EA201892175A1 - Биодоступные полиамины - Google Patents

Биодоступные полиамины

Info

Publication number
EA201892175A1
EA201892175A1 EA201892175A EA201892175A EA201892175A1 EA 201892175 A1 EA201892175 A1 EA 201892175A1 EA 201892175 A EA201892175 A EA 201892175A EA 201892175 A EA201892175 A EA 201892175A EA 201892175 A1 EA201892175 A1 EA 201892175A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pharmaceutical
salts
pharmaceutical agent
protonated
bioavailable
Prior art date
Application number
EA201892175A
Other languages
English (en)
Other versions
EA037149B1 (ru
Inventor
Марк Р. Бернс
Original Assignee
Аминекс Терапьютикс, Инк.
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 Аминекс Терапьютикс, Инк. filed Critical Аминекс Терапьютикс, Инк.
Publication of EA201892175A1 publication Critical patent/EA201892175A1/ru
Publication of EA037149B1 publication Critical patent/EA037149B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/74Synthetic polymeric materials
    • A61K31/785Polymers containing nitrogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846Poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/126Acids containing more than four carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

В настоящем документе описаны фармацевтические соли катионного протонированного полиаминового фармацевтического агента и анионного органического карбоксилата, который является гидрофобным в протонированной форме, особенно подходящие для перорального введения, где эти соли обладают хорошей биодоступностью в виде твердой лекарственной формы и могут быть использованы для лечения злокачественного новообразования и других фармацевтических состояний, для которых предназначен фармацевтический агент.
EA201892175A 2016-03-25 2017-03-20 Биодоступные полиамины EA037149B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662313657P 2016-03-25 2016-03-25
PCT/US2017/023250 WO2017165313A1 (en) 2016-03-25 2017-03-20 Bioavailable polyamines

Publications (2)

Publication Number Publication Date
EA201892175A1 true EA201892175A1 (ru) 2019-02-28
EA037149B1 EA037149B1 (ru) 2021-02-11

Family

ID=59899774

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201892175A EA037149B1 (ru) 2016-03-25 2017-03-20 Биодоступные полиамины

Country Status (20)

Country Link
US (3) US10632145B2 (ru)
EP (2) EP3785706B1 (ru)
JP (1) JP6949098B2 (ru)
KR (1) KR102454783B1 (ru)
CN (1) CN109069594B (ru)
AU (1) AU2017236905B2 (ru)
CA (1) CA3015849A1 (ru)
CY (1) CY1123636T1 (ru)
DK (2) DK3432914T3 (ru)
EA (1) EA037149B1 (ru)
ES (2) ES2836289T3 (ru)
HR (1) HRP20201844T1 (ru)
HU (1) HUE052620T2 (ru)
IL (1) IL261512A (ru)
LT (1) LT3432914T (ru)
MX (1) MX2018010768A (ru)
PL (1) PL3432914T3 (ru)
PT (1) PT3432914T (ru)
SI (1) SI3432914T1 (ru)
WO (1) WO2017165313A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037149B1 (ru) 2016-03-25 2021-02-11 Аминекс Терапьютикс, Инк. Биодоступные полиамины
EP4221698A1 (en) * 2020-09-30 2023-08-09 Aminex Therapeutics, Inc. Combination drug substance of polyamine transport inhibitor and dfmo
WO2023102402A1 (en) * 2021-12-01 2023-06-08 Aminex Therapeutics, Inc. Methods to treat cancer with amxt 1501 and dfmo

