AR099052A1 - Derivados de azaindol - Google Patents

Derivados de azaindol

Info

Publication number
AR099052A1
AR099052A1 ARP150100043A ARP150100043A AR099052A1 AR 099052 A1 AR099052 A1 AR 099052A1 AR P150100043 A ARP150100043 A AR P150100043A AR P150100043 A ARP150100043 A AR P150100043A AR 099052 A1 AR099052 A1 AR 099052A1
Authority
AR
Argentina
Prior art keywords
independently selected
alkyl
halo
oxo
hydrogen
Prior art date
Application number
ARP150100043A
Other languages
English (en)
Original Assignee
Takeda Pharmaceuticals 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
Application filed by Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of AR099052A1 publication Critical patent/AR099052A1/es

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Classifications

    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/55—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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente se refiere a materiales y métodos para preparar compuestos, composiciones farmacéuticas que los contienen y su uso para tratar trastornos inmunológicos, enfermedad cardiovascular, cáncer y otras enfermedades, trastornos o afecciones asociadas con PI3Kd (fosfoinositida 3-quinasas). Reivindicación 1: Un compuesto de fórmula (1), o su sal farmacéuticamente aceptable, donde: R¹ se selecciona de: (a) cicloalquilo C₃₋₈, sustituido con -NHR¹³ y opcionalmente sustituido con uno o dos sustituyentes adicionales seleccionados independientemente de halo, oxo, -CN, R¹¹ y R¹²; (b) cicloalquenilo C₃₋₈, sustituido con -NHR¹³ y opcionalmente sustituido con uno o dos sustituyentes adicionales seleccionados independientemente de halo, oxo, -CN, R¹¹ y R¹²; (c) heterociclilo C₂₋₆, que se encuentra unido directamente a un resto de azaindol mostrado en la fórmula (1) a través de un átomo de carbono, tiene al menos un heteroátomo que es nitrógeno insustituido y se encuentra opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente de halo, oxo -CN, R¹¹ y R¹²; (d) heterociclilo C₂₋₆, que se encuentra unido directamente al resto de azaindol a través de un heteroátomo de nitrógeno, se encuentra sustituido con -NHR¹³ o tiene al menos un heteroátomo adicional que es nitrógeno insustituido y se encuentra opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente de halo, oxo -CN, R¹¹ y R¹²; y (e) heterociclilo C₂₋₆-N(R¹³)-, donde el resto de heterociclilo tiene al menos un heteroátomo que es nitrógeno insustituido y se encuentra opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente de halo, oxo, -CN, R¹¹ y R¹²; cada R², R⁴ y R⁵ se selecciona independientemente de hidrógeno, halo, -OH, -CN, alquilo C₁₋₃ y haloalquilo C₁₋₃; R³ se selecciona de hidrógeno, alquilo C₁₋₃ y haloalquilo C₁₋₃; cada R⁶ y R⁷ se selecciona independientemente de hidrógeno, alquilo C₁₋₃ y haloalquilo C₁₋₃; R⁸ se selecciona de hidrogeno, alquilo C₁₋₃ y -NH₂; R⁹ se selecciona de hidrógeno, halo, -CN, haloalquilo