EA201190237A1 - Аналоги изоксазол-3(2н)-она в качестве терапевтических агентов - Google Patents

Аналоги изоксазол-3(2н)-она в качестве терапевтических агентов

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Publication number
EA201190237A1
EA201190237A1 EA201190237A EA201190237A EA201190237A1 EA 201190237 A1 EA201190237 A1 EA 201190237A1 EA 201190237 A EA201190237 A EA 201190237A EA 201190237 A EA201190237 A EA 201190237A EA 201190237 A1 EA201190237 A1 EA 201190237A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
optionally substituted
deuterium
heteroaryl
aryl
Prior art date
Application number
EA201190237A
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English (en)
Other versions
EA020825B1 (ru
Inventor
Йонас Бострём
Лейфенг Ченг
Томас Фекс
Михель Карле
Даниель Петтерсен
Петер Шелль
Original Assignee
Астразенека Аб
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.)
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Publication date
Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of EA201190237A1 publication Critical patent/EA201190237A1/ru
Publication of EA020825B1 publication Critical patent/EA020825B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Соединение I или его фармацевтически приемлемая соль, где R1 и R2 независимо представляют собой водород, дейтерий, арил, гетероарил, C-C-алкил, возможно замещенный одним или более заместителями, независимо представляющими собой R3, R3 представляет собой арил, гетероарил, фтор, C-C-алкил, содержащий один или более чем один фтор, C-C-алкил, содержащий один или более чем один дейтерий, C-C-алкил, содержащий гидрокси, где арил и гетероарил возможно замещены одним или более чем одним галогеном, фторированным алкокси, фторированным алкилом, сульфонилом, одним или более чем одним дейтерием, Cалкилом, Cалкокси, нитрилом, или R3 представляет собой C-алкил, возможно замещенный одной или более из следующих групп: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; где R4 представляет собой Cалкил, возможно замещенный одним или более чем одним фтором, дейтерием, алкокси, арилкарбоксилатом, алкилкарбоксилатом; R5 и R6 независимо выбраны из водорода, алкила или они могут вместе образовывать 4-8-членное углеродное кольцо; или R1 и R2 образуют 3-10-членное углеродное кольцо, возможно содержащее О или N и возможно замещенное Cалкилом или арилом, гетероарилом, возможно замещенным R3.
EA201190237A 2009-04-07 2010-04-06 Аналоги изоксазол-3(2h)-она в качестве терапевтических агентов EA020825B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16722409P 2009-04-07 2009-04-07
US17195609P 2009-04-23 2009-04-23
PCT/SE2010/050375 WO2010117323A1 (en) 2009-04-07 2010-04-06 Method and apparatus for producing heat energy and carbon dioxide

Publications (2)

Publication Number Publication Date
EA201190237A1 true EA201190237A1 (ru) 2012-04-30
EA020825B1 EA020825B1 (ru) 2015-02-27

Family

ID=42934883

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190237A EA020825B1 (ru) 2009-04-07 2010-04-06 Аналоги изоксазол-3(2h)-она в качестве терапевтических агентов

Country Status (21)

Country Link
US (1) US8415378B2 (ru)
EP (1) EP2417131A4 (ru)
JP (1) JP5711723B2 (ru)
KR (1) KR101675607B1 (ru)
CN (1) CN102459246B (ru)
AR (1) AR076219A1 (ru)
AU (1) AU2010235236B2 (ru)
BR (1) BRPI1013984A2 (ru)
CA (1) CA2757879C (ru)
CO (1) CO6440580A2 (ru)
CU (1) CU20110190A7 (ru)
EA (1) EA020825B1 (ru)
EC (1) ECSP11011385A (ru)
IL (1) IL215336A0 (ru)
MX (1) MX2011010647A (ru)
NI (1) NI201100181A (ru)
SG (1) SG174463A1 (ru)
TW (1) TW201040166A (ru)
UY (1) UY32543A (ru)
WO (1) WO2010117323A1 (ru)
ZA (1) ZA201108119B (ru)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ601483A (en) 2008-08-04 2013-10-25 Chdi Foundation Inc Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
CN102811620B (zh) 2010-01-25 2015-03-25 Chdi基金会股份有限公司 一些犬尿氨酸-3-单加氧酶抑制剂、药物组合物及其使用方法
WO2012047156A1 (en) * 2010-10-04 2012-04-12 Astrazeneca Ab Isoxazol-3(2h)-one analogs as plasminogen inhibitors and their use in the treatment of fibrinolysis related diseases
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AU2012300246A1 (en) 2011-08-30 2014-03-06 Chdi Foundation, Inc. Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
BR112014004741B1 (pt) 2011-08-30 2021-10-13 Chdi Foundation, Inc Entidade química, seu uso e composição farmacêutica compreendendo a mesma
US9073881B2 (en) 2011-09-23 2015-07-07 Hoffmann-La Roche Inc. Benzoic acid derivatives
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
CN102977050B (zh) * 2012-11-20 2015-04-22 浙江工业大学 一种2-苯并噻唑二甲缩醛和2-苯并噻唑甲醛的合成方法
CN102977040B (zh) * 2012-11-20 2015-06-03 浙江工业大学 一种2-喹喔啉基二甲缩醛和2-喹喔啉基甲醛的合成方法
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
UY35809A (es) 2013-11-05 2015-05-29 Bayer Pharma AG (aza)piridopirazolopirimidinonas e indazolopirimidinonas y sus usos
AU2015289492B2 (en) 2014-07-17 2020-02-20 Chdi Foundation, Inc. Methods and compositions for treating HIV-related disorders
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016071216A1 (en) 2014-11-03 2016-05-12 Bayer Pharma Aktiengesellschaft Piperidinylpyrazolopyrimidinones and their use
CA2967268A1 (en) 2014-12-19 2016-06-23 Emeriti Pharma Ab 3-(piperidin-4-yl)-isoxazol-3(2h)-ones for treatment of dermatologic disorders
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
CN104725300A (zh) * 2015-02-28 2015-06-24 宁波九胜创新医药科技有限公司 一种1-(6-甲基吡啶-3-基)-2-(4-甲磺酰基苯基)乙酮的制备方法
WO2016173948A1 (en) 2015-04-30 2016-11-03 Bayer Pharma Aktiengesellschaft Indazolopyrimidinones as fibrinolysis inhibitors
CN107459514B (zh) * 2016-06-06 2020-10-23 南开大学 一类手性哌啶衍生物及其制备方法和用途
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107857725A (zh) * 2017-12-19 2018-03-30 苏州艾缇克药物化学有限公司 一种2‑氨基吡啶‑4‑甲醇的合成方法
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4289850A4 (en) * 2021-02-05 2024-12-11 Scinnohub Pharmaceutical Co., Ltd Plasmin inhibitor, preparation method therefor, and application thereof
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ276633A (en) 1993-11-24 1998-04-27 Du Pont Merck Pharma Isoxazole and isoxazoline derivatives and pharmaceutical compositions thereof
AU1735200A (en) * 1998-11-18 2000-06-05 Du Pont Pharmaceuticals Company Novel isoxazoline fibrinogen receptor antagonists
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2004231087B2 (en) * 2003-04-15 2007-01-04 Merck Sharp & Dohme Corp. Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
US7598243B2 (en) * 2003-04-17 2009-10-06 Merck & Co., Inc. Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
CN101328173B (zh) * 2008-07-31 2010-12-15 石药集团欧意药业有限公司 一种制备6-氟-3-(4-哌啶基)-1,2-苯并异噁唑盐酸盐的方法

Also Published As

Publication number Publication date
KR101675607B1 (ko) 2016-11-11
CA2757879C (en) 2017-06-06
MX2011010647A (es) 2012-02-21
AR076219A1 (es) 2011-05-26
EP2417131A1 (en) 2012-02-15
CU20110190A7 (es) 2012-02-15
NI201100181A (es) 2012-06-14
CA2757879A1 (en) 2010-10-14
CN102459246B (zh) 2014-05-07
SG174463A1 (en) 2011-10-28
JP2012522836A (ja) 2012-09-27
WO2010117323A8 (en) 2010-11-18
IL215336A0 (en) 2011-12-29
US20100261755A1 (en) 2010-10-14
AU2010235236B2 (en) 2013-10-24
EA020825B1 (ru) 2015-02-27
AU2010235236A1 (en) 2011-10-20
JP5711723B2 (ja) 2015-05-07
BRPI1013984A2 (pt) 2018-06-19
ECSP11011385A (es) 2011-11-30
CN102459246A (zh) 2012-05-16
WO2010117323A1 (en) 2010-10-14
KR20120034611A (ko) 2012-04-12
UY32543A (es) 2010-11-30
EP2417131A4 (en) 2014-08-27
TW201040166A (en) 2010-11-16
US8415378B2 (en) 2013-04-09
ZA201108119B (en) 2012-07-25
CO6440580A2 (es) 2012-05-15

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