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR3517M (fr) * 1962-12-07 1965-09-06 Hoffmann La Roche Médicament a base de compositions vitaminées.
US4309442A (en) 1977-07-11 1982-01-05 Merrell Toraude Et Compagnie Method for controlling fertility in mammals
US4590288A (en) 1983-06-29 1986-05-20 Exxon Research And Engineering Co. Bi- or polymetallic coordination complex
HU200093B (en) 1983-12-20 1990-04-28 Adam Kovacs Process for production of medical compositions against tumour
ATE40572T1 (de) 1985-01-10 1989-02-15 Molecular Diagnostics Inc Photochemisches verfahren zum markieren von nucleinsaeuren zum nachweis in hybridisationsproben.
US4818770A (en) 1986-10-22 1989-04-04 Boyce Thompson Institute For Plant Research Prevention of a plant disease by specific inhibition of fungal polyamine biosynthesis
US5342945A (en) 1986-12-02 1994-08-30 University Of Florida Research Foundation, Inc. Anti-neoplastic, anti-viral or anti-retroviral spermine derivatives
US4774339A (en) 1987-08-10 1988-09-27 Molecular Probes, Inc. Chemically reactive dipyrrometheneboron difluoride dyes
JP3072108B2 (ja) 1988-12-09 2000-07-31 ダイセル化学工業株式会社 新規なポリアミン化合物及びグルタミン酸レセプター遮断剤
AU5957390A (en) 1989-07-03 1991-02-06 New York University Use of polyamines as ionic-channel regulating agents
US5433896A (en) 1994-05-20 1995-07-18 Molecular Probes, Inc. Dibenzopyrrometheneboron difluoride dyes
US5274113A (en) 1991-11-01 1993-12-28 Molecular Probes, Inc. Long wavelength chemically reactive dipyrrometheneboron difluoride dyes and conjugates
US5252714A (en) 1990-11-28 1993-10-12 The University Of Alabama In Huntsville Preparation and use of polyethylene glycol propionaldehyde
US5561136A (en) 1990-12-13 1996-10-01 Merrell Pharmaceuticals Inc. Method of treating cancer by conjunctive therapy with N,N'-bis[ethylamino)propyl]-1,7-heptanediamine and a cytotoxic agent
US5248782A (en) 1990-12-18 1993-09-28 Molecular Probes, Inc. Long wavelength heteroaryl-substituted dipyrrometheneboron difluoride dyes
US5312928A (en) 1991-02-11 1994-05-17 Cambridge Neuroscience Calcium channel antagonists and methodology for their identification
US5187288A (en) 1991-05-22 1993-02-16 Molecular Probes, Inc. Ethenyl-substituted dipyrrometheneboron difluoride dyes and their synthesis
US6743419B1 (en) 1992-12-22 2004-06-01 The Gillette Company Method of reducing hair growth employing sulfhydryl active compounds
US5648394A (en) 1993-05-27 1997-07-15 Boxall; Brian Alfred Topical composition for inhibiting hair growth
US5541230A (en) 1993-11-05 1996-07-30 Us Health Therapeutic polyamines
ES2156162T3 (es) 1994-02-08 2001-06-16 Nps Pharma Inc Compuestos activos en un nuevo sitio sobre canales del calcio accionados por un receptor, utiles para el tratamiento de trastornos y enfermedades neurologicas.
EP0805769B1 (en) 1995-01-25 1998-08-19 Sealed Air Corporation Inflatable cushion and method of making same
US5583239A (en) 1995-05-30 1996-12-10 Lehigh University Antimicrobial sterol conjugates
JPH09235271A (ja) 1996-02-29 1997-09-09 Suntory Ltd ポリアミン誘導体
DE69721780T2 (de) 1996-03-14 2004-03-25 Schering-Plough Healthcare Products, Inc., Memphis Präparat und verfahren zur künstlichen hautbräunung
