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)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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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KR101260116B1 (ko) * 2008-04-29 2013-05-02 일라이 릴리 앤드 캄파니 이치환된 프탈라진 헤지호그 경로 길항제
CA2742539C (en) * 2008-11-03 2014-05-06 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists
ES2392759T3 (es) 2008-11-17 2012-12-13 Eli Lilly And Company Piridazina tetrasustituida como antagonistas de la vía Hedgehog.
EA018372B1 (ru) * 2008-11-17 2013-07-30 Эли Лилли Энд Компани Тетразамещенные пиридазины в качестве антагонистов пути hedgehog
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
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
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
CA2988289C (en) 2015-06-04 2023-12-05 PellePharm, Inc. Topical formulations for delivery of hedgehog inhibitor compounds and use thereof
AU2016271432A1 (en) * 2015-06-05 2017-12-07 Dana-Farber Cancer Institute, Inc. Compounds and methods for treating cancer
AU2017233898B2 (en) 2016-03-15 2022-12-15 Oryzon Genomics, S.A. Combinations of LSD1 inhibitors for use in the treatment of solid tumors
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
WO2018211007A1 (en) 2017-05-18 2018-11-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of mast cell diseases
CA3184767A1 (en) 2020-06-26 2021-12-30 Raqualia Pharma Inc. Method for selecting cancer patients for whom combination therapy with retinoid and cancer therapeutic agent is effective, and combination medicament with retinoid and cancer therapeutic agent
KR20230107568A (ko) * 2020-10-13 2023-07-17 엔데버 바이오메디신스, 인크. 섬유증 치료 방법
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

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IN148482B (enExample) 1977-06-03 1981-03-07 Pfizer
MY117098A (en) 1996-01-15 2004-05-31 Janssen Pharmaceutica Nv Angiogenesis inhibiting pyridazinamines
WO1999052534A1 (en) 1998-04-09 1999-10-21 Johns Hopkins University School Of Medicine Use of steroidal alkaloid derivatives as inhibitors of hedgehog signaling pathways
GB0013674D0 (en) 1999-06-08 2000-07-26 Lorantis Ltd Therapeutic use
US8354397B2 (en) * 2001-07-27 2013-01-15 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
EP1997494A3 (en) * 2002-04-22 2009-06-10 Johns Hopkins University School of Medicine Modulators of hedgehog signaling pathways, compositions and uses related thereto
AU2003265853A1 (en) 2002-08-29 2004-03-19 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
JP5221952B2 (ja) 2004-05-08 2013-06-26 ノバルティス・インターナショナル・ファーマシューティカル・リミテッド 3−アリール−5,6−ジ置換ピリダジン類
KR20150002863A (ko) 2004-09-02 2015-01-07 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
DK2137162T3 (en) * 2007-03-15 2018-11-26 Novartis Ag Organic compounds and their applications
CA2690378A1 (en) * 2007-06-25 2008-12-31 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
EA017918B1 (ru) * 2007-12-13 2013-04-30 СИЕНА БИОТЕК С.п.А. Антагонисты пути hedgehog и их терапевтические применения
KR101260116B1 (ko) 2008-04-29 2013-05-02 일라이 릴리 앤드 캄파니 이치환된 프탈라진 헤지호그 경로 길항제
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
WO2010017240A2 (en) * 2008-08-04 2010-02-11 Amgen Inc. Aurora kinase modulators and methods of use
CA2742539C (en) 2008-11-03 2014-05-06 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists
ES2392759T3 (es) 2008-11-17 2012-12-13 Eli Lilly And Company Piridazina tetrasustituida como antagonistas de la vía Hedgehog.
EA018372B1 (ru) 2008-11-17 2013-07-30 Эли Лилли Энд Компани Тетразамещенные пиридазины в качестве антагонистов пути hedgehog
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
KR20120024783A (ko) 2012-03-14
MA33363B1 (fr) 2012-06-01
MY156667A (en) 2016-03-15
DOP2011000386A (es) 2012-02-29
BRPI1011601A2 (pt) 2016-03-22
SG177289A1 (en) 2012-02-28
US20120316174A1 (en) 2012-12-13
AU2010260244B2 (en) 2013-09-05
SI2443104T1 (sl) 2013-07-31
JP5596139B2 (ja) 2014-09-24
PT2443104E (pt) 2013-05-07
PL2443104T3 (pl) 2013-08-30
IL216599A (en) 2015-09-24
JP2012530705A (ja) 2012-12-06
HRP20130408T1 (en) 2013-06-30
ZA201108587B (en) 2013-05-29
EA201270049A1 (ru) 2012-05-30
TW201113268A (en) 2011-04-16
JO2931B1 (en) 2015-09-15
US9000023B2 (en) 2015-04-07
TWI385165B (zh) 2013-02-11
CN102459233A (zh) 2012-05-16
IL216599A0 (en) 2012-03-01
WO2010147917A1 (en) 2010-12-23
PE20121050A1 (es) 2012-08-09
ES2409054T3 (es) 2013-06-24
AU2010260244A1 (en) 2012-01-19
EP2443104A1 (en) 2012-04-25
KR101389165B1 (ko) 2014-04-24
TN2011000627A1 (en) 2013-05-24
US20100324048A1 (en) 2010-12-23
EA019059B1 (ru) 2013-12-30
AR077014A1 (es) 2011-07-27
NZ596882A (en) 2013-08-30
CN102459233B (zh) 2014-07-02
US8273742B2 (en) 2012-09-25
EP2443104B1 (en) 2013-04-17
MX2011014029A (es) 2012-02-21
CR20110658A (es) 2012-02-20
ECSP11011541A (es) 2012-01-31
CL2011003147A1 (es) 2012-07-20
CA2764542A1 (en) 2010-12-23
HN2011003139A (es) 2013-07-29
HK1164872A1 (en) 2012-09-28
CO6480932A2 (es) 2012-07-16
DK2443104T3 (da) 2013-05-06
UA106755C2 (uk) 2014-10-10

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EEER Examination request
MKLA Lapsed

Effective date: 20220301

MKLA Lapsed

Effective date: 20200831