CA2764542C - Disubstituted phthalazine hedgehog pathway antagonists - Google Patents

Disubstituted phthalazine hedgehog pathway antagonists Download PDF

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Publication number
CA2764542C
CA2764542C CA2764542A CA2764542A CA2764542C CA 2764542 C CA2764542 C CA 2764542C CA 2764542 A CA2764542 A CA 2764542A CA 2764542 A CA2764542 A CA 2764542A CA 2764542 C CA2764542 C CA 2764542C
Authority
CA
Canada
Prior art keywords
methyl
compound
piperidin
phthalazin
pyrazol
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2764542A
Other languages
English (en)
French (fr)
Other versions
CA2764542A1 (en
Inventor
Philip Arthur Hipskind
Bharvin Kumar Patel
Wilson (Nee Takakuwa), Takako
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CA2764542A1 publication Critical patent/CA2764542A1/en
Application granted granted Critical
Publication of CA2764542C publication Critical patent/CA2764542C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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)
CA2764542A 2009-06-19 2010-06-15 Disubstituted phthalazine hedgehog pathway antagonists Expired - Fee Related CA2764542C (en)

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
CA2764542A1 CA2764542A1 (en) 2010-12-23
CA2764542C true CA2764542C (en) 2013-09-10

Family

ID=42332981

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2764542A Expired - Fee Related CA2764542C (en) 2009-06-19 2010-06-15 Disubstituted phthalazine hedgehog pathway antagonists

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

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IN148482B (enExample) 1977-06-03 1981-03-07 Pfizer
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
ATE404200T1 (de) 2002-04-22 2008-08-15 Univ Johns Hopkins Med Modulatoren von hedgehog signalpfaden, zusammensetzungen und verwandte verwendungen
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
JP5550352B2 (ja) * 2007-03-15 2014-07-16 ノバルティス アーゲー 有機化合物およびその使用
AU2008269128B2 (en) * 2007-06-25 2012-08-02 Amgen Inc. Phthalazine compounds, compositions and methods of use
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

Also Published As

Publication number Publication date
PT2443104E (pt) 2013-05-07
KR101389165B1 (ko) 2014-04-24
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
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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Effective date: 20220301

MKLA Lapsed

Effective date: 20200831