EA201391233A1 - Кристаллические формы и способы получения модуляторов каннабиноидного рецептора - Google Patents

Кристаллические формы и способы получения модуляторов каннабиноидного рецептора

Info

Publication number
EA201391233A1
EA201391233A1 EA201391233A EA201391233A EA201391233A1 EA 201391233 A1 EA201391233 A1 EA 201391233A1 EA 201391233 A EA201391233 A EA 201391233A EA 201391233 A EA201391233 A EA 201391233A EA 201391233 A1 EA201391233 A1 EA 201391233A1
Authority
EA
Eurasian Patent Office
Prior art keywords
disease
hyperalgesia
inflammatory
cannabinoid receptor
osteoarthritis
Prior art date
Application number
EA201391233A
Other languages
English (en)
Other versions
EA035989B1 (ru
Inventor
Энтони К. Блэкберн
Сангдон Хан
Роберт М. Джонс
Антонио Гарридо Монтальбан
Байман Б. Пэл
Джейми Карин Рютер
Original Assignee
Арена Фармасьютикалз, 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 Арена Фармасьютикалз, Инк. filed Critical Арена Фармасьютикалз, Инк.
Publication of EA201391233A1 publication Critical patent/EA201391233A1/ru
Publication of EA035989B1 publication Critical patent/EA035989B1/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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

Настоящее изобретение относится к кристаллическим формам ((S)-1-гидроксиметил-2,2-диметилпропил)амида (1aS,5aS)-2-(4-оксипиразин-2-ил)-1a,2,5,5а-тетрагидро-1Н-2,3-диазациклопропа[а]пентален-4-карбоновой кислоты (соединение 1) и содержащим их фармацевтическим композициям, которые модулируют активность каннабиноидного рецептора СВи поэтому применимы для лечения опосредуемых рецептором CBнарушений, например остеоартрита; боли; гипералгезии; аллодинии; воспалительной гипералгезии; невропатической гипералгезии; острой ноцицепции; остеопороза; спастичности, связанной с рассеянным склерозом; аутоиммунных нарушений; аллергических реакций; воспаления ЦНС, например; атеросклероза; нежелательной активности иммунных клеток и воспаления, связанного с нарушением, выбранным из группы, включающей остеоартрит, анафилаксию, болезнь Бехчета, отторжение трансплантата, васкулит, подагру, спондилит, вирусное заболевание, бактериальное заболевание, волчанку, воспалительную болезнь кишечника, аутоиммунный гепатит и сахарный диабет типа 1; возрастной дегенерации желтого пятна; кашля; лейкоза; лимфомы; опухолей ЦНС; рака предстательной железы; болезни Альцгеймера; вызванного ударом поражения; слабоумия; бокового амиотрофического склероза и болезни Паркинсона.
EA201391233A 2011-02-25 2012-02-24 Кристаллические формы и способы получения модуляторов каннабиноидного рецептора EA035989B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161446732P 2011-02-25 2011-02-25
US201161448542P 2011-03-02 2011-03-02
PCT/US2012/026506 WO2012116276A1 (en) 2011-02-25 2012-02-24 Crystalline forms and processes for the preparation of condensed azacycles ( cannabinoid receptor modulators)

Publications (2)

Publication Number Publication Date
EA201391233A1 true EA201391233A1 (ru) 2014-02-28
EA035989B1 EA035989B1 (ru) 2020-09-09

Family

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EA201391233A EA035989B1 (ru) 2011-02-25 2012-02-24 Кристаллические формы и способы получения модуляторов каннабиноидного рецептора

Country Status (19)

Country Link
US (4) US9458136B2 (ru)
EP (3) EP2678330A1 (ru)
JP (1) JP5945554B2 (ru)
KR (1) KR102036932B1 (ru)
CN (1) CN103608343B (ru)
AU (1) AU2012222146B2 (ru)
BR (1) BR112013021549B1 (ru)
CA (1) CA2827057C (ru)
CL (1) CL2013002436A1 (ru)
CO (1) CO6852066A2 (ru)
DK (1) DK3395812T3 (ru)
EA (1) EA035989B1 (ru)
ES (1) ES2932441T3 (ru)
IL (1) IL227782A (ru)
MX (1) MX346533B (ru)
MY (1) MY165767A (ru)
SG (1) SG192817A1 (ru)
WO (1) WO2012116276A1 (ru)
ZA (1) ZA201306402B (ru)

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Also Published As

Publication number Publication date
NZ614787A (en) 2014-08-29
CN103608343B (zh) 2019-02-01
BR112013021549A2 (pt) 2016-11-01
AU2012222146B2 (en) 2017-05-11
EA035989B1 (ru) 2020-09-09
AU2012222146A1 (en) 2013-09-19
US20140135345A1 (en) 2014-05-15
ZA201306402B (en) 2022-03-30
US10183930B2 (en) 2019-01-22
EP3395812B8 (en) 2022-11-02
CN103608343A (zh) 2014-02-26
IL227782A (en) 2017-02-28
EP2678330A1 (en) 2014-01-01
US20210380560A1 (en) 2021-12-09
US20190308952A1 (en) 2019-10-10
JP2014506602A (ja) 2014-03-17
MX2013009760A (es) 2014-06-11
CL2013002436A1 (es) 2014-01-24
US11560369B2 (en) 2023-01-24
CA2827057C (en) 2022-06-07
WO2012116276A1 (en) 2012-08-30
US20170144993A1 (en) 2017-05-25
IL227782A0 (en) 2013-09-30
JP5945554B2 (ja) 2016-07-05
MX346533B (es) 2017-03-14
SG192817A1 (en) 2013-09-30
KR102036932B1 (ko) 2019-10-25
KR20140025353A (ko) 2014-03-04
ES2932441T3 (es) 2023-01-19
US9458136B2 (en) 2016-10-04
CO6852066A2 (es) 2014-01-30
BR112013021549B1 (pt) 2022-01-11
DK3395812T3 (da) 2022-11-28
CA2827057A1 (en) 2012-08-30
MY165767A (en) 2018-04-23
EP3395812B1 (en) 2022-09-28
EP4166552A1 (en) 2023-04-19
EP3395812A1 (en) 2018-10-31
US10981895B2 (en) 2021-04-20

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