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

    • 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
    • A61K31/74—Synthetic polymeric materials
    • A61K31/785—Polymers containing nitrogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886—Dragees; 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C07C237/06—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/22—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/126—Acids containing more than four carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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) EP3432914B1 (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
HUE052620T2 (hu) 2016-03-25 2021-05-28 Aminex Therapeutics Inc Biológiailag hozzáférhetõ poliaminok
WO2022072586A1 (en) 2020-09-30 2022-04-07 Aminex Therapeutics, Inc. Combination drug substance of polyamine transport inhibitor and dfmo
US20230321012A1 (en) * 2021-12-01 2023-10-12 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
EP0187332B1 (en) 1985-01-10 1989-02-01 Molecular Diagnostics, Inc. Photochemical method of labelling nucleic acids for detection in hybridization assays
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
EP0597830A1 (en) 1989-07-03 1994-05-25 New York University Nyu Medical Center Use of polyamines as ionic-channel regulating agents
US5274113A (en) 1991-11-01 1993-12-28 Molecular Probes, Inc. Long wavelength chemically reactive dipyrrometheneboron difluoride dyes and conjugates
US5433896A (en) 1994-05-20 1995-07-18 Molecular Probes, Inc. Dibenzopyrrometheneboron difluoride dyes
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
JPH09509484A (ja) 1994-02-08 1997-09-22 エヌピーエス・ファルマシューティカルズ，インコーポレイテッド 神経障害および神経病の治療に有用な受容体作動性カルシウムチャネル上の新規部位で活性な化合物
KR19980701677A (ko) 1995-01-25 1998-06-25 에이치. 캐서린 화이트 팽창 쿠션 및 그 제조 방법
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
AU723825B2 (en) 1996-03-14 2000-09-07 Msd Consumer Care, Inc. Sunless tanning composition and method
US6172261B1 (en) 1997-07-15 2001-01-09 Oridigm Corporation 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
AU1998899A (en) 1998-12-10 2000-06-26 Ilex Oncology, Inc. Polyamine transport inhibitors
ATE308515T1 (de) 1999-02-05 2005-11-15 Oridigm Corp Antizymmodulatoren sowie deren verwendung
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
US6872852B2 (en) 2000-03-24 2005-03-29 Mediquest Therapeutics, Inc. Polyamine analogues as cytotoxic agents
USRE43327E1 (en) 2001-01-08 2012-04-24 Aminex Therapeutics, Inc. Hydrophobic polyamine analogs and methods for their use
KR100859929B1 (ko) * 2001-01-08 2008-09-23 메디퀘스트 세라퓨틱스 아이엔씨 소수성 폴리아민 유사체들과 그 사용
US7432302B2 (en) 2001-01-08 2008-10-07 Mediquest Therapeutics, Inc. Composition containing polyamine transport inhibitor and use thereof
US6914079B2 (en) 2002-09-23 2005-07-05 Mediquest Therapeutics, Inc. Polyamine analogs that activate antizyme frameshifting
US7144920B2 (en) 2002-09-23 2006-12-05 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
WO2007001455A2 (en) 2004-11-12 2007-01-04 Mediquest Therapeutics, Inc. Hydrophobic polyamine amides as potent lipopolysaccharide sequestrants
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
ES2715173T3 (es) 2009-07-16 2019-06-03 Pathologica Llc Producto farmacéutico para administración oral que comprende MGBG y métodos de tratamiento de enfermedades
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
HUE052620T2 (hu) 2016-03-25 2021-05-28 Aminex Therapeutics Inc Biológiailag hozzáférhetõ poliaminok

Also Published As

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

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