AU758570B2 (en) 1997-07-15 2003-03-27 Mediquest Therapeutics, Inc. Novel polyamine analogues as therapeutic and diagnostic agents
US6646149B1 (en) 1997-07-15 2003-11-11 Nicolaas M. J. Vermeulin Polyamine analogues as therapeutic and diagnostic agents
US7208528B1 (en) 1997-07-15 2007-04-24 Mediquest Therapeutics, Inc. Polyamine analogues as therapeutic and diagnostic agents
EP1003715A1 (en) 1998-04-21 2000-05-31 Universite Laval Polyamine transport inhibitors
WO2000034226A1 (en) 1998-12-10 2000-06-15 Universite Laval Polyamine transport inhibitors
WO2000046187A2 (en) 1999-02-05 2000-08-10 Oridigm Corporation Antizyme modulators and their use
CA2318004A1 (en) 1999-09-15 2001-03-15 Oridigm Corporation Novel polyamine analogues as therapeutic and diagnostic agents
US6235737B1 (en) 2000-01-25 2001-05-22 Peter Styczynski Reduction of hair growth
HUP0400494A3 (en) 2000-03-24 2004-08-30 Mediquest Therapeutics Inc Sea Polyamine analogues as cytotoxic agents and pharmaceutical compositions containing them
USRE43327E1 (en) 2001-01-08 2012-04-24 Aminex Therapeutics, Inc. Hydrophobic polyamine analogs and methods for their use
US7432302B2 (en) 2001-01-08 2008-10-07 Mediquest Therapeutics, Inc. Composition containing polyamine transport inhibitor and use thereof
EP1373185B1 (en) * 2001-01-08 2017-03-01 Aminex Therapeutics, Inc. Hydrophobic polyamine analogs and methods for their use
US7144920B2 (en) 2002-09-23 2006-12-05 Mediquest Therapeutics, Inc. Polyamine analogs that activate antizyme frameshifting
US6914079B2 (en) 2002-09-23 2005-07-05 Mediquest Therapeutics, Inc. Polyamine analogs that activate antizyme frameshifting
US6919483B2 (en) 2003-05-23 2005-07-19 Mediquest Therapeutics, Inc. Immunomodulation with novel pharmaceutical compositions
JP2008519856A (ja) 2004-11-12 2008-06-12 メディクエスト セラピューティックス インク 強力なリポ多糖金属イオン封鎖剤としての疎水性ポリアミンアミド類
US7199267B1 (en) 2005-10-21 2007-04-03 Mediquest Therapeutics, Inc. Recognition of oligiosaccaride molecular targets by polycationic small molecule inhibitors and treatment of immunological disorders and infectious diseases
US7411002B2 (en) 2006-06-07 2008-08-12 The University Of Kansas Polycationic sulfonamides and use thereof
WO2009110939A2 (en) 2007-12-10 2009-09-11 Massachusetts Institute Of Technology Drug delivery system for pharmaceuticals and radiation
US8366600B2 (en) * 2008-06-19 2013-02-05 Nupathe Inc. Polyamine enhanced formulations for triptan compound iontophoresis
DE102009000505A1 (de) * 2009-01-30 2010-08-05 Evonik Goldschmidt Gmbh Zusammensetzungen enthaltend Reaktionsprodukte aus Alkylamidoaminen, Alkylaminoimidazolinen und freiem Amin sowie deren Verwendung
NZ628513A (en) 2009-07-16 2016-01-29 Pathologica Llc Pharmaceutical for oral delivery comprising mgbg and methods of treating disease
US20110256161A1 (en) * 2010-04-19 2011-10-20 Aminex Therapeutics Inc. Methods for enhancing immune response
CN104540813A (zh) * 2012-06-27 2015-04-22 默沙东公司 磺酰胺衍生物以及使用它们用于改善药物的药物动力学的方法
US9439433B2 (en) * 2013-05-22 2016-09-13 Curza Global, Llc Compositions and methods comprising a biocidal polyamine
EA037149B1 (ru) 2016-03-25 2021-02-11 Аминекс Терапьютикс, Инк. Биодоступные полиамины

