JP2017505808A5 - - Google Patents
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- Publication number
- JP2017505808A5 JP2017505808A5 JP2016562078A JP2016562078A JP2017505808A5 JP 2017505808 A5 JP2017505808 A5 JP 2017505808A5 JP 2016562078 A JP2016562078 A JP 2016562078A JP 2016562078 A JP2016562078 A JP 2016562078A JP 2017505808 A5 JP2017505808 A5 JP 2017505808A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- thiadiazol
- acetamido
- pyridin
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 14
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- -1 nitro, amino Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 102000009127 Glutaminase Human genes 0.000 claims 4
- 108010073324 Glutaminase Proteins 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
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- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 3
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- 239000000203 mixture Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
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- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
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- 208000015338 Autoimmune hepatitis type 1 Diseases 0.000 claims 1
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
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- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000003923 Hereditary Corneal Dystrophies Diseases 0.000 claims 1
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- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
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- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
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- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
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- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 241000243985 Onchocerca volvulus Species 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
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- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
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- 206010038389 Renal cancer Diseases 0.000 claims 1
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- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
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- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
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- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
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- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
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Applications Claiming Priority (19)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN39CH2014 | 2014-01-06 | ||
| IN39/CHE/2014 | 2014-01-06 | ||
| IN36/CHE/2014 | 2014-01-06 | ||
| IN36CH2014 | 2014-01-06 | ||
| IN2647/CHE/2014 | 2014-05-29 | ||
| IN2639CH2014 | 2014-05-29 | ||
| IN2647CH2014 | 2014-05-29 | ||
| IN2639/CHE/2014 | 2014-05-29 | ||
| IN2783CH2014 | 2014-06-06 | ||
| IN2783/CHE/2014 | 2014-06-06 | ||
| IN3525/CHE/2014 | 2014-07-18 | ||
| IN3525CH2014 | 2014-07-18 | ||
| IN3612CH2014 | 2014-07-24 | ||
| IN3613CH2014 | 2014-07-24 | ||
| IN3612/CHE/2014 | 2014-07-24 | ||
| IN3613/CHE/2014 | 2014-07-24 | ||
| IN5438CH2014 | 2014-10-31 | ||
| IN5438/CHE/2014 | 2014-10-31 | ||
| PCT/IB2015/050075 WO2015101957A2 (en) | 2014-01-06 | 2015-01-05 | Novel glutaminase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019090711A Division JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505808A JP2017505808A (ja) | 2017-02-23 |
| JP2017505808A5 true JP2017505808A5 (enExample) | 2018-01-25 |
| JP6783663B2 JP6783663B2 (ja) | 2020-11-11 |
Family
ID=52478027
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016562079A Expired - Fee Related JP6666263B2 (ja) | 2014-01-06 | 2015-01-05 | グルタミナーゼの新規阻害剤 |
| JP2016562078A Expired - Fee Related JP6783663B2 (ja) | 2014-01-06 | 2015-01-05 | 新規グルタミナーゼ阻害剤 |
| JP2019090711A Pending JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016562079A Expired - Fee Related JP6666263B2 (ja) | 2014-01-06 | 2015-01-05 | グルタミナーゼの新規阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019090711A Pending JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US20160297761A1 (enExample) |
| EP (2) | EP3092236B1 (enExample) |
| JP (3) | JP6666263B2 (enExample) |
| KR (3) | KR20220013017A (enExample) |
| CN (5) | CN105960405B (enExample) |
| AU (1) | AU2015204210B2 (enExample) |
| BR (1) | BR112016015706A8 (enExample) |
| CA (2) | CA2934700A1 (enExample) |
| CL (1) | CL2016001715A1 (enExample) |
| DK (1) | DK3092236T3 (enExample) |
| EA (3) | EA035499B1 (enExample) |
| ES (1) | ES2833576T3 (enExample) |
| IL (1) | IL246362B (enExample) |
| SG (1) | SG11201605478XA (enExample) |
| WO (2) | WO2015101958A2 (enExample) |
| ZA (1) | ZA201604272B (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX369691B (es) | 2012-11-21 | 2019-11-19 | Agios Pharmaceuticals Inc | Inhibidores de glutaminasa y métodos de empleo. |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| CN105960405B (zh) * | 2014-01-06 | 2021-02-19 | 理森制药股份公司 | 谷氨酰胺酶抑制剂 |
| WO2015143340A1 (en) * | 2014-03-21 | 2015-09-24 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| US20170050958A1 (en) * | 2014-04-30 | 2017-02-23 | Pfizer Inc. | Cycloalkyl-Linked Diheterocycle Derivatives |
| US9809588B2 (en) | 2014-07-03 | 2017-11-07 | Board Of Regents, The University Of Texas System | GLS1 inhibitors for treating disease |
| WO2016007647A1 (en) | 2014-07-09 | 2016-01-14 | The Johns Hopkins University | Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy |
| CN107921044B (zh) * | 2015-06-30 | 2022-01-21 | 德州大学系统董事会 | 用于治疗疾病的gls1抑制剂 |
| US10842763B2 (en) | 2015-07-31 | 2020-11-24 | The Johns Hopkins University | Methods for cancer and immunotherapy using prodrugs of glutamine analogs |
| CN108135875B (zh) * | 2015-07-31 | 2021-12-31 | 约翰霍普金斯大学 | 用于治疗代谢重编程病症的方法和组合物 |
| KR102666477B1 (ko) | 2015-07-31 | 2024-05-17 | 더 존스 홉킨스 유니버시티 | 글루타민 유사체의 프로드럭 |
| WO2017021177A1 (en) * | 2015-08-04 | 2017-02-09 | Universitat De Barcelona | Pharmaceutical combinations for use in the treatment of cancer |
| GB201520959D0 (en) | 2015-11-27 | 2016-01-13 | Astrazeneca Ab And Cancer Res Technology Ltd | Bis-pyridazine compounds and their use in treating cancer |
| TW201731511A (zh) | 2015-11-30 | 2017-09-16 | 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 |
| 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 |
| WO2017109793A1 (en) * | 2015-12-21 | 2017-06-29 | Council Of Scientific & Industrial Research | Novel 1,2,3 triazole-thiazole compounds, process for preparation and use thereof |
| MX384732B (es) * | 2015-12-22 | 2025-03-14 | Univ Texas | Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorociclobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorobutil)-n-metil-1h-1,2,3-triazol-4-carboxamida. |
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- 2015-01-05 EP EP15705095.6A patent/EP3092235A2/en not_active Withdrawn
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