CN102202737B - 二取代的2,3-二氮杂萘hedgehog通路拮抗剂 - Google Patents

二取代的2,3-二氮杂萘hedgehog通路拮抗剂 Download PDF

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Publication number
CN102202737B
CN102202737B CN200980143394.3A CN200980143394A CN102202737B CN 102202737 B CN102202737 B CN 102202737B CN 200980143394 A CN200980143394 A CN 200980143394A CN 102202737 B CN102202737 B CN 102202737B
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China
Prior art keywords
compound
cancer
pharmacology
acceptable salt
hydrogen
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Expired - Fee Related
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CN200980143394.3A
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English (en)
Chinese (zh)
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CN102202737A (zh
Inventor
J·A·巴斯蒂安
P·A·希普斯金
D·J·萨尔
T·威尔逊
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Eli Lilly and Co
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Eli Lilly and Co
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN102202737A publication Critical patent/CN102202737A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K31/495Heterocyclic 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
    • A61P35/00Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN200980143394.3A 2008-11-03 2009-10-22 二取代的2,3-二氮杂萘hedgehog通路拮抗剂 Expired - Fee Related CN102202737B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US11070308P 2008-11-03 2008-11-03
US61/110703 2008-11-03
US61/110,703 2008-11-03
PCT/US2009/061573 WO2010062507A1 (en) 2008-11-03 2009-10-22 Disubstituted phthalazine hedgehog pathway antagonists

Publications (2)

Publication Number Publication Date
CN102202737A CN102202737A (zh) 2011-09-28
CN102202737B true CN102202737B (zh) 2014-03-26

Family

ID=41566219

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980143394.3A Expired - Fee Related CN102202737B (zh) 2008-11-03 2009-10-22 二取代的2,3-二氮杂萘hedgehog通路拮抗剂

Country Status (29)

Country Link
US (1) US8404687B2 (enExample)
EP (1) EP2364185B1 (enExample)
JP (1) JP2012507535A (enExample)
KR (1) KR101335746B1 (enExample)
CN (1) CN102202737B (enExample)
AU (1) AU2009320251C1 (enExample)
BR (1) BRPI0921437A2 (enExample)
CA (1) CA2742539C (enExample)
CL (1) CL2011000979A1 (enExample)
CO (1) CO6382123A2 (enExample)
CR (1) CR20110202A (enExample)
CY (1) CY1114023T1 (enExample)
DK (1) DK2364185T3 (enExample)
EA (1) EA018931B1 (enExample)
EC (1) ECSP11011021A (enExample)
ES (1) ES2418479T3 (enExample)
HR (1) HRP20130527T1 (enExample)
IL (1) IL211841A0 (enExample)
MA (1) MA32726B1 (enExample)
MX (1) MX2011004683A (enExample)
NZ (1) NZ591945A (enExample)
PE (1) PE20110433A1 (enExample)
PL (1) PL2364185T3 (enExample)
PT (1) PT2364185E (enExample)
SI (1) SI2364185T1 (enExample)
TN (1) TN2011000166A1 (enExample)
UA (1) UA102115C2 (enExample)
WO (1) WO2010062507A1 (enExample)
ZA (1) ZA201102448B (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
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
WO2022081661A1 (en) 2020-10-13 2022-04-21 Endeavor Biomedicines, Inc. Methods of treating fibrosis
IL319619A (en) * 2022-09-23 2025-05-01 Merck Sharp & Dohme Llc Phthalazine derivatives used as NOD-LIKE PROTEIN 3 receptor inhibitors
WO2025188802A1 (en) 2024-03-05 2025-09-12 Endeavor Biomedicines, Inc. Methods of improving lung function

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005033288A2 (en) * 2003-09-29 2005-04-14 The Johns Hopkins University Hedgehog pathway antagonists
WO2006028958A2 (en) * 2004-09-02 2006-03-16 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
WO2008110611A1 (en) * 2007-03-15 2008-09-18 Novartis Ag Organic compounds and their uses

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1293565A (en) 1969-05-03 1972-10-18 Aspro Nicholas Ltd Aminophthalazines and pharmaceutical compositions thereof
CA2237273C (en) 1996-01-15 2009-01-13 Janssen Pharmaceutica N.V. Angiogenesis inhibiting pyridazinamines
AU719392B2 (en) * 1996-10-01 2000-05-11 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing heterocyclic compounds
US6432970B2 (en) 1998-04-09 2002-08-13 Johns Hopkins University School Of Medicine Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
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
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
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
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
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
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
AU2009314288B2 (en) 2008-11-17 2013-05-02 Eli Lilly And Company Tetrasubstituted pyridazines hedgehog pathway antagonists
BRPI0921782A2 (pt) 2008-11-17 2019-09-24 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005033288A2 (en) * 2003-09-29 2005-04-14 The Johns Hopkins University Hedgehog pathway antagonists
WO2006028958A2 (en) * 2004-09-02 2006-03-16 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
WO2008110611A1 (en) * 2007-03-15 2008-09-18 Novartis Ag Organic compounds and their uses

Also Published As

Publication number Publication date
TN2011000166A1 (en) 2012-12-17
HRP20130527T1 (en) 2013-07-31
CO6382123A2 (es) 2012-02-15
CR20110202A (es) 2011-06-09
DK2364185T3 (da) 2013-06-03
KR20110066212A (ko) 2011-06-16
AU2009320251C1 (en) 2013-08-15
CL2011000979A1 (es) 2011-10-07
WO2010062507A1 (en) 2010-06-03
AU2009320251A1 (en) 2010-06-03
CA2742539A1 (en) 2010-06-03
JP2012507535A (ja) 2012-03-29
HK1159010A1 (en) 2012-07-27
EA201170640A1 (ru) 2011-12-30
US8404687B2 (en) 2013-03-26
ECSP11011021A (es) 2011-06-30
MX2011004683A (es) 2011-06-20
US20110190304A1 (en) 2011-08-04
CY1114023T1 (el) 2016-07-27
EP2364185A1 (en) 2011-09-14
EP2364185B1 (en) 2013-05-22
NZ591945A (en) 2012-10-26
CN102202737A (zh) 2011-09-28
AU2009320251B2 (en) 2013-01-24
KR101335746B1 (ko) 2013-12-12
SI2364185T1 (sl) 2013-07-31
PT2364185E (pt) 2013-07-24
PE20110433A1 (es) 2011-07-09
MA32726B1 (fr) 2011-10-02
UA102115C2 (ru) 2013-06-10
PL2364185T3 (pl) 2013-10-31
ES2418479T3 (es) 2013-08-14
EA018931B1 (ru) 2013-11-29
CA2742539C (en) 2014-05-06
BRPI0921437A2 (pt) 2018-10-30
ZA201102448B (en) 2012-09-26
IL211841A0 (en) 2011-06-30

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