CN105051041B - 杂环谷氨酰胺酶抑制剂 - Google Patents
杂环谷氨酰胺酶抑制剂 Download PDFInfo
- Publication number
- CN105051041B CN105051041B CN201380069950.3A CN201380069950A CN105051041B CN 105051041 B CN105051041 B CN 105051041B CN 201380069950 A CN201380069950 A CN 201380069950A CN 105051041 B CN105051041 B CN 105051041B
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- China
- Prior art keywords
- alkyl
- aryl
- represent
- heteroaryl
- compound
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- 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)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (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 | |
| US61/727195 | 2012-11-16 | ||
| US201361824434P | 2013-05-17 | 2013-05-17 | |
| US61/824434 | 2013-05-17 | ||
| PCT/US2013/070277 WO2014078645A1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic glutaminase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105051041A CN105051041A (zh) | 2015-11-11 |
| CN105051041B true CN105051041B (zh) | 2018-03-30 |
Family
ID=50731715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380069950.3A Active CN105051041B (zh) | 2012-11-16 | 2013-11-15 | 杂环谷氨酰胺酶抑制剂 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US10793535B2 (https=) |
| EP (2) | EP2920168B1 (https=) |
| JP (1) | JP6275153B2 (https=) |
| KR (1) | KR102220175B1 (https=) |
| CN (1) | CN105051041B (https=) |
| AU (1) | AU2013344560B2 (https=) |
| BR (1) | BR112015010955A2 (https=) |
| CA (1) | CA2891667A1 (https=) |
| CY (1) | CY1125279T1 (https=) |
| DK (1) | DK2920168T3 (https=) |
| EA (1) | EA029707B1 (https=) |
| ES (1) | ES2899461T3 (https=) |
| HR (1) | HRP20211610T1 (https=) |
| HU (1) | HUE056078T2 (https=) |
| IL (1) | IL238787A0 (https=) |
| LT (1) | LT2920168T (https=) |
| MX (1) | MX381260B (https=) |
| PL (1) | PL2920168T3 (https=) |
| PT (1) | PT2920168T (https=) |
| RS (1) | RS62447B1 (https=) |
| SG (1) | SG11201503720SA (https=) |
| SI (1) | SI2920168T1 (https=) |
| SM (1) | SMT202100589T1 (https=) |
| WO (1) | WO2014078645A1 (https=) |
| ZA (2) | ZA201504294B (https=) |
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 |
| BR112015010955A2 (pt) | 2012-11-16 | 2017-07-11 | Calithera Biosciences Inc | inibidores de glutaminase heterocíclica |
| BR112015012536A2 (pt) * | 2012-12-03 | 2017-07-11 | Calithera Biosciences Inc | tratamento de câncer com inibidores heterocíclicos da glutaminase |
| CA2934700A1 (en) | 2014-01-06 | 2015-07-09 | Rhizen Pharmaceuticals Sa | Glutaminase inhibitors |
| EP3556757A1 (en) * | 2014-04-30 | 2019-10-23 | Pfizer Inc | Cycloalkyl-linked diheterocycle derivatives |
| GB201409624D0 (en) | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| KR20170012562A (ko) * | 2014-06-13 | 2017-02-02 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제 억제제를 사용하는 병용 요법 |
| WO2016004404A2 (en) * | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| WO2016004413A2 (en) * | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| ES2921989T3 (es) * | 2014-07-03 | 2022-09-05 | Univ Texas | Terapia con inhibidores de glutaminasa |
| 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 |
| CN107921031A (zh) * | 2015-03-30 | 2018-04-17 | 卡利泰拉生物科技公司 | 给予谷氨酰胺酶抑制剂的方法 |
| BR112017021312A2 (pt) * | 2015-04-06 | 2018-06-26 | Calithera Biosciences Inc | tratamento de câncer de pulmão com inibidores de glutaminase |
| WO2017004359A1 (en) * | 2015-06-30 | 2017-01-05 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| 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 |
| US10323028B2 (en) * | 2015-11-30 | 2019-06-18 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| US9938265B2 (en) * | 2015-11-30 | 2018-04-10 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| SG11201804664XA (en) | 2015-12-22 | 2018-07-30 | Univ Texas | Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1h-1,2,3-triazole-4-carboxamide |
| WO2018039441A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| WO2018039442A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Treatment of cancer with inhibitors of glutaminase |
| KR20190040302A (ko) * | 2016-08-25 | 2019-04-17 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 글루타미나제 억제제와의 병용 요법 |
| ES2903182T3 (es) | 2017-06-13 | 2022-03-31 | Medshine Discovery Inc | Compuesto como inhibidor GLS1 |
| RU2020112558A (ru) | 2017-10-18 | 2021-11-18 | Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем | Терапия на основе ингибитора глутаминазы |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011143160A2 (en) * | 2010-05-10 | 2011-11-17 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
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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 |
| 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 |
| US6310093B1 (en) | 1997-08-29 | 2001-10-30 | Elan Pharmaceuticals, Inc. | Method of preventing neuronal death |
| 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 |
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| US20110281234A1 (en) | 2010-05-12 | 2011-11-17 | Colton Crane | System and methods for removing a loose tooth |
| WO2012006506A1 (en) * | 2010-07-09 | 2012-01-12 | 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 |
| US8604016B2 (en) * | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| ES2761866T3 (es) * | 2011-11-21 | 2020-05-21 | Calithera Biosciences Inc | Inhibidores heterocíclicos de glutaminasa |
| 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 |
| 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 |
| 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 |
| KR20170012562A (ko) | 2014-06-13 | 2017-02-02 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제 억제제를 사용하는 병용 요법 |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| CN107921031A (zh) | 2015-03-30 | 2018-04-17 | 卡利泰拉生物科技公司 | 给予谷氨酰胺酶抑制剂的方法 |
| BR112017021312A2 (pt) | 2015-04-06 | 2018-06-26 | Calithera Biosciences Inc | tratamento de câncer de pulmão com inibidores de 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 |
| KR20190040302A (ko) | 2016-08-25 | 2019-04-17 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 글루타미나제 억제제와의 병용 요법 |
| WO2018165516A1 (en) | 2017-03-10 | 2018-09-13 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
-
2013
- 2013-11-15 BR BR112015010955A patent/BR112015010955A2/pt not_active Application Discontinuation
- 2013-11-15 SG SG11201503720SA patent/SG11201503720SA/en unknown
- 2013-11-15 KR KR1020157015874A patent/KR102220175B1/ko active Active
- 2013-11-15 PT PT138550397T patent/PT2920168T/pt unknown
- 2013-11-15 CA CA2891667A patent/CA2891667A1/en not_active Abandoned
- 2013-11-15 EP EP13855039.7A patent/EP2920168B1/en active Active
- 2013-11-15 PL PL13855039T patent/PL2920168T3/pl unknown
- 2013-11-15 EP EP21184626.6A patent/EP3954686A1/en not_active Withdrawn
- 2013-11-15 HR HRP20211610TT patent/HRP20211610T1/hr unknown
- 2013-11-15 RS RS20211273A patent/RS62447B1/sr unknown
- 2013-11-15 CN CN201380069950.3A patent/CN105051041B/zh active Active
- 2013-11-15 JP JP2015542813A patent/JP6275153B2/ja active Active
- 2013-11-15 US US14/081,175 patent/US10793535B2/en active Active
- 2013-11-15 HU HUE13855039A patent/HUE056078T2/hu unknown
- 2013-11-15 DK DK13855039.7T patent/DK2920168T3/da active
- 2013-11-15 SI SI201331934T patent/SI2920168T1/sl unknown
- 2013-11-15 ES ES13855039T patent/ES2899461T3/es active Active
- 2013-11-15 AU AU2013344560A patent/AU2013344560B2/en active Active
- 2013-11-15 LT LTEPPCT/US2013/070277T patent/LT2920168T/lt unknown
- 2013-11-15 SM SM20210589T patent/SMT202100589T1/it unknown
- 2013-11-15 EA EA201590941A patent/EA029707B1/ru not_active IP Right Cessation
- 2013-11-15 MX MX2015005963A patent/MX381260B/es unknown
- 2013-11-15 WO PCT/US2013/070277 patent/WO2014078645A1/en not_active Ceased
-
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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011143160A2 (en) * | 2010-05-10 | 2011-11-17 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
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| Structural basis for the allosteric inhibitorymechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism;Thangavelu et al.;《proceedings of the national academy of sciences of the united states of america》;20120515;第109卷(第20期);7705–7710 * |
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| UBER DIE EINWIRKUNG VON ISOCYANATEN AUF SUBSTITUIERTE 2-AMINO-1.3.4-OXDIAZOLE;GEHELEN,H.,等;《JUSTUS LIEBIGS ANNALEN DER CHEMIE》;19661231;第692卷;151-165 * |
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