CN102216285B - 四取代的哒嗪hedgehog途径拮抗剂 - Google Patents

四取代的哒嗪hedgehog途径拮抗剂 Download PDF

Info

Publication number: CN102216285B
Authority: CN; China
Prior art keywords: compound; cancer; pharmaceutically acceptable; methyl; trifluoromethyl
Prior art date: 2008-11-17
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

CN200980145554.8A

Other languages

English (en)

Chinese (zh)

Other versions

CN102216285A (zh

Inventor

J·A·巴斯蒂安

J·M·克雷

J·D·科恩

P·A·希普斯金德

K·L·洛伯

D·J·萨尔

T·威尔森(尼高桑)

M·L·汤普森

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.)

2008-11-17

Filing date

2009-11-05

Publication date

2014-08-13

2009-11-05 Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co

2011-10-12 Publication of CN102216285A publication Critical patent/CN102216285A/zh

2014-08-13 Application granted granted Critical

2014-08-13 Publication of CN102216285B publication Critical patent/CN102216285B/zh

Status Expired - Fee Related legal-status Critical Current

2029-11-05 Anticipated expiration legal-status Critical

Links

UVGQDKASMXFUKZ-UHFFFAOYSA-N CC(C)(C)OC(N(C)C(CC1)CCN1c(nn1)c(C)c(C)c1Cl)=O Chemical compound CC(C)(C)OC(N(C)C(CC1)CCN1c(nn1)c(C)c(C)c1Cl)=O UVGQDKASMXFUKZ-UHFFFAOYSA-N 0.000 description 1
VYXIHSAEOXPAEY-UHFFFAOYSA-N CCOC(c1c[nH]nc1C(F)(F)F)=O Chemical compound CCOC(c1c[nH]nc1C(F)(F)F)=O VYXIHSAEOXPAEY-UHFFFAOYSA-N 0.000 description 1
FGQLCONVJIPCBG-UHFFFAOYSA-N CCOC(c1c[n](Cc(cc2)ccc2OC)nc1C(F)(F)F)=O Chemical compound CCOC(c1c[n](Cc(cc2)ccc2OC)nc1C(F)(F)F)=O FGQLCONVJIPCBG-UHFFFAOYSA-N 0.000 description 1
KWSNDYYVWNDCJT-UHFFFAOYSA-N COc1ccc(C[n]2nc(C(F)(F)F)c(C(O)=O)c2)cc1 Chemical compound COc1ccc(C[n]2nc(C(F)(F)F)c(C(O)=O)c2)cc1 KWSNDYYVWNDCJT-UHFFFAOYSA-N 0.000 description 1
QCFSVDFDHTXNSC-UHFFFAOYSA-N Cc1c(-c(cc2)ccc2C#N)nnc(N(CC2)CCC2N(C)C(c2c(C(F)(F)F)nccc2)=O)c1C Chemical compound Cc1c(-c(cc2)ccc2C#N)nnc(N(CC2)CCC2N(C)C(c2c(C(F)(F)F)nccc2)=O)c1C QCFSVDFDHTXNSC-UHFFFAOYSA-N 0.000 description 1
UPKAWXPCGXNWEM-UHFFFAOYSA-N Cc1c(-c(cc2)ccc2F)nnc(N(CC2)CCC2NC)c1C Chemical compound Cc1c(-c(cc2)ccc2F)nnc(N(CC2)CCC2NC)c1C UPKAWXPCGXNWEM-UHFFFAOYSA-N 0.000 description 1

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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
- 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
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)

CN200980145554.8A 2008-11-17 2009-11-05 四取代的哒嗪hedgehog途径拮抗剂 Expired - Fee Related CN102216285B (zh)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US11533208P	2008-11-17	2008-11-17
US61/115,332		2008-11-17
PCT/US2009/063370 WO2010056588A1 (en)	2008-11-17	2009-11-05	Tetrasubstituted pyridazine hedgehog pathway antagonists

Publications (2)

Publication Number	Publication Date
CN102216285A CN102216285A (zh)	2011-10-12
CN102216285B true CN102216285B (zh)	2014-08-13

Family

ID=41722877

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CN200980145554.8A Expired - Fee Related CN102216285B (zh)	2008-11-17	2009-11-05	四取代的哒嗪hedgehog途径拮抗剂

Country Status (18)

