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AR071281A1 - Derivados de naftiridina moduladores de receptores trl, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades autoinmunes, dermatologicas y respiratorias. - Google Patents

Derivados de naftiridina moduladores de receptores trl, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades autoinmunes, dermatologicas y respiratorias.

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Publication number
AR071281A1
AR071281A1 ARP090100743A ARP090100743A AR071281A1 AR 071281 A1 AR071281 A1 AR 071281A1 AR P090100743 A ARP090100743 A AR P090100743A AR P090100743 A ARP090100743 A AR P090100743A AR 071281 A1 AR071281 A1 AR 071281A1
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AR
Argentina
Prior art keywords
heterocycloalkyl
alkyl
cycloalkyl
independently selected
heteroalkyl
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Application number
ARP090100743A
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English (en)
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Irm Llc
Novartis Ag
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40677604&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR071281(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Irm Llc, Novartis Ag filed Critical Irm Llc
Publication of AR071281A1 publication Critical patent/AR071281A1/es

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    • 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
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P17/04—Antipruritics
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    • A61P17/06—Antipsoriatics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P37/02—Immunomodulators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
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    • 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
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • C07D491/04—Ortho-condensed systems
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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
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  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de la formula (1), o una sal aceptable para uso farmacéutico o un solvato aceptable para uso farmacéutico de dicho compuesto donde: X3 es N; X4 es N o CR3, X5 es -CR4=CR5-, R3 es H; R4 y R5 seleccionan, de manera independiente, de H, halogeno,-C(O)OR7, -C(O)R7, -C(O)N(R11R12), -N(R11R12), -N(R9)2, -NHN(R9)2, -SR7, -(CH2)nOR7, -(CH2)nR7, -LR8, -LR10, -OLR8, -OLR10, alquilo C1-6, heteroalquilo C1-6, haloalquilo C1-6, alqueno C2-8, alquino C2-8, alcoxi C1-6, haloalcoxi C1-6, arilo, heteroarilo cicloalquilo C3-8 y heterocicloalquilo C3-8, donde los grupos alquilo C1-6, heteroalquilo C1-6, haloalquilo C1-6, alqueno C2-8, alquino C2-8, alcoxi C1-6, haloalcoxi C1-6 arilo, heteroarilo, cicloalquilo C3-C8 y heterocicloalquilo C3-8 de R4 y R5, de manera independiente, están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados de modo independiente de halogeno, -CN, -NO2, -R7, -OR8, -C(O)R8, -OC(O)R8, -C(O)OR8, -N(R9)2, -P(O)(OR8)2, -OP(O)(OR8)2, -P(O)(OR10)2, -OP(O)(OR10)2, -C(O)N(R9)2, -S(O)2R8, -S(O)R8, -S(O)2N(R9)2 y -NR9S(O)2R8; o R3 y R4, o R4 y R5, cuando se presentan en átomos de anillo adyacentes, pueden estar opcionalmente ligados para formar un anillo de 5-6 miembros, donde el anillo de 5-6 miembros está opcionalmente sustituido con R7; cada L se selecciona de manera independiente de un enlace, -(O(CH2)m)t-, alquilo C1-6, alquenileno C2-6 y alquinileno C2-6, donde los grupos alquilo C1-6, alquenileno C2-6 y alquinileno C2-6 de L están, cada uno, opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados independientemente de halogeno, -R8, -OR8, -N(R9)2, -P(O)(OR8)2, -OP(O)(OR8)2, -P(O)(OR10)2, y -OP(O)(OR10)2; R7 se selecciona de H, alquilo C1-6, arilo, heteroarilo, cicloalquilo C3-8, heteroalquilo C1-6, haloalquilo C1-6, alqueno C2-8, alquino C2-8, alcoxi C1-6, haloalcoxi C1-6 y heterocicloalquilo C3-8, donde los grupos alquilo C1-6, arilo, heteroarilo, cicloalquilo C3-8, heteroalquilo C1-6, haloalquilo C1-6, alqueno C2-8, alquino C2-8, alcoxi C1-6, haloalcoxi C1-6 y heterocicloalquilo C3-8 de R7, de manera independiente, están opcionalmente sustituidos con 1 a 3 grupos R13, y cada R13 se selecciona de modo independiente de halogeno, -CN, -LR9, -LOR9, -OLR9, -LR10, -LOR10, -OLR10, -LR8, -LOR8, -OLR8, -LSR8, -LSR10, -LC(O)R8, -OLC(O)R8, -LC(O)OR8, -LC(O)R10, -LOC(O)OR8, -LC(O)NR9R11, -LC(O)NR9R8, -LN(R9)2, -LNR9R8, -LNR9R10, -LC(O)N(R9)2, -LS(O)2R8, -LS(O)R8, -LC(O)NR8OH, -LNR9C(O)R8, -LNR9C(O)OR8, -LS(O)2N(R9)2, -OLS(O)2N(R9)2, -LNR9S(O)2R8, -LC(O)NR9LN(R9)2, -LP(O)(OR8)2, -LOP(O)(OR8)2, -LP(O)(OR10)2 