RU2731095C2 - Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar - Google Patents

Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar Download PDF

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RU2731095C2
RU2731095C2 RU2018134262A RU2018134262A RU2731095C2 RU 2731095 C2 RU2731095 C2 RU 2731095C2 RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2731095 C2 RU2731095 C2 RU 2731095C2
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compound
formula
taar
htaar1
pyrazole
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RU2018134262A
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Russian (ru)
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RU2018134262A (ru
RU2018134262A3 (enExample
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Гуидо Галлей
Мариус Хёнер
Роджер НОРКРОСС
Филипп ПФЛИГЕР
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Ф. Хоффманн-Ля Рош Аг
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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. fats
    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/06—Antihyperlipidemics
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P9/12—Antihypertensives
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
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  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
RU2018134262A 2016-03-17 2017-03-14 Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar RU2731095C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16160790 2016-03-17
EP16160790.8 2016-03-17
PCT/EP2017/055885 WO2017157873A1 (en) 2016-03-17 2017-03-14 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar

Publications (3)

Publication Number Publication Date
RU2018134262A RU2018134262A (ru) 2020-04-17
RU2018134262A3 RU2018134262A3 (enExample) 2020-04-17
RU2731095C2 true RU2731095C2 (ru) 2020-08-28

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RU2018134262A RU2731095C2 (ru) 2016-03-17 2017-03-14 Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar

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US (2) US10508107B2 (enExample)
EP (2) EP3757102A1 (enExample)
JP (1) JP6814814B2 (enExample)
KR (2) KR102537050B1 (enExample)
CN (1) CN108713019B (enExample)
AR (1) AR107878A1 (enExample)
AU (1) AU2017234042B2 (enExample)
BR (1) BR112018015389B1 (enExample)
CA (1) CA3013696C (enExample)
CL (1) CL2018002583A1 (enExample)
CO (1) CO2018007515A2 (enExample)
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PL (1) PL3430010T3 (enExample)
PT (1) PT3430010T (enExample)
RS (1) RS60825B1 (enExample)
RU (1) RU2731095C2 (enExample)
SG (2) SG11201807516UA (enExample)
SI (1) SI3430010T1 (enExample)
TW (1) TWI634117B (enExample)
UA (1) UA122881C2 (enExample)
WO (1) WO2017157873A1 (enExample)
ZA (1) ZA201804943B (enExample)

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CN114144412A (zh) * 2019-07-11 2022-03-04 豪夫迈·罗氏有限公司 用于制备经取代的吡唑衍生物的方法
IL294301A (en) * 2020-03-19 2022-08-01 Hoffmann La Roche Salts and crystalline forms of the taar1 agonist
JP2024538464A (ja) 2021-11-08 2024-10-22 エフ． ホフマン－ラ ロシュ アーゲー 芳香族ニトロ化合物の接触水素化
CN114288304A (zh) * 2021-12-31 2022-04-08 江苏海洋大学 一种抗精神分裂症组合物及其应用
AR129909A1 (es) 2022-07-15 2024-10-09 Hoffmann La Roche Cetorreductasa mutante con mayor actividad de cetorreductasa así como métodos y usos de esta
CN119654138A (zh) 2022-08-12 2025-03-18 豪夫迈·罗氏有限公司 包含5-乙基-4-甲基-n-[4-[(2s)吗啉-2-基]苯基]-1h-吡唑-3-甲酰胺的药物组合物
WO2024033460A1 (en) * 2022-08-12 2024-02-15 F. Hoffmann-La Roche Ag Use of co-processed excipients in continuous manufacturing of solid dosage forms
TW202440563A (zh) * 2022-11-28 2024-10-16 美商住友製藥美國公司 2-苯基嗎啉與2-苯基(硫代)嗎啉化合物及其用途
TW202444712A (zh) * 2023-04-28 2024-11-16 大陸商江蘇豪森藥業集團有限公司 一種嗎啉雜環類化合物的鹽及其製備方法和應用
CN121568694A (zh) * 2023-06-13 2026-02-24 乔治亚大学研究基金会 恶性疟原虫红内期抑制剂

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