UA111756C2 - Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона - Google Patents

Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона

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Publication number
UA111756C2
UA111756C2 UAA201405799A UAA201405799A UA111756C2 UA 111756 C2 UA111756 C2 UA 111756C2 UA A201405799 A UAA201405799 A UA A201405799A UA A201405799 A UAA201405799 A UA A201405799A UA 111756 C2 UA111756 C2 UA 111756C2
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UA
Ukraine
Prior art keywords
compounds
heteroarylpyridone
azapiridone
bruton
formula
Prior art date
Application number
UAA201405799A
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English (en)
Inventor
Джеймс Джон Кроуфорд
Даніель Фред Ортвайн
БінКінг Вей
Венді Б. Янг
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of UA111756C2 publication Critical patent/UA111756C2/uk

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    • 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
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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    • 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
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • 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
    • C07D401/14—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 three or more hetero rings
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    • 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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    • 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
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
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    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
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Abstract

Запропоновані гетероарильні піридонові та азапіридонові сполуки формули І, де один або два з X, Xта Xпозначають N, включаючи їх стереоізомери, таутомери та фармацевтично прийнятні солі, корисні для інгібування тирозинкінази Брутона (Btk; від англ. Bruton's Tyrosine Kinase) та для лікування імунних розладів, таких як запалення, опосередковане кіназою Btk. Розкриті способи застосування сполук формули І для діагностики та лікування таких розладів в клітинах ссавців або асоційованих патологічних станів in vitro, in situ та in vivo.I
UAA201405799A 2011-11-03 2012-02-11 Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона UA111756C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555393P 2011-11-03 2011-11-03
PCT/US2012/063194 WO2013067274A1 (en) 2011-11-03 2012-11-02 Heteroaryl pyridone and aza-pyridone compounds as inhibitors of btk activity

Publications (1)

Publication Number Publication Date
UA111756C2 true UA111756C2 (uk) 2016-06-10

Family

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UAA201405799A UA111756C2 (uk) 2011-11-03 2012-02-11 Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона

Country Status (34)

Country Link
US (10) US8716274B2 (uk)
EP (5) EP3521288B1 (uk)
JP (5) JP5976827B2 (uk)
KR (2) KR20160003328A (uk)
CN (2) CN104125959B (uk)
AR (2) AR088641A1 (uk)
AU (5) AU2012332365B2 (uk)
CA (1) CA2853975C (uk)
CL (1) CL2014001103A1 (uk)
CO (1) CO6950472A2 (uk)
CR (1) CR20140194A (uk)
CY (1) CY1117097T1 (uk)
DK (2) DK2773638T3 (uk)
EA (1) EA023263B1 (uk)
ES (3) ES2898938T3 (uk)
HK (1) HK1201265A1 (uk)
HR (2) HRP20151442T1 (uk)
HU (2) HUE044959T2 (uk)
IL (1) IL232060A (uk)
IN (1) IN2014CN03250A (uk)
LT (1) LT3002284T (uk)
MA (1) MA35819B1 (uk)
MX (2) MX2014005331A (uk)
PE (1) PE20141586A1 (uk)
PL (3) PL3002284T3 (uk)
PT (2) PT2773638E (uk)
RS (2) RS54505B1 (uk)
SG (1) SG11201401992YA (uk)
SI (2) SI2773638T1 (uk)
TR (1) TR201909849T4 (uk)
TW (4) TWI701250B (uk)
UA (1) UA111756C2 (uk)
WO (1) WO2013067274A1 (uk)
ZA (1) ZA201804727B (uk)

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