JP2015500885A5 - - Google Patents
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- Publication number
- JP2015500885A5 JP2015500885A5 JP2014548917A JP2014548917A JP2015500885A5 JP 2015500885 A5 JP2015500885 A5 JP 2015500885A5 JP 2014548917 A JP2014548917 A JP 2014548917A JP 2014548917 A JP2014548917 A JP 2014548917A JP 2015500885 A5 JP2015500885 A5 JP 2015500885A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- formula
- heteroalkyl
- aryl
- alkyl
- 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.)
- Pending
Links
- 239000003112 inhibitor Substances 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 101150113535 chek1 gene Proteins 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 206010021143 Hypoxia Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000003435 aroyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 230000007954 hypoxia Effects 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- IAYGCINLNONXHY-LBPRGKRZSA-N 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamide Chemical compound NC(=O)NC=1C=C(C=2C=C(F)C=CC=2)SC=1C(=O)N[C@H]1CCCNC1 IAYGCINLNONXHY-LBPRGKRZSA-N 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 2
- SYYBDNPGDKKJDU-ZDUSSCGKSA-N 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)urea Chemical compound C1=NC(C)=CN=C1NC(=O)NC1=CC(Br)=C(C)C=C1OC[C@H]1OCCNC1 SYYBDNPGDKKJDU-ZDUSSCGKSA-N 0.000 claims 2
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 2
- YFNWWNRZJGMDBR-LJQANCHMSA-N PF-00477736 Chemical compound C1=NN(C)C=C1C1=NC2=CC(NC(=O)[C@H](N)C3CCCCC3)=CC3=C2C1=CNNC3=O YFNWWNRZJGMDBR-LJQANCHMSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 230000002950 deficient Effects 0.000 claims 2
- YUCFVHQCAFKDQG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH] YUCFVHQCAFKDQG-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- GMIZZEXBPRLVIV-SECBINFHSA-N 6-bromo-3-(1-methylpyrazol-4-yl)-5-[(3r)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidin-7-amine Chemical compound C1=NN(C)C=C1C1=C2N=C([C@H]3CNCCC3)C(Br)=C(N)N2N=C1 GMIZZEXBPRLVIV-SECBINFHSA-N 0.000 claims 1
- 230000000259 anti-tumor effect Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 210000004881 tumor cell Anatomy 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579605P | 2011-12-22 | 2011-12-22 | |
| US61/579,605 | 2011-12-22 | ||
| US201261617576P | 2012-03-29 | 2012-03-29 | |
| US61/617,576 | 2012-03-29 | ||
| PCT/US2012/071074 WO2013096687A1 (en) | 2011-12-22 | 2012-12-20 | Administration of hypoxia activated prodrugs in combination with chk1 inhibitors for treating cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017182053A Division JP2017218459A (ja) | 2011-12-22 | 2017-09-22 | 癌を治療するためのｃｈｋ１阻害剤と組み合わせた低酸素活性化プロドラッグの投与 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015500885A JP2015500885A (ja) | 2015-01-08 |
| JP2015500885A5 true JP2015500885A5 (https=) | 2016-02-18 |
Family
ID=48669508
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548917A Pending JP2015500885A (ja) | 2011-12-22 | 2012-12-20 | 癌を治療するためのｃｈｋ１阻害剤と組み合わせた低酸素活性化プロドラッグの投与 |
| JP2017182053A Withdrawn JP2017218459A (ja) | 2011-12-22 | 2017-09-22 | 癌を治療するためのｃｈｋ１阻害剤と組み合わせた低酸素活性化プロドラッグの投与 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017182053A Withdrawn JP2017218459A (ja) | 2011-12-22 | 2017-09-22 | 癌を治療するためのｃｈｋ１阻害剤と組み合わせた低酸素活性化プロドラッグの投与 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9254299B2 (https=) |
