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MX2012003720A - N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos. - Google Patents

N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos.

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Publication number
MX2012003720A
MX2012003720A MX2012003720A MX2012003720A MX2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A
Authority
MX
Mexico
Prior art keywords
tert
oxopyrrolidin
triazin
ylamino
butylamino
Prior art date
Application number
MX2012003720A
Other languages
English (en)
Inventor
Percy H Carter
Robert J Cherney
Victor W Rosso
Li Jun
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MX2012003720A publication Critical patent/MX2012003720A/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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Abstract

La presente invención proporciona un antagonista novedoso: N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-3-(7-tert-butilpirazolo[ 1,5-a] [1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida: (ver fórmula) o su sal, solvato o profármaco, farmacéuticamente aceptable, que tiene una actividad del receptor dual de CCR-2 y CCR-5 inesperada. También se describen formas cristalinas, metabolitos, composiciones farmacéuticas que contienen los mismos y procesos de uso de los mismos como agentes para el tratamiento de enfermedades inflamatorias, alérgicas, autoinmunes, metabólicas, cáncer y/o cardiovasculares. La presente invención también proporciona procesos de preparación de compuestos de Fórmula (I) como los provistos en la presente, incluyendo N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-3-(7-tert-buti lpirazolo[1,5-a] [1,3,S]triazin-4-ilamino)-2-oxopirrolidin-1-il)ci clohexil)acetamida. También se proporcionan en la presente compuestos que son intermediarios útiles del proceso.
MX2012003720A 2009-10-13 2010-10-12 N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos. MX2012003720A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25097809P 2009-10-13 2009-10-13
PCT/US2010/052288 WO2011046916A1 (en) 2009-10-13 2010-10-12 N-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes

Publications (1)

Publication Number Publication Date
MX2012003720A true MX2012003720A (es) 2012-04-30

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MX2012003720A MX2012003720A (es) 2009-10-13 2010-10-12 N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos.

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US (3) US8383812B2 (es)
EP (2) EP2664620A3 (es)
JP (1) JP5759999B2 (es)
KR (1) KR20120102052A (es)
CN (1) CN102648201B (es)
AR (1) AR078627A1 (es)
AU (1) AU2010306968B2 (es)
BR (1) BR112012008650B1 (es)
CA (1) CA2777563A1 (es)
CL (1) CL2014000753A1 (es)
CO (1) CO6460737A2 (es)
DK (1) DK2488523T3 (es)
EA (2) EA201490744A1 (es)
ES (1) ES2442897T3 (es)
HK (1) HK1174614A1 (es)
HR (1) HRP20140072T1 (es)
IL (2) IL219121A0 (es)
MX (1) MX2012003720A (es)
NZ (2) NZ613580A (es)
PE (1) PE20121349A1 (es)
PL (1) PL2488523T3 (es)
PT (1) PT2488523E (es)
RS (1) RS53131B (es)
SI (1) SI2488523T1 (es)
SM (1) SMT201400020B (es)
TN (1) TN2012000132A1 (es)
TW (1) TW201120042A (es)
WO (1) WO2011046916A1 (es)
ZA (1) ZA201305994B (es)

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US8383812B2 (en) * 2009-10-13 2013-02-26 Bristol-Myers Squibb Company N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes
KR20170029513A (ko) * 2014-07-17 2017-03-15 산텐 세이야꾸 가부시키가이샤 후안부 질환의 예방 또는 치료제
US11052069B2 (en) 2016-09-14 2021-07-06 Novartis Ag Regimes of FXR agonists
JOP20190040A1 (ar) 2016-09-14 2019-03-10 Novartis Ag توليفة من ناهضات fxr
KR20200031656A (ko) 2017-07-20 2020-03-24 브리스톨-마이어스 스큅 컴퍼니 N-((1R,2S,5R)-5-(tert-부틸아미노)-2-((S)-3-(7-tert-부틸피라졸로[1,5-a][1,3,5]트리아진-4-일아미노)-2-옥소피롤리딘-1-일)시클로헥실)아세트아미드의 제조 방법
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