AR104934A1 - NUCLEAR RECEIVERS MODULATORS - Google Patents

NUCLEAR RECEIVERS MODULATORS

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Publication number
AR104934A1
AR104934A1 ARP160101700A ARP160101700A AR104934A1 AR 104934 A1 AR104934 A1 AR 104934A1 AR P160101700 A ARP160101700 A AR P160101700A AR P160101700 A ARP160101700 A AR P160101700A AR 104934 A1 AR104934 A1 AR 104934A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
independently
cycloalkyl
cra
Prior art date
Application number
ARP160101700A
Other languages
Spanish (es)
Inventor
E Kort Michael
Mounier Laurent
Poupardin Olivia
Amaudrut Jerome
Barth Martine
Potin Dominique
C Hobson Adrian
P Cusack Kevin
C Breinlinger Eric
A Argiriadi Maria
Original Assignee
Abbvie 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 Abbvie Inc filed Critical Abbvie Inc
Publication of AR104934A1 publication Critical patent/AR104934A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente solicitud se refiere a compuestos y sales farmacéuticamente aceptables de los mismos útiles para tratar trastornos inmunológicos. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), una sal farmacéuticamente aceptable, o un estereoisómero del mismo, donde W es C o CRᵃ, L¹ está conectado a W o Y; y A y E son en forma independiente C o N con la condición de que no son ambos N; V es CR³ o N; X es CRᵃ, NRᵃ, N, ó O; Y es C, CRᵃ, NRᵃ, N, O ó S; Z es CR³ o N; o W es N o NRᵃ, L¹ está conectado a W o Y; y A y E son en forma independiente C o N con la condición de que no son ambos N; V es CR³ o N; X es CRᵃ, NRᵃ, o N; Y es C, CRᵃ, o N; Z es CR³ o N; o Cy es un anillo aromático, heteroaromático o parcialmente saturado de seis miembros sustituido con R¹ y R²; L¹ es -CH(Rᵇ)-, -C(Rᵇ)(Rᵈ)-, -C(O)- o -N(Rᶜ)-; L² es -C(O)-, -O-, -C(Rᵇ)(Rᵈ)-, -S-, -S(O)-, -S(O)₂-; R¹ y R² son en forma independiente halo, -O-C₁₋₃ alquilo, -O-C₃₋₆ cicloalquilo, C₃₋₆ cicloalquilo opcionalmente sustituido, o -C₁₋₃ alquilo; cada R³ es en forma independiente H, CF₃, CN, halo, -C(=O)C₁₋₃ alquilo, -C(O)N(Rᵉ)₂, -NRᵉCORᵉ, -OCHF₂, OCF₃, -O-C₁₋₃ alquilo, -O-C₃₋₆ cicloalquilo, -S-C₁₋₃ alquilo, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₆ cicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heterociclo opcionalmente sustituido; R⁴ es H, -OH, C₁₋₆ alquilo opcionalmente sustituido, -NR⁵R⁶, C₃₋₆ cicloalquilo opcionalmente sustituido o -(CH₂)ₘ-heterociclo opcionalmente sustituido; donde R⁵ es H o -C₁₋₃ alquilo, y R⁶ es C₁₋₄ alquilo opcionalmente sustituido, C₃₋₆ cicloalquilo opcionalmente sustituido o -(CH₂)ₘ-heterociclo opcionalmente sustituido; o R⁵ y R⁶, junto con el átomo de nitrógeno al que están unidos, forman un heterociclo opcionalmente sustituido; cada Rᵃ es en forma independiente H, -C(O)CH₃, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₆ cicloalquilo opcionalmente sustituido o -S(O)₂-fenilo; cada Rᵇ es en forma independiente H, F, OH, -O-C₁₋₃ alquilo, o C₁₋₃ alquilo; Rᶜ es en forma independiente H o -C₁₋₃ alquilo; cada Rᵈ es en forma independiente H, F, o C₁₋₃ alquilo; o Rᵈ y Rᵇ forman un C₃₋₅ espirociclo; Rᵉ es en forma independiente H o -C₁₋₃ alquilo; y m es en forma independiente 0 ó 1; con la condición de que no más que dos de A, E, W, X e Y son N.The present application relates to pharmaceutically acceptable compounds and salts thereof useful for treating immunological disorders. Claim 1: A compound characterized in that it is of formula (1), a pharmaceutically acceptable salt, or a stereoisomer thereof, wherein W is C or CRᵃ, L¹ is connected to W or Y; and A and E are independently C or N with the proviso that they are not both N; V is CR³ or N; X is CRᵃ, NRᵃ, N, or O; Y is C, CRᵃ, NRᵃ, N, O or S; Z is CR³ or N; or W is N or NRᵃ, L¹ is connected to W or Y; and A and E are independently C or N with the proviso that they are not both N; V is CR³ or N; X is CRᵃ, NRᵃ, or N; Y is C, CRᵃ, or N; Z is CR³ or N; or Cy is a six-membered aromatic, heteroaromatic or partially saturated ring substituted with R¹ and R²; L¹ is -CH (Rᵇ) -, -C (Rᵇ) (Rᵈ) -, -C (O) - or -N (Rᶜ) -; L² is -C (O) -, -O-, -C (Rᵇ) (Rᵈ) -, -S-, -S (O) -, -S (O) ₂-; R¹ and R² are independently halo, -O-C₁₋₃ alkyl, -O-C₃₋₆ cycloalkyl, optionally substituted C₃₋₆ cycloalkyl, or -C₁₋₃ alkyl; each R³ is independently H, CF₃, CN, halo, -C (= O) C₁₋₃ alkyl, -C (O) N (Rᵉ) ₂, -NRᵉCORᵉ, -OCHF₂, OCF₃, -O-C₁₋₃ alkyl, -O-C₃₋₆ cycloalkyl, -S-C₁₋₃ alkyl, C₁₋₆ optionally substituted alkyl, C₃₋₆ optionally substituted cycloalkyl, optionally substituted heteroaryl or optionally substituted heterocycle; R⁴ is H, -OH, C₁₋₆ optionally substituted alkyl, -NR⁵R⁶, C₃₋₆ optionally substituted cycloalkyl or - (CH₂) ₘ-optionally substituted heterocycle; where R⁵ is H or -C₁₋₃ alkyl, and R⁶ is C₁₋₄ optionally substituted alkyl, C₃₋₆ cycloalkyl optionally substituted or - (CH₂) ₘ-heterocycle optionally substituted; or R⁵ and R⁶, together with the nitrogen atom to which they are attached, form an optionally substituted heterocycle; each Rᵃ is independently H, -C (O) CH₃, C₁₋₆ optionally substituted alkyl, C₃₋₆ optionally substituted cycloalkyl or -S (O) ₂-phenyl; each Rᵇ is independently H, F, OH, -O-C₁₋₃ alkyl, or C₁₋₃ alkyl; Rᶜ is independently H or -C₁₋₃ alkyl; each Rᵈ is independently H, F, or C₁₋₃ alkyl; or Rᵈ and Rᵇ form a C₃₋₅ spirocycle; Rᵉ is independently H or -C₁₋₃ alkyl; and m is independently 0 or 1; with the proviso that no more than two of A, E, W, X and Y are N.