Country	Link
US (1)	US8507490B2 (2)
EP (1)	EP2358698B1 (2)
JP (1)	JP5518887B2 (2)
KR (1)	KR101342184B1 (2)
CN (1)	CN102216285B (2)
AU (1)	AU2009314349B2 (2)
BR (1)	BRPI0921782A2 (2)
CA (1)	CA2743483C (2)
CY (1)	CY1113377T1 (2)
DK (1)	DK2358698T3 (2)
EA (1)	EA017386B1 (2)
ES (1)	ES2392759T3 (2)
HR (1)	HRP20120762T1 (2)
MX (1)	MX2011005177A (2)
PL (1)	PL2358698T3 (2)
PT (1)	PT2358698E (2)
SI (1)	SI2358698T1 (2)
WO (1)	WO2010056588A1 (2)

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Publication number	Priority date	Publication date	Assignee	Title
TW200817354A (en) *	2006-07-17	2008-04-16	Syngenta Participations Ag	Novel pyridazine derivatives
UA102250C2 (ru)	2008-04-29	2013-06-25	Эли Лилли Энд Компани	Двухзамещенные фталазины - антагонисты проводящего пути hedgehog
MX2011004683A (es)	2008-11-03	2011-06-20	Lilly Co Eli	Antagonistas de la via hedgehog de ftalazina disustituida.
BRPI0921777A2 (pt)	2008-11-17	2016-01-12	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
GB201309508D0 (en) *	2013-05-28	2013-07-10	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
GB2528298A (en) *	2014-07-16	2016-01-20	Redx Pharma Plc	Compounds
CN105130980B (zh) *	2015-09-09	2018-05-22	沈阳药科大学	N-3-苯并咪唑噻唑胺类衍生物及其制备方法与应用
CN107163028B (zh) *	2017-05-24	2019-07-12	东南大学	一种苯甲酰胺类Hedgehog抑制剂及其制备方法和应用
CN110208424A (zh) *	2019-06-28	2019-09-06	江苏恒生检测有限公司	一种农药氟啶虫酰胺中含有杂质的分析方法
WO2021071981A1 (en) *	2019-10-08	2021-04-15	Skyhawk Therapeutics, Inc.	Compounds for modulating splicing
US12605377B2 (en)	2020-10-13	2026-04-21	Endeavor Biomedicines, Inc.	Methods of treating fibrosis
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
WO2023034836A1 (en) *	2021-08-30	2023-03-09	Remix Therapeutics Inc.	Compounds and methods for modulating splicing
WO2025188802A1 (en)	2024-03-05	2025-09-12	Endeavor Biomedicines, Inc.	Methods of improving lung function

Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2008110611A1 (en) *	2007-03-15	2008-09-18	Novartis Ag	Organic compounds and their uses

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GB1293565A (en)	1969-05-03	1972-10-18	Aspro Nicholas Ltd	Aminophthalazines and pharmaceutical compositions thereof
MY117098A (en)	1996-01-15	2004-05-31	Janssen Pharmaceutica Nv	Angiogenesis inhibiting pyridazinamines
US6432970B2 (en)	1998-04-09	2002-08-13	Johns Hopkins University School Of Medicine	Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
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
ATE283700T1 (de)	1999-06-08	2004-12-15	Lorantis Ltd	Therapeutische verwendung eines inhibitors des hedgehog signalübertragungsweges
EP1496905B1 (en)	2002-04-22	2008-08-13	Johns Hopkins University School of Medicine	Modulators of hedgehog signaling pathways, compositions and uses related thereto
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
WO2006004589A2 (en)	2004-05-08	2006-01-12	Neurogen Corporation	3-aryl-5,6-disubstituted pyridazines
ES2377430T3 (es)	2004-09-02	2012-03-27	Genentech, Inc.	Inhibidores piridílicos de la señalización de hedgehog
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
US8153633B2 (en)	2007-06-25	2012-04-10	Amgen Inc.	Phthalazine compounds, compositions and methods of use
US8222251B2 (en)	2007-09-07	2012-07-17	Amgen Inc.	Pyridopyridazine compounds, compositions and methods of use
UA102250C2 (ru)	2008-04-29	2013-06-25	Эли Лилли Энд Компани	Двухзамещенные фталазины - антагонисты проводящего пути hedgehog
US20100041663A1 (en)	2008-07-18	2010-02-18	Novartis Ag	Organic Compounds as Smo Inhibitors
MX2011004683A (es)	2008-11-03	2011-06-20	Lilly Co Eli	Antagonistas de la via hedgehog de ftalazina disustituida.
BRPI0921777A2 (pt)	2008-11-17	2016-01-12	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

