AR104720A1 - Moduladores de ccr2 - Google Patents

Moduladores de ccr2

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Publication number
AR104720A1
AR104720A1 ARP160101482A ARP160101482A AR104720A1 AR 104720 A1 AR104720 A1 AR 104720A1 AR P160101482 A ARP160101482 A AR P160101482A AR P160101482 A ARP160101482 A AR P160101482A AR 104720 A1 AR104720 A1 AR 104720A1
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Argentina
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alkyl
group
cycloalkyl
heteroaryl
aryl
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ARP160101482A
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English (en)
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Zhang Penglie
Zeng Yibin
Tanaka Hiroko
P Powers Jay
P Mmahon Jeffrey
Reddy Mali Venkat
M Lui Rebecca
Kalisiak Jaroslaw
Fan Junfa
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Chemocentryx Inc
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Publication of AR104720A1 publication Critical patent/AR104720A1/es

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    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrane Compounds (AREA)
  • Amplifiers (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Compuestos que son moduladores del receptor de CCR2 y son útiles en composiciones farmacéuticas, métodos para el tratamiento de enfermedades y trastornos que involucran la activación patológica de receptores de CCR2. Reivindicación 1: Un compuesto caracterizado porque que tiene la fórmula (1); o una sal aceptable farmacéuticamente, hidrato, estereoisómero o rotámero del mismo; donde A es C(R⁵)(R⁶) o N(R⁵) los subíndices m y n son en forma independiente entre sí enteros de 0 a 2, y m + n es £ 3; R¹ se selecciona entre el grupo que consiste en arilo, aril-C₁₋₄ alquilo, heteroarilo y heteroaril-C₁₋₄ alquilo, donde la porción heteroarilo tiene entre 1 - 3 heteroátomos como miembros del anillo que se seleccionan entre N, O y S; y donde dichos grupos o porciones arilo y heteroarilo están sustituidos opcionalmente con entre 1 y 5 sustituyentes Rˣ; R² se selecciona entre el grupo que consiste en H, C₁₋₈ alquilo, C₃₋₈ cicloalquilo, C₃₋₈ cicloalquil-C₁₋₄ alquilo, arilo, aril-C₁₋₄ alquilo, heteroarilo y heteroaril-C₁₋₄ alquilo, donde la porción heteroarilo tiene entre 1 - 3 heteroátomos como miembros del anillo que se seleccionan entre N, O y S; y donde dichos grupos o porciones arilo y heteroarilo están sustituidos opcionalmente con entre 1 y 4 sustituyentes Rˣ; u opcionalmente, R¹ y R² se combinan con el átomo de nitrógeno al cual cada uno está unido para formar un anillo monocíclico de 6 a 11 miembros o anillo fusionado bicíclico - heterocíclico o heteroarilo, donde el grupo -NR¹R² está además opcionalmente sustituido con entre 1 y 4 sustituyentes Rˣ; R³ se selecciona entre el grupo que consiste en H, C₁₋₈ alquilo, C₃₋₈ cicloalquilo y C₃₋₈ cicloalquil-C₁₋₄ alquilo, cada uno de los cuales está opcionalmente sustituido con entre 1 - 3 sustituyentes Rʸ; R⁴ se selecciona entre el grupo que consiste en H, C₁₋₈ alquilo opcionalmente sustituido con 1 a 2 Rʸ, y -CO₂H; R⁵ se selecciona entre el grupo que consiste en C₁₋₈ alquilo, C₁₋₈ alcoxi, C₃₋₈ cicloalquilo, C₃₋₈ cicloalquiloxi, C₃₋₈ cicloalquil-C₁₋₄ alquilo, C₁₋₈ alquilamino, di-C₁₋₈ alquilamino, arilo, ariloxi, arilamino, aril-C₁₋₄ alquilo, heteroarilo, heteroariloxi, heteroarilamino y heteroaril-C₁₋₄ alquilo, cada uno de los cuales está opcionalmente sustituido con entre 1 y 5 sustituyentes Rᶻ; R⁶ se selecciona entre el grupo que