JP6275153B2 - ヘテロ環式グルタミナーゼ阻害剤 - Google Patents
ヘテロ環式グルタミナーゼ阻害剤 Download PDFInfo
- Publication number
- JP6275153B2 JP6275153B2 JP2015542813A JP2015542813A JP6275153B2 JP 6275153 B2 JP6275153 B2 JP 6275153B2 JP 2015542813 A JP2015542813 A JP 2015542813A JP 2015542813 A JP2015542813 A JP 2015542813A JP 6275153 B2 JP6275153 B2 JP 6275153B2
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- compound
- pharmaceutically acceptable
- substituted
- acceptable salt
- 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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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/135—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261727195P | 2012-11-16 | 2012-11-16 | |
| US61/727,195 | 2012-11-16 | ||
| US201361824434P | 2013-05-17 | 2013-05-17 | |
| US61/824,434 | 2013-05-17 | ||
| PCT/US2013/070277 WO2014078645A1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic glutaminase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505526A JP2016505526A (ja) | 2016-02-25 |
| JP2016505526A5 JP2016505526A5 (OSRAM) | 2017-01-05 |
| JP6275153B2 true JP6275153B2 (ja) | 2018-02-07 |
Family
ID=50731715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542813A Active JP6275153B2 (ja) | 2012-11-16 | 2013-11-15 | ヘテロ環式グルタミナーゼ阻害剤 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US10793535B2 (OSRAM) |
| EP (2) | EP3954686A1 (OSRAM) |
| JP (1) | JP6275153B2 (OSRAM) |
| KR (1) | KR102220175B1 (OSRAM) |
| CN (1) | CN105051041B (OSRAM) |
| AU (1) | AU2013344560B2 (OSRAM) |
| BR (1) | BR112015010955A2 (OSRAM) |
| CA (1) | CA2891667A1 (OSRAM) |
| CY (1) | CY1125279T1 (OSRAM) |
| DK (1) | DK2920168T3 (OSRAM) |
| EA (1) | EA029707B1 (OSRAM) |
| ES (1) | ES2899461T3 (OSRAM) |
| HR (1) | HRP20211610T1 (OSRAM) |
| HU (1) | HUE056078T2 (OSRAM) |
| IL (1) | IL238787A0 (OSRAM) |
| LT (1) | LT2920168T (OSRAM) |
| MX (1) | MX381260B (OSRAM) |
| PL (1) | PL2920168T3 (OSRAM) |
| PT (1) | PT2920168T (OSRAM) |
| RS (1) | RS62447B1 (OSRAM) |
| SG (1) | SG11201503720SA (OSRAM) |
| SI (1) | SI2920168T1 (OSRAM) |
| SM (1) | SMT202100589T1 (OSRAM) |
| WO (1) | WO2014078645A1 (OSRAM) |
| ZA (2) | ZA201504294B (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| EP3954686A1 (en) | 2012-11-16 | 2022-02-16 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| KR20150091389A (ko) * | 2012-12-03 | 2015-08-10 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제의 헤테로사이클릭 억제제에 의한 암 치료 |
| KR20160100407A (ko) | 2014-01-06 | 2016-08-23 | 리젠 파마슈티컬스 소시에떼 아노님 | 신규한 글루타미나제의 저해제 |
| EA033919B1 (ru) | 2014-04-30 | 2019-12-10 | Пфайзер Инк. | Соединённые циклоалкилом дигетероциклические производные |
| GB201409624D0 (en) | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| BR112016029041A8 (pt) | 2014-06-13 | 2021-07-20 | Calithera Biosciences Inc | uso de um inibidor de glutaminase, composição farmacêutica e kit farmacêutico |
| EP3164195B1 (en) * | 2014-07-03 | 2022-06-15 | Board of Regents, The University of Texas System | Glutaminase inhibitor therapy |
| HUE049600T2 (hu) | 2014-07-03 | 2020-10-28 | Univ Texas | GLS1 inhibitorok betegségek kezelésére |
| WO2016004413A2 (en) * | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| US10660861B2 (en) | 2014-07-09 | 2020-05-26 | The Johns Hopkins University | Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy |
| CA2957225A1 (en) * | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| EP3277276B1 (en) * | 2015-03-30 | 2020-11-04 | Calithera Biosciences, Inc. | Methods of administering glutaminase inhibitors |
