EA200900245A1 - Модуляторы активности рецептора хемокина, кристалические формы и способ их получения - Google Patents

Модуляторы активности рецептора хемокина, кристалические формы и способ их получения

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Publication number
EA200900245A1
EA200900245A1 EA200900245A EA200900245A EA200900245A1 EA 200900245 A1 EA200900245 A1 EA 200900245A1 EA 200900245 A EA200900245 A EA 200900245A EA 200900245 A EA200900245 A EA 200900245A EA 200900245 A1 EA200900245 A1 EA 200900245A1
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Eurasian Patent Office
Prior art keywords
present
hemokin
reception
receptor activity
crystal forms
Prior art date
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EA200900245A
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English (en)
Other versions
EA016563B1 (ru
Inventor
Перси Х. Картер
Джон В. Данциа
Богуслав М. Мадрик
Майкл Е. Рандаззо
Цили Сяо
Майкл Г. Ян
Рулин Чжао
Original Assignee
Бристол-Маерс Сквибб Компани
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Publication of EA200900245A1 publication Critical patent/EA200900245A1/ru
Publication of EA016563B1 publication Critical patent/EA016563B1/ru

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    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
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    • C07D317/72—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 spiro-condensed with carbocyclic rings

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Abstract

Настоящее изобретение обеспечивает новый антагонист или частичный агонист/антагонист активности MCP-I рецептора: N-((1R,2S,5R)-5-(-бутиламино)-2-((S)-2-оксо-3-(6-(трифторметил)хиназолин-4-иламино)пирролидин-1-ил)циклогексил)ацетамид или его фармацевтически приемлемую соль, сольват или пролекарство, имеющий неожиданную комбинацию из требуемых фармакологических характеристик. Также обеспечиваются кристаллические формы по настоящему изобретению. Фармацевтические композиции, содержащие их, и способы их применения в виде агентов лечения воспалительных заболеваний, аллергических, аутоиммунных, метаболических, раковых и/или сердечно-сосудистых заболеваний, являются также целью настоящего изобретения. Настоящее изобретение также обеспечивает способ получения соединений формулы (I), включая N-((1R,2S,5R)-5-(-бутиламино)-2-((S)-2-оксо-3-(6-(трифторметил)хиназолин-4-иламино)пирролидин-1-ил)циклогексил)ацетамид, где R, R, R, Rи "НЕТ" являются теми, как описано в настоящем изобретении. Соединения, которые являются полезными промежуточными соединениями процесса, также обеспечены в настоящем изобретении.
EA200900245A 2006-07-28 2007-07-26 Модуляторы активности рецептора хемокина, кристаллические формы и способ их получения EA016563B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US83423506P 2006-07-28 2006-07-28
US89602607P 2007-03-21 2007-03-21
US11/782,742 US7629351B2 (en) 2006-07-28 2007-07-25 N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process
PCT/US2007/074377 WO2008014360A2 (en) 2006-07-28 2007-07-26 Modulators of chemokine receptor activity, crystalline forms and process

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EA200900245A1 true EA200900245A1 (ru) 2009-08-28
EA016563B1 EA016563B1 (ru) 2012-05-30

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US (2) US7629351B2 (ru)
EP (2) EP2046779B1 (ru)
JP (1) JP5236643B2 (ru)
KR (1) KR20090033915A (ru)
CN (1) CN101535301B (ru)
AR (1) AR062124A1 (ru)
AT (2) ATE522522T1 (ru)
AU (1) AU2007279333B2 (ru)
BR (1) BRPI0715415A2 (ru)
CA (2) CA2659253A1 (ru)
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DK (1) DK2046779T3 (ru)
EA (1) EA016563B1 (ru)
ES (1) ES2365264T3 (ru)
HK (1) HK1130476A1 (ru)
HR (1) HRP20110465T1 (ru)
IL (2) IL196427A (ru)
MX (1) MX2009000808A (ru)
NO (1) NO20090190L (ru)
NZ (1) NZ574425A (ru)
PE (1) PE20080732A1 (ru)
PL (1) PL2046779T3 (ru)
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EP2046779B1 (en) 2011-05-18
AR062124A1 (es) 2008-10-15
ATE522522T1 (de) 2011-09-15
CA2659253A1 (en) 2008-01-31
CN101535301B (zh) 2014-06-18
MX2009000808A (es) 2009-01-29
DK2046779T3 (da) 2011-09-05
CA2831219A1 (en) 2008-01-31
US7629351B2 (en) 2009-12-08
US20100113489A1 (en) 2010-05-06
ES2365264T3 (es) 2011-09-27
PT2046779E (pt) 2011-07-25
WO2008014360A2 (en) 2008-01-31
NO20090190L (no) 2009-01-29
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CY1111744T1 (el) 2015-10-07
PL2046779T3 (pl) 2011-09-30
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IL196427A (en) 2013-02-28
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KR20090033915A (ko) 2009-04-06
TW201414729A (zh) 2014-04-16
IL206679A0 (en) 2010-12-30
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CN101535301A (zh) 2009-09-16
ATE509926T1 (de) 2011-06-15
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SI2046779T1 (sl) 2011-09-30
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HRP20110465T1 (hr) 2011-07-31
AU2007279333A1 (en) 2008-01-31
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EA016563B1 (ru) 2012-05-30
WO2008014360A3 (en) 2008-12-31
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PE20080732A1 (es) 2008-06-13

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