consiste en H, F, OH, C₁₋₈ alquilo y C₁₋₈ alcoxi, donde los grupos C₁₋₈ alquilo y C₁₋₈ alcoxi están sustituidos opcionalmente con entre 1 y 3 sustituyentes Rᶻ; u opcionalmente, R⁵ y R⁶ se unen para formar un anillo cicloalquilo espirocíclico de 5 ó 6 miembros que es opcionalmente insaturado, y tiene un grupo arilo fusionado que está opcionalmente sustituido con entre 1 y 4 sustituyentes Rᶻ; cada Rˣ se selecciona en forma independiente entre el grupo que consiste en halógeno, -CN, -Rᶜ, -CO₂Rᵃ, -CONRᵃRᵇ, -C(O)Rᵃ, -OC(O)NRᵃRᵇ, -NRᵇC(O)Rᵃ, -NRᵇC(O)₂Rᶜ, -NRᵃ-C(O)NRᵃRᵇ, NRᵃC(O)NRᵃRᵇ, -NRᵃRᵇ, -ORᵃ, -O-X¹-ORᵃ, -O-X¹-NRᵃRᵇ, -O-X¹-CO₂Rᵃ, -O-X¹-CONRᵃRᵇ, -X¹-ORᵃ, -X¹-NRᵃRᵇ, -X¹-CO₂Rᵃ, -X¹-CONRᵃRᵇ, -SF₅, -S(O)₂NRᵃRᵇ, y arilo o heteroarilo de 5 ó 6 miembros, donde cada X¹ es un C₁₋₄ alquileno; cada Rᵃ y Rᵇ se selecciona en forma independiente entre hidrógeno, C₁₋₈ alquilo, y C₁₋₈ haloalquilo, o cuando está unido al mismo átomo de nitrógeno se puede combinar con el átomo de nitrógeno para formar un anillo de 5 ó 6 miembros con entre 0 a 2 heteroátomos adicionales como miembros del anillo que se seleccionan entre N, O ó S, y opcionalmente sustituido con oxo; cada Rᶜ se selecciona en forma independiente entre el grupo que consiste en C₁₋₈ alquilo, C₁₋₈ haloalquilo y C₃₋₆ cicloalquilo; y opcionalmente cuando dos sustituyentes Rˣ están sobre átomos adyacentes, se combinan para formar un anillo carbocíclico fusionado de 5 ó 6 miembros, y donde los grupos arilo o heteroarilo están sustituidos opcionalmente con 1 - 3 miembros que se seleccionan entre halógeno, hidroxilo, C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, y C₁₋₄ haloalcoxi; cada Rʸ se selecciona en forma independiente entre el grupo que consiste en halógeno, -CN, -Rᶠ, -CO₂Rᵈ, -CONRᵈRᵉ, -C(O)Rᵈ, -OC(O)NRᵈRᵉ, -NRᵉC(O)Rᵈ, -NRᵉC(O)₂Rᶠ, -NRᵈC(O)NRᵈRᵉ, -NRᵈC(O)NRᵈRᵉ, -NRᵈRᵉ, -ORᵈ, y -S(O)₂NRᵈRᵉ; donde cada Rᵈ y Rᵉ se selecciona en forma independiente entre hidrógeno, C₁₋₈ alquilo, y C₁₋₈ haloalquilo, o cuando está unido al mismo átomo de nitrógeno se puede combinar con el átomo de nitrógeno para formar un anillo de 5 ó 6 miembros con entre 0 a 2 heteroátomos adicionales como miembros del anillo que se seleccionan entre N, O ó S; cada Rᶠ se selecciona en forma independiente entre el grupo que consiste en C₁₋₈ alquilo, C₁₋₈ haloalquilo y C₃₋₆ cicloalquilo; cada Rᶻ se selecciona en forma independiente entre el grupo que consiste en halógeno, -CN, -Rⁱ, -CO₂Rᵍ, -CONRᵍRʰ, -C(O)Rᵍ, -OC(O)NRᵍRʰ, NRʰC(O)Rᵍ, -NRʰC(O)₂Rⁱ, -NRᵍC(O)NRᵍRʰ, -NRᵍRʰ-, -ORᵍ, -S(O)₂NRᵍRʰ, -X¹-Rʲ, -X¹-NRᵍRʰ, -X¹-CONRᵍRʰ, -X¹-NRʰC(O)Rᵍ, -NHRʲ, -NHCH₂Rʲ, y tetrazol; donde cada Rᵍ y Rʰ se selecciona en forma independiente entre hidrógeno, C₁₋₈ alquilo, C₃₋₆ cicloalquilo y C₁₋₈ haloalquilo, o cuando está unido al mismo átomo de nitrógeno se puede combinar con el átomo de nitrógeno para formar un anillo de 5 ó 6 miembros con entre 0 a 2 heteroátomos adicionales como miembros del anillo que se seleccionan entre N, O ó S y está opcionalmente sustituido con uno o dos oxo; cada Rⁱ se selecciona en forma independiente entre el grupo que consiste en C₁₋₈ alquilo, C₁₋₈ haloalquilo y C₃₋₆ cicloalquilo; y cada Rʲ se selecciona entre el grupo que consiste en C₃₋₆ cicloalquilo, pirrolinilo, piperidinilo, morfolinilo, tetrahidrofuranilo, y tetrahidropiranilo.
ARP160101482A 2015-05-21 2016-05-20 Moduladores de ccr2 AR104720A1 (es)

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TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
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