AR074870A1 - DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINA - Google Patents

DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINA

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Publication number
AR074870A1
AR074870A1 ARP090105067A ARP090105067A AR074870A1 AR 074870 A1 AR074870 A1 AR 074870A1 AR P090105067 A ARP090105067 A AR P090105067A AR P090105067 A ARP090105067 A AR P090105067A AR 074870 A1 AR074870 A1 AR 074870A1
Authority
AR
Argentina
Prior art keywords
4alkyl
alkyl
ring
optionally
haloc1
Prior art date
Application number
ARP090105067A
Other languages
Spanish (es)
Inventor
Soliva Robert Soliva
Porras Jose Javier Pastor
Rosales Carmen Almansa
Solana Jorge Salas
Ustrell Montserrat Fontes
Espuga Josep Comelles
Original Assignee
Palau Pharma Sa
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 Palau Pharma Sa filed Critical Palau Pharma Sa
Publication of AR074870A1 publication Critical patent/AR074870A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

Abstract

Estos compuestos son útiles como inhibidores de la cinasa JAK3. Composición farmacéutica y proceso. Reivindicación 1: Un compuesto caracterizado por la fórmula 1 o una sal del mismo, donde R1 representa hidrógeno, alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R7-alquilo C1-4, halógeno, -CN, -CONR4R4, -COR5, -CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R2 representa hidrógeno, alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R7-alquilo C1-4 o Cy2, donde Cy2 puede estar opcionalmente sustituido por uno o más R8; R3 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4, -CONR9R9, -COR10, -CO2R10, -SO2R10, -SO2NR9R9 o Cy3, donde Cy3 puede estar opcionalmente sustituido por uno o más R12; o bien R2 y R3 pueden estar unidos formando, junto con el átomo de N, un grupo Cy4, donde Cy4 puede estar opcionalmente sustituido por uno o más grupos R12; R4 representa hidrógeno o R5; R5 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, Cy1-alquilo C1-4 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R6 representa hidrógeno o alquilo C1-4; R7 representa -CN, -CONR4R4, -COR5, --CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 o Cy1, donde Cy1 puede estar opcionalmente sustituido por uno o más R8; R8 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, halógeno o hidroxilo; R9 representa hidrógeno o R10; R10 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R11 representa halógeno, -CN, -CONR14R14, -COR15, -CO2R15, -OR14, -OCONR14R14, -SO2R15, -SO2NR14R4, -NR14R14, -NR6COR14, -NR5CONR14R14, -NR6CO2R15, -NR6SO2R15 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R12 representa alquilo C1-4, haloC1-4alquilo, hidroxiC1-4alquilo, R11-alquilo C1-4; o bien R12 representa cualquiera de los significados descritos para R11; R13 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo, halógeno, -CN, -CONR16R16, -COR17, -CO2R17, -OR16, -OCONR16R16, -SO2R17, -SO2NR16R16, -NR16R16, -NR6COR16, -NR6CONR16R16, -NR6CO2R17 o -NR6SO2R17; R14 representa hidrógeno o R15; R15 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo, cianoC1-4alquilo,Cy5-alquilo C1-4 o Cy5, donde Cy5 puede estar opcionalmente sustituido por uno o más R13; R16 representa H o R17; R17 representa alquilo C1-4, haloC1-4alquilo, alcoxi C1-4-alquilo C1-4, hidroxiC1-4alquilo o cianoC1-4alquilo, Cy1 representa un anillo carbocíclico monocíclico de 3 a 7 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 3 heteroátomos seleccionados de N, S y O, donde dicho anillo puede estar unido al resto de la molécula a través de cualquier átomo de C o N disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy2 representa un anillo carbocíclico monocíclico de 3 a 7 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 3 heteroátomos seleccionados de N, S y O donde dicho anillo esta unido al resto de la molécula a través de cualquier átomo de C disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy3 representa un anillo carbocíclico monocíclico de 3 a 7 miembros o bicíclico de 8 a 12 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 4 heteroátomos seleccionados de N, S y O donde dicho anillo está unido al resto de la molécula a través de cualquier átomo de C disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; Cy4 representa un anillo heterocíclico monocíclico de 3 a 7 miembros saturado o parcialmente insaturado, que puede estar opcionalmente fusionado a un anillo de 5 o 6 miembros carbocíclico o heterocíclico saturado, parcialmente insaturado o aromático, donde Cy4 puede contener en total de 1 a 4 heteroátomos seleccionados de N, O y S, y donde uno o más átomos de C o S de Cy4 pueden estar opcionalmente oxidados formando grupos CO, SO o SO2; y Cy5 representa un anillo carbocíclico monocíclico de 3 a 7 miembros o bicíclico de 8 a 12 miembros que puede ser saturado, parcialmente insaturado o aromático, y que puede contener opcionalmente de 1 a 4 heteroátomos seleccionados de N, S y O, donde dicho anillo puede estar unido al resto de la molécula a través de cualquier átomo de C o N disponible, y donde uno o más átomos de C o S del anillo pueden estar opcionalmente oxidados formando grupos CO, SO o SO2.These compounds are useful as inhibitors of JAK3 kinase. Pharmaceutical composition and process. Claim 1: A compound characterized by the formula 1 or a salt thereof, wherein R1 represents hydrogen, C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R7-C1-4 alkyl, halogen, -CN, -CONR4R4, - COR5, -CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 or Cy1, where Cy1 can be optionally substituted by one or more R8; R2 represents hydrogen, C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R7-C1-4 alkyl or Cy2, where Cy2 may be optionally substituted by one or more R8; R3 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl, -CONR9R9, -COR10, -CO2R10, -SO2R10, -SO2NR9R9 or Cy3, where Cy3 may be optionally substituted by one or more R12 ; or R2 and R3 can be linked together, together with the N atom, a Cy4 group, where Cy4 can be optionally substituted by one or more R12 groups; R4 represents hydrogen or R5; R5 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy1-C1-4alkyl or Cy1, where Cy1 may be optionally substituted by one or more R8; R6 represents hydrogen or C1-4 alkyl; R7 represents -CN, -CONR4R4, -COR5, --CO2R5, -OR4, -SO2R5, -SO2NR4R4, -NR4R4, -NR6COR4, -NR6CONR4R4, -NR6CO2R5, -NR6SO2R5 or Cy1, where Cy1 may be optionally substituted plus R8; R8 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, halogen or hydroxyl; R9 represents hydrogen or R10; R10 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl or Cy5, where Cy5 may be optionally substituted by one or more R13; R11 represents halogen, -CN, -CONR14R14, -COR15, -CO2R15, -OR14, -OCONR14R14, -SO2R15, -SO2NR14R4, -NR14R14, -NR6COR14, -NR5CONR14R14, -NR6CO2R15, -NR6SO2, can optionally be replaced by one or more R13; R12 represents C1-4 alkyl, haloC1-4alkyl, hydroxyC1-4alkyl, R11-C1-4 alkyl; or R12 represents any of the meanings described for R11; R13 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, halogen, -CN, -CONR16R16, -COR17, -CO2R17, -OR16, -OCONR16R16, - SO2R17, -SO2NR16R16, -NR16R16, -NR6COR16, -NR6CONR16R16, -NR6CO2R17 or -NR6SO2R17; R14 represents hydrogen or R15; R15 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy5-C1-4 alkyl or Cy5, where Cy5 may be optionally substituted by one or more R13; R16 represents H or R17; R17 represents C1-4 alkyl, haloC1-4alkyl, C1-4 alkoxy-C1-4 alkyl, hydroxyC1-4alkyl or cyanoC1-4alkyl, Cy1 represents a 3- to 7-membered monocyclic carbocyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 3 heteroatoms selected from N, S and O, where said ring can be attached to the rest of the molecule through any available C or N atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy2 represents a 3- to 7-membered monocyclic carbocyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 3 heteroatoms selected from N, S and O where said ring is attached to the rest of the molecule through of any available C atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy3 represents a 3- to 7-membered monocyclic carbocyclic or 8 to 12-membered bicyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 4 heteroatoms selected from N, S and O where said ring is attached to the rest of the molecule through any available C atom, and where one or more C or S atoms of the ring may optionally be oxidized forming CO, SO or SO2 groups; Cy4 represents a 3 to 7-membered saturated or partially unsaturated monocyclic heterocyclic ring, which may be optionally fused to a saturated, partially unsaturated or aromatic carbocyclic or heterocyclic 5 or 6-membered ring, where Cy4 may contain a total of 1 to 4 heteroatoms selected from N, O and S, and where one or more C or S atoms of Cy4 may optionally be oxidized forming CO, SO or SO2 groups; and Cy5 represents a 3- to 7-membered monocyclic carbocyclic or 8 to 12-membered bicyclic ring that can be saturated, partially unsaturated or aromatic, and which may optionally contain 1 to 4 heteroatoms selected from N, S and O, wherein said ring it can be attached to the rest of the molecule through any available C or N atom, and where one or more C or S atoms of the ring can be optionally oxidized forming CO, SO or SO2 groups.

ARP090105067A 2008-12-24 2009-12-22 DERIVATIVES OF PIRAZOLO (1,5-A) PIRIDINA AR074870A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08382087 2008-12-24
US15571309P 2009-02-26 2009-02-26

Publications (1)

Publication Number Publication Date
AR074870A1 true AR074870A1 (en) 2011-02-16

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AR (1) AR074870A1 (en)
TW (1) TW201035095A (en)
WO (1) WO2010072823A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33213A (en) * 2010-02-18 2011-09-30 Almirall Sa PIRAZOL DERIVATIVES AS JAK INHIBITORS
WO2011136264A1 (en) * 2010-04-28 2011-11-03 第一三共株式会社 [5,6] heterocyclic compound
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
WO2015089218A1 (en) * 2013-12-10 2015-06-18 David Wustrow Monocyclic pyrimidine/pyridine compounds as inhibitors of p97 complex
SG11201605699QA (en) 2014-01-20 2016-08-30 Cleave Biosciences Inc FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX
CA3026149A1 (en) 2016-06-02 2017-12-07 Cadent Therapeutics, Inc. Potassium channel modulators
BR112019014814B1 (en) 2017-01-23 2024-03-12 Novartis Ag COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USES IN THE TREATMENT OF DISEASES ASSOCIATED WITH DYSFUNCTION OF POTASSIUM ION CHANNELS
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7279473B2 (en) * 2001-12-17 2007-10-09 Smithkline Beecham Corporation Pyrazolopyridazine derivatives
MXPA06011327A (en) * 2004-03-30 2006-12-15 Vertex Pharma Azaindoles useful as inhibitors of jak and other protein kinases.
AU2007258567B2 (en) * 2006-06-06 2012-04-19 Medicinova, Inc. Substituted pyrazolo (1,5-alpha) pyridine compounds and their methods of use

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TW201035095A (en) 2010-10-01

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