EA201690373A1 - СОЛЬ КРИСТАЛЛИЧЕСКОГО ПОЛИМОРФА ФОРМЫ 2 N-[1-6-(ЭТИНИЛ-3-ОКСОГЕКСАГИДРОФУРО[3,2-b]ПИРРОЛ-4-КАРБОНИЛ)-3-МЕТИЛБУТИЛ]-4-[5-ФТОР-2-(4-МЕТИЛПИПЕРАЗИНИЛ)ТИАЗОЛ-4-ИЛ]БЕНЗАМИДА, ПОЛЕЗНАЯ В КАЧЕСТВЕ ИНГИБИТОРА ЦИСТЕИНПРОТЕАЗЫ - Google Patents

СОЛЬ КРИСТАЛЛИЧЕСКОГО ПОЛИМОРФА ФОРМЫ 2 N-[1-6-(ЭТИНИЛ-3-ОКСОГЕКСАГИДРОФУРО[3,2-b]ПИРРОЛ-4-КАРБОНИЛ)-3-МЕТИЛБУТИЛ]-4-[5-ФТОР-2-(4-МЕТИЛПИПЕРАЗИНИЛ)ТИАЗОЛ-4-ИЛ]БЕНЗАМИДА, ПОЛЕЗНАЯ В КАЧЕСТВЕ ИНГИБИТОРА ЦИСТЕИНПРОТЕАЗЫ

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Publication number
EA201690373A1
EA201690373A1 EA201690373A EA201690373A EA201690373A1 EA 201690373 A1 EA201690373 A1 EA 201690373A1 EA 201690373 A EA201690373 A EA 201690373A EA 201690373 A EA201690373 A EA 201690373A EA 201690373 A1 EA201690373 A1 EA 201690373A1
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EA
Eurasian Patent Office
Prior art keywords
methylbutyl
thi
ethinyl
carbonyl
benzamide
Prior art date
Application number
EA201690373A
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English (en)
Other versions
EA032409B1 (ru
Inventor
Урсула Грабовска
Лурдес Сальвадоре-Оден
Виктор М. Диас Перес
Эндрю Карр
Original Assignee
Медивир Аб
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Publication date
Application filed by Медивир Аб filed Critical Медивир Аб
Publication of EA201690373A1 publication Critical patent/EA201690373A1/ru
Publication of EA032409B1 publication Critical patent/EA032409B1/ru

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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

Предложен кристаллический полиморф формы 2, состоящий из моногидрохлорида N-[1-6-(этинил-3-оксогексагидрофуро[3,2-b]пиррол-4-карбонил)-3-метилбутил]-4-[5-фтор-2-(4-метилпиперазин-1-ил)тиазол-4-ил]бензамида и моногидрохлорида N-[1-6-(этинил-3-оксогексагидрофуро[3,2-b]пиррол-4-карбонил)-3-метилбутил]-4-[5-фтор-2-(4-метилпиперазин-1-ил)тиазол-4-ил]бензамидгидрата, его применение в качестве медицинского средства и способы его получения.
EA201690373A 2013-08-13 2014-08-13 СОЛЬ КРИСТАЛЛИЧЕСКОГО ПОЛИМОРФА ФОРМЫ 2 N-[1-6-(ЭТИНИЛ-3-ОКСОГЕКСАГИДРОФУРО[3,2-b]ПИРРОЛ-4-КАРБОНИЛ)-3-МЕТИЛБУТИЛ]-4-[5-ФТОР-2-(4-МЕТИЛПИПЕРАЗИНИЛ)ТИАЗОЛ-4-ИЛ]БЕНЗАМИДА, ПОЛЕЗНАЯ В КАЧЕСТВЕ ИНГИБИТОРА ЦИСТЕИНПРОТЕАЗЫ EA032409B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1314503.2A GB201314503D0 (en) 2013-08-13 2013-08-13 Cysteine protease inhibitor salt
PCT/EP2014/067374 WO2015022385A1 (en) 2013-08-13 2014-08-13 Form 2 crystalline polymorph of a salt of n-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazinyl)thiazol-4-yl]-benzamide useful as cysteine protease inhibitor

Publications (2)

Publication Number Publication Date
EA201690373A1 true EA201690373A1 (ru) 2016-07-29
EA032409B1 EA032409B1 (ru) 2019-05-31

Family

ID=49262126

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690373A EA032409B1 (ru) 2013-08-13 2014-08-13 СОЛЬ КРИСТАЛЛИЧЕСКОГО ПОЛИМОРФА ФОРМЫ 2 N-[1-6-(ЭТИНИЛ-3-ОКСОГЕКСАГИДРОФУРО[3,2-b]ПИРРОЛ-4-КАРБОНИЛ)-3-МЕТИЛБУТИЛ]-4-[5-ФТОР-2-(4-МЕТИЛПИПЕРАЗИНИЛ)ТИАЗОЛ-4-ИЛ]БЕНЗАМИДА, ПОЛЕЗНАЯ В КАЧЕСТВЕ ИНГИБИТОРА ЦИСТЕИНПРОТЕАЗЫ

Country Status (17)

Country Link
US (1) US9650388B2 (ru)
EP (1) EP3033345B1 (ru)
JP (1) JP6530752B2 (ru)
KR (1) KR102271944B1 (ru)
CN (1) CN105612160B (ru)
AU (1) AU2014307850B8 (ru)
BR (1) BR112016003169B1 (ru)
CA (1) CA2920797C (ru)
EA (1) EA032409B1 (ru)
GB (1) GB201314503D0 (ru)
HK (1) HK1218915A1 (ru)
MX (1) MX369144B (ru)
MY (1) MY180170A (ru)
SG (1) SG11201600979SA (ru)
TW (1) TWI648278B (ru)
WO (1) WO2015022385A1 (ru)
ZA (1) ZA201600952B (ru)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0817425D0 (en) * 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors
GB0817424D0 (en) * 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors
CN102858751A (zh) * 2009-12-10 2013-01-02 美迪维尔英国有限公司 半胱氨酸蛋白酶抑制剂

Also Published As

Publication number Publication date
EP3033345A1 (en) 2016-06-22
KR20160042107A (ko) 2016-04-18
AU2014307850A1 (en) 2016-03-03
EP3033345B1 (en) 2017-07-26
JP6530752B2 (ja) 2019-06-12
MX369144B (es) 2019-10-30
CA2920797C (en) 2021-06-15
JP2016530260A (ja) 2016-09-29
HK1218915A1 (zh) 2017-03-17
KR102271944B1 (ko) 2021-07-02
BR112016003169A2 (ru) 2017-08-01
CN105612160A (zh) 2016-05-25
CA2920797A1 (en) 2015-02-19
BR112016003169B1 (pt) 2023-02-23
SG11201600979SA (en) 2016-03-30
WO2015022385A1 (en) 2015-02-19
US20160194334A1 (en) 2016-07-07
MX2016001978A (es) 2017-01-26
TW201536788A (zh) 2015-10-01
CN105612160B (zh) 2017-11-24
AU2014307850A8 (en) 2017-03-02
EA032409B1 (ru) 2019-05-31
MY180170A (en) 2020-11-24
AU2014307850B2 (en) 2017-02-02
TWI648278B (zh) 2019-01-21
GB201314503D0 (en) 2013-09-25
AU2014307850B8 (en) 2017-03-02
US9650388B2 (en) 2017-05-16
ZA201600952B (en) 2017-07-26

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