JP2015500884A5 - - Google Patents
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- JP2015500884A5 JP2015500884A5 JP2014548915A JP2014548915A JP2015500884A5 JP 2015500884 A5 JP2015500884 A5 JP 2015500884A5 JP 2014548915 A JP2014548915 A JP 2014548915A JP 2014548915 A JP2014548915 A JP 2014548915A JP 2015500884 A5 JP2015500884 A5 JP 2015500884A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- group
- composition according
- mtor inhibitor
- formula
- 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.)
- Withdrawn
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- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 229940124302 mTOR inhibitor Drugs 0.000 claims 8
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 206010021143 Hypoxia Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 230000007954 hypoxia Effects 0.000 claims 5
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 4
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 4
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 229960005167 everolimus Drugs 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 229960000235 temsirolimus Drugs 0.000 claims 4
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- RGHYDLZMTYDBDT-UHFFFAOYSA-N 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone Chemical compound O=C1N(CC)C2=NC(N)=NC(C)=C2C=C1C=1C=CNN=1 RGHYDLZMTYDBDT-UHFFFAOYSA-N 0.000 claims 2
- BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims 2
- KVLFRAWTRWDEDF-IRXDYDNUSA-N AZD-8055 Chemical group C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3[C@H](COCC3)C)N3[C@H](COCC3)C)C2=N1 KVLFRAWTRWDEDF-IRXDYDNUSA-N 0.000 claims 2
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010052399 Neuroendocrine tumour Diseases 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 125000003435 aroyl group Chemical group 0.000 claims 2
- JROFGZPOBKIAEW-HAQNSBGRSA-N chembl3120215 Chemical compound N1C=2C(OC)=CC=CC=2C=C1C(=C1C(N)=NC=NN11)N=C1[C@H]1CC[C@H](C(O)=O)CC1 JROFGZPOBKIAEW-HAQNSBGRSA-N 0.000 claims 2
- 229950006418 dactolisib Drugs 0.000 claims 2
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000016065 neuroendocrine neoplasm Diseases 0.000 claims 2
- 201000011519 neuroendocrine tumor Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 2
- 229960001302 ridaforolimus Drugs 0.000 claims 2
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 2
- 229960002930 sirolimus Drugs 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- YUCFVHQCAFKDQG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH] YUCFVHQCAFKDQG-UHFFFAOYSA-N 0.000 claims 1
- 201000000062 kidney sarcoma Diseases 0.000 claims 1
- 208000010658 metastatic prostate carcinoma Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579607P | 2011-12-22 | 2011-12-22 | |
| US61/579,607 | 2011-12-22 | ||
| US201261617579P | 2012-03-29 | 2012-03-29 | |
| US61/617,579 | 2012-03-29 | ||
| PCT/US2012/071070 WO2013096684A1 (en) | 2011-12-22 | 2012-12-20 | Hypoxia activated prodrugs and mtor inhibitors for treating cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015500884A JP2015500884A (ja) | 2015-01-08 |
| JP2015500884A5 true JP2015500884A5 (https=) | 2016-02-18 |
Family
ID=48669506
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548915A Withdrawn JP2015500884A (ja) | 2011-12-22 | 2012-12-20 | 癌を治療するための低酸素活性化プロドラッグおよびｍＴＯＲ阻害剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20150005262A1 (https=) |
| EP (1) | EP2793899A4 (https=) |
| JP (1) | JP2015500884A (https=) |
| WO (1) | WO2013096684A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1896040B1 (en) | 2005-06-29 | 2012-08-01 | Threshold Pharmaceuticals, Inc. | Phosphoramidate alkylator prodrugs |
| EP2793882A4 (en) | 2011-12-22 | 2015-04-29 | Threshold Pharmaceuticals Inc | ADMINISTRATION OF HYPOXIA-ACTIVATED PRODRUGS IN COMBINATION WITH CHK1 INHIBITORS FOR THE TREATMENT OF CANCER |
| 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 |
| KR101692150B1 (ko) * | 2015-05-08 | 2017-01-03 | 계명대학교 산학협력단 | m-TOR 복합체 1,2 억제제 및 커큐민을 유효성분으로 포함하는 신장암 예방 또는 치료용 조성물 |
| AU2016260317B2 (en) * | 2015-05-13 | 2021-02-04 | Memorial Sloan Kettering Cancer Center | Macropinocytosis in cancer |
| 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 |
| 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 |
| 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 (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1896040B1 (en) * | 2005-06-29 | 2012-08-01 | Threshold Pharmaceuticals, Inc. | Phosphoramidate alkylator prodrugs |
| 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 |
| 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 |
| ES2877629T3 (es) * | 2010-07-12 | 2021-11-17 | Immunogenesis Inc | Administración de profármacos activados por hipoxia y agentes antiangiogénicos para el tratamiento del cáncer |
| RU2013147744A (ru) * | 2011-04-15 | 2015-05-20 | Тресхолд Фармасьютикалз, Инк. | Дозированная лекарственная форма для перорального применения |
-
2012
- 2012-12-20 EP EP12859382.9A patent/EP2793899A4/en not_active Withdrawn
- 2012-12-20 JP JP2014548915A patent/JP2015500884A/ja not_active Withdrawn
- 2012-12-20 US US14/367,152 patent/US20150005262A1/en not_active Abandoned
- 2012-12-20 WO PCT/US2012/071070 patent/WO2013096684A1/en not_active Ceased
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