JP5596139B2 - 二置換フタラジンヘッジホッグ経路アンタゴニスト - Google Patents

二置換フタラジンヘッジホッグ経路アンタゴニスト Download PDF

Info

Publication number
JP5596139B2
JP5596139B2 JP2012516178A JP2012516178A JP5596139B2 JP 5596139 B2 JP5596139 B2 JP 5596139B2 JP 2012516178 A JP2012516178 A JP 2012516178A JP 2012516178 A JP2012516178 A JP 2012516178A JP 5596139 B2 JP5596139 B2 JP 5596139B2
Authority
JP
Japan
Prior art keywords
methyl
cancer
pharmaceutically acceptable
trifluoromethyl
fluoro
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.)
Active
Application number
JP2012516178A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012530705A (ja
JP2012530705A5 (enExample
Inventor
フィリップ・アーサー・ヒップスカインド
バービン・クマー・ペイテル
ウィルソン貴子
Original Assignee
イーライ リリー アンド カンパニー
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 イーライ リリー アンド カンパニー filed Critical イーライ リリー アンド カンパニー
Publication of JP2012530705A publication Critical patent/JP2012530705A/ja
Publication of JP2012530705A5 publication Critical patent/JP2012530705A5/ja
Application granted granted Critical
Publication of JP5596139B2 publication Critical patent/JP5596139B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
JP2012516178A 2009-06-19 2010-06-15 二置換フタラジンヘッジホッグ経路アンタゴニスト Active JP5596139B2 (ja)

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 (3)

Publication Number Publication Date
JP2012530705A JP2012530705A (ja) 2012-12-06
JP2012530705A5 JP2012530705A5 (enExample) 2014-07-17
JP5596139B2 true JP5596139B2 (ja) 2014-09-24

Family

ID=42332981

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012516178A Active JP5596139B2 (ja) 2009-06-19 2010-06-15 二置換フタラジンヘッジホッグ経路アンタゴニスト

