JP2017517548A5 - - Google Patents
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- JP2017517548A5 JP2017517548A5 JP2016572636A JP2016572636A JP2017517548A5 JP 2017517548 A5 JP2017517548 A5 JP 2017517548A5 JP 2016572636 A JP2016572636 A JP 2016572636A JP 2016572636 A JP2016572636 A JP 2016572636A JP 2017517548 A5 JP2017517548 A5 JP 2017517548A5
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- JP
- Japan
- Prior art keywords
- cancer
- inhibitor
- substituted
- composition
- tumor
- 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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| US10059003B1 (en) | 2016-01-28 | 2018-08-28 | X Development Llc | Multi-resolution localization system |
| WO2018039441A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| KR20190040302A (ko) * | 2016-08-25 | 2019-04-17 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 글루타미나제 억제제와의 병용 요법 |
| US10980835B2 (en) * | 2016-12-02 | 2021-04-20 | Beth Israel Deaconess Medical Center, Inc. | Arsenic trioxide for treatment of PIN1-associated disorders |
| CN108210461A (zh) * | 2016-12-16 | 2018-06-29 | 中国科学院上海药物研究所 | 一种Talazoparib药物组合物及其应用 |
| WO2018165516A1 (en) * | 2017-03-10 | 2018-09-13 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| CN108721304B (zh) * | 2017-04-17 | 2020-10-16 | 北京大学 | 用于治疗肿瘤的药物组合物及其用途 |
| TWI753178B (zh) * | 2017-06-22 | 2022-01-21 | 法商施維雅藥廠 | Mcl-1抑制劑與血液癌症標準療法之組合，其用途及醫藥組合物 |
| US20190269705A1 (en) * | 2017-11-27 | 2019-09-05 | Regents Of The University Of Minnesota | Methods and materials for treating graft versus host disease |
| US20210380683A1 (en) * | 2018-04-12 | 2021-12-09 | The Methodist Hospital System | Modulation of irf-4 and uses thereof |
| CN108715882A (zh) * | 2018-05-31 | 2018-10-30 | 中国人民解放军军事科学院军事医学研究院 | 通过有丝分裂阻滞诱导的细胞叠套结构模型及其制备方法 |
| CN110732025A (zh) * | 2018-07-19 | 2020-01-31 | 中国人民解放军军事科学院军事医学研究院 | 一种cell-in-cell结构的动物模型及其制备方法 |
| IT201800009974A1 (it) * | 2018-10-31 | 2020-05-01 | Universita' Degli Studi Di Milano - Bicocca | Trattamento combinato farmacologico per cancro |
| US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
| WO2020246737A1 (ko) * | 2019-06-04 | 2020-12-10 | 사회복지법인 삼성생명공익재단 | 콰시노이드를 포함하는 거세 저항성 전립선암 치료용 조성물 |
| CN111643669A (zh) * | 2020-06-30 | 2020-09-11 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | 谷氨酰胺酶抑制剂在制备治疗银屑病的药物中的应用 |
| JP2024511277A (ja) | 2021-02-19 | 2024-03-13 | メビオン・メディカル・システムズ・インコーポレーテッド | 粒子線治療システムのためのガントリー |
| CN114699398A (zh) * | 2022-04-26 | 2022-07-05 | 中国人民解放军陆军特色医学中心 | 一种用于治疗肾透明细胞癌的抑制剂 |
| EP4514336A1 (en) * | 2022-04-28 | 2025-03-05 | Scirosbio (FZC) | Compositions and methods for treatment of cancer |
| CN121177294B (zh) * | 2025-11-27 | 2026-02-27 | 四川省医学科学院·四川省人民医院 | Akt抑制剂在制备诱导胰岛移植免疫耐受药物中的应用 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4172896A (en) | 1978-06-05 | 1979-10-30 | Dainippon Pharmaceutical Co., Ltd. | Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same |
| GB9217295D0 (en) | 1992-08-14 | 1992-09-30 | Wellcome Found | Controlled released tablets |
| US5358970A (en) | 1993-08-12 | 1994-10-25 | Burroughs Wellcome Co. | Pharmaceutical composition containing bupropion hydrochloride and a stabilizer |
| GB9315856D0 (en) | 1993-07-30 | 1993-09-15 | Wellcome Found | Stabilized pharmaceutical |
| US5541231A (en) | 1993-07-30 | 1996-07-30 | Glaxo Wellcome Inc. | Stabilized Pharmaceutical |
| DK0999825T3 (da) | 1997-07-29 | 2004-02-09 | Alcon Lab Inc | Oftalmiske sammensætninger indeholdende galactomannanpolymerer og borater |
| US6110973A (en) | 1998-01-29 | 2000-08-29 | Sepracor | Methods for treating obesity and weight gain using optically pure (-)-bupropion |
| US8889112B2 (en) | 1999-09-16 | 2014-11-18 | Ocularis Pharma, Llc | Ophthalmic formulations including selective alpha 1 antagonists |
| US6451828B1 (en) | 2000-08-10 | 2002-09-17 | Elan Pharmaceuticals, Inc. | Selective inhibition of glutaminase by bis-thiadiazoles |
| US6933289B2 (en) | 2003-07-01 | 2005-08-23 | Allergan, Inc. | Inhibition of irritating side effects associated with use of a topical ophthalmic medication |
| CA2534484A1 (en) | 2003-08-07 | 2005-02-17 | Allergan, Inc. | Compositions for delivery of therapeutics into the eyes and methods for making and using same |
| US20050059744A1 (en) | 2003-09-12 | 2005-03-17 | Allergan, Inc. | Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions |
| CA2578680C (en) | 2004-04-15 | 2011-06-14 | University Of Florida Research Foundation, Inc. | Proteolytic markers as diagnostic biomarkers for cancer, organ injury and muscle rehabilitation/exercise overtraining |
| KR101325374B1 (ko) | 2008-02-19 | 2013-11-08 | 가부시키가이샤 오츠까 세이야꾸 고죠 | 신체 기능의 회복에 유용한 경구 또는 경장 조성물 |
| US20130109643A1 (en) | 2010-05-10 | 2013-05-02 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| WO2012006506A1 (en) | 2010-07-09 | 2012-01-12 | Massachusetts Institute Of Technology | Metabolic gene, enzyme, and flux targets for cancer therapy |
| US20120302605A1 (en) | 2010-11-18 | 2012-11-29 | Deuteria Pharmaceuticals, Llc | 3-deutero-pomalidomide |
| CA2742342A1 (en) * | 2011-02-12 | 2012-08-12 | Baylor Research Institute | Msh3 expression status determines the responsiveness of cancer cells to the chemotherapeutic treatment with parp inhibitors and platinum drugs |
| US9713803B2 (en) | 2011-07-13 | 2017-07-25 | Dr. Hielscher Gmbh | Method and device for changing the properties of at least one liquid medium |
| FI20115876A0 (fi) * | 2011-09-06 | 2011-09-06 | Turun Yliopisto | Yhdistelmähoito |
| CN103030597B (zh) * | 2011-09-30 | 2014-10-01 | 南昌滨西科技有限公司 | 肾脏型谷氨酰胺酶抑制剂及其制备方法和用途 |
| ES2761866T3 (es) | 2011-11-21 | 2020-05-21 | Calithera Biosciences Inc | Inhibidores heterocíclicos de glutaminasa |
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| MX2015003114A (es) | 2012-09-10 | 2015-07-06 | Celgene Corp | Metodos para el tratamiento de cancer de mama localmente avanzado. |
| WO2014043633A1 (en) * | 2012-09-17 | 2014-03-20 | Agios Pharmaceuticals, Inc. | Use of e-cadherin and vimentin for selection of treatment responsive patients |
| BR112015010955A2 (pt) | 2012-11-16 | 2017-07-11 | Calithera Biosciences Inc | inibidores de glutaminase heterocíclica |
| SG11201504022RA (en) * | 2012-11-21 | 2015-06-29 | Agios Pharmaceuticals Inc | Glutamase inhibitors and method of use |
| US9029531B2 (en) * | 2012-11-22 | 2015-05-12 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| BR112015012536A2 (pt) * | 2012-12-03 | 2017-07-11 | Calithera Biosciences Inc | tratamento de câncer com inibidores heterocíclicos da glutaminase |
| WO2015061432A1 (en) | 2013-10-25 | 2015-04-30 | Calithera Biosciences, Inc. | Treatment of viral infections with inhibitors of glutaminase |
| EP3116872A4 (en) | 2014-03-14 | 2017-08-30 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| US10221459B2 (en) | 2014-05-13 | 2019-03-05 | Case Western Reserve University | Compositions and methods of treating cancer harboring PIKC3A mutations |
| KR20170012562A (ko) | 2014-06-13 | 2017-02-02 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제 억제제를 사용하는 병용 요법 |
| WO2016004418A1 (en) | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Glutaminase inhibitor therapy |
| WO2016014890A1 (en) | 2014-07-24 | 2016-01-28 | Calithera Biosciences, Inc. | Treatment of multiple myeloma with heterocyclic inhibitors of glutaminase |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| US10245254B2 (en) | 2014-10-03 | 2019-04-02 | University of Pittsburgh—of the Commonwealth System of Higher Education | Glutaminase inhibitors |
| WO2016077632A2 (en) | 2014-11-13 | 2016-05-19 | Buck Institute For Research On Aging | Inhibition of proline catabolism for the treatment of cancer and other therapeutic applications |
-
2015
- 2015-06-12 KR KR1020177000816A patent/KR20170012562A/ko not_active Withdrawn
- 2015-06-12 CN CN201580043239.XA patent/CN107027291B/zh not_active Expired - Fee Related
- 2015-06-12 BR BR112016029041A patent/BR112016029041A8/pt not_active Application Discontinuation
- 2015-06-12 EA EA201692511A patent/EA036001B1/ru not_active IP Right Cessation
- 2015-06-12 AU AU2015274361A patent/AU2015274361B2/en not_active Ceased
- 2015-06-12 EP EP15805792.7A patent/EP3154590B1/en active Active
- 2015-06-12 CA CA2952213A patent/CA2952213A1/en not_active Abandoned
- 2015-06-12 MX MX2016016364A patent/MX374924B/es active IP Right Grant
- 2015-06-12 JP JP2016572636A patent/JP6798890B2/ja not_active Expired - Fee Related
- 2015-06-12 SG SG11201610333VA patent/SG11201610333VA/en unknown
- 2015-06-12 US US14/738,279 patent/US9687485B2/en not_active Expired - Fee Related
- 2015-06-12 WO PCT/US2015/035577 patent/WO2015192014A1/en not_active Ceased
-
2016
- 2016-12-11 IL IL249476A patent/IL249476A0/en active IP Right Grant
-
2017
- 2017-05-03 US US15/585,523 patent/US20170333430A1/en not_active Abandoned
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