y -OLP(O)(OR10)2; cada R8 se selecciona de manera independiente de H, -CH(R10)2, alquilo C1-8, alqueno C2-8, alquino C2-8, haloalquilo C1-6, alcoxi C1-6, heteroalquilo C1-6, cicloalquilo C3-8, heterocicloalquilo C2-8, hidroxialquilo C1-6, y haloalcoxi C1-6, donde los grupos alquilo C1-8, alqueno C2-8, alquino C2-8, heteroalquilo C1-6, haloalquilo C1-6, alcoxi C1-6, cicloalquilo C3-8, heterocicloalquilo C2-8, hidroxialquilo C1-6 y haloalcoxi C1-6 de R8 están, cada uno, opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados independientemente de -CN, R11, -OR11, SR1, -C(O)R11, -OC(O)R11, -C(O)N(R9)2, -C(O)OR11, NR9C(O)R11, -NR9R10, -NR11R12, -N(R9)2, -OR9, -OR10, -C(O)NR11R12, -C(O)NR11OH, -S(O)2R11, -S(O)R11, -S(O)2NR11R12, -NR11S(O)2R11, -P(O)(OR11)2, y -OP(O)(OR11)2; cada R9 se selecciona de manera independiente de H, -C(O)R8, -C(O)OR8, -C(O)R10, -C(O)OR10, -S(O)2R10, alquilo C1-6, heteroalquilo C1-6 y cicloalquilo C3-6; o cada R9 es, de modo independiente, un alquilo C1-6 que junto con N, se une para formar un heterocicloalquilo C3-8, donde el anillo heterocicloalquilo C3-8 contiene opcionalmente un heteroátomo adicional seleccionado de N, O y S, y donde los grupos alquilo C1-6, heteroalquilo C1-6, cicloalquilo C3-6, o heterocicloalquilo C3-8 de R9 están, cada uno, opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente de -CN, R11, -OR11, -SR11, -C(O)R11, -OC(O)R11, -C(O)OR11, -NR11R12, -C(O)NR11R12, -C(O)NR11OH, -S(O)2R11, -S(O)R11, -S(O)2NR11R12, -NR11S(O)2R11, -P(O)(OR11)2, y -OP(O)(OR11)2; cada R10 se selecciona de manera independiente de arilo, cicloalquilo C3-8, heterocicloalquilo C3-8 y heteroarilo, donde los grupos arilo, cicloalquilo C3-8, heterocicloalquilo C3-8 y heteroarilo están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados de halogeno, -R8, -OR8, -LR9, -LOR9, -N(R9)2, -NR9C(O)R8, -NR9CO2R8, -CO2R8, -C(O)R8 y -C(O)N(R9)2; R11 y R12 se seleccionan de manera independiente de H, alquilo C1-6, heteroalquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo C3-8 y heterocicloalquilo C3-8, donde lo grupos alquilo C1-6, heteroalquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo C3-8 y heterocicloalquilo C3-8 de R11 y R12, de modo independiente, están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados de manera independiente de halogeno, -CN, -OR8, -C(O)R8, -OC(O)R8, -C(O)OR8, -N(R9)2, -NR8C(O)R8, -NR8C(O)OR8, -C(O)N(R9)2, heterocicloalquilo C3-8, -S(O)2R8, -S(O)2N(R9)2, -NR9S(O)2R8, haloalquilo C1-6 y haloalcoxi C1-6; o R11 y R12 son, de manera independiente, alquilo C1-6, y tomados junto con el átomo de N al cual están unidos forman un anillo heterocicloalquilo C3-8 opcionalmente sustituido que contiene opcionalmente un heteroátomo adicional seleccionado de N, O y S; el anillo A es un arilo o un heteroarilo, donde los grupos arilo y heteroarilo del anillo A están opcionalmente sustituidos con 1 a 3 grupos RA, donde cada RA se selecciona de manera independiente de -R8, -R7, -O7, -OR8, -R10, -OR10, -SR8, -NO2, -CN, -N(R9)2, -NR9C(O)R8, -NR9C(S)R8, -NR9C(O)N(R9)2, -NR9C(S)N(R9)2, -NR9CO2R8, -NR9NR9C(O)R8, -NR9NR9C(O)N(R9)2, -NR9NR9CO2R8, -C(O)C(O)R8, -C(O)CH2C(O)R8, -CO2R8, -(CH2)CO2R8, -C(O)R8, -C(S)R8, -C(O)N(R9)2, -C(S)N(R9)2, -OC(O)N(R9)2, -OC(O)R8, -C(O)N(OR8)R8, -C(NOR8)R8, -S(O)2R8, -S(O)3R8, -SO2N(R9)2, -S(O)R8, -NR9SO2N(R9)2, -NR9SO2R8, -P(O)(OR8)2, -OP(O)(OR8)2, -P(O)(OR10)2, -OP(O)(OR10)2, -N(OR8)R8, -CH=CHCO2R8, -C(=NH)-N(R9)2 y -(CH2)nNHC(O)R8; o dos sustituyentes RA adyacentes en el anillo A forman un anillo de 5-6 miembros que contiene hasta dos heteroátomos como miembros de anillo; y n es, de manera independiente en cada aparicion, 0; 1; 2; 3; 4; 5; 6; 7 u 8; cada m se selecciona de manera independiente de 1; 2; 3; 4; 5 y 6, y t es 1; 2; 3; 4; 5; 6; 7 u 8.
ARP090100743A 2008-03-03 2009-03-03 Derivados de naftiridina moduladores de receptores trl, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades autoinmunes, dermatologicas y respiratorias. AR071281A1 (es)

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US3313908P 2008-03-03 2008-03-03
US14833609P 2009-01-29 2009-01-29

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US (2) US8466167B2 (es)
EP (1) EP2268618B1 (es)
JP (1) JP5380465B2 (es)
KR (1) KR101208778B1 (es)
CN (1) CN102015651B (es)
AR (1) AR071281A1 (es)
AU (1) AU2009222105B2 (es)
BR (1) BRPI0909037B8 (es)
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