TWI385165B - 經二取代之呔猬狀途徑拮抗劑 - Google Patents

經二取代之呔猬狀途徑拮抗劑 Download PDF

Info

Publication number
TWI385165B
TWI385165B TW099119158A TW99119158A TWI385165B TW I385165 B TWI385165 B TW I385165B TW 099119158 A TW099119158 A TW 099119158A TW 99119158 A TW99119158 A TW 99119158A TW I385165 B TWI385165 B TW I385165B
Authority
TW
Taiwan
Prior art keywords
cancer
methyl
pharmaceutically acceptable
acceptable salt
compound
Prior art date
Application number
TW099119158A
Other languages
English (en)
Chinese (zh)
Other versions
TW201113268A (en
Inventor
Philip Arthur Hipskind
Bharvin Kumar Patel
Takako Wilson
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of TW201113268A publication Critical patent/TW201113268A/zh
Application granted granted Critical
Publication of TWI385165B publication Critical patent/TWI385165B/zh

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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW099119158A 2009-06-19 2010-06-11 經二取代之呔猬狀途徑拮抗劑 TWI385165B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US21862809P 2009-06-19 2009-06-19

Publications (2)

Publication Number Publication Date
TW201113268A TW201113268A (en) 2011-04-16
TWI385165B true TWI385165B (zh) 2013-02-11

Family

ID=42332981

Family Applications (1)

Application Number Title Priority Date Filing Date
TW099119158A TWI385165B (zh) 2009-06-19 2010-06-11 經二取代之呔猬狀途徑拮抗劑

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 (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5442717B2 (ja) * 2008-04-29 2014-03-12 イーライ リリー アンド カンパニー 二置換フタラジンヘッジホッグ経路アンタゴニスト
CA2742539C (en) * 2008-11-03 2014-05-06 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists
EP2358703B1 (en) * 2008-11-17 2013-12-25 Eli Lilly and Company Tetrasubstituted pyridazines hedgehog pathway antagonists
DK2358698T3 (da) 2008-11-17 2012-10-08 Lilly Co Eli Tetrasubstitueret pyridazin som hedgehog-pathway antagonister
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
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
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
JP6796638B2 (ja) 2015-06-04 2020-12-09 ペレファーム, インク.Pellepharm, Inc. ヘッジホッグ阻害性化合物の送達のための局所的製剤及びその使用
CA2987067A1 (en) * 2015-06-05 2016-12-08 Dana-Farber Cancer Institute, Inc. Compounds and methods for treating cancer
WO2017157825A1 (en) 2016-03-15 2017-09-21 F. Hoffmann-La Roche Ag 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
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
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
JP2023546536A (ja) * 2020-10-13 2023-11-02 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
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008028689A1 (en) * 2006-09-07 2008-03-13 Bayer Schering Pharma Aktiengesellschaft N-(1-phthalazin-1-ylpiperidin-4-yl)amides as ep2 receptor modulators
TW200848414A (en) * 2007-03-15 2008-12-16 Novartis Ag Organic compounds and their uses
US20090048259A1 (en) * 2007-06-25 2009-02-19 Amgen Inc. Phthalazine compounds, compositions and methods of use

Family Cites Families (20)

