EA019059B1 - Дизамещенные фталазиновые антагонисты пути hedgehog - Google Patents

Дизамещенные фталазиновые антагонисты пути hedgehog Download PDF

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Publication number
EA019059B1
EA019059B1 EA201270049A EA201270049A EA019059B1 EA 019059 B1 EA019059 B1 EA 019059B1 EA 201270049 A EA201270049 A EA 201270049A EA 201270049 A EA201270049 A EA 201270049A EA 019059 B1 EA019059 B1 EA 019059B1
Authority
EA
Eurasian Patent Office
Prior art keywords
methyl
cancer
pharmaceutically acceptable
acceptable salt
trifluoromethyl
Prior art date
Application number
EA201270049A
Other languages
English (en)
Russian (ru)
Other versions
EA201270049A1 (ru
Inventor
Филип Артур Хипскинд
Бхарвин Кумар Пател
Уилсон (урожденная Такакува), Такако
Original Assignee
Эли Лилли Энд Компани
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 Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201270049A1 publication Critical patent/EA201270049A1/ru
Publication of EA019059B1 publication Critical patent/EA019059B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
EA201270049A 2009-06-19 2010-06-15 Дизамещенные фталазиновые антагонисты пути hedgehog EA019059B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21862809P 2009-06-19 2009-06-19
PCT/US2010/038568 WO2010147917A1 (en) 2009-06-19 2010-06-15 Disubstituted phthalazine hedgehog pathway antagonists

Publications (2)

Publication Number Publication Date
EA201270049A1 EA201270049A1 (ru) 2012-05-30
EA019059B1 true EA019059B1 (ru) 2013-12-30

Family

ID=42332981

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270049A EA019059B1 (ru) 2009-06-19 2010-06-15 Дизамещенные фталазиновые антагонисты пути hedgehog

Country Status (35)

Country Link
US (2) US8273742B2 (enExample)
EP (1) EP2443104B1 (enExample)
JP (1) JP5596139B2 (enExample)
KR (1) KR101389165B1 (enExample)
CN (1) CN102459233B (enExample)
AR (1) AR077014A1 (enExample)
AU (1) AU2010260244B2 (enExample)
BR (1) BRPI1011601A2 (enExample)
CA (1) CA2764542C (enExample)
CL (1) CL2011003147A1 (enExample)
CO (1) CO6480932A2 (enExample)
CR (1) CR20110658A (enExample)
DK (1) DK2443104T3 (enExample)
DO (1) DOP2011000386A (enExample)
EA (1) EA019059B1 (enExample)
EC (1) ECSP11011541A (enExample)
ES (1) ES2409054T3 (enExample)
HN (1) HN2011003139A (enExample)
HR (1) HRP20130408T1 (enExample)
IL (1) IL216599A (enExample)
JO (1) JO2931B1 (enExample)
MA (1) MA33363B1 (enExample)
MX (1) MX2011014029A (enExample)
MY (1) MY156667A (enExample)
NZ (1) NZ596882A (enExample)
PE (1) PE20121050A1 (enExample)
PL (1) PL2443104T3 (enExample)
PT (1) PT2443104E (enExample)
SG (1) SG177289A1 (enExample)
SI (1) SI2443104T1 (enExample)
TN (1) TN2011000627A1 (enExample)
TW (1) TWI385165B (enExample)
UA (1) UA106755C2 (enExample)
WO (1) WO2010147917A1 (enExample)
ZA (1) ZA201108587B (enExample)

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UA102250C2 (ru) * 2008-04-29 2013-06-25 Эли Лилли Энд Компани Двухзамещенные фталазины - антагонисты проводящего пути hedgehog
MX2011004683A (es) * 2008-11-03 2011-06-20 Lilly Co Eli Antagonistas de la via hedgehog de ftalazina disustituida.
KR101342184B1 (ko) 2008-11-17 2013-12-19 일라이 릴리 앤드 캄파니 사치환된 피리다진 헷지호그 경로 길항제
BRPI0921777A2 (pt) * 2008-11-17 2016-01-12 Lilly Co Eli antagonistas da via hedgehog de piridazina tetrassubstituída
AR077014A1 (es) 2009-06-19 2011-07-27 Lilly Co Eli Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer
AU2012232670A1 (en) 2011-03-23 2013-09-12 Ariel-University Research And Development Company Ltd. Treatment of proliferative disorders with a chemiluminescent agent
GB201309508D0 (en) * 2013-05-28 2013-07-10 Redx Pharma Ltd Compounds
GB201311953D0 (en) * 2013-07-03 2013-08-14 Redx Pharma Ltd Compounds
WO2015073691A1 (en) 2013-11-14 2015-05-21 The Board Of Trustees Of The Leland Stanford Junior University Methods for treating cancer by activation of bmp signaling
CN105017140B (zh) * 2014-04-28 2017-12-29 复旦大学 邻氨基苯甲酰胺化合物及其制备方法和用途
GB2528298A (en) * 2014-07-16 2016-01-20 Redx Pharma Plc Compounds
CN105985319B (zh) * 2015-02-11 2019-02-26 复旦大学 芳基酞嗪化合物及其制备方法和用途
CN105985320B (zh) * 2015-02-11 2018-10-26 复旦大学 苄基酞嗪化合物及其制备方法和用途
CN105985321B (zh) * 2015-02-11 2018-10-26 复旦大学 吡唑酞嗪化合物及其制备方法和用途
PL3302428T3 (pl) 2015-06-04 2026-04-13 Sol-Gel Technologies Ltd. Preparaty do zastosowania miejscowego do dostarczania związków inhibitora hedgehog i ich zastosowanie
WO2016196879A1 (en) * 2015-06-05 2016-12-08 Dana-Farber Cancer Institute, Inc. Compounds and methods for treating cancer
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
CN106279114B (zh) * 2016-08-04 2019-01-29 东南大学 一种Taladegib的合成方法
US10548908B2 (en) * 2016-09-15 2020-02-04 Nostopharma, LLC Compositions and methods for preventing and treating heterotopic ossification and pathologic calcification
CN106831718B (zh) * 2016-12-30 2019-05-07 上海科技大学 平滑受体配体及其应用
US11389434B2 (en) 2017-05-18 2022-07-19 Inserm Methods and pharmaceutical compositions for the treatment of mast cell diseases
WO2021261601A1 (ja) 2020-06-26 2021-12-30 ラクオリア創薬株式会社 レチノイドとがん治療薬との併用療法が有効ながん患者の選択方法およびレチノイドとがん治療薬との併用医薬
JP2023546536A (ja) * 2020-10-13 2023-11-02 エンデバー バイオメディシンズ, インコーポレイテッド 線維症を処置する方法
US12605377B2 (en) 2020-10-13 2026-04-21 Endeavor Biomedicines, Inc. Methods of treating fibrosis
WO2025188802A1 (en) 2024-03-05 2025-09-12 Endeavor Biomedicines, Inc. Methods of improving lung function
WO2025189041A1 (en) * 2024-03-07 2025-09-12 Endeavor Biomedicines, Inc. Methods of treating fibrosis
WO2025242197A1 (zh) * 2024-05-24 2025-11-27 成都思倍博医药科技有限公司 氘代的Hedgehog通路SMO受体抑制剂

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003088970A2 (en) * 2002-04-22 2003-10-30 Johns Hopkins University School Of Medicine Modulators of hedgehog signaling pathways, compositions and uses related thereto
WO2008110611A1 (en) * 2007-03-15 2008-09-18 Novartis Ag Organic compounds and their uses
WO2009002469A1 (en) * 2007-06-25 2008-12-31 Amgen Inc. Phthalazine compounds, compositions and methods of use
WO2009134574A2 (en) * 2008-04-29 2009-11-05 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists

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JP5067986B2 (ja) 1998-04-09 2012-11-07 ジョンズ ホプキンズ ユニヴァーシティー スクール オブ メディシン ヘッジホッグシグナリング経路の阻害剤としてのステロイドアルカロイド誘導体の使用
ATE283700T1 (de) 1999-06-08 2004-12-15 Lorantis Ltd Therapeutische verwendung eines inhibitors des hedgehog signalübertragungsweges
BR0211513A (pt) * 2001-07-27 2005-08-30 Curis Inc Mediadores de caminhos sinalizantes de hedgehog, composições e usos relacionados ao mesmo
WO2004020599A2 (en) 2002-08-29 2004-03-11 Curis, Inc. Hedgehog antagonists, methods and uses related thereto
WO2005033288A2 (en) 2003-09-29 2005-04-14 The Johns Hopkins University Hedgehog pathway antagonists
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WO2006004589A2 (en) 2004-05-08 2006-01-12 Neurogen Corporation 3-aryl-5,6-disubstituted pyridazines
ES2377430T3 (es) 2004-09-02 2012-03-27 Genentech, Inc. Inhibidores piridílicos de la señalización de hedgehog
EP1900731A1 (de) * 2006-09-07 2008-03-19 Bayer Schering Pharma Aktiengesellschaft N-(1-Phthalazin-1-yl-piperidin-4-yl)-amide als EP2-Rezeptor Modulatoren
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WO2010017240A2 (en) * 2008-08-04 2010-02-11 Amgen Inc. Aurora kinase modulators and methods of use
MX2011004683A (es) 2008-11-03 2011-06-20 Lilly Co Eli Antagonistas de la via hedgehog de ftalazina disustituida.
BRPI0921777A2 (pt) 2008-11-17 2016-01-12 Lilly Co Eli antagonistas da via hedgehog de piridazina tetrassubstituída
KR101342184B1 (ko) 2008-11-17 2013-12-19 일라이 릴리 앤드 캄파니 사치환된 피리다진 헷지호그 경로 길항제
AR077014A1 (es) 2009-06-19 2011-07-27 Lilly Co Eli Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2003088970A2 (en) * 2002-04-22 2003-10-30 Johns Hopkins University School Of Medicine Modulators of hedgehog signaling pathways, compositions and uses related thereto
WO2008110611A1 (en) * 2007-03-15 2008-09-18 Novartis Ag Organic compounds and their uses
WO2009002469A1 (en) * 2007-06-25 2008-12-31 Amgen Inc. Phthalazine compounds, compositions and methods of use
WO2009134574A2 (en) * 2008-04-29 2009-11-05 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists

Also Published As

Publication number Publication date
CL2011003147A1 (es) 2012-07-20
PT2443104E (pt) 2013-05-07
CA2764542A1 (en) 2010-12-23
DK2443104T3 (da) 2013-05-06
MY156667A (en) 2016-03-15
PE20121050A1 (es) 2012-08-09
DOP2011000386A (es) 2012-02-29
US9000023B2 (en) 2015-04-07
CO6480932A2 (es) 2012-07-16
EP2443104B1 (en) 2013-04-17
US8273742B2 (en) 2012-09-25
JP5596139B2 (ja) 2014-09-24
TW201113268A (en) 2011-04-16
JO2931B1 (en) 2015-09-15
MX2011014029A (es) 2012-02-21
ECSP11011541A (es) 2012-01-31
US20100324048A1 (en) 2010-12-23
CN102459233B (zh) 2014-07-02
EA201270049A1 (ru) 2012-05-30
KR20120024783A (ko) 2012-03-14
IL216599A (en) 2015-09-24
HRP20130408T1 (en) 2013-06-30
IL216599A0 (en) 2012-03-01
PL2443104T3 (pl) 2013-08-30
AR077014A1 (es) 2011-07-27
WO2010147917A1 (en) 2010-12-23
MA33363B1 (fr) 2012-06-01
SG177289A1 (en) 2012-02-28
TWI385165B (zh) 2013-02-11
JP2012530705A (ja) 2012-12-06
CA2764542C (en) 2013-09-10
CN102459233A (zh) 2012-05-16
AU2010260244A1 (en) 2012-01-19
KR101389165B1 (ko) 2014-04-24
EP2443104A1 (en) 2012-04-25
HK1164872A1 (en) 2012-09-28
SI2443104T1 (sl) 2013-07-31
ZA201108587B (en) 2013-05-29
AU2010260244B2 (en) 2013-09-05
HN2011003139A (es) 2013-07-29
NZ596882A (en) 2013-08-30
US20120316174A1 (en) 2012-12-13
ES2409054T3 (es) 2013-06-24
UA106755C2 (uk) 2014-10-10
TN2011000627A1 (en) 2013-05-24
CR20110658A (es) 2012-02-20
BRPI1011601A2 (pt) 2016-03-22

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ BY KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM KZ RU