| SG11201708153XA (en) * | 2015-04-06 | 2017-11-29 | Calithera Biosciences Inc | Treatment of lung cancer with inhibitors of glutaminase |
| CA2990457C (en) * | 2015-06-30 | 2024-07-02 | Board Of Regents, University Of Texas System | PYRROLIDINYL AND PIPERIDINYL DERIVATIVES AND RELATED PHARMACEUTICAL COMPOSITIONS USEFUL AS GLS1 INHIBITORS |
| CN108601767A (zh) | 2015-10-05 | 2018-09-28 | 卡利泰拉生物科技公司 | 用谷氨酰胺酶抑制剂和免疫肿瘤学药剂的组合疗法 |
| TW201730188A (zh) * | 2015-11-30 | 2017-09-01 | 阿斯特捷利康公司 | 1,3,4-噻二唑化合物及其在治療癌症中之用途 |
| US10323028B2 (en) * | 2015-11-30 | 2019-06-18 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| KR102777513B1 (ko) | 2015-12-22 | 2025-03-06 | 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 | (ｒ)-1-(4-(6-(2-(4-(3,3-디플루오로시클로부톡시)-6-메틸피리딘-2-일)아세트아미도)피리다진-3-일)-2-플루오로부틸)-ｎ-메틸-1ｈ-1,2,3-트리아졸-4-카르복사미드의 염 형태 및 다형체 |
| BR112019003533A2 (pt) * | 2016-08-25 | 2019-05-21 | Calithera Biosciences Inc. | terapia de combinação com inibidores de glutaminase |
| WO2018039442A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Treatment of cancer with inhibitors of glutaminase |
| WO2018039441A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| JP7275053B2 (ja) * | 2017-06-13 | 2023-05-17 | メッドシャイン ディスカバリー インコーポレイテッド | Ｇｌｓ１阻害剤としての化合物 |
| US10722487B2 (en) | 2017-10-18 | 2020-07-28 | Board Of Regents, The University Of Texas System | Glutaminase inhibitor therapy |
| CN110746416A (zh) * | 2019-09-05 | 2020-02-04 | 中国药科大学 | 含有三氮唑结构的谷氨酰胺酶gls1抑制剂或其可药用的盐、其制备方法及用途 |
| CN114805346A (zh) * | 2021-07-08 | 2022-07-29 | 成都硕德药业有限公司 | 杂环类衍生物、其制备方法及用途 |
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| US1019519A (en) | 1911-07-11 | 1912-03-05 | Oscar Martin Polin | Apparatus for making backing for teeth. |
| 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 |
| US5541231A (en) | 1993-07-30 | 1996-07-30 | Glaxo Wellcome Inc. | Stabilized Pharmaceutical |
| GB9315856D0 (en) | 1993-07-30 | 1993-09-15 | Wellcome Found | Stabilized pharmaceutical |
| US5358970A (en) | 1993-08-12 | 1994-10-25 | Burroughs Wellcome Co. | Pharmaceutical composition containing bupropion hydrochloride and a stabilizer |
| US6403609B1 (en) | 1997-07-29 | 2002-06-11 | Alcon Manufacturing, Ltd. | Ophthalmic compositions containing galactomannan polymers and borate |
| US6310093B1 (en) | 1997-08-29 | 2001-10-30 | Elan Pharmaceuticals, Inc. | Method of preventing neuronal death |
| CA2318920A1 (en) | 1998-01-29 | 1999-08-05 | James W. Young | Pharmaceutical uses of 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 |
| DE602004023516D1 (de) | 2003-08-07 | 2009-11-19 | Allergan Inc | Zusammensetzungen zur abgabe von therapeutika in die augen und verfahren zu ihrer herstellung und verwendung |
| 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 |
| ES2367311T3 (es) | 2004-04-15 | 2011-11-02 | University Of Florida Research Foundation, Inc. | Productos de degradación proteolítica de map-2 como biomarcadores de diagnóstico para las lesiones neurales. |
| WO2011143160A2 (en) * | 2010-05-10 | 2011-11-17 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| US20110281234A1 (en) | 2010-05-12 | 2011-11-17 | Colton Crane | System and methods for removing a loose tooth |
| US10064885B2 (en) * | 2010-07-09 | 2018-09-04 | Massachusetts Institute Of Technology | Metabolic gene, enzyme, and flux targets for cancer therapy |
| 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 |
| FI20115876A0 (fi) | 2011-09-06 | 2011-09-06 | Turun Yliopisto | Yhdistelmähoito |
| EA026656B1 (ru) * | 2011-11-21 | 2017-05-31 | Калитера Байосайенсиз Инк. | Гетероциклические ингибиторы глютаминазы |
