁸Xₐₐ⁹Xₐₐ¹⁰Xₐₐ¹¹Xₐₐ¹²Xₐₐ¹³Xₐₐ¹⁴Asp¹⁵Xₐₐ¹⁶Xₐₐ¹⁷Xₐₐ¹⁸Xₐₐ¹⁹Xₐₐ²⁰Xₐₐ²¹Xₐₐ²²Xₐₐ²³Xₐₐ²⁴Xₐₐ²⁵Xₐₐ²⁶Xₐₐ²⁷Xₐₐ²⁸Xₐₐ²⁹Xₐₐ³⁰Xₐₐ³¹Lys³²Xₐₐ³³Xₐₐ³⁴Xₐₐ³⁵Xₐₐ³⁶Xₐₐ³⁷Xₐₐ³⁸ // SEQ ID Nº 475 o una sal farmacéuticamente aceptable del mismo, en donde: Xₐₐ¹Xₐₐ² está ausente; o Xₐₐ¹ es un residuo aminoácido y Xₐₐ² es un residuo aminoácido; o Xₐₐ¹ está ausente y Xₐₐ² es un residuo aminoácido; Xₐₐ³ es Cys, si Xₐₐ¹⁸ es Cys; o Xₐₐ³ es SeCys, si Xₐₐ¹⁸ es SeCys; o Xₐₐ³ es un residuo alquil aminoácido, si Xₐₐ¹⁸ es un residuo aminoácido alquílico; Xₐₐ⁴ es un residuo aminoácido ácido, hidrofóbico, básico, o neutro hidrofílico; Xₐₐ⁵ es un residuo aminoácido Gly, Ala, hidrofóbico o básico; Xₐₐ⁶ es un residuo aminoácido Gly, Ala, 2-Abu, Nle, Nva, o hidrofóbico; Xₐₐ⁷ es un residuo aminoácido Gly, Ala, aromático o hidrofóbico; Xₐₐ⁸ es un residuo aminoácido básico, ácido, o neutro hidrofílico, o un residuo Ala; Xₐₐ⁹ es un residuo aminoácido hidrofílico básico o neutro; Xₐₐ¹⁰ es Cys si Xₐₐ²⁴ es Cys; o Xₐₐ¹⁰ es SeCys si Xₐₐ²⁴ es SeCys; Xₐₐ¹¹ es cualquier residuo aminoácido; Xₐₐ¹² es un residuo aminoácido Pro, ácido, neutro o hidrofóbico; Xₐₐ¹³ es cualquier residuo aminoácido; Xₐₐ¹⁴ es cualquier residuo aminoácido; Xₐₐ¹⁶ es un residuo aminoácido básico, neutro hidrofílico, o ácido, o un residuo Ala; Xₐₐ¹⁷ es Cys si Xₐₐ³¹ es Cys; o Xₐₐ¹⁷ es SeCys si Xₐₐ³¹ es SeCys; Xₐₐ¹⁸ es Cys, SeCys, o un residuo aminoácido alquílico; Xₐₐ¹⁹ es cualquier residuo aminoácido; Xₐₐ²⁰ es un Pro, Gly, o un residuo básico, o neutro hidrofílico; Xₐₐ²¹ es un residuo aminoácido básico, hidrofóbico, o neutro hidrofílico; Xₐₐ²² es un residuo aminoácido hidrofóbico o básico; Xₐₐ²³ es un residuo aminoácido hidrofóbico, básico o neutro hidrofílico; Xₐₐ²⁴ es un residuo Cys o SeCys; Xₐₐ²⁵ es un residuo aminoácido Ser, Ala, o neutro hidrofílico; Xₐₐ²⁶ es un residuo aminoácido Ala, ácido, básico o neutro hidrofílico; Xₐₐ²⁷ es un residuo ácido, básico, neutro hidrofílico o hidrofóbico; Xₐₐ²⁸ es un residuo aminoácido aromático o básico; Xₐₐ²⁹ es un residuo aminoácido ácido, básico, o neutro hidrofílico; Xₐₐ³⁰ es un residuo Trp, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, o tioTrp; Xₐₐ³¹ es Cys o SeCys; Xₐₐ³³ es un residuo aminoácido hidrofóbico o aromático; Xₐₐ³⁴ es cualquier residuo aminoácido; Xₐₐ³⁵ es un residuo aminoácido hidrofóbico; cada uno de Xₐₐ³⁶, Xₐₐ³⁷, y Xₐₐ³⁸ está ausente independientemente o es independientemente un residuo aminoácido neutro, básico o hidrofóbico; en donde: si Xₐₐ³ y Xₐₐ¹⁸ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xₐₐ³ y el residuo Xₐₐ¹⁸; o si Xₐₐ³ y Xₐₐ¹⁸ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xₐₐ³ y el residuo Xₐₐ¹⁸; si Xₐₐ¹⁰ y Xₐₐ²⁴ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xₐₐ¹⁰ y el residuo Xₐₐ²⁴; o si Xₐₐ¹⁰ y Xₐₐ²⁴ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xₐₐ¹⁰ y el residuo Xₐₐ²⁴; si Xₐₐ¹⁷ y Xₐₐ³¹ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xₐₐ¹⁷ y el residuo Xₐₐ³¹; o si Xₐₐ¹⁷ y Xₐₐ³¹ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xₐₐ¹⁷ y el residuo Xₐₐ³¹; el residuo amino terminal está opcionalmente acetilado, biotinilado o 4-pentinoilado, o PEGilado; y el residuo carboxi terminal está opcionalmente amidado.
ARP120100896A 2011-03-16 2012-03-19 INHIBIDORES POTENTES Y SELECTIVOS DE NaV1.3 Y NaV1.7 AR088413A1 (es)