| EP (1) | EP2793882A4 (https=) |
| JP (2) | JP2015500885A (https=) |
| WO (1) | WO2013096687A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016528217A (ja) | 2013-07-26 | 2016-09-15 | スレッショルド ファーマシューティカルズ，インコーポレイテッド | 低酸素活性化プロドラッグおよびタキサンの組合せを用いた膵臓癌の治療 |
| WO2015069489A1 (en) | 2013-11-06 | 2015-05-14 | Merck Patent Gmbh | Predictive biomarker for hypoxia-activated prodrug therapy |
| SG11201610500WA (en) | 2014-06-17 | 2017-01-27 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
| EP3313819A1 (en) * | 2015-06-23 | 2018-05-02 | Case Western Reserve University | Compositions and methods for treating cancer |
| CA3065803A1 (en) * | 2017-06-01 | 2018-12-06 | Sierra Oncology, Inc. | Biomarkers and patient selection strategies |
| MX2021013905A (es) * | 2019-05-14 | 2022-05-18 | Sierra Oncology Inc | Métodos de tratamiento del cáncer mediante el uso de inhibidores de chk1. |
| TW202204348A (zh) | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| CN117651548B (zh) | 2021-08-27 | 2026-03-03 | 深圳艾欣达伟医药科技有限公司 | 冻干制剂溶液及冻干制剂、方法和用途 |
| WO2023025312A1 (zh) | 2021-08-27 | 2023-03-02 | 深圳艾欣达伟医药科技有限公司 | 使用th-302治疗parp抑制剂耐药的患者 |
| US20250186468A1 (en) | 2022-03-15 | 2025-06-12 | Ascentawits Pharmaceuticals, Ltd. | Method for treating patient with brca-mutated cancer |
| CN119384281A (zh) | 2022-04-15 | 2025-01-28 | 深圳艾欣达伟医药科技有限公司 | 使用th-302单药或联用parp抑制剂治疗癌症的方法 |
| CN119233822A (zh) | 2022-05-23 | 2024-12-31 | 深圳艾欣达伟医药科技有限公司 | 烷化剂前药与细胞周期抑制剂联用治疗癌症的方法 |
| CN119894521A (zh) | 2022-09-22 | 2025-04-25 | 深圳艾欣达伟医药科技有限公司 | 乏氧激活的化合物在制备治疗癌症患者的药物中的用途 |
| KR20250160163A (ko) | 2023-02-27 | 2025-11-11 | 아센타위츠 파마슈티컬즈 리미티드 | 용액, 동결건조 제형, 동결건조 제형 단위 패키지, 주사제, 및 주사제 제조 방법 |
| WO2025026214A1 (zh) | 2023-07-28 | 2025-02-06 | 深圳艾欣达伟医药科技有限公司 | 治疗p53基因突变或缺陷阴性癌症、肿瘤患者 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5306727A (en) | 1993-04-30 | 1994-04-26 | Research Corporation Technologies, Inc. | Phosphoramidates useful as antitumor agents |
| US7914994B2 (en) | 1998-12-24 | 2011-03-29 | Cepheid | Method for separating an analyte from a sample |
| GB9909612D0 (en) | 1999-04-26 | 1999-06-23 | Cancer Res Campaign Tech | N-protected amines and their use as prodrugs |
| CA2441228A1 (en) | 2001-03-23 | 2002-10-03 | Aphton Corporation | Combination treatment of pancreatic cancer |
| HUE026218T2 (en) | 2002-02-21 | 2016-05-30 | Inst Virology | MN / CA IX-Specific Monoclonal Antibodies and Methods for MN / CA IX Deficient Mice |
| DE10237931A1 (de) | 2002-08-14 | 2004-02-26 | Endress + Hauser Gmbh + Co. Kg | Vorrichtung zur Überwachung eines vorbestimmten Füllstands eines Messmediums in einem Behälter |
| NZ521851A (en) | 2002-10-08 | 2005-02-25 | Auckland Uniservices Ltd | Nitroaniline-based unsymmetrical mustard alkylating agents for gene dependent enzyme prodrug therapy |
| JP3990718B2 (ja) | 2003-01-09 | 2007-10-17 | ファイザー・インク | キナーゼ阻害剤としてのジアゼピノインドール誘導体 |
| ZA200507752B (en) | 2003-03-28 | 2007-01-31 | Threshold Pharmaceuticals Inc | Compositions and methods for treating cancer |
| AU2004285831B2 (en) | 2003-10-31 | 2011-09-15 | Auckland Uniservices Limited | Novel nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents |
| US7432106B2 (en) | 2004-03-24 | 2008-10-07 | Applied Biosystems Inc. | Liquid processing device including gas trap, and system and method |
| US8545881B2 (en) | 2004-04-19 | 2013-10-01 | Eurand Pharmaceuticals, Ltd. | Orally disintegrating tablets and methods of manufacture |