2009
- 2009-11-05 KR KR1020117011148A patent/KR101342184B1/ko not_active Expired - Fee Related
- 2009-11-05 CA CA2743483A patent/CA2743483C/en not_active Expired - Fee Related
- 2009-11-05 EA EA201170699A patent/EA017386B1/ru not_active IP Right Cessation
- 2009-11-05 HR HRP20120762AT patent/HRP20120762T1/hr unknown
- 2009-11-05 DK DK09752059.7T patent/DK2358698T3/da active
- 2009-11-05 PT PT09752059T patent/PT2358698E/pt unknown
- 2009-11-05 JP JP2011536395A patent/JP5518887B2/ja not_active Expired - Fee Related
- 2009-11-05 MX MX2011005177A patent/MX2011005177A/es active IP Right Grant
- 2009-11-05 SI SI200930351T patent/SI2358698T1/sl unknown
- 2009-11-05 ES ES09752059T patent/ES2392759T3/es active Active
- 2009-11-05 US US13/122,216 patent/US8507490B2/en not_active Expired - Fee Related
- 2009-11-05 PL PL09752059T patent/PL2358698T3/pl unknown
- 2009-11-05 CN CN200980145554.8A patent/CN102216285B/zh not_active Expired - Fee Related
- 2009-11-05 WO PCT/US2009/063370 patent/WO2010056588A1/en not_active Ceased
- 2009-11-05 BR BRPI0921782A patent/BRPI0921782A2/pt not_active IP Right Cessation
- 2009-11-05 EP EP09752059A patent/EP2358698B1/en not_active Not-in-force
- 2009-11-05 AU AU2009314349A patent/AU2009314349B2/en not_active Ceased
2012
- 2012-10-25 CY CY20121101019T patent/CY1113377T1/el unknown

Patent Citations (1)

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Publication number	Priority date	Publication date	Assignee	Title
WO2008110611A1 (en) *	2007-03-15	2008-09-18	Novartis Ag	Organic compounds and their uses

Also Published As

Publication number	Publication date
US20110263602A1 (en)	2011-10-27
PT2358698E (pt)	2012-10-24
EA201170699A1 (ru)	2011-12-30
MX2011005177A (es)	2011-05-30
AU2009314349B2 (en)	2013-04-18
BRPI0921782A2 (pt)	2019-09-24
KR101342184B1 (ko)	2013-12-19
EA017386B1 (ru)	2012-12-28
WO2010056588A1 (en)	2010-05-20
JP5518887B2 (ja)	2014-06-11
EP2358698A1 (en)	2011-08-24
JP2012509263A (ja)	2012-04-19
ES2392759T3 (es)	2012-12-13
CA2743483A1 (en)	2010-05-20
PL2358698T3 (pl)	2013-01-31
CN102216285A (zh)	2011-10-12
SI2358698T1 (sl)	2012-11-30
CY1113377T1 (el)	2016-06-22
DK2358698T3 (da)	2012-10-08
CA2743483C (en)	2014-03-11
KR20110070920A (ko)	2011-06-24
EP2358698B1 (en)	2012-09-05
AU2009314349A1 (en)	2010-05-20
HRP20120762T1 (hr)	2012-10-31
US8507490B2 (en)	2013-08-13

Legal Events

Date	Code	Title	Description
2011-10-12	C06	Publication
2011-10-12	PB01	Publication
2011-11-30	C10	Entry into substantive examination
2011-11-30	SE01	Entry into force of request for substantive examination
2014-08-13	C14	Grant of patent or utility model
2014-08-13	GR01	Patent grant
2016-12-21	CF01	Termination of patent right due to non-payment of annual fee	Granted publication date: 20140813 Termination date: 20151105
2016-12-21	EXPY	Termination of patent right or utility model

Publication	Publication Date	Title
CN102216285B (zh)	2014-08-13	四取代的哒嗪hedgehog途径拮抗剂
CN102459233B (zh)	2014-07-02	二取代的酞嗪hedgehog途径拮抗剂
KR101260116B1 (ko)	2013-05-02	이치환된 프탈라진 헤지호그 경로 길항제
CN102216292B (zh)	2014-08-13	四取代的哒嗪hedgehog途径拮抗剂
MX2011004683A (es)	2011-06-20	Antagonistas de la via hedgehog de ftalazina disustituida.