PE20151072A1 - Derivados de (cicloalquilen) bis (1, 3, 4-tiadiazol) como inhibidores de glutaminasa - Google Patents
Derivados de (cicloalquilen) bis (1, 3, 4-tiadiazol) como inhibidores de glutaminasaInfo
- Publication number
- PE20151072A1 PE20151072A1 PE2015000674A PE2015000674A PE20151072A1 PE 20151072 A1 PE20151072 A1 PE 20151072A1 PE 2015000674 A PE2015000674 A PE 2015000674A PE 2015000674 A PE2015000674 A PE 2015000674A PE 20151072 A1 PE20151072 A1 PE 20151072A1
- Authority
- PE
- Peru
- Prior art keywords
- cycloalkylene
- compounds
- tiadiazol
- bis
- derivatives
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Abstract
En la presente se describen compuestos y composiciones que comprenden compuestos que inhiben la glutaminasa. En la presente tambien se describen metodos para emplear los compuestos que inhiben la glutaminasa en el tratamiento del cancer. Los compuestos de la invencion son de formula (I), donde X es cicloalquileno C3-C7; W, Y y Z son S, etc; R1, R2 son NH2, etc; R3 es H, etc, R6 es H, etc, m y n son 0, 1 o 2, o y p son 1, 2 o 3. Los compuestos preferidos son (S)-N-(5-((1S,3S)-3-(5-(2-(6-(3,3-difluoroazetidin-1-il)piridin-2-il)acetamido)-1,3,4-tiadiazol-2-il) ciclohexil)-1, 3, 4-tiadiazol-2-il) -2-hidroxi-2-fenilacetamida; 2-(6-(3,3-difluoroazetidin-1-il) piridin-2-il)-N-(5-((1S, 3S)-3-(5-(2-(3-(trifluorometoxi) fenil)acetamido)-1, 3, 4-tiadiazol-2-il) ciclohexil) -1, 3, 4-tiadiazol-2-il) acetamida
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2012/085023 WO2014079011A1 (en) | 2012-11-22 | 2012-11-22 | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
PCT/CN2013/000294 WO2014079136A1 (en) | 2012-11-22 | 2013-03-15 | Compounds, pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof |
PCT/CN2013/001428 WO2014079150A1 (en) | 2012-11-22 | 2013-11-21 | Compounds and their methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20151072A1 true PE20151072A1 (es) | 2015-08-26 |
Family
ID=50775393
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2015000674A PE20151072A1 (es) | 2012-11-22 | 2013-11-21 | Derivados de (cicloalquilen) bis (1, 3, 4-tiadiazol) como inhibidores de glutaminasa |
Country Status (36)
Country | Link |
---|---|
US (2) | US10087172B2 (es) |
EP (2) | EP2922850B1 (es) |
JP (2) | JP6333277B2 (es) |
KR (1) | KR20150085079A (es) |
CN (2) | CN108727307A (es) |
AR (1) | AR093598A1 (es) |
AU (2) | AU2013347771B2 (es) |
BR (1) | BR112015011830A2 (es) |
CA (1) | CA2893510C (es) |
CL (1) | CL2015001392A1 (es) |
CR (1) | CR20150316A (es) |
CY (1) | CY1120581T1 (es) |
DK (1) | DK2922850T3 (es) |
EA (2) | EA201890754A1 (es) |
EC (1) | ECSP15026557A (es) |
ES (1) | ES2690390T3 (es) |
HK (1) | HK1214593A1 (es) |
HR (1) | HRP20181628T1 (es) |
HU (1) | HUE040111T2 (es) |
IL (1) | IL238958B (es) |
LT (1) | LT2922850T (es) |
MX (1) | MX367389B (es) |
MY (1) | MY177344A (es) |
NZ (1) | NZ708382A (es) |
PE (1) | PE20151072A1 (es) |
PH (2) | PH12015501150B1 (es) |
PL (1) | PL2922850T3 (es) |
PT (1) | PT2922850T (es) |
RS (1) | RS57859B1 (es) |
SA (1) | SA515360469B1 (es) |
SG (2) | SG10201609940RA (es) |
SI (1) | SI2922850T1 (es) |
TR (1) | TR201812360T4 (es) |
TW (2) | TW201906825A (es) |
UA (1) | UA117360C2 (es) |
WO (3) | WO2014079011A1 (es) |
Families Citing this family (35)
Publication number | Priority date | Publication date | Assignee | Title |
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US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
DK2920168T3 (da) | 2012-11-16 | 2021-10-18 | Calithera Biosciences Inc | Heterocykliske glutaminase-inhibitorer |
US10011574B2 (en) | 2012-11-21 | 2018-07-03 | Agios Pharmaceuticals, Inc. | Glutaminase 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 |
CN105283182A (zh) * | 2012-12-03 | 2016-01-27 | 卡利泰拉生物科技公司 | 用谷氨酰胺酶的杂环抑制剂治疗癌症 |
WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
EA035929B1 (ru) | 2013-01-15 | 2020-09-02 | Инсайт Холдингс Корпорейшн | ТИАЗОЛКАРБОКСАМИДЫ И ПИРИДИНКАРБОКСАМИДЫ, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Pim-КИНАЗЫ |
SG11201601259YA (en) | 2013-08-23 | 2016-03-30 | Incyte Corp | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
CA2934700A1 (en) | 2014-01-06 | 2015-07-09 | Rhizen Pharmaceuticals Sa | Glutaminase inhibitors |
KR20160127149A (ko) | 2014-03-21 | 2016-11-02 | 아지오스 파마슈티컬스 아이엔씨. | 화합물 및 이의 사용 방법 |
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 |
BR112016030730B1 (pt) * | 2014-07-03 | 2023-05-02 | Board Of Regents, The University Of Texas System | Composto |
WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
WO2016014890A1 (en) * | 2014-07-24 | 2016-01-28 | Calithera Biosciences, Inc. | Treatment of multiple myeloma with heterocyclic inhibitors of glutaminase |
MX2017001620A (es) | 2014-08-07 | 2017-05-10 | Calithera Biosciences Inc | Formas cristalinas de inhibidores de glutaminasa. |
US10245254B2 (en) | 2014-10-03 | 2019-04-02 | University of Pittsburgh—of the Commonwealth System of Higher Education | Glutaminase inhibitors |
US10441587B2 (en) | 2015-04-06 | 2019-10-15 | Calithera Biosciences, Inc. | Treatment of lung cancer with inhibitors of glutaminase |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
CN107921044B (zh) | 2015-06-30 | 2022-01-21 | 德州大学***董事会 | 用于治疗疾病的gls1抑制剂 |
TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
US10258619B2 (en) | 2015-10-05 | 2019-04-16 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors and immuno-oncology agents |
US10040789B2 (en) * | 2015-11-30 | 2018-08-07 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
CN109503570B (zh) * | 2015-12-18 | 2020-08-25 | 诺言医药科技(上海)有限公司 | 一种含有索拉非尼的药物组合物及其应用 |
CA3009355A1 (en) | 2015-12-22 | 2017-06-29 | Board Of Regents, The University Of Texas System | 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 |
JP2019524852A (ja) | 2016-08-25 | 2019-09-05 | キャリセラ バイオサイエンシーズ, インコーポレイテッド | グルタミナーゼ阻害剤を用いる併用療法 |
JP2019526560A (ja) * | 2016-08-25 | 2019-09-19 | キャリセラ バイオサイエンシーズ, インコーポレイテッド | グルタミナーゼ阻害剤との併用療法 |
RU2020112558A (ru) | 2017-10-18 | 2021-11-18 | Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем | Терапия на основе ингибитора глутаминазы |
TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
WO2020096916A2 (en) | 2018-11-08 | 2020-05-14 | Merck Sharp & Dohme Corp. | Inhibitors of histone deacetylase useful for the treatment or prevention of hiv infection |
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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 |
CN112898200A (zh) * | 2021-01-20 | 2021-06-04 | 都创(上海)医药科技股份有限公司 | 5-溴-6-甲氧基吡啶-2-羧酸酯的合成方法 |
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WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
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2012
- 2012-11-22 WO PCT/CN2012/085023 patent/WO2014079011A1/en active Application Filing
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2013
- 2013-03-15 WO PCT/CN2013/000294 patent/WO2014079136A1/en active Application Filing
- 2013-11-21 EA EA201890754A patent/EA201890754A1/ru unknown
- 2013-11-21 PT PT13857585T patent/PT2922850T/pt unknown
- 2013-11-21 WO PCT/CN2013/001428 patent/WO2014079150A1/en active Application Filing
- 2013-11-21 PE PE2015000674A patent/PE20151072A1/es unknown
- 2013-11-21 JP JP2015543242A patent/JP6333277B2/ja not_active Expired - Fee Related
- 2013-11-21 SG SG10201609940RA patent/SG10201609940RA/en unknown
- 2013-11-21 NZ NZ708382A patent/NZ708382A/en unknown
- 2013-11-21 SG SG11201504049VA patent/SG11201504049VA/en unknown
- 2013-11-21 CN CN201810824418.2A patent/CN108727307A/zh active Pending
- 2013-11-21 EP EP13857585.7A patent/EP2922850B1/en active Active
- 2013-11-21 EP EP18183580.2A patent/EP3456719A1/en not_active Withdrawn
- 2013-11-21 US US14/646,634 patent/US10087172B2/en active Active
- 2013-11-21 UA UAA201506066A patent/UA117360C2/uk unknown
- 2013-11-21 KR KR1020157016414A patent/KR20150085079A/ko not_active Application Discontinuation
- 2013-11-21 MY MYPI2015001355A patent/MY177344A/en unknown
- 2013-11-21 LT LTEP13857585.7T patent/LT2922850T/lt unknown
- 2013-11-21 CN CN201380070365.5A patent/CN104936954B/zh not_active Expired - Fee Related
- 2013-11-21 ES ES13857585.7T patent/ES2690390T3/es active Active
- 2013-11-21 BR BR112015011830A patent/BR112015011830A2/pt not_active Application Discontinuation
- 2013-11-21 EA EA201590987A patent/EA030646B1/ru not_active IP Right Cessation
- 2013-11-21 HU HUE13857585A patent/HUE040111T2/hu unknown
- 2013-11-21 CA CA2893510A patent/CA2893510C/en active Active
- 2013-11-21 AU AU2013347771A patent/AU2013347771B2/en not_active Ceased
- 2013-11-21 DK DK13857585.7T patent/DK2922850T3/en active
- 2013-11-21 PL PL13857585T patent/PL2922850T3/pl unknown
- 2013-11-21 RS RS20181133A patent/RS57859B1/sr unknown
- 2013-11-21 TR TR2018/12360T patent/TR201812360T4/tr unknown
- 2013-11-21 MX MX2015006493A patent/MX367389B/es active IP Right Grant
- 2013-11-21 SI SI201331140T patent/SI2922850T1/sl unknown
- 2013-11-22 TW TW107111990A patent/TW201906825A/zh unknown
- 2013-11-22 AR ARP130104322A patent/AR093598A1/es unknown
- 2013-11-22 TW TW102142566A patent/TWI629268B/zh not_active IP Right Cessation
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2015
- 2015-05-21 IL IL238958A patent/IL238958B/en not_active IP Right Cessation
- 2015-05-22 PH PH12015501150A patent/PH12015501150B1/en unknown
- 2015-05-22 CL CL2015001392A patent/CL2015001392A1/es unknown
- 2015-05-22 SA SA515360469A patent/SA515360469B1/ar unknown
- 2015-06-15 CR CR20150316A patent/CR20150316A/es unknown
- 2015-06-22 EC ECIEPI201526557A patent/ECSP15026557A/es unknown
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2016
- 2016-03-04 HK HK16102486.9A patent/HK1214593A1/zh not_active IP Right Cessation
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2017
- 2017-11-24 PH PH12017502141A patent/PH12017502141A1/en unknown
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2018
- 2018-04-24 JP JP2018082754A patent/JP2018150316A/ja active Pending
- 2018-04-30 AU AU2018202954A patent/AU2018202954A1/en not_active Abandoned
- 2018-08-17 CY CY20181100864T patent/CY1120581T1/el unknown
- 2018-08-21 US US16/107,220 patent/US10689375B2/en active Active
- 2018-10-10 HR HRP20181628TT patent/HRP20181628T1/hr unknown
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