C₁₋₃, -OR¹⁶, -C(O)R¹⁶, -C(O)OR¹⁶, -C(O)N(R¹⁶)R¹⁷, -C(O)N(R¹⁶)OR¹⁷, -C(O)N(R¹⁶)S(O)₂R¹⁸, -SR¹⁶, -S(O)R¹⁸, -S(O)₂R¹⁸ y -S(O)₂N(R¹⁶)R¹⁷; R¹⁰ se selecciona de halo, -OH, alquilo C₁₋₃, -NHR¹⁶, -NHC(O)R¹⁶; cada R¹¹ se selecciona independientemente de -OR¹³, -N(R¹³)R¹⁴, -NR¹³C(O)R¹⁴, -NHC(O)NR¹³R¹⁴, -NR¹³C(O)NHR¹⁴, -C(O)R¹³, -C(O)OR¹³, -C(O)N(R¹³)R¹⁴, -C(O)N(R¹³)OR¹⁴, -C(O)N(R¹³)S(O)₂R¹², -N(R¹³)S(O)₂R¹², -SR¹³, -S(O)R¹², -S(O)₂R¹² y -S(O)₂N(R¹³)R¹⁴; cada R¹² se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈-(CH₂)ₘ-, arilo C₆₋₁₄-(CH₂)ₘ-, heterociclilo C₂₋₆-(CH₂)ₘ- y heteroarilo C₁₋₉-(CH₂)ₘ-, cada uno opcionalmente sustituido con uno a cinco sustituyentes seleccionados independientemente de halo oxo, -CN, alquilo C₁₋₆, haloalquilo C₁₋₆ y R¹⁵; cada R¹³ y R¹⁴ se selecciona independientemente de (a) hidrógeno; y (b) alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆-(CH₂)ₘ-, arilo C₆₋₁₄-(CH₂)ₘ-, heterociclilo C₂₋₆-(CH₂)ₘ- y heteroarilo C₁₋₉-(CH₂)ₘ-, cada uno opcionalmente sustituido con uno a cinco sustituyentes seleccionados independientemente de halo, oxo, -CN, alquilo C₁₋₆, haloalquilo C₁₋₆ y R¹⁵; cada R¹⁵ se selecciona independientemente de -OR¹⁶, -N(R¹⁶)R¹⁷, -N(R¹⁶)C(O)R¹⁷, -NHC(O)NR¹⁶R¹⁷, -NR¹⁶C(O)NHR¹⁷, -C(O)R¹⁶, -C(O)OR¹⁶, -C(O)N(R¹⁶)R¹⁷, -C(O)N(R¹⁶)OR¹⁷, -C(O)N(R¹⁶)S(O)₂R¹⁸, -NR¹⁶S(O)₂R¹⁸, -SR¹⁶, -S(O)R¹⁸, -S(O)₂R¹⁸ y -S(O)₂N(R¹⁶)R¹⁷; cada R¹⁶ y R¹⁷ se selecciona independientemente de hidrógeno, alquilo C₁₋₆ y cicloalquilo C₃₋₆; cada R¹⁸ se selecciona independientemente de alquilo C₁₋₆ y cicloalquilo C₃₋₆; cada m se selecciona independientemente de 0, 1, 2, 3 y 4; donde cada uno de los restos de heteroarilo mencionados anteriormente tiene independientemente 1 a 4 heteroátomos seleccionados independientemente de N, O y S y cada uno de los restos heterociclilo mencionados anteriormente tiene independientemente 1 a 4 heteroátomos seleccionados independientemente de N, O y S.
ARP150100043A 2014-01-09 2015-01-08 Derivados de azaindol AR099052A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461925598P 2014-01-09 2014-01-09

Publications (1)

Publication Number Publication Date
AR099052A1 true AR099052A1 (es) 2016-06-29

Family

ID=52392263

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150100043A AR099052A1 (es) 2014-01-09 2015-01-08 Derivados de azaindol

Country Status (5)

Country Link
US (1) US9371321B2 (es)
AR (1) AR099052A1 (es)
TW (1) TW201620904A (es)
UY (1) UY35945A (es)
WO (1) WO2015106012A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY34893A (es) * 2012-07-10 2014-02-28 Takeda Pharmaceutical Derivados de azaindol
UY35945A (es) 2014-01-09 2015-08-31 Takeda Pharmaceutical Derivados de azaindol
WO2019119207A1 (en) * 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta

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Also Published As

Publication number Publication date
UY35945A (es) 2015-08-31
US9371321B2 (en) 2016-06-21
WO2015106012A1 (en) 2015-07-16
US20150191465A1 (en) 2015-07-09
TW201620904A (zh) 2016-06-16

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