CN102459233B - 二取代的酞嗪hedgehog途径拮抗剂 - Google Patents
二取代的酞嗪hedgehog途径拮抗剂 Download PDFInfo
- Publication number
- CN102459233B CN102459233B CN201080027189.3A CN201080027189A CN102459233B CN 102459233 B CN102459233 B CN 102459233B CN 201080027189 A CN201080027189 A CN 201080027189A CN 102459233 B CN102459233 B CN 102459233B
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- CN
- China
- Prior art keywords
- cancer
- methyl
- compound
- acceptable salt
- pharmaceutically acceptable
- 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.)
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- 0 CC(C)(C)OC(N(C)C(CC1)CCN1c1c(cccc2)c2c(*)nn1)=O Chemical compound CC(C)(C)OC(N(C)C(CC1)CCN1c1c(cccc2)c2c(*)nn1)=O 0.000 description 1
- PTPBVYUUWFYLOF-UHFFFAOYSA-N CC1c2c(-c3ccn[nH]3)nnc(N(CC3)CCC3N(C)C(OC(C)(C)C)=O)c2C=CC1 Chemical compound CC1c2c(-c3ccn[nH]3)nnc(N(CC3)CCC3N(C)C(OC(C)(C)C)=O)c2C=CC1 PTPBVYUUWFYLOF-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
- C07D401/14—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)
- 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)
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 |
|---|---|
| CN102459233A CN102459233A (zh) | 2012-05-16 |
| CN102459233B true CN102459233B (zh) | 2014-07-02 |
Family
ID=42332981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080027189.3A Active CN102459233B (zh) | 2009-06-19 | 2010-06-15 | 二取代的酞嗪hedgehog途径拮抗剂 |
Country Status (35)
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2723042A1 (en) * | 2008-04-29 | 2009-11-05 | Eli Lilly And Company | Disubstituted phthalazine hedgehog pathway antagonists |
| DK2364185T3 (da) * | 2008-11-03 | 2013-06-03 | Lilly Co Eli | Disubstituerede phthalazin-hedgehog-pathway-antagonister |
| CN102216292B (zh) * | 2008-11-17 | 2014-08-13 | 伊莱利利公司 | 四取代的哒嗪hedgehog途径拮抗剂 |
| AU2009314349B2 (en) | 2008-11-17 | 2013-04-18 | Eli Lilly And Company | Tetrasubstituted pyridazine 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 |
| 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 |
| 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 |
| 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 |
| CA2988289C (en) | 2015-06-04 | 2023-12-05 | PellePharm, Inc. | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| EP3303289A4 (en) * | 2015-06-05 | 2018-11-14 | Dana-Farber Cancer Institute, Inc. | Compounds and methods for treating cancer |
| JP7158023B2 (ja) | 2016-03-15 | 2022-10-21 | オリソン ヘノミクス エセ． アー． | 固形腫瘍の治療における使用のための、ｌｓｄ１阻害剤の組合せ |
| 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 |
| US20230301950A1 (en) | 2020-06-26 | 2023-09-28 | 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 |
| AU2021360767A1 (en) * | 2020-10-13 | 2023-04-27 | Endeavor Biomedicines, Inc. | Methods of treating fibrosis |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1638765A (zh) * | 2001-07-27 | 2005-07-13 | 柯里斯公司 | Hedgehog信号转导途径介质、其相关组合物以及应用 |
| WO2009002469A1 (en) * | 2007-06-25 | 2008-12-31 | Amgen Inc. | Phthalazine compounds, compositions and methods of use |
| WO2009074300A2 (en) * | 2007-12-13 | 2009-06-18 | Siena Biotech S.P.A. | Hedgehog pathway antagonists and therapeutic applications thereof |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN148482B (cg-RX-API-DMAC7.html) * | 1977-06-03 | 1981-03-07 | Pfizer | |
| ZA97288B (en) | 1996-01-15 | 1998-07-14 | Janssen Pharmaceutica Nv | 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 |
| CA2376210A1 (en) | 1999-06-08 | 2000-12-14 | Lorantis Limited | Therapeutic use of an inhibitor of a hedgehog or a hedgehog-related signalling pathway |
| JP2005529876A (ja) * | 2002-04-22 | 2005-10-06 | ジョンズ ホプキンス ユニバーシティー スクール オブ メディシン | Ｈｅｄｇｅｈｏｇシグナル伝達経路の調節因子、それに関連する組成物および使用 |
| AU2003265853A1 (en) | 2002-08-29 | 2004-03-19 | Curis, Inc. | Hedgehog antagonists, methods and uses related thereto |
| US8067608B2 (en) | 2003-09-29 | 2011-11-29 | The Johns Hopkins University | Hedgehog pathway antagonists |
| TW200533356A (en) | 2004-02-24 | 2005-10-16 | Mitsubishi Pharma Corp | Fused pyridazine derivatives |
| CA2564996A1 (en) | 2004-05-08 | 2006-01-12 | Taeyoung Yoon | 3-aryl-5,6-disubstituted pyridazines |
| KR101225018B1 (ko) | 2004-09-02 | 2013-01-23 | 쿠리스 인코퍼레이션 | 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 |
| 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 |
| CA2697682A1 (en) | 2007-09-07 | 2009-03-19 | Amgen Inc. | Annelated pyridazines for the treatment of tumors driven by inapropriate hedgehog signalling |
| CA2723042A1 (en) * | 2008-04-29 | 2009-11-05 | Eli Lilly And Company | Disubstituted phthalazine hedgehog pathway antagonists |
| US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| EP2321298B1 (en) * | 2008-08-04 | 2013-10-02 | Amgen Inc. | Aurora kinase modulators and methods of use |
| DK2364185T3 (da) | 2008-11-03 | 2013-06-03 | Lilly Co Eli | Disubstituerede phthalazin-hedgehog-pathway-antagonister |
| CN102216292B (zh) | 2008-11-17 | 2014-08-13 | 伊莱利利公司 | 四取代的哒嗪hedgehog途径拮抗剂 |
| AU2009314349B2 (en) | 2008-11-17 | 2013-04-18 | Eli Lilly And Company | Tetrasubstituted pyridazine 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 |
-
2010
- 2010-06-08 AR ARP100102003A patent/AR077014A1/es active IP Right Grant
- 2010-06-10 JO JO2010188A patent/JO2931B1/en active
- 2010-06-11 TW TW099119158A patent/TWI385165B/zh not_active IP Right Cessation
- 2010-06-15 MY MYPI2011006137A patent/MY156667A/en unknown
- 2010-06-15 NZ NZ596882A patent/NZ596882A/xx not_active IP Right Cessation
- 2010-06-15 PE PE2011002119A patent/PE20121050A1/es active IP Right Grant
- 2010-06-15 HR HRP20130408AT patent/HRP20130408T1/hr unknown
- 2010-06-15 SG SG2011094190A patent/SG177289A1/en unknown
- 2010-06-15 WO PCT/US2010/038568 patent/WO2010147917A1/en not_active Ceased
- 2010-06-15 EP EP10726756.9A patent/EP2443104B1/en active Active
- 2010-06-15 PL PL10726756T patent/PL2443104T3/pl unknown
- 2010-06-15 EA EA201270049A patent/EA019059B1/ru not_active IP Right Cessation
- 2010-06-15 MA MA34455A patent/MA33363B1/fr unknown
- 2010-06-15 KR KR1020117030157A patent/KR101389165B1/ko not_active Expired - Fee Related
- 2010-06-15 AU AU2010260244A patent/AU2010260244B2/en not_active Ceased
- 2010-06-15 UA UAA201114996A patent/UA106755C2/uk unknown
- 2010-06-15 SI SI201030200T patent/SI2443104T1/sl unknown
- 2010-06-15 PT PT107267569T patent/PT2443104E/pt unknown
- 2010-06-15 BR BRPI1011601A patent/BRPI1011601A2/pt not_active Application Discontinuation
- 2010-06-15 ES ES10726756T patent/ES2409054T3/es active Active
- 2010-06-15 CN CN201080027189.3A patent/CN102459233B/zh active Active
- 2010-06-15 US US12/815,439 patent/US8273742B2/en active Active
- 2010-06-15 DK DK10726756.9T patent/DK2443104T3/da active
- 2010-06-15 MX MX2011014029A patent/MX2011014029A/es active IP Right Grant
- 2010-06-15 JP JP2012516178A patent/JP5596139B2/ja active Active
- 2010-06-15 CA CA2764542A patent/CA2764542C/en not_active Expired - Fee Related
-
2011
- 2011-11-22 ZA ZA2011/08587A patent/ZA201108587B/en unknown
- 2011-11-24 IL IL216599A patent/IL216599A/en not_active IP Right Cessation
- 2011-11-29 HN HN2011003139A patent/HN2011003139A/es unknown
- 2011-12-07 TN TNP2011000627A patent/TN2011000627A1/en unknown
- 2011-12-08 CR CR20110658A patent/CR20110658A/es unknown
- 2011-12-13 DO DO2011000386A patent/DOP2011000386A/es unknown
- 2011-12-14 CL CL2011003147A patent/CL2011003147A1/es unknown
- 2011-12-16 EC EC2011011541A patent/ECSP11011541A/es unknown
- 2011-12-22 CO CO11177210A patent/CO6480932A2/es not_active Application Discontinuation
-
2012
- 2012-08-21 US US13/590,481 patent/US9000023B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1638765A (zh) * | 2001-07-27 | 2005-07-13 | 柯里斯公司 | Hedgehog信号转导途径介质、其相关组合物以及应用 |
| WO2009002469A1 (en) * | 2007-06-25 | 2008-12-31 | Amgen Inc. | Phthalazine compounds, compositions and methods of use |
| WO2009074300A2 (en) * | 2007-12-13 | 2009-06-18 | Siena Biotech S.P.A. | Hedgehog pathway antagonists and therapeutic applications thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |