PE20181020A1 - MUCLEAR RECEIVER MODULATORS - Google Patents

MUCLEAR RECEIVER MODULATORS

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Publication number
PE20181020A1
PE20181020A1 PE2017002535A PE2017002535A PE20181020A1 PE 20181020 A1 PE20181020 A1 PE 20181020A1 PE 2017002535 A PE2017002535 A PE 2017002535A PE 2017002535 A PE2017002535 A PE 2017002535A PE 20181020 A1 PE20181020 A1 PE 20181020A1
Authority
PE
Peru
Prior art keywords
cra
muclear
nra
present
halo
Prior art date
Application number
PE2017002535A
Other languages
Spanish (es)
Inventor
Maria A Argiriadi
Eric C Breinlinger
Kevin P Cusack
Adrian D Hobson
Dominique Potin
Martine Barth
Jerôme Amaudrut
Olivia Poupardin
Laurent Mounier
Michael E Kort
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 PE20181020A1 publication Critical patent/PE20181020A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/10Heterocyclic 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
    • 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
    • C07D403/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presenten invencion refiere un compuesto de formula (I) en donde W es C o CRa; A y E son independientemente C o N con la condicion de que no sean ambos N; V es CR3 o N; X es CRa, NRa, N u O; Y es C, CRa, NRa,N, O o S; Z es CR3 o N; Cy es un anillo aromatico de 6 miembros, heteroaromatico o parcialmente sustituido con R1 o R2; L1 es -CH(Rb)-, -C(O)-, entre otros; L2 es -C(O)-, -O-, entre otros; R1 y R2 son independientemente halo, cicloalquilo (C3-C6), entre otros; R3 es H, CF3, CN, halo, entre otros; R4 es H, -OH, entre otros; Ra es H, -C(O)CH3, alquilo (C1-C6), entre otros: Rb es H,F,OH, entre otros. Es compuesto preferido: acido 1-(2,4-dicloro-3-((1,4-dimetil-6-(trifluorometil)-1H-indol-2-il)metil)benzoil)piperidin-4-carboxilico; entre otros. La presente invencion es util para el tratamiento de enfermedades inflamatorias y autoinmunes, como es el caso de artritis reumatoide, colitis ulcerosa, entre otras referidas en la invencionThe present invention relates to a compound of formula (I) wherein W is C or CRa; A and E are independently C or N provided 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; Cy is a 6-membered aromatic ring, heteroaromatic or partially substituted with R1 or R2; L1 is -CH (Rb) -, -C (O) -, among others; L2 is -C (O) -, -O-, among others; R1 and R2 are independently halo, (C3-C6) cycloalkyl, among others; R3 is H, CF3, CN, halo, among others; R4 is H, -OH, among others; Ra is H, -C (O) CH3, (C1-C6) alkyl, among others: Rb is H, F, OH, among others. The preferred compound is: 1- (2,4-dichloro-3 - ((1,4-dimethyl-6- (trifluoromethyl) -1H-indol-2-yl) methyl) benzoyl) piperidine-4-carboxylic acid; among others. The present invention is useful for the treatment of inflammatory and autoimmune diseases, such as rheumatoid arthritis, ulcerative colitis, among others referred to in the invention.

PE2017002535A 2015-06-09 2016-06-08 MUCLEAR RECEIVER MODULATORS PE20181020A1 (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)

Publication Number Publication Date
PE20181020A1 true PE20181020A1 (en) 2018-06-27

Family

ID=54293273

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002535A PE20181020A1 (en) 2015-06-09 2016-06-08 MUCLEAR RECEIVER MODULATORS

Country Status (3)

Country Link
AR (1) AR104934A1 (en)
PE (1) PE20181020A1 (en)
WO (1) WO2016198908A1 (en)

Families Citing this family (6)

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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
US11834441B2 (en) 2019-12-06 2023-12-05 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
BR112022020131A2 (en) 2020-04-06 2022-11-29 Basf Se COMPOUND OF THE FORMULA, MIXTURE OF PESTICIDES, USE OF COMPOUNDS OF THE FORMULA, METHODS FOR COMBAT OR CONTROL OF INVERTEBRATE PEST AND PROTECTION OF GROWING PLANTS AND SEEDS
EP4347031A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
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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WO2003060078A2 (en) 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Heterocyclic modulators of nuclear receptors
BR0317525A (en) 2002-12-20 2005-11-16 Pharmacia Corp Acyclic pyrazole compounds, therapeutic and pharmaceutical composition, kit, as well as their uses
US7312215B2 (en) 2003-07-29 2007-12-25 Bristol-Myers Squibb Company Benzimidazole C-2 heterocycles as kinase inhibitors
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WO2016198908A1 (en) 2016-12-15

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