* 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
AU768130B2 (en) 1998-04-09 2003-12-04 Johns Hopkins University School Of Medicine, The Use of steroidal alkaloid derivatives as inhibitors of hedgehog signaling pathways
ATE283700T1 (de) 1999-06-08 2004-12-15 Lorantis Ltd Therapeutische verwendung eines inhibitors des hedgehog signalübertragungsweges
AU2002327390B2 (en) * 2001-07-27 2008-06-26 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US7655674B2 (en) * 2002-04-22 2010-02-02 The Johns Hopkins University 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
WO2006004589A2 (en) 2004-05-08 2006-01-12 Neurogen Corporation 3-aryl-5,6-disubstituted pyridazines
AU2005282722C1 (en) 2004-09-02 2011-08-18 Curis, Inc. Pyridyl inhibitors of hedgehog signalling
EP2188283B1 (en) 2007-09-07 2012-08-15 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
JP5442717B2 (ja) 2008-04-29 2014-03-12 イーライ リリー アンド カンパニー 二置換フタラジンヘッジホッグ経路アンタゴニスト
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
ES2433469T3 (es) * 2008-08-04 2013-12-11 Amgen Inc. Moduladores de la aurora cinasa y métodos de uso
CA2742539C (en) 2008-11-03 2014-05-06 Eli Lilly And Company Disubstituted phthalazine hedgehog pathway antagonists
DK2358698T3 (da) 2008-11-17 2012-10-08 Lilly Co Eli Tetrasubstitueret pyridazin som hedgehog-pathway antagonister
EP2358703B1 (en) 2008-11-17 2013-12-25 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008028689A1 (en) * 2006-09-07 2008-03-13 Bayer Schering Pharma Aktiengesellschaft N-(1-phthalazin-1-ylpiperidin-4-yl)amides as ep2 receptor modulators
TW200848414A (en) * 2007-03-15 2008-12-16 Novartis Ag Organic compounds and their uses
US20090048259A1 (en) * 2007-06-25 2009-02-19 Amgen Inc. Phthalazine compounds, compositions and methods of use

Also Published As

Publication number Publication date
AU2010260244A1 (en) 2012-01-19
ECSP11011541A (es) 2012-01-31
HK1164872A1 (en) 2012-09-28
CA2764542A1 (en) 2010-12-23
ES2409054T3 (es) 2013-06-24
AR077014A1 (es) 2011-07-27
TN2011000627A1 (en) 2013-05-24
US8273742B2 (en) 2012-09-25
MY156667A (en) 2016-03-15
WO2010147917A1 (en) 2010-12-23
IL216599A (en) 2015-09-24
JP5596139B2 (ja) 2014-09-24
MX2011014029A (es) 2012-02-21
KR101389165B1 (ko) 2014-04-24
EA201270049A1 (ru) 2012-05-30
NZ596882A (en) 2013-08-30
EP2443104B1 (en) 2013-04-17
CR20110658A (es) 2012-02-20
SI2443104T1 (sl) 2013-07-31
HN2011003139A (es) 2013-07-29
TW201113268A (en) 2011-04-16
ZA201108587B (en) 2013-05-29
HRP20130408T1 (en) 2013-06-30
US20100324048A1 (en) 2010-12-23
CL2011003147A1 (es) 2012-07-20
EP2443104A1 (en) 2012-04-25
CA2764542C (en) 2013-09-10
US9000023B2 (en) 2015-04-07
JP2012530705A (ja) 2012-12-06
US20120316174A1 (en) 2012-12-13
CO6480932A2 (es) 2012-07-16
UA106755C2 (uk) 2014-10-10
BRPI1011601A2 (pt) 2016-03-22
AU2010260244B2 (en) 2013-09-05
MA33363B1 (fr) 2012-06-01
DK2443104T3 (da) 2013-05-06
DOP2011000386A (es) 2012-02-29
PE20121050A1 (es) 2012-08-09
SG177289A1 (en) 2012-02-28
PL2443104T3 (pl) 2013-08-30
IL216599A0 (en) 2012-03-01
PT2443104E (pt) 2013-05-07
EA019059B1 (ru) 2013-12-30
KR20120024783A (ko) 2012-03-14
CN102459233A (zh) 2012-05-16
CN102459233B (zh) 2014-07-02
JO2931B1 (en) 2015-09-15

Similar Documents

Publication Publication Date Title
TWI385165B (zh) 經二取代之呔猬狀途徑拮抗劑
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
KR101335746B1 (ko) 이치환된 프탈라진 헷지호그 경로 길항제
WO2009134574A2 (en) Disubstituted phthalazine hedgehog pathway antagonists
ES2446307T3 (es) Piridazinas tetrasustituidas antagonistas de la ruta de Hedgehog
HK1164872B (en) Disubstituted phthalazine hedgehog pathway antagonists

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees