AR119882A2 - Derivados de pirimidin-4-ilamino-benzooxazol - Google Patents

Derivados de pirimidin-4-ilamino-benzooxazol

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Publication number
AR119882A2
AR119882A2 ARP200102456A ARP200102456A AR119882A2 AR 119882 A2 AR119882 A2 AR 119882A2 AR P200102456 A ARP200102456 A AR P200102456A AR P200102456 A ARP200102456 A AR P200102456A AR 119882 A2 AR119882 A2 AR 119882A2
Authority
AR
Argentina
Prior art keywords
membered
ora
independently
attached
nra
Prior art date
Application number
ARP200102456A
Other languages
English (en)
Inventor
Rajinder Singh
Yan Chen
Rose Yen
Pingyu Ding
Sambaiah Thota
Thilo Heckrodt
Darren John Mmurtrie
Hui Li
Vanessa Taylor
Original Assignee
Rigel Pharmaceuticals 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 Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of AR119882A2 publication Critical patent/AR119882A2/es

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    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Compuestos derivados de pirimidin-4-ilamino-benzo[d]oxazol-2(3H)-ona como inhibidores de la JAK quinasa. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), R¹ es H o R⁵⁰; R⁴ es H o C₁₋₆alquilo; R⁵ es H, halo, o C₁₋₆alquilo; cada R⁵⁰ es -C(R⁹)₂-A-R¹⁰, donde A es O ó S; cada R⁹ es independientemente en cada caso H, C₁₋₆alquilo, C₆₋₁₀arilo o C₇₋₁₆arilalquilo; o de manera alternativa, dos R⁹, juntos con el carbono al que están unidos forman un grupo C₃₋₈cicloalquilo o un heteroaliciclilo de 3 a 8 miembros; R¹⁰ es Rᵃ, -P(O)(OR¹¹)₂, -P(O)(OR¹¹)N(R¹²)₂ o -P(O)(N(R¹²)₂)₂; cada R¹¹ es independientemente en cada caso Rᵃ o un grupo catiónico monovalente; o dos R¹¹, juntos con los átomos a los que están unidos, forman un grupo fosfato cíclico de 4 a 8 miembros; cada R¹² es independientemente en cada caso Rᶜ o -C₁₋₃alquilo-N(Rᶜ)₂; o dos R¹², cada uno en nitrógenos separados de -P(O)(N(R¹²)₂)₂ juntos con los átomos a los que están unidos, forman un grupo bis amida de ácido fosfónico cíclico de 4 a 8 miembros; o un R¹² junto con R¹¹ del grupo -P(O)(OR¹¹)N(R¹²)₂, junto con los átomos a los que están unidos, forman un grupo fosfonamidato cíclico de 4 a 8 miembros; R²ᵃ, R²ᵇ, R²ᶜ y R²ᵈ se selecciona independientemente de H, F, CH₃, y OCH₃; R²ᵉ es H, halo o CH₃; cada Rᵃ es independientemente en cada caso H, deuterio, C₁₋₆alquilo, C₃₋₈cicloalquilo, C₄₋₁₁cicloalquiloalquilo, C₆₋₁₀arilo, C₇₋₁₆arilalquilo, heteroalquilo de 2 a 6 miembros, heteroaliciclilo de 3 a 10 miembros, heteroalicicliloalquilo de 4 a 11 miembros, heteroarilo de 5 a 15 miembros o heteroarilalquilo de 6 a 16 miembros; cada Rᶜ es independientemente en cada caso Rᵃ, o, de manera alternativa, dos Rᶜ tomados juntos con el átomo de nitrógeno al que están unidos forman un heteroaliciclilo 3 a 10 miembros o un heteroarilo de 5 a 10 miembros que puede incluir uno o más heteroátomos adicionales iguales o distintos y que pueden estar sustituidos por uno o más de los grupos Rᵃ y/o Rᵈ iguales o diferentes; cada Rᵈ es =O, -ORᵃ, haloC₁₋₃alquilooxi, C₁₋₆alquilo, =S, -SRᵃ, =NRᵃ, =NORᵃ, -N(Rᵃ)₂, halo, -CF₃, -CN, -NC, -OCN, -SCN, -NO, -NO₂, =N₂, -N₃, -S(O)Rᵃ, -S(O₂)Rᵃ, -SO₃Rᵃ, -S(O)N(Rᵃ)₂, -S(O)₂N(Rᵃ)₂, -OS(O)Rᵃ, -OS(O)₂Rᵃ, -OSO₃Rᵃ, -OS(O)₂N(Rᵃ)₂, -C(O)Rᵃ, -CO₂Rᵃ, -C(O)N(Rᵃ)₂, -C(NRᵃ)N(Rᵃ)₂, -C(NOH)Rᵃ, -C(NOH)N(Rᵃ)₂, -OCO₂Rᵃ, -OC(O)N(Rᵃ)₂, -OC(NRᵃ)N(Rᵃ)₂, -[N(Rᵃ)C(O)]ₙRᵃ, -(C(Rᵃ)₂)ₙ-ORᵃ, -N(Rᵃ)-S(O)₂Rᵃ, -C(O)-C₁₋₆haloalquilo, -S(O)₂C₁₋₆haloalquilo, -OC(O)Rᵃ, -O(C(Rᵃ)₂)ₘ-ORᵃ, -S(C(Rᵃ)₂)ₘ-ORᵃ, -N(Rᵃ)C₁₋₆haloalquilo, -P(O)(ORᵃ)₂, -N(Rᵃ)-(C(Rᵃ)₂)ₘ-ORᵃ, -[N(Rᵃ)C(O)]ₙORᵃ, -[N(Rᵃ)C(O)]ₙN(Rᵃ)₂, -[N(Rᵃ)C(NRᵃ)]ₙN(Rᵃ)₂ o -N(Rᵃ)C(O)C₁₋₆haloalquilo; o dos Rᵈ, tomados juntos con el átomo o átomos al que están unidos se combinan para formar un anillo mono o bicíclico de 3 a 10 miembros parcial o totalmente saturado que puede contener uno o más heteroátomos y puede estar sustituido por uno o más Rᵃ; cada m es 1, 2 ó 3; y cada n es 0, 1, 2 ó 3.
ARP200102456A 2010-07-28 2020-09-02 Derivados de pirimidin-4-ilamino-benzooxazol AR119882A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US36857010P 2010-07-28 2010-07-28

Publications (1)

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AR119882A2 true AR119882A2 (es) 2022-01-19

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ARP110102733A AR082408A1 (es) 2010-07-28 2011-07-28 Derivados de pirimidina, composiciones y metodos para inhibicion de la via jak
ARP200102456A AR119882A2 (es) 2010-07-28 2020-09-02 Derivados de pirimidin-4-ilamino-benzooxazol

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EP (1) EP2598500B1 (es)
JP (2) JP6073221B2 (es)
KR (1) KR101937495B1 (es)
CN (1) CN103201280B (es)
AR (2) AR082408A1 (es)
AU (1) AU2011282742B2 (es)
BR (1) BR112013001632B1 (es)
CA (1) CA2804199C (es)
DK (1) DK2598500T3 (es)
EA (1) EA201390015A1 (es)
ES (1) ES2880622T3 (es)
IL (1) IL223855A (es)
MX (2) MX347331B (es)
PL (1) PL2598500T3 (es)
PT (1) PT2598500T (es)
RU (1) RU2672100C2 (es)
TW (1) TWI582090B (es)
WO (1) WO2012015972A1 (es)
ZA (1) ZA201300388B (es)

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AR082408A1 (es) 2012-12-05
EA201390015A1 (ru) 2013-07-30
US10479783B2 (en) 2019-11-19
EP2598500B1 (en) 2021-05-19
JP2017061518A (ja) 2017-03-30
US9067925B2 (en) 2015-06-30
JP6073221B2 (ja) 2017-02-01
ZA201300388B (en) 2013-09-25
US11174251B2 (en) 2021-11-16
AU2011282742A2 (en) 2013-04-04
EP2598500A1 (en) 2013-06-05
AU2011282742B2 (en) 2015-08-27
PL2598500T3 (pl) 2021-11-29
KR101937495B1 (ko) 2019-01-10
AU2011282742A1 (en) 2013-02-07
IL223855A (en) 2016-05-31
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