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AR102427A1 - Derivados de carbazol inhibidores de quinasas - Google Patents

Derivados de carbazol inhibidores de quinasas

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Publication number
AR102427A1
AR102427A1 ARP150103455A ARP150103455A AR102427A1 AR 102427 A1 AR102427 A1 AR 102427A1 AR P150103455 A ARP150103455 A AR P150103455A AR P150103455 A ARP150103455 A AR P150103455A AR 102427 A1 AR102427 A1 AR 102427A1
Authority
AR
Argentina
Prior art keywords
remainder
formula
cyclopropyl
formulas
group
Prior art date
Application number
ARP150103455A
Other languages
English (en)
Inventor
Kumar Maishal Tarun
Kesavan Nair Satheesh
Hunter Watterson Scott
A Tino Joseph
E Macor John
Liu Qingjie
G Batt Douglas
Ahmad Saleem
Original Assignee
Bristol Myers Squibb Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54427879&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR102427(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR102427A1 publication Critical patent/AR102427A1/es

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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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/435—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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/06—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 only aliphatic carbon atoms
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D471/10—Spiro-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
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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

Landscapes

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

Abstract

También métodos de uso de tales compuestos como inhibidores de la tirosina quinasa de Bruton (Btk) y composiciones farmacéuticas que comprenden tales compuestos. Estos compuestos son de utilidad en el tratamiento, prevención o lentificación de la progresión de enfermedades o trastornos en una variedad de áreas terapéuticas, tales como enfermedades autoinmunes y enfermedad vascular. Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una de sus sales, en donde: las dos líneas de puntos representan dos enlaces simples o dos enlaces dobles; y R¹ᵇ y R²ᵇ, están presentes sólo si dichas dos líneas de puntos son dos enlaces simples; Q es: (i) un resto del grupo de fórmulas (2); (ii) un resto del grupo de fórmulas (3); (iii) un resto del grupo de fórmulas (4); o (iv) un resto del grupo de fórmulas (5); R¹ᵃ es: (i) H, -CN, -CF₃, -CH₃, -CR⁸ᵃR⁸ᵇOH, -CR⁸ᵃR⁸ᵇCR⁸ᵃR⁸ᵇOH, -CH(OH)CH₂OH, -NHR⁹, -C(O)NR¹⁰ᵃR¹⁰ᵇ, -C(O)(morfolinilo), -C(O)(piperazinilo), o -C(O)(metilpiperazinilo); o (ii) un compuesto de fórmula (6); R¹ᵇ, de estar presente, es H o -CH₃, siempre que, si R¹ᵃ es H entonces R¹ᵇ, también sea H; R²ᵃ es H, F, o Cl, siempre que, si R¹ᵃ es distinto de H entonces R²ᵃ es H; R²ᵇ, de estar presente, es igual que R²ᵃ; R³ es H, F, o Cl; R⁴ es H, F, Cl, o -CH₃; R⁵ᵃ es H, F, Cl, -OCH₃, o -OCF₃; R⁵ᵇ es H, F, Cl, -OCH₃, o -OCF₃; R⁶ᵃ es H, -CH₃ o ciclopropilo; R⁶ᶜ es H, -CH₃ o ciclopropilo; R⁷ᵃ es -C(O)CH=CH(R¹¹), -C(O)CºCR¹², o -S(O)₂CH=CH₂; R⁷ᵇ es -C(O)CH=CH₂; R⁷ᶜ es -C(O)CH=CH₂ o -C(O)CºCR¹²; R⁷ᵈ es -CN, -C(O)CH=CH₂, o -C(O)CºCR¹³; R⁷ᵉ es -CH=CH₂ o -CºCR¹³; R⁷ᶠ es pirrolidinilo sustituido con R⁷ᶜ, -CH=CHC(O)(morfolinilo) o -CH=CHC(O)(pirrolidinilo); R⁸ᵃ es H o -CH₃; R⁸ᵇ es H o -CH₃; R⁹ es alquilo C₁₋₄; R¹⁰ᵃ y R¹⁰ᵇ, son, de modo independiente, H o -CH₃; R¹¹ es H o -CH₃; R¹² es H, alquilo C₁₋₄, o ciclopropilo; y R¹³ es H, alquilo C₁₋₄, o ciclopropilo; siempre que: (a) si Q es un resto de fórmula (7) y R⁷ᵈ es -CN o -C(O)CH=CH₂, entonces R³ sea H; y (b) si las líneas de puntos representan dos enlaces simples, entonces: (i) Q no es un resto de fórmula (8), (9), ó (10); (ii) R¹¹, si está presente, es H; y (iii) el compuesto de la fórmula (1) no es un compuesto de fórmula (11).
ARP150103455A 2014-10-24 2015-10-23 Derivados de carbazol inhibidores de quinasas AR102427A1 (es)

Applications Claiming Priority (1)

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US201462068234P 2014-10-24 2014-10-24

Publications (1)

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AR102427A1 true AR102427A1 (es) 2017-03-01

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Country Status (34)

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US (3) US10266491B2 (es)
EP (1) EP3209651B9 (es)
JP (1) JP6599983B2 (es)
KR (1) KR102514914B1 (es)
CN (1) CN107074804B (es)
AR (1) AR102427A1 (es)
AU (1) AU2015335703B2 (es)
BR (1) BR112017007545A2 (es)
CA (1) CA2965523A1 (es)
CL (1) CL2017001001A1 (es)
CO (1) CO2017004517A2 (es)
CY (1) CY1122549T1 (es)
DK (1) DK3209651T3 (es)
EA (1) EA032361B1 (es)
ES (1) ES2761903T3 (es)
HR (1) HRP20192197T2 (es)
HU (1) HUE048321T2 (es)
IL (1) IL251798B (es)
LT (1) LT3209651T (es)
MA (1) MA40302B1 (es)
ME (1) ME03754B (es)
MX (1) MX374724B (es)
MY (1) MY190568A (es)
PE (1) PE20171239A1 (es)
PH (1) PH12017500724B1 (es)
PL (1) PL3209651T3 (es)
PT (1) PT3209651T (es)
RS (1) RS59707B1 (es)
SG (2) SG10201903619YA (es)
SI (1) SI3209651T1 (es)
SM (1) SMT202000035T1 (es)
TN (1) TN2017000158A1 (es)
TW (1) TWI676618B (es)
WO (1) WO2016065236A1 (es)

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