AR076329A1 - 4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades. - Google Patents

4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades.

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Publication number
AR076329A1
AR076329A1 ARP100101288A ARP100101288A AR076329A1 AR 076329 A1 AR076329 A1 AR 076329A1 AR P100101288 A ARP100101288 A AR P100101288A AR P100101288 A ARP100101288 A AR P100101288A AR 076329 A1 AR076329 A1 AR 076329A1
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Argentina
Prior art keywords
alkyl
so2ch3
4alkyl
benzo
group
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ARP100101288A
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English (en)
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Janssen Pharmaceutica Nv
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Publication of AR076329A1 publication Critical patent/AR076329A1/es

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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract

Reivindicacion 1: Un compuesto de formula (1) X es H, F, OH, o NH2; R1 es formulas (2), -O-benzoisotiazol-3-ilo, -O-benzoisoxazolilo, -O-benzotiazolilo, -O-benzoxazolilo, -O-benzofurilo, -O-indolilo, -O-benzoimidazolilo, -O-indazolilo, -O-furilo, -O-imidazolilo, -O-oxazolilo, -O-isoxazolilo, -O-tiofenilo, -O-benzotiofenilo, -O-tiazolilo, -O-isotiazolilo, -O-piridazilo, -O-pirazolilo, -O-pirrolilo, -O-benzo[1,3]dioxolilo, -O-pirimidilo, indazol-1-ilo, -O-piridilo, imidazol-1-ilo, piridon-1-ilo, pirimidon-1-ilo, pirazol-1-ilo, indol-1-ilo, piridaz-1-ilo, o pirrol-1-ilo; alternativamente, R1 y X pueden tomarse conjuntamente con su carbono adjunto para formar un anillo seleccionado del grupo que consiste de formulas 3 a 7 y en donde en formula 7 cualquier R1 puede ser sustituido con hasta dos grupos metilo, o un sustituyente seleccionado del grupo que consiste de: alquilo de OC1-4, cicloalquilo de OC3-6, OCH2CF3, OCH2Ph, F, I, CN, CI, OCF3, CF3, CH2CN, alquilo C1-4, CH2CF3, N(alquilo C1-4)2, alquilo C1-4OH, Si(CH3)3, :::-x-, (CH3)3Si-:::-z, SCH3, S(O)CH3, pirrolidinilo de SO2CH3, OH, NH2, NHCN, CO2H, CONH2, alquilo de NHCO2C1-4, N(SO2CH3)2, NHSO2CH3, NHC(O)CF3, alquilo de NHC1-4, NHCO2H, alquilo de NHCO2C1-4, NHCOC1-4alquilo, NHCONH2, alquilo de NHCONHC1-4 y Br; R2 es alquilo C1-4, NH2, NO2, NHCH2CH2OH, alquilo de N(C1-4)2, N(SO2CH3)2, CN, F, CI, Br, CF3, cicloalquilo, heterociclilo, OCF3, OCF2H, CF2H, o alquilo de OC1-4; R3 es H, F, CI, CF3, o OC1-4alquilo; alternativamente, R2 y R3 pueden tomarse juntos con su fenilo adjunto para formar un grupo benzo[1,3]dioxolilo, 2,3-dihidro-benzofuranilo, o 2,3-dihidro-benzo[1,4]dioxinilo; R4 es H, OC1-4alquilo, o F; y solvatos, hidratos, tautomeros y sales farmacéuticamente aceptables de éstos.
ARP100101288A 2009-04-17 2010-04-19 4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades. AR076329A1 (es)

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US17022509P 2009-04-17 2009-04-17

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AR076329A1 true AR076329A1 (es) 2011-06-01

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US (1) US8324186B2 (es)
EP (1) EP2419418B1 (es)
JP (1) JP5685581B2 (es)
KR (1) KR20120006051A (es)
CN (1) CN102459226B (es)
AR (1) AR076329A1 (es)
AU (1) AU2010236336B2 (es)
BR (1) BRPI1016205A2 (es)
CA (1) CA2758929A1 (es)
ES (1) ES2541607T3 (es)
MX (1) MX2011010963A (es)
NZ (1) NZ595433A (es)
TW (1) TW201102379A (es)
WO (1) WO2010121036A1 (es)

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JP5685580B2 (ja) * 2009-04-16 2015-03-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ Ｃｃｒ２の４−アゼチジニル−１−ヘテロアリール−シクロヘキサンアンタゴニスト
CN102459226B (zh) 2009-04-17 2014-09-17 詹森药业有限公司 Ccr2的4-氮杂环丁烷基-1-杂原子连接的-环己烷拮抗剂
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JP5685580B2 (ja) 2009-04-16 2015-03-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ Ｃｃｒ２の４−アゼチジニル−１−ヘテロアリール−シクロヘキサンアンタゴニスト
EP2419419B1 (en) 2009-04-17 2014-12-03 Janssen Pharmaceutica NV 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2
CN102459226B (zh) 2009-04-17 2014-09-17 詹森药业有限公司 Ccr2的4-氮杂环丁烷基-1-杂原子连接的-环己烷拮抗剂

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US8324186B2 (en) 2012-12-04
AU2010236336B2 (en) 2015-01-15
JP2012524110A (ja) 2012-10-11
MX2011010963A (es) 2011-11-02
CN102459226B (zh) 2014-09-17
US20100267668A1 (en) 2010-10-21
EP2419418B1 (en) 2015-04-15
WO2010121036A1 (en) 2010-10-21
CN102459226A (zh) 2012-05-16
BRPI1016205A2 (pt) 2016-04-19
TW201102379A (en) 2011-01-16
CA2758929A1 (en) 2010-10-21
KR20120006051A (ko) 2012-01-17
NZ595433A (en) 2013-12-20
AU2010236336A1 (en) 2011-11-03
ES2541607T3 (es) 2015-07-22
JP5685581B2 (ja) 2015-03-18

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