Applications Claiming Priority (2)

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US201161453492P 2011-03-16 2011-03-16
US201261608088P 2012-03-07 2012-03-07

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AR088413A1 true AR088413A1 (es) 2014-06-11

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US (2) US9340590B2 (es)
EP (1) EP2686340A2 (es)
JP (2) JP2014509859A (es)
KR (1) KR20140145947A (es)
CN (1) CN103930437A (es)
AP (1) AP2013007173A0 (es)
AR (1) AR088413A1 (es)
AU (1) AU2012228990B2 (es)
BR (1) BR112013023674A2 (es)
CA (1) CA2830065A1 (es)
CL (1) CL2013002673A1 (es)
CO (1) CO6821886A2 (es)
CR (1) CR20130533A (es)
EA (1) EA201391331A1 (es)
HK (1) HK1198173A1 (es)
MA (1) MA35385B1 (es)
MX (1) MX2013010497A (es)
PE (1) PE20140593A1 (es)
SG (2) SG193434A1 (es)
TW (1) TW201300407A (es)
UY (1) UY33959A (es)
WO (1) WO2012125973A2 (es)
ZA (1) ZA201306920B (es)

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AR096927A1 (es) 2013-03-12 2016-02-10 Amgen Inc INHIBIDORES POTENTES Y SELECTIVOS DE NaV1.7
EP2970408B1 (en) 2013-03-12 2018-01-10 Amgen Inc. Potent and selective inhibitors of nav1.7
EP2968495B1 (en) * 2013-03-15 2019-07-03 Daniel J. Capon Hybrid immunoglobulin containing non-peptidyl linkage
EP3116486B1 (en) 2014-03-14 2019-12-04 Daniel J. Capon Hybrid immunoglobulin containing non-peptidyl linkage
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
EP3512870B1 (en) * 2016-09-16 2022-08-03 Olipass Corporation Scn9a antisense oligonucleotides
IL267881B2 (en) * 2017-01-24 2024-03-01 Olipass Corp SCN9A antisense painkiller
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
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
WO2023205463A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205465A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
TW202408501A (zh) 2022-04-22 2024-03-01 美商維泰克斯製藥公司 用於治療疼痛之雜芳基化合物
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