JP2017505808A5 - - Google Patents
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- 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
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 4
- 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
- 201000004624 Dermatitis Diseases 0.000 claims 3
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 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
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
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- 206010025323 Lymphomas Diseases 0.000 claims 2
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- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 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
- 208000030507 AIDS Diseases 0.000 claims 1
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- 206010003571 Astrocytoma Diseases 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
- 208000023514 Barrett esophagus Diseases 0.000 claims 1
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- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
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- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 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
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 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
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 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
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
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- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- 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
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010046914 Vaginal infection Diseases 0.000 claims 1
- 201000008100 Vaginitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
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- 230000000735 allogeneic effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
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- 210000004369 blood Anatomy 0.000 claims 1
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- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
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- 201000010881 cervical cancer Diseases 0.000 claims 1
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- 206010011005 corneal dystrophy Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
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- 201000008482 osteoarthritis Diseases 0.000 claims 1
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- 229940127084 other anti-cancer agent Drugs 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
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- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004550 quinolin-6-yl group Chemical group N1=CC=CC2=CC(=CC=C12)* 0.000 claims 1
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Applications Claiming Priority (19)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN39CH2014 | 2014-01-06 | ||
| IN36CH2014 | 2014-01-06 | ||
| IN39/CHE/2014 | 2014-01-06 | ||
| IN36/CHE/2014 | 2014-01-06 | ||
| IN2639/CHE/2014 | 2014-05-29 | ||
| IN2647CH2014 | 2014-05-29 | ||
| IN2639CH2014 | 2014-05-29 | ||
| IN2647/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 | ||
| IN3613/CHE/2014 | 2014-07-24 | ||
| IN3612CH2014 | 2014-07-24 | ||
| IN3612/CHE/2014 | 2014-07-24 | ||
| IN3613CH2014 | 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 (https=) | 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 (https=) |
| EP (2) | EP3092235A2 (https=) |
| JP (3) | JP6666263B2 (https=) |
| KR (3) | KR20160100407A (https=) |
| CN (5) | CN111393431A (https=) |
| AU (1) | AU2015204210B2 (https=) |
| BR (1) | BR112016015706A8 (https=) |
| CA (2) | CA2934700A1 (https=) |
| CL (1) | CL2016001715A1 (https=) |
| DK (1) | DK3092236T3 (https=) |
| EA (3) | EA035499B1 (https=) |
| ES (1) | ES2833576T3 (https=) |
| IL (1) | IL246362B (https=) |
| SG (1) | SG11201605478XA (https=) |
| WO (2) | WO2015101958A2 (https=) |
| ZA (1) | ZA201604272B (https=) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CA2934700A1 (en) * | 2014-01-06 | 2015-07-09 | Rhizen Pharmaceuticals Sa | Glutaminase inhibitors |
| US10000479B2 (en) * | 2014-03-21 | 2018-06-19 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| EP3556757A1 (en) * | 2014-04-30 | 2019-10-23 | Pfizer Inc | Cycloalkyl-linked diheterocycle derivatives |
| WO2016004404A2 (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 |
| WO2017004359A1 (en) * | 2015-06-30 | 2017-01-05 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| CA2994165A1 (en) * | 2015-07-31 | 2017-02-09 | The Johns Hopkins University | Methods for cancer and immunotherapy using glutamine analogues, including don |
| AU2016302940B2 (en) | 2015-07-31 | 2021-02-04 | The Johns Hopkins University | Prodrugs of glutamine analogs |
