EA201491749A1 - Трис-(гидроксиметил)аминометановые соли низкомолекулярного агониста glp1r, их фармацевтические композиции и применение - Google Patents

Трис-(гидроксиметил)аминометановые соли низкомолекулярного агониста glp1r, их фармацевтические композиции и применение

Info

Publication number
EA201491749A1
EA201491749A1 EA201491749A EA201491749A EA201491749A1 EA 201491749 A1 EA201491749 A1 EA 201491749A1 EA 201491749 A EA201491749 A EA 201491749A EA 201491749 A EA201491749 A EA 201491749A EA 201491749 A1 EA201491749 A1 EA 201491749A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydroxymethyl
tris
glp1r
aminomethane salts
agonist
Prior art date
Application number
EA201491749A
Other languages
English (en)
Inventor
Данило Алмариго
Дхарма Рао Полисетти
Эрик Бенджамин
Хассан Эл Абделлаоуи
Соумиа П. Сахоо
Original Assignee
ТРАНСТЕК ФАРМА, ЭлЭлСи
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 ТРАНСТЕК ФАРМА, ЭлЭлСи filed Critical ТРАНСТЕК ФАРМА, ЭлЭлСи
Publication of EA201491749A1 publication Critical patent/EA201491749A1/ru

Links

Classifications

    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2013—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
    • B01J2/02—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Inorganic Chemistry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к трис-(гидроксиметил)аминометановым солям низкомолекулярного агониста GLP1R. Кроме того, изобретение относится к твердым композициям, включающим трис-(гидроксиметил)аминометановые соли низкомолекулярного агониста GLP1R. Помимо этого, изобретение относится к применению трис-(гидроксиметил)аминометановых солей низкомолекулярного агониста GLP1R, например, для лечения диабета 1 типа, диабета 2 типа или ожирения. Изобретение относится также к твердым составам, дополнительно включающим остаток после упаривания и связующее вещество, например ацетат сукцинат гидроксипропил метил целлюлозы (HPMCAS).
EA201491749A 2012-03-22 2013-03-20 Трис-(гидроксиметил)аминометановые соли низкомолекулярного агониста glp1r, их фармацевтические композиции и применение EA201491749A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261614265P 2012-03-22 2012-03-22
PCT/US2013/033091 WO2013142569A1 (en) 2012-03-22 2013-03-20 Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof

Publications (1)

Publication Number Publication Date
EA201491749A1 true EA201491749A1 (ru) 2015-01-30

Family

ID=49223316

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201491749A EA201491749A1 (ru) 2012-03-22 2013-03-20 Трис-(гидроксиметил)аминометановые соли низкомолекулярного агониста glp1r, их фармацевтические композиции и применение

Country Status (16)

Country Link
US (1) US9198901B2 (ru)
EP (1) EP2854526B1 (ru)
JP (1) JP2015510947A (ru)
KR (1) KR102158992B1 (ru)
CN (1) CN104202977A (ru)
AU (1) AU2013235167B2 (ru)
CA (1) CA2868033A1 (ru)
EA (1) EA201491749A1 (ru)
ES (1) ES2674951T3 (ru)
HK (1) HK1199371A1 (ru)
IL (1) IL234615B (ru)
IN (1) IN2014DN07867A (ru)
MX (1) MX352804B (ru)
NZ (1) NZ629203A (ru)
SG (1) SG11201405353VA (ru)
WO (1) WO2013142569A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210005843A (ko) * 2018-05-08 2021-01-15 브이티브이 테라퓨틱스 엘엘씨 Glp1r 작용제의 치료적 용도
CN115315426B (zh) * 2020-04-01 2023-12-12 杭州中美华东制药有限公司 Glp-1受体激动剂游离碱的药学上可接受的酸式盐及其制备方法
EP4130005A4 (en) * 2020-04-01 2024-04-24 Hangzhou Zhongmeihuadong Pharmaceutical Co Ltd CRYSTALLINE FORM A OF GLP-1 RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2248850T3 (es) * 1996-05-20 2006-03-16 G.D. Searle Llc. Formulaciones farmaceuticas que contienen sales de potasiom sodio y tris de oxaprozina.
AR024076A1 (es) * 1999-05-25 2002-09-04 Smithkline Beecham Corp Sales de cis-[4-ciano-4-(3-ciclopentiloxi-4-metoxifenil) ciclohexan-1-carboxilato]
EP1363913A2 (en) * 2001-02-05 2003-11-26 Dr. Reddy's Laboratories Ltd. Salts of pyrimidine derivatives for use against coronary heart disease and atherosclerose
WO2003037328A1 (en) * 2001-10-30 2003-05-08 Applied Research Systems Ars Holding N.V. Oxindole hydrazide modulators of protein tyrosine phosphatases (ptps)
JP2006523724A (ja) * 2003-04-18 2006-10-19 インサイト サン ディエゴ インコーポレイテッド 代謝障害、癌および他の疾患の治療のための置換イソクロマン化合物
MX2010009752A (es) 2008-03-07 2010-09-30 Transtech Pharma Inc Compuestos de oxadiazoantraceno para el tratamiento de diabetes.
JP5627453B2 (ja) * 2008-03-31 2014-11-19 株式会社レナサイエンス プラスミノーゲンアクチベーターインヒビター−１阻害剤
JP5025795B2 (ja) * 2008-06-05 2012-09-12 旭化成ファーマ株式会社 スルホンアミド化合物及びその用途
AU2009324811B2 (en) * 2008-12-08 2013-01-24 Glaxosmithkline Llc Novel compounds
US20110064806A1 (en) * 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

Also Published As

Publication number Publication date
SG11201405353VA (en) 2014-09-26
US9198901B2 (en) 2015-12-01
EP2854526A1 (en) 2015-04-08
IL234615B (en) 2018-02-28
EP2854526A4 (en) 2016-02-24
JP2015510947A (ja) 2015-04-13
WO2013142569A1 (en) 2013-09-26
HK1199371A1 (en) 2015-07-03
MX2014010366A (es) 2015-05-15
KR102158992B1 (ko) 2020-09-23
IN2014DN07867A (ru) 2015-04-24
CA2868033A1 (en) 2013-09-26
KR20140138758A (ko) 2014-12-04
EP2854526B1 (en) 2018-04-25
AU2013235167A1 (en) 2014-09-18
US20150005339A1 (en) 2015-01-01
ES2674951T8 (es) 2018-08-23
ES2674951T3 (es) 2018-07-05
AU2013235167B2 (en) 2017-03-30
MX352804B (es) 2017-12-08
NZ629203A (en) 2015-12-24
CN104202977A (zh) 2014-12-10

Similar Documents

Publication Publication Date Title
CY1121843T1 (el) Σκευασματα ετανερσεπτης σταθεροποιημενα με ιοντα μαγνησιου
BR112018003595A2 (pt) análogos de nucleosídeos substituídos no anel aromático 6-6 bicíclico para uso como inibidores de prmt5
BR112018006448A2 (pt) derivado de oxaespiro, método de preparação dos mesmos, e aplicações dos mesmos em medicamentos
BR112018076169A2 (pt) derivados azabenzimidazol como inibidores de pi3k beta
EA201170772A1 (ru) Органические соединения
BR112016012146A2 (pt) Compostos derivados de aminopiridina como inibidores quinase da família tam, composição farmacêutica compreendendo ditos compostos e uso terapêutico dos mesmos
BRPI0908637B8 (pt) composto e composição farmacêutica do mesmo
BR112014033080A2 (pt) inibidores do vírus da hepatite c
CL2013002414A1 (es) Compuestos derivados de azabencimidazol ciclico, activadores de la proteina cinasa activada por amp; composicion farmaceutica que los comprende; y su uso para el tratamiento o enfermedad tal como diabetes tipo 2, hiperglicemia, sindrome metabolico, obesidad, hipercolesterolemia e hipertension.
BR112016028835A2 (pt) derivados de auristatina e conjugados dos mesmos
EA201591632A1 (ru) Цитотоксические и антимитотические соединения и способы их применения
CR20120634A (es) Derivados de heteroaril imidazolona como inhibidores de jak
EA201492011A1 (ru) Безводные фармацевтические составы для местного применения
MA32383B1 (fr) DÉRIVÉS D'INDAZOLES à SUBSTITUTIONS PHÉNYLE ET BENZODIOXYNYLE
CL2011000087A1 (es) Compuestos derivados de heteroarilo sustituido, inhibidores de los receptores dgat1; composicion farmaceutica; y su uso para tratar la diabetes tipo ll y obesidad.
BR112014009006B8 (pt) Compostos heterocíclicos e métodos de uso dos mesmos
BR112014010644A2 (pt) novos derivados de aril-quinolina
BR112015012720A2 (pt) derivados de feniletilpiridina como inibidores de pde4
EA201401193A1 (ru) Триарильные соединения и композиции, их содержащие
BR112014017735A8 (pt) Compostos derivados de amida heterocíclicos como antagonistas do receptor de p2x7, composição farmacêutica, e, uso de um composto
BR112015012716A2 (pt) derivados de feniletilpiridina como inibidores de pde4
AR082963A1 (es) Composicion para aerosol de control de plagas
EA201500821A1 (ru) Производные 2-замещенных-6-биарилметиламино-9-циклопентил-9н-пуринов, их использование в качестве лекарственных средств и фармацевтических составов
BR112018007068A2 (pt) derivados de quinoxalina e piridopirazina como inibidores de pi3kbeta
BR112015007879A2 (pt) inibidores do vírus da hepatite c