| EP1743038A4 (en) | 2004-05-04 | 2007-11-21 | Bayer Healthcare | MN / CA IX / CA9 AND KIDNEY CANCER PROGNOSIS |
| US20070117784A1 (en) | 2005-03-04 | 2007-05-24 | Novacea, Inc. | Treatment of hyperproliferative diseases with anthraquinones |
| EP1896040B1 (en) | 2005-06-29 | 2012-08-01 | Threshold Pharmaceuticals, Inc. | Phosphoramidate alkylator prodrugs |
| CA2624707A1 (en) | 2005-10-03 | 2007-04-12 | Genetix Pharmaceuticals, Inc. | Method for selectively depleting hypoxic cells |
| WO2008033041A1 (en) | 2006-09-11 | 2008-03-20 | Auckland Uniservices Limited | Cancer treatment |
| US7807454B2 (en) | 2006-10-18 | 2010-10-05 | The Regents Of The University Of California | Microfluidic magnetophoretic device and methods for using the same |
| ES2884044T3 (es) | 2006-12-26 | 2021-12-10 | Immunogenesis Inc | Profármaco alquilante de fosforamidato para el tratamiento del cáncer |
| US8216607B2 (en) | 2008-03-17 | 2012-07-10 | Roger Williams Hospital | Combination of ceramide and gemcitabine for inducing cell death and uses thereof in treating cancer |
| CN104043125B (zh) | 2008-04-10 | 2018-01-12 | 弗吉尼亚州立邦联大学 | 诱导肿瘤缺氧以治疗癌症 |
| JP2011523551A (ja) | 2008-05-15 | 2011-08-18 | ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル | 血管形成の調節の新規ターゲット |
| TWI466886B (zh) | 2008-06-11 | 2015-01-01 | Genentech Inc | 二氮雜咔唑及使用方法 |
| EP2350664B1 (en) | 2008-10-21 | 2021-05-19 | ImmunoGenesis, Inc. | Treatment of cancer using the hypoxia activated prodrug th-302 in combination with docetaxel or pemetrexed |
| US8281672B2 (en) | 2009-03-20 | 2012-10-09 | Pbs Biotech, Inc. | Automatable aseptic sample withdrawal system |
| US20120114637A1 (en) | 2009-05-04 | 2012-05-10 | Santen Pharmaceutical Co., Ltd. | Mtor pathway inhibitors for treating ocular disorders |
| US20110135739A1 (en) | 2009-11-06 | 2011-06-09 | Bennett Carter | Oral Formulations of a Hedgehog Pathway Inhibitor |
| US20130296273A1 (en) | 2010-06-28 | 2013-11-07 | Threshold Pharmaceuticals, Inc. | Treatment of blood cancer |
| ES2877629T3 (es) | 2010-07-12 | 2021-11-17 | Immunogenesis Inc | Administración de profármacos activados por hipoxia y agentes antiangiogénicos para el tratamiento del cáncer |
| EP2593796A4 (en) | 2010-07-16 | 2016-07-27 | Auckland Uniservices Ltd | BACTERIAL NITROREDUCTASE ENZYMES AND METHOD THEREFOR |
| WO2012135757A2 (en) | 2011-04-01 | 2012-10-04 | Threshold Pharmaceuticals, Inc. | Methods for treating cancer |
| RU2013147744A (ru) | 2011-04-15 | 2015-05-20 | Тресхолд Фармасьютикалз, Инк. | Дозированная лекарственная форма для перорального применения |
| JP5805989B2 (ja) | 2011-04-26 | 2015-11-10 | 大塚電子株式会社 | 電気泳動移動度測定用セル並びにそれを用いた測定装置及び測定方法 |
| EP2793899A4 (en) | 2011-12-22 | 2015-06-17 | Threshold Pharmaceuticals Inc | HYPOXIA-ACTIVATED PRODRUGS AND MTOR INHIBITORS FOR CANCER TREATMENT |
| JP2015511226A (ja) | 2012-01-31 | 2015-04-16 | スレッショルド ファーマシューティカルズ，インコーポレイテッド | 低酸素活性化プロドラッグ療法のための予測バイオマーカー |
-
2012
- 2012-12-20 EP EP12860951.8A patent/EP2793882A4/en not_active Withdrawn
- 2012-12-20 JP JP2014548917A patent/JP2015500885A/ja active Pending
- 2012-12-20 US US14/367,168 patent/US9254299B2/en not_active Expired - Fee Related
- 2012-12-20 WO PCT/US2012/071074 patent/WO2013096687A1/en not_active Ceased
-
2017
- 2017-09-22 JP JP2017182053A patent/JP2017218459A/ja not_active Withdrawn
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