| US10842763B2 (en) | 2015-07-31 | 2020-11-24 | The Johns Hopkins University | Methods for cancer and immunotherapy using prodrugs of glutamine analogs |
| 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 |
| US9938265B2 (en) * | 2015-11-30 | 2018-04-10 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| US10323028B2 (en) | 2015-11-30 | 2019-06-18 | Astrazeneca Ab | 1,3,4-thiadiazole 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 |
| JP6586528B2 (ja) * | 2015-12-21 | 2019-10-02 | カウンシル オブ サイエンティフィック アンド インダストリアル リサーチ | 新規の１，２，３−トリアゾール−チアゾール化合物とその調製方法と利用 |
| 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 |
| CN107474024B (zh) * | 2016-06-08 | 2022-12-13 | 北京赛林泰医药技术有限公司 | 一种谷氨酰酶抑制剂及其组合物和用途 |
| WO2018102715A1 (en) * | 2016-12-02 | 2018-06-07 | Indiana University Research And Technology Corporation | Compositions and methods for treating and/or reducing corneal dystrophy |
| BR112019015141A2 (pt) * | 2017-01-27 | 2020-03-24 | Cornell University | Polímeros e hidrogéis modificados com zwitteríon |
| 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 |
| SG10202011632RA (en) | 2017-10-27 | 2021-01-28 | Boehringer Ingelheim Int | Pyridine carbonyl derivatives and therapeutic uses thereof as trpc6 inhibitors |
| US20190269705A1 (en) * | 2017-11-27 | 2019-09-05 | Regents Of The University Of Minnesota | Methods and materials for treating graft versus host disease |
| CA3108158C (en) * | 2018-07-31 | 2023-05-16 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| PE20211591A1 (es) | 2018-09-19 | 2021-08-18 | Biogen Ma Inc | Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| EP3878470A4 (en) * | 2018-11-08 | 2022-08-31 | The University of Tokyo | METHOD FOR ELIMINATING SENESCENE CELLS AND METHOD FOR PREPARING SENESCENE CELLS |
| CN109223778B (zh) * | 2018-11-16 | 2021-07-27 | 上海市肺科医院 | C24h24n6o2s3在制备抗结核菌药物中的用途 |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| JP7530384B2 (ja) | 2019-05-01 | 2024-08-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | （ｒ）－（２－メチルオキシラン－２－イル）メチル ４－ブロモベンゼンスルホネート |
| 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 |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| 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 |
| CA3188340A1 (en) | 2020-08-13 | 2022-02-17 | Boehringer Ingelheim International Gmbh | Treatment of cognitive impairement associated with schizophrenia |
| CA3195702A1 (en) | 2020-10-13 | 2022-04-21 | Boehringer Ingelheim International Gmbh | Process of reworking |
| WO2022079290A2 (en) * | 2020-10-16 | 2022-04-21 | Cemm - Forschungszentrum Für Molekulare Medizin Gmbh | Cullin ring ubiquitin ligase compounds and uses thereof |
| US11919879B2 (en) | 2021-06-16 | 2024-03-05 | Celgene Corporation | Carboxylic acid containing azetidinyl compounds for the treatment of neurodegenerative diseases |
| 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 |
| CN116023375A (zh) * | 2021-10-25 | 2023-04-28 | 成都苑东生物制药股份有限公司 | 一种杂环类衍生物、其制备方法及用途 |
| CA3236890A1 (en) | 2021-12-14 | 2023-06-22 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors for treating chronic kidney disease |
| US20250288577A1 (en) * | 2022-04-29 | 2025-09-18 | Cornell University | Methods of treating a virus infection and methods of inhibiting viral replication |
| CN114874186B (zh) * | 2022-05-16 | 2023-07-11 | 深圳大学 | 一种谷氨酰胺酰基环化酶同工酶抑制剂及其制备方法与应用 |
| AU2024267793A1 (en) * | 2023-05-10 | 2025-12-18 | Leal Therapeutics, Inc. | Small molecule inhibitors of glutaminase |
| CN121586707A (zh) * | 2023-10-17 | 2026-02-27 | 楚浦创制（武汉）医药科技有限公司 | 硫代羰基化合物及其应用 |
| CN119192178B (zh) * | 2024-09-23 | 2025-08-05 | 浙江师范大学行知学院 | 一种氨基脲衍生物及其制备方法与应用 |
| CN119656315B (zh) * | 2024-12-23 | 2025-10-17 | 重庆医科大学 | Gls1抑制剂在缓解溃疡性结肠炎中的应用 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2104783A1 (en) * | 1970-07-14 | 1972-04-21 | Berlin Chemie Veb | 2,5-disubstd 2-amino-1,3,4-thiadiazoles-from 4-substd 1-acylthiosemic - virustatics |
| JPH0358980A (ja) * | 1989-07-28 | 1991-03-14 | Canon Inc | 液晶性化合物、これを含む液晶組成物、およびこれを使用した液晶素子 |
| EP0656210A1 (en) | 1993-11-19 | 1995-06-07 | Takeda Chemical Industries, Ltd. | Imidazole derivatives as glutaminose inhibitors |
| US6310093B1 (en) | 1997-08-29 | 2001-10-30 | Elan Pharmaceuticals, Inc. | Method of preventing neuronal death |
| EP1181045A4 (en) | 1999-04-02 | 2003-04-23 | Los Angeles Childrens Hospital | USE OF ASPARAGINASE AND GLUTAMINASE FOR THE TREATMENT OF AUTOIMMUNE DISEASES AND DISEASES OF REJECTION OF BONE MARK AND RECIPIENT |
| US6451828B1 (en) | 2000-08-10 | 2002-09-17 | Elan Pharmaceuticals, Inc. | Selective inhibition of glutaminase by bis-thiadiazoles |
| NO315152B1 (no) | 2001-06-28 | 2003-07-21 | Tomm Slater | Anordning for rensing av luft |
| WO2003022261A1 (en) | 2001-09-13 | 2003-03-20 | Miller Kenneth E | Method of alleviating pain |
| SE0300456D0 (sv) * | 2003-02-19 | 2003-02-19 | Astrazeneca Ab | Novel compounds |
| JP2006518368A (ja) * | 2003-02-21 | 2006-08-10 | ファイザー・インク | プロテインキナーゼ阻害剤としてのｎ−ヘテロシクリル置換アミノチアゾール誘導体 |
| DE10326821A1 (de) | