KR101389165B1 - 이치환된 프탈라진 헤지호그 (hedgehog) 경로 길항제 - Google Patents

이치환된 프탈라진 헤지호그 (hedgehog) 경로 길항제 Download PDF

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Publication number
KR101389165B1
KR101389165B1 KR1020117030157A KR20117030157A KR101389165B1 KR 101389165 B1 KR101389165 B1 KR 101389165B1 KR 1020117030157 A KR1020117030157 A KR 1020117030157A KR 20117030157 A KR20117030157 A KR 20117030157A KR 101389165 B1 KR101389165 B1 KR 101389165B1
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South Korea
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methyl
cancer
compound
pharmaceutically acceptable
trifluoromethyl
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English (en)
Korean (ko)
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KR20120024783A (ko
Inventor
필립 아더 힙스킨드
바빈 쿠마르 파텔
윌슨 (니 다카쿠와), 다카코
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일라이 릴리 앤드 캄파니
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (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)
KR1020117030157A 2009-06-19 2010-06-15 이치환된 프탈라진 헤지호그 (hedgehog) 경로 길항제 Expired - Fee Related KR101389165B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21862809P 2009-06-19 2009-06-19
US61/218,628 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
KR20120024783A KR20120024783A (ko) 2012-03-14
KR101389165B1 true KR101389165B1 (ko) 2014-04-24

Family

ID=42332981

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020117030157A Expired - Fee Related KR101389165B1 (ko) 2009-06-19 2010-06-15 이치환된 프탈라진 헤지호그 (hedgehog) 경로 길항제

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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EA201071248A1 (ru) * 2008-04-29 2011-06-30 Эли Лилли Энд Компани Дизамещенные фталазиновые антагонисты пути hedgehog
NZ591945A (en) * 2008-11-03 2012-10-26 Lilly Co Eli Disubstituted phthalazine hedgehog pathway antagonists
BRPI0921782A2 (pt) 2008-11-17 2019-09-24 Lilly Co Eli antagonistas da via hedgehog de piridazina tetrassubstituída
AU2009314288B2 (en) * 2008-11-17 2013-05-02 Eli Lilly And Company Tetrasubstituted pyridazines hedgehog pathway antagonists
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
CA2829755A1 (en) 2011-03-23 2012-09-27 Semorex Technologies 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
US9814703B2 (en) 2013-11-14 2017-11-14 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
US10369147B2 (en) 2015-06-04 2019-08-06 PellePharm, Inc. Topical formulations for delivery of hedgehog inhibitor compounds and use thereof
EP3303289A4 (en) 2015-06-05 2018-11-14 Dana-Farber Cancer Institute, Inc. Compounds and methods for treating cancer
CN120661674A (zh) 2016-03-15 2025-09-19 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
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
EP3624798A1 (en) 2017-05-18 2020-03-25 Institut National de la Sante et de la Recherche Medicale (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
WO2022081661A1 (en) * 2020-10-13 2022-04-21 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 (3)

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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

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CA2237273C (en) 1996-01-15 2009-01-13 Janssen Pharmaceutica N.V. Angiogenesis inhibiting pyridazinamines
EP1067939B1 (en) 1998-04-09 2015-09-16 The Johns Hopkins University Use of steroidal alkaloid derivatives as inhibitors of hedgehog protein signaling pathways
GB0013674D0 (en) 1999-06-08 2000-07-26 Lorantis Ltd Therapeutic use
WO2003011219A2 (en) * 2001-07-27 2003-02-13 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
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
TW200533356A (en) 2004-02-24 2005-10-16 Mitsubishi Pharma Corp Fused pyridazine derivatives
US8338591B2 (en) 2004-05-08 2012-12-25 Novartis International Pharmaceutical Ltd. 3-aryl-5,6-disubstituted pyridazines
KR20170001725A (ko) 2004-09-02 2017-01-04 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
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
WO2009035568A1 (en) 2007-09-07 2009-03-19 Amgen Inc. Annelated pyridazines for the treatment of tumors driven by inappropriate hedgehog signalling
WO2009074300A2 (en) * 2007-12-13 2009-06-18 Siena Biotech S.P.A. Hedgehog pathway antagonists and therapeutic applications thereof
EA201071248A1 (ru) * 2008-04-29 2011-06-30 Эли Лилли Энд Компани Дизамещенные фталазиновые антагонисты пути hedgehog
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
EP2321298B1 (en) * 2008-08-04 2013-10-02 Amgen Inc. Aurora kinase modulators and methods of use
NZ591945A (en) 2008-11-03 2012-10-26 Lilly Co Eli Disubstituted phthalazine hedgehog pathway antagonists
BRPI0921782A2 (pt) 2008-11-17 2019-09-24 Lilly Co Eli antagonistas da via hedgehog de piridazina tetrassubstituída
AU2009314288B2 (en) 2008-11-17 2013-05-02 Eli Lilly And Company Tetrasubstituted pyridazines hedgehog pathway antagonists
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 (3)

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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

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Publication number Publication date
PT2443104E (pt) 2013-05-07
PL2443104T3 (pl) 2013-08-30
IL216599A0 (en) 2012-03-01
DOP2011000386A (es) 2012-02-29
HK1164872A1 (en) 2012-09-28
EP2443104B1 (en) 2013-04-17
WO2010147917A1 (en) 2010-12-23
HN2011003139A (es) 2013-07-29
HRP20130408T1 (en) 2013-06-30
SI2443104T1 (sl) 2013-07-31
IL216599A (en) 2015-09-24
TN2011000627A1 (en) 2013-05-24
CN102459233B (zh) 2014-07-02
AR077014A1 (es) 2011-07-27
AU2010260244A1 (en) 2012-01-19
JO2931B1 (en) 2015-09-15
SG177289A1 (en) 2012-02-28
MY156667A (en) 2016-03-15
EA019059B1 (ru) 2013-12-30
US8273742B2 (en) 2012-09-25
CA2764542C (en) 2013-09-10
TW201113268A (en) 2011-04-16
DK2443104T3 (da) 2013-05-06
EA201270049A1 (ru) 2012-05-30
PE20121050A1 (es) 2012-08-09
MX2011014029A (es) 2012-02-21
CL2011003147A1 (es) 2012-07-20
CO6480932A2 (es) 2012-07-16
CR20110658A (es) 2012-02-20
AU2010260244B2 (en) 2013-09-05
CN102459233A (zh) 2012-05-16
NZ596882A (en) 2013-08-30
EP2443104A1 (en) 2012-04-25
JP2012530705A (ja) 2012-12-06
MA33363B1 (fr) 2012-06-01
JP5596139B2 (ja) 2014-09-24
ECSP11011541A (es) 2012-01-31
ZA201108587B (en) 2013-05-29
CA2764542A1 (en) 2010-12-23
TWI385165B (zh) 2013-02-11
US20120316174A1 (en) 2012-12-13
ES2409054T3 (es) 2013-06-24
KR20120024783A (ko) 2012-03-14
BRPI1011601A2 (pt) 2016-03-22
US9000023B2 (en) 2015-04-07
UA106755C2 (uk) 2014-10-10
US20100324048A1 (en) 2010-12-23

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