Also Published As

Publication number Publication date
EP3432914B1 (en) 2020-09-23
MX2018010768A (es) 2018-11-29
JP2019513153A (ja) 2019-05-23
LT3432914T (lt) 2020-12-10
WO2017165313A1 (en) 2017-09-28
EP3785706A1 (en) 2021-03-03
PL3432914T3 (pl) 2021-03-08
US11395834B2 (en) 2022-07-26
AU2017236905A1 (en) 2018-09-06
KR20180123133A (ko) 2018-11-14
CA3015849A1 (en) 2017-09-28
DK3432914T3 (da) 2020-11-30
EP3432914A4 (en) 2019-11-13
CN109069594B (zh) 2022-03-08
AU2017236905B2 (en) 2024-03-28
US20190008892A1 (en) 2019-01-10
JP6949098B2 (ja) 2021-10-13
US10632145B2 (en) 2020-04-28
ES2955255T3 (es) 2023-11-29
CN109069594A (zh) 2018-12-21
SI3432914T1 (sl) 2021-01-29
PT3432914T (pt) 2020-12-24
EA037149B1 (ru) 2021-02-11
CY1123636T1 (el) 2022-03-24
US20200352983A1 (en) 2020-11-12
HUE052620T2 (hu) 2021-05-28
EP3785706B1 (en) 2023-06-07
IL261512A (en) 2018-10-31
HRP20201844T1 (hr) 2021-04-02
ES2836289T3 (es) 2021-06-24
DK3785706T3 (da) 2023-09-11
US20230088829A1 (en) 2023-03-23
KR102454783B1 (ko) 2022-10-13
EP3432914A1 (en) 2019-01-30

Similar Documents

Publication Publication Date Title
CY1122566T1 (el) Παραγωγο 6,7,8,9-tetpaϋδpo-3h-πυραζολo[4,3-f] ισοκινολινης χρησιμο στη θεραπευτικη αντιμετωπιση του καρκινου
EA201690287A1 (ru) 1,4-дизамещенные аналоги пиридазин хинолина и способы лечения состояний, связанных с smn-дефицитом
EA201790024A1 (ru) Модуляторы toll-подобных рецепторов для лечения вич
EA202091115A1 (ru) Производные хиназолина, применяемые для лечения вич
EA201600204A1 (ru) Производные хиназолина, фармацевтическая композиция на их основе и их применение для профилактики или лечения опухоли
BR112016027048A8 (pt) uso de um composto de fórmula i no tratamento de câncer cerebral e glioblastoma multiforme mgmt positivo
EA201791420A1 (ru) Соединения триазолопиримидина и их применения
EA201891063A1 (ru) Производные дигидроимидазопиразинона, применимые в лечении рака
BR112015029455A8 (pt) compostos químicos, uso, métodos e composições para prevenção ou tratamento de câncer
EA201691151A1 (ru) Соединения для лечения пациентов с ros1-мутантными раковыми клетками
EA201691988A1 (ru) Производные бороновой кислоты и их терапевтическое применение
EA201591532A1 (ru) Ингибиторы carm1 и их применение
EA201990424A1 (ru) Спиролактамовые модуляторы nmda-рецептора и их применение
EA201591825A1 (ru) Антагонизм миостатина у субъектов - людей
MX368903B (es) Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas.
CY1123636T1 (el) Διαθεσιμες πολυαμινες
EA201990425A1 (ru) Спиролактамовые и бис-спиролактамовые модуляторы nmda-рецептора и их применение
EA201792591A1 (ru) Фармацевтические препараты
BR112017000730B8 (pt) Derivados de pirrolidinona como inibidores de metap-2, e medicamentos
EA201692032A1 (ru) Антибактериальные соединения
EA201591391A1 (ru) Производное 2-ациламинотиазола или его соль
CA3011073A1 (en) Transdermal patch
MA39765A (fr) Formulation pharmaceutique d'un inhibiteur de la kinase pan-raf, ses procédés de préparation, et procédés d'utilisation
EA201990095A1 (ru) КОНДЕНСИРОВАННЫЕ ТИОФЕНОВЫЕ ПРОИЗВОДНЫЕ, ПРИЕМЛЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ NAPI-IIb
EA201690974A1 (ru) Гидроморфон и налоксон для лечения боли и индуцированного опиоидами синдрома дисфункции кишечника