JP2011527666A5 - - Google Patents
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- Publication number
- JP2011527666A5 JP2011527666A5 JP2011507512A JP2011507512A JP2011527666A5 JP 2011527666 A5 JP2011527666 A5 JP 2011527666A5 JP 2011507512 A JP2011507512 A JP 2011507512A JP 2011507512 A JP2011507512 A JP 2011507512A JP 2011527666 A5 JP2011527666 A5 JP 2011527666A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- compound according
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- KYOIKJWTHIOKJH-UHFFFAOYSA-N 4-fluoro-n-[1-[4-(4-fluorophenyl)phthalazin-1-yl]piperidin-4-yl]-n-methyl-2-(trifluoromethyl)benzamide Chemical group C=1C=C(F)C=C(C(F)(F)F)C=1C(=O)N(C)C(CC1)CCN1C(C1=CC=CC=C11)=NN=C1C1=CC=C(F)C=C1 KYOIKJWTHIOKJH-UHFFFAOYSA-N 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 201000009036 biliary tract cancer Diseases 0.000 claims 1
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4872908P | 2008-04-29 | 2008-04-29 | |
| US61/048,729 | 2008-04-29 | ||
| PCT/US2009/039065 WO2009134574A2 (en) | 2008-04-29 | 2009-04-01 | Disubstituted phthalazine hedgehog pathway antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011527666A JP2011527666A (ja) | 2011-11-04 |
| JP2011527666A5 true JP2011527666A5 (enExample) | 2013-05-23 |
| JP5442717B2 JP5442717B2 (ja) | 2014-03-12 |
Family
ID=40846962
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011507512A Expired - Fee Related JP5442717B2 (ja) | 2008-04-29 | 2009-04-01 | 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 (22)
| Country | Link |
|---|---|
| US (1) | US7981892B2 (enExample) |
| EP (1) | EP2294061A2 (enExample) |
| JP (1) | JP5442717B2 (enExample) |
| KR (1) | KR101260116B1 (enExample) |
| CN (1) | CN102066353B (enExample) |
| AU (1) | AU2009241561B2 (enExample) |
| BR (1) | BRPI0911618A2 (enExample) |
| CA (1) | CA2723042A1 (enExample) |
| CO (1) | CO6300945A2 (enExample) |
| CR (1) | CR11741A (enExample) |
| DO (1) | DOP2010000302A (enExample) |
| EA (1) | EA201071248A1 (enExample) |
| EC (1) | ECSP10010577A (enExample) |
| HN (1) | HN2010002157A (enExample) |
| IL (1) | IL208211A0 (enExample) |
| MA (1) | MA32349B1 (enExample) |
| MX (1) | MX2010011948A (enExample) |
| MY (1) | MY159491A (enExample) |
| NZ (1) | NZ588001A (enExample) |
| UA (1) | UA102250C2 (enExample) |
| WO (1) | WO2009134574A2 (enExample) |
| ZA (1) | ZA201006695B (enExample) |
Families Citing this family (19)
| 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 |
| JP2013511526A (ja) * | 2009-11-18 | 2013-04-04 | ノバルティス アーゲー | 固形腫瘍及びその他の悪性腫瘍を治療するための方法及び組成物 |
| CN102702108A (zh) * | 2012-06-27 | 2012-10-03 | 上海大学 | 1,2-二氢酞嗪类化合物及其合成方法 |
| CA2878082A1 (en) * | 2012-09-17 | 2014-03-20 | Duke University | Smoothened modulators and methods of use thereof |
| CN102863393A (zh) * | 2012-09-26 | 2013-01-09 | 上海大学 | 1,2-二氢酞嗪类化合物及其合成方法 |
| GB201309508D0 (en) | 2013-05-28 | 2013-07-10 | Redx Pharma Ltd | Compounds |
| 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 |
| 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 |
| 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 |
| 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 |
| CN119907797A (zh) * | 2022-09-23 | 2025-04-29 | 默沙东有限责任公司 | 用作nod样受体蛋白3抑制剂的酞嗪衍生物 |
| US12447148B2 (en) | 2024-03-05 | 2025-10-21 | Endeavor Biomedicines, Inc. | Methods of improving lung function |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1293565A (en) * | 1969-05-03 | 1972-10-18 | Aspro Nicholas Ltd | Aminophthalazines and pharmaceutical compositions thereof |
| AU717744B2 (en) | 1996-01-15 | 2000-03-30 | Janssen Pharmaceutica N.V. | 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 |
| GB0013674D0 (en) | 1999-06-08 | 2000-07-26 | Lorantis Ltd | Therapeutic use |
| 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 |
| 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 |
| 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 |
-
2009
- 2009-04-01 CN CN2009801152085A patent/CN102066353B/zh not_active Expired - Fee Related
- 2009-04-01 MY MYPI2010005097A patent/MY159491A/en unknown
- 2009-04-01 UA UAA201012722A patent/UA102250C2/ru unknown
- 2009-04-01 EP EP09739376A patent/EP2294061A2/en not_active Withdrawn
- 2009-04-01 KR KR1020107024209A patent/KR101260116B1/ko not_active Expired - Fee Related
- 2009-04-01 MX MX2010011948A patent/MX2010011948A/es active IP Right Grant
- 2009-04-01 US US12/935,655 patent/US7981892B2/en not_active Expired - Fee Related
- 2009-04-01 CA CA2723042A patent/CA2723042A1/en not_active Abandoned
- 2009-04-01 JP JP2011507512A patent/JP5442717B2/ja not_active Expired - Fee Related
- 2009-04-01 EA EA201071248A patent/EA201071248A1/ru unknown
- 2009-04-01 NZ NZ588001A patent/NZ588001A/en not_active IP Right Cessation
- 2009-04-01 BR BRPI0911618A patent/BRPI0911618A2/pt not_active IP Right Cessation
- 2009-04-01 AU AU2009241561A patent/AU2009241561B2/en not_active Ceased
- 2009-04-01 WO PCT/US2009/039065 patent/WO2009134574A2/en not_active Ceased
-
2010
- 2010-09-16 IL IL208211A patent/IL208211A0/en unknown
- 2010-09-17 ZA ZA2010/06695A patent/ZA201006695B/en unknown
- 2010-10-11 DO DO2010000302A patent/DOP2010000302A/es unknown
- 2010-10-15 CR CR11741A patent/CR11741A/es unknown
- 2010-10-21 HN HN2010002157A patent/HN2010002157A/es unknown
- 2010-10-25 MA MA33284A patent/MA32349B1/fr unknown
- 2010-10-27 EC EC2010010577A patent/ECSP10010577A/es unknown
- 2010-11-11 CO CO10141824A patent/CO6300945A2/es not_active Application Discontinuation
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