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| EP3954686A1 (en) | 2012-11-16 | 2022-02-16 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| HK1213889A1 (zh) | 2012-11-21 | 2016-07-15 | 安吉奥斯医药品有限公司 | 殼氨醯胺酶抑制劑及使用方法 |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| US9029531B2 (en) | 2012-11-22 | 2015-05-12 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| KR20150091389A (ko) | 2012-12-03 | 2015-08-10 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제의 헤테로사이클릭 억제제에 의한 암 치료 |
| WO2015061432A1 (en) | 2013-10-25 | 2015-04-30 | Calithera Biosciences, Inc. | Treatment of viral infections with inhibitors of glutaminase |
| US20150258082A1 (en) | 2014-03-14 | 2015-09-17 | Francesco Parlati | Combination therapy with glutaminase inhibitors |
| BR112016029041A8 (pt) | 2014-06-13 | 2021-07-20 | Calithera Biosciences Inc | uso de um inibidor de glutaminase, composição farmacêutica e kit farmacêutico |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| EP3277276B1 (en) | 2015-03-30 | 2020-11-04 | Calithera Biosciences, Inc. | Methods of administering glutaminase inhibitors |
| SG11201708153XA (en) | 2015-04-06 | 2017-11-29 | Calithera Biosciences Inc | Treatment of lung cancer with inhibitors of glutaminase |
| CN108601767A (zh) | 2015-10-05 | 2018-09-28 | 卡利泰拉生物科技公司 | 用谷氨酰胺酶抑制剂和免疫肿瘤学药剂的组合疗法 |
| BR112019003533A2 (pt) | 2016-08-25 | 2019-05-21 | Calithera Biosciences Inc. | terapia de combinação com inibidores de glutaminase |
| EP3592354A4 (en) | 2017-03-10 | 2021-04-07 | Calithera Biosciences, Inc. | COMBINATION THERAPY WITH GLUTAMINASE INHIBITORS |
-
2013
- 2013-11-15 EP EP21184626.6A patent/EP3954686A1/en not_active Withdrawn
- 2013-11-15 RS RS20211273A patent/RS62447B1/sr unknown
- 2013-11-15 SI SI201331934T patent/SI2920168T1/sl unknown
- 2013-11-15 HR HRP20211610TT patent/HRP20211610T1/hr unknown
- 2013-11-15 KR KR1020157015874A patent/KR102220175B1/ko active Active
- 2013-11-15 AU AU2013344560A patent/AU2013344560B2/en active Active
- 2013-11-15 JP JP2015542813A patent/JP6275153B2/ja active Active
- 2013-11-15 PL PL13855039T patent/PL2920168T3/pl unknown
- 2013-11-15 SM SM20210589T patent/SMT202100589T1/it unknown
- 2013-11-15 DK DK13855039.7T patent/DK2920168T3/da active
- 2013-11-15 BR BR112015010955A patent/BR112015010955A2/pt not_active Application Discontinuation
- 2013-11-15 WO PCT/US2013/070277 patent/WO2014078645A1/en not_active Ceased
- 2013-11-15 US US14/081,175 patent/US10793535B2/en active Active
- 2013-11-15 CA CA2891667A patent/CA2891667A1/en not_active Abandoned
- 2013-11-15 PT PT138550397T patent/PT2920168T/pt unknown
- 2013-11-15 CN CN201380069950.3A patent/CN105051041B/zh active Active
- 2013-11-15 ES ES13855039T patent/ES2899461T3/es active Active
- 2013-11-15 HU HUE13855039A patent/HUE056078T2/hu unknown
- 2013-11-15 SG SG11201503720SA patent/SG11201503720SA/en unknown
- 2013-11-15 EA EA201590941A patent/EA029707B1/ru not_active IP Right Cessation
- 2013-11-15 LT LTEPPCT/US2013/070277T patent/LT2920168T/lt unknown
- 2013-11-15 EP EP13855039.7A patent/EP2920168B1/en active Active
- 2013-11-15 MX MX2015005963A patent/MX381260B/es unknown
-
2015
- 2015-05-13 IL IL238787A patent/IL238787A0/en unknown
- 2015-06-12 ZA ZA2015/04294A patent/ZA201504294B/en unknown
-
2016
- 2016-09-23 ZA ZA2016/06590A patent/ZA201606590B/en unknown
-
2020
- 2020-10-05 US US17/063,066 patent/US20210292289A1/en not_active Abandoned
-
2021
- 2021-10-19 CY CY20211100905T patent/CY1125279T1/el unknown
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