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 (https=) | 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 (https=) |
| EP (1) | EP2294061A2 (https=) |
| JP (1) | JP5442717B2 (https=) |
| KR (1) | KR101260116B1 (https=) |
| CN (1) | CN102066353B (https=) |
| AU (1) | AU2009241561B2 (https=) |
| BR (1) | BRPI0911618A2 (https=) |
| CA (1) | CA2723042A1 (https=) |
| CO (1) | CO6300945A2 (https=) |
| CR (1) | CR11741A (https=) |
| DO (1) | DOP2010000302A (https=) |
| EA (1) | EA201071248A1 (https=) |
| EC (1) | ECSP10010577A (https=) |
| HN (1) | HN2010002157A (https=) |
| IL (1) | IL208211A0 (https=) |
| MA (1) | MA32349B1 (https=) |
| MX (1) | MX2010011948A (https=) |
| MY (1) | MY159491A (https=) |
| NZ (1) | NZ588001A (https=) |
| UA (1) | UA102250C2 (https=) |
| WO (1) | WO2009134574A2 (https=) |
| ZA (1) | ZA201006695B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA102250C2 (ru) | 2008-04-29 | 2013-06-25 | Эли Лилли Энд Компани | Двухзамещенные фталазины - антагонисты проводящего пути hedgehog |
| EP2364185B1 (en) | 2008-11-03 | 2013-05-22 | Eli Lilly And Company | Disubstituted phthalazine hedgehog pathway antagonists |
| MX2011005176A (es) | 2008-11-17 | 2011-05-30 | Lilly Co Eli | Antagonistas de la trayectoria hedgehog de piridazinas tetrasustituidas. |
| CA2743483C (en) | 2008-11-17 | 2014-03-11 | 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 |
| CA2781210A1 (en) * | 2009-11-18 | 2011-05-26 | Novartis Ag | Methods and compositions for treating solid tumors and other malignancies |
| 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 |
| EP2895474B1 (en) * | 2012-09-17 | 2019-12-11 | Duke University | Smoothened receptor 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 |
| 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 |
| 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 |
| 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 |
| GEAP202516743A (en) * | 2022-09-23 | 2025-08-11 | Merck Sharp & Dohme Llc | Phthalazine derivatives useful as inhibitors of nod-like receptor protein 3 |
| WO2025188802A1 (en) | 2024-03-05 | 2025-09-12 | 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 |
| ATE203534T1 (de) * | 1996-01-15 | 2001-08-15 | Janssen Pharmaceutica Nv | Angiogenesis hemmende pyridazinamine |
| IL138645A0 (en) | 1998-04-09 | 2001-10-31 | Univ Johns Hopkins Med | Use of steroidal alkaloid derivatives as inhibitors of hedghog signalling pathways |
| US6432970B2 (en) * | 1998-04-09 | 2002-08-13 | Johns Hopkins University School Of Medicine | Inhibitors of hedgehog signaling pathways, compositions and uses related thereto |
| CA2376210A1 (en) | 1999-06-08 | 2000-12-14 | Lorantis Limited | Therapeutic use of an inhibitor of a hedgehog or a hedgehog-related signalling pathway |
| DE60322869D1 (de) | 2002-04-22 | 2008-09-25 | Univ Johns Hopkins | Modulatoren von hedgehog signalpfaden, zusammensetzungen und verwandte verwendungen |
| 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 |
| EP1745039A4 (en) | 2004-05-08 | 2009-07-22 | Neurogen Corp | 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES |
| DK1789390T3 (da) | 2004-09-02 | 2012-02-27 | Genentech Inc | Pyridyl-inhibitorer af hedgehog-signalering |
| 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 |
| PE20090188A1 (es) * | 2007-03-15 | 2009-03-20 | Novartis Ag | Compuestos heterociclicos como moduladores de la senda de hedgehog |
| US8153633B2 (en) * | 2007-06-25 | 2012-04-10 | Amgen Inc. | Phthalazine compounds, compositions and methods of use |
| WO2009035568A1 (en) | 2007-09-07 | 2009-03-19 | Amgen Inc. | Annelated pyridazines for the treatment of tumors driven by inappropriate hedgehog signalling |
| 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 |
| EP2364185B1 (en) | 2008-11-03 | 2013-05-22 | Eli Lilly And Company | Disubstituted phthalazine hedgehog pathway antagonists |
| MX2011005176A (es) | 2008-11-17 | 2011-05-30 | Lilly Co Eli | Antagonistas de la trayectoria hedgehog de piridazinas tetrasustituidas. |
| CA2743483C (en) | 2008-11-17 | 2014-03-11 | 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 |
-
2009
- 2009-04-01 UA UAA201012722A patent/UA102250C2/ru unknown
- 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 MX MX2010011948A patent/MX2010011948A/es active IP Right Grant
- 2009-04-01 EA EA201071248A patent/EA201071248A1/ru unknown
- 2009-04-01 BR BRPI0911618A patent/BRPI0911618A2/pt not_active IP Right Cessation
- 2009-04-01 KR KR1020107024209A patent/KR101260116B1/ko not_active Expired - Fee Related
- 2009-04-01 US US12/935,655 patent/US7981892B2/en not_active Expired - Fee Related
- 2009-04-01 NZ NZ588001A patent/NZ588001A/en not_active IP Right Cessation
- 2009-04-01 WO PCT/US2009/039065 patent/WO2009134574A2/en not_active Ceased
- 2009-04-01 CN CN2009801152085A patent/CN102066353B/zh not_active Expired - Fee Related
- 2009-04-01 EP EP09739376A patent/EP2294061A2/en not_active Withdrawn
- 2009-04-01 AU AU2009241561A patent/AU2009241561B2/en not_active Ceased
- 2009-04-01 MY MYPI2010005097A patent/MY159491A/en unknown
-
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