AR076550A1 - Inhibidores de la janus tirosina kinasa (jak) - Google Patents

Inhibidores de la janus tirosina kinasa (jak)

Info

Publication number
AR076550A1
AR076550A1 ARP100101558A ARP100101558A AR076550A1 AR 076550 A1 AR076550 A1 AR 076550A1 AR P100101558 A ARP100101558 A AR P100101558A AR P100101558 A ARP100101558 A AR P100101558A AR 076550 A1 AR076550 A1 AR 076550A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
aryl
heteroalkyl
heteroaryl
Prior art date
Application number
ARP100101558A
Other languages
English (en)
Inventor
Jack W Rose
Yonghong Song
Qing Xu
Mukund Mehrotra
Anjali Pandey
Shawn M Bauer
Wolin Huang
Original Assignee
Portola Pharm Inc
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 Portola Pharm Inc filed Critical Portola Pharm Inc
Publication of AR076550A1 publication Critical patent/AR076550A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

Abstract

Compuestos de formula 1 y tautomeros y sales de los mismos farmacéuticamente aceptables que son inhibidores selectivos de JAK. También se refiere a intermediarios que se utilizan para hacer dichos compuestos, a la preparacion de un compuesto con dichas características, a composiciones farmacéuticas que lo contienen, a métodos para inhibir la actividad de la JAK, y a métodos para impedir o tratar varias condiciones mediadas por lo menos en parte por la actividad de la JAK. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) o un tautomero o sales farmacéuticamente aceptables del mismo, donde Y1 es N o CR1c; R1a es (a) cicloalquilo C3-8, opcionalmente sustituido con entre 1 y 3 sustituyentes R1d donde cada R1d se selecciona independientemente entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; o si se encuentran en átomos de carbono adyacentes del cicloalquilo C3-8, se pueden combinar con los átomos a los cuales están unidos para formar un grupo arilo; (b) alquilo C1-8, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquenilo C2-8, alquinilo C2-8, amino, hidroxilo, halogeno, heteroalquilo C1-8, ciano, cicloalquilo C3-8, arilo, haloarilo, alquilarilo C1-8, alcoxiarilo C1-8, heteroarilo, heterociclilo C3-8 y heterociclilcarbonilo C3-8; (c) heterociclilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; (c) arilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en aIquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo, amino y alquilsulfonilo; y (d) heteroarilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; R1b es H o aIquilo C1-8; R1c es H, alquilo C1-8 o halogeno; R2 es H, alquilo C1-8, heteroalquilo C1-8, heterociclil C1-8alcoxi, halogeno o heterociclilo; R3 es H o alquilo C1-8 o cicloalquilo C3-8; R4 se selecciona entre el grupo formado por amino, alquilo C1-8, amino C1-8alquilo, alquenilo C2-8, alquinilo C2-8, heteroalquilo C1-8, cicloalquilo C3-8, arilo, heteroarilo y heterociclilo C3-8; y m es 0, 1, 2 o 3.
ARP100101558A 2009-05-06 2010-05-06 Inhibidores de la janus tirosina kinasa (jak) AR076550A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17607709P 2009-05-06 2009-05-06
US25623909P 2009-10-29 2009-10-29

Publications (1)

Publication Number Publication Date
AR076550A1 true AR076550A1 (es) 2011-06-22

Family

ID=42558558

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101558A AR076550A1 (es) 2009-05-06 2010-05-06 Inhibidores de la janus tirosina kinasa (jak)

Country Status (4)

Country Link
US (2) US8367689B2 (es)
AR (1) AR076550A1 (es)
TW (1) TW201040162A (es)
WO (1) WO2010129802A1 (es)

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Also Published As

Publication number Publication date
US20130137673A1 (en) 2013-05-30
US8853230B2 (en) 2014-10-07
TW201040162A (en) 2010-11-16
US20110005947A1 (en) 2011-01-13
WO2010129802A1 (en) 2010-11-11
US8367689B2 (en) 2013-02-05

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