PE20121433A1 - Compuestos de indazol y pirazolopiridina como antagonistas del receptor de ccr1 - Google Patents

Compuestos de indazol y pirazolopiridina como antagonistas del receptor de ccr1

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Publication number
PE20121433A1
PE20121433A1 PE2012000493A PE2012000493A PE20121433A1 PE 20121433 A1 PE20121433 A1 PE 20121433A1 PE 2012000493 A PE2012000493 A PE 2012000493A PE 2012000493 A PE2012000493 A PE 2012000493A PE 20121433 A1 PE20121433 A1 PE 20121433A1
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Peru
Prior art keywords
pyridin
alkyl
alcoxy
pyrazolo
cyclopropyl
Prior art date
Application number
PE2012000493A
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English (en)
Inventor
Brian Nicholas Cook
Daniel Kuzmich
Can Mao
Hossein Razavi
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Boehringer Ingelheim Int
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43126891&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121433(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20121433A1 publication Critical patent/PE20121433A1/es

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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62Oxygen or sulfur atoms
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    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: Ar1 ES CARBOCICLO, HETEROARILO O HETEROCICLILO CADA UNO OPCIONALMENTE SUSTITUIDO CON UNO A TRES Ra; Ar2 ES CARBOCICLO, HETEROARILO O HETEROCICLILO CADA UNO OPCIONALMENTE SUSTITUIDO CON UNO A TRES Rb; X ES N O C-R2; G ES CARBOCICLO O HETEROCICLILO CADA UNO OPCIONALMENTE SUSTITUIDO CON UNO A DOS Rg; R1 ES H, ALQUILO C1-6 O (ALCOXI C1-6)-(ALQUILO C1-6); R2 ES H O Ra; Ra ES ALQUILO C1-6, CICLOALQUILO C3-10, ALCOXI C1-6, ALQUIL C1-6-TIO, ENTRE OTROS; Rb ES HIDROXILO, CARBOXILO, HALOGENO, NITRO, ENTRE OTROS; Rg ES ALQUENILO C2-6, CARBOCICLO, ALCOXI C1-6, HIDROXILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (1-1,3,4-TIADIAZOL-2-IL-CICLOPROPIL)-AMIDA DEL ACIDO 1-(4-FLUORO-FENIL)-1H-PIRAZOLO[3,4-c]PIRIDIN-4-CARBOXILICO; [1-(6-BROMO-PIRIDIN-3-IL)-CICLOPROPIL]-AMIDA DEL ACIDO 1-(4-FLUORO-FENIL)-1H-PIRAZOLO[3,4-c]PIRIDIN-4-CARBOXILICO;ESTER METILICO DEL ACIDO 3-(1-{[1-(4-FLUORO-FENIL)-1H-PIRAZOLO[3,4-c]PIRIDIN-4-CARBONIL]-AMINO}-CICLOPROPIL)-BENZOICO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHO COMPUESTO ES ANTAGONISTA DE LA ACTIVIDAD DEL RECEPTOR DE CITOQUINA QUIMIOTACTICO 1 (CCR1), SIENDO UTIL EN EL TRATAMIENTO DE ENFERMEDADES AUTOINMUNES
PE2012000493A 2009-10-21 2010-10-19 Compuestos de indazol y pirazolopiridina como antagonistas del receptor de ccr1 PE20121433A1 (es)

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US25359009P 2009-10-21 2009-10-21

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PE20121433A1 true PE20121433A1 (es) 2012-11-10

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US (1) US9056858B2 (es)
EP (1) EP2491028B1 (es)
JP (1) JP5542946B2 (es)
KR (1) KR20120087923A (es)
CN (1) CN102666526A (es)
AP (1) AP2012006204A0 (es)
AU (1) AU2010308277A1 (es)
BR (1) BR112012009331A2 (es)
CA (1) CA2778060A1 (es)
CL (1) CL2012000967A1 (es)
CO (1) CO6531488A2 (es)
DK (1) DK2491028T3 (es)
EA (1) EA021015B1 (es)
EC (1) ECSP12011904A (es)
ES (1) ES2444780T3 (es)
GE (1) GEP20146103B (es)
HR (1) HRP20140213T1 (es)
IL (1) IL218823A0 (es)
IN (1) IN2012DN03449A (es)
MA (1) MA33675B1 (es)
MX (1) MX2012004644A (es)
NZ (1) NZ599132A (es)
PE (1) PE20121433A1 (es)
PL (1) PL2491028T3 (es)
PT (1) PT2491028E (es)
RS (1) RS53130B (es)
SI (1) SI2491028T1 (es)
TN (1) TN2012000180A1 (es)
WO (1) WO2011049917A1 (es)

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RS53130B (en) 2009-10-21 2014-06-30 Boehringer Ingelheim International Gmbh INDASOL AND PYRAZOLOPYRIDINE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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HRP20140213T1 (hr) 2014-04-11
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US9056858B2 (en) 2015-06-16
DK2491028T3 (da) 2014-01-13
WO2011049917A1 (en) 2011-04-28
NZ599132A (en) 2014-05-30
PT2491028E (pt) 2014-02-04
BR112012009331A2 (pt) 2019-09-24
CO6531488A2 (es) 2012-09-28
PL2491028T3 (pl) 2014-05-30
SI2491028T1 (sl) 2014-03-31
JP2013508376A (ja) 2013-03-07
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