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)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102066353B (zh) * 2008-04-29 2013-12-11 伊莱利利公司 二取代的酞嗪Hedgehog通路拮抗剂
ES2418479T3 (es) * 2008-11-03 2013-08-14 Eli Lilly And Company Antagonistas de la ruta erizo de ftalazinas disustituidas
MX2011005177A (es) 2008-11-17 2011-05-30 Lilly Co Eli Antagonistas de la trayectoria hedgehog de piridazinas tetrasustituidas.
JP5518088B2 (ja) * 2008-11-17 2014-06-11 イーライ リリー アンド カンパニー 四置換ピリダジンヘッジホッグ経路アンタゴニスト
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
EP2688565A1 (en) 2011-03-23 2014-01-29 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
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
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
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
BR112017026103B1 (pt) 2015-06-04 2023-10-03 Sol-Gel Technologies Ltd Composições tópicas com composto inibidor de hedgehog, sistema de entrega tópica e seus usos
AU2016271432A1 (en) * 2015-06-05 2017-12-07 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
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
EP4173639A4 (en) 2020-06-26 2024-03-13 RaQualia Pharma Inc. METHOD FOR SELECTING A CANCER PATIENT FOR WHICH COMBINATION THERAPY OF A RETINOID AND A CANCER TREATMENT AGENT WILL BE EFFECTIVE, AND COMBINATION DRUG OF A RETINOID AND A CANCER TREATMENT AGENT
US12605377B2 (en) 2020-10-13 2026-04-21 Endeavor Biomedicines, Inc. Methods of treating fibrosis
JP7868066B2 (ja) * 2020-10-13 2026-06-01 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
US12447148B2 (en) 2024-03-05 2025-10-21 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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN148482B (enExample) * 1977-06-03 1981-03-07 Pfizer
AU717744B2 (en) 1996-01-15 2000-03-30 Janssen Pharmaceutica N.V. Angiogenesis inhibiting pyridazinamines
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
GB0013674D0 (en) 1999-06-08 2000-07-26 Lorantis Ltd Therapeutic use
EA007339B1 (ru) * 2001-07-27 2006-08-25 Кьюэрис, Инк. Медиаторы путей передачи сигналов генами hedgehog, содержащие их композиции и способы применения указанных веществ
AU2003231032B2 (en) * 2002-04-22 2008-07-10 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
WO2005080378A1 (ja) 2004-02-24 2005-09-01 Mitsubishi Pharma Corporation 縮合ピリダジン誘導体
EP1745039A4 (en) 2004-05-08 2009-07-22 Neurogen Corp 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES
WO2006028958A2 (en) 2004-09-02 2006-03-16 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
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
US8536168B2 (en) * 2007-03-15 2013-09-17 Novartis Ag Benzyl and pyridinyl derivatives as modulators of the hedgehog signaling pathway
US8153633B2 (en) * 2007-06-25 2012-04-10 Amgen Inc. Phthalazine compounds, compositions and methods of use
AU2008300019A1 (en) 2007-09-07 2009-03-19 Amgen Inc. Annelated pyridazines for the treatment of tumors driven by inappropriate hedgehog signalling
CA2709203A1 (en) * 2007-12-13 2009-06-18 Siena Biotech S.P.A. Hedgehog pathway antagonists and therapeutic applications thereof
CN102066353B (zh) * 2008-04-29 2013-12-11 伊莱利利公司 二取代的酞嗪Hedgehog通路拮抗剂
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
CA2732101C (en) * 2008-08-04 2013-09-17 Amgen Inc. Aurora kinase modulators and methods of use
ES2418479T3 (es) 2008-11-03 2013-08-14 Eli Lilly And Company Antagonistas de la ruta erizo de ftalazinas disustituidas
JP5518088B2 (ja) 2008-11-17 2014-06-11 イーライ リリー アンド カンパニー 四置換ピリダジンヘッジホッグ経路アンタゴニスト
MX2011005177A (es) 2008-11-17 2011-05-30 Lilly Co Eli Antagonistas de la trayectoria hedgehog de piridazinas tetrasustituidas.
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
WO2010147917A1 (en) 2010-12-23
JP2012530705A (ja) 2012-12-06
ZA201108587B (en) 2013-05-29
AU2010260244B2 (en) 2013-09-05
CA2764542C (en) 2013-09-10
SG177289A1 (en) 2012-02-28
TW201113268A (en) 2011-04-16
ES2409054T3 (es) 2013-06-24
JO2931B1 (en) 2015-09-15
MY156667A (en) 2016-03-15
SI2443104T1 (sl) 2013-07-31
DOP2011000386A (es) 2012-02-29
HRP20130408T1 (en) 2013-06-30
CA2764542A1 (en) 2010-12-23
CR20110658A (es) 2012-02-20
IL216599A (en) 2015-09-24
CL2011003147A1 (es) 2012-07-20
NZ596882A (en) 2013-08-30
EP2443104A1 (en) 2012-04-25
AU2010260244A1 (en) 2012-01-19
DK2443104T3 (da) 2013-05-06
UA106755C2 (uk) 2014-10-10
US8273742B2 (en) 2012-09-25
CO6480932A2 (es) 2012-07-16
TN2011000627A1 (en) 2013-05-24
MA33363B1 (fr) 2012-06-01
US20120316174A1 (en) 2012-12-13
EA201270049A1 (ru) 2012-05-30
PE20121050A1 (es) 2012-08-09
ECSP11011541A (es) 2012-01-31
HN2011003139A (es) 2013-07-29
KR101389165B1 (ko) 2014-04-24
PL2443104T3 (pl) 2013-08-30
US9000023B2 (en) 2015-04-07
BRPI1011601A2 (pt) 2016-03-22
CN102459233A (zh) 2012-05-16
EP2443104B1 (en) 2013-04-17
US20100324048A1 (en) 2010-12-23
EA019059B1 (ru) 2013-12-30
TWI385165B (zh) 2013-02-11
MX2011014029A (es) 2012-02-21
KR20120024783A (ko) 2012-03-14
PT2443104E (pt) 2013-05-07
CN102459233B (zh) 2014-07-02
HK1164872A1 (en) 2012-09-28
IL216599A0 (en) 2012-03-01
AR077014A1 (es) 2011-07-27

Similar Documents

Publication Publication Date Title
EP2443104B1 (en) Disubstituted phthalazine hedgehog pathway antagonists
JP5518887B2 (ja) 四置換ピリダジンヘッジホッグ経路アンタゴニスト
KR101260116B1 (ko) 이치환된 프탈라진 헤지호그 경로 길항제
KR101335746B1 (ko) 이치환된 프탈라진 헷지호그 경로 길항제
JP5518088B2 (ja) 四置換ピリダジンヘッジホッグ経路アンタゴニスト
HK1164872B (en) Disubstituted phthalazine hedgehog pathway antagonists
HK1122025B (en) 4-(3-benzoylaminophenyl)-6,7-dimethoxy-2- methylaminoquinazoline derivative

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130614

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130614

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140527

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140708

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140806

R150 Certificate of patent or registration of utility model

Ref document number: 5596139

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250