ARP160101700A 2015-06-09 2016-06-08 NUCLEAR RECEIVERS MODULATORS AR104934A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IB2015/001693 WO2016198908A1 (en) 2015-06-09 2015-06-09 Ror nuclear receptor modulators

Publications (1)

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AR104934A1 true AR104934A1 (en) 2017-08-23

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PE (1) PE20181020A1 (en)
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Families Citing this family (6)

* Cited by examiner, † Cited by third party
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CN108689942B (en) * 2017-04-11 2023-06-09 广东东阳光药业有限公司 Nitrogen-containing bicyclic compound, and preparation method and application thereof
US11427596B2 (en) * 2019-07-19 2022-08-30 Indian Institute of Technology Indore Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications
BR112022010924A2 (en) 2019-12-06 2022-09-06 Vertex Pharma SUBSTITUTED TETRAHYDROFURANS AS SODIUM CHANNEL MODULATION
EP4132927A1 (en) 2020-04-06 2023-02-15 Basf Se Imidazo-pyrimidone compounds as pesticides
PE20241335A1 (en) 2021-06-04 2024-07-03 Vertex Pharma N-(HYDROXYALKYL (HETERO)ARYL) TETRAHYDROFURAN CARBOXAMIDES AS SODIUM CHANNEL MODULATORS
CN116283753A (en) * 2023-03-20 2023-06-23 武汉朗克环境科技有限公司 Trifluoromethyl pyridine amide derivative and preparation method and application thereof

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PE20181020A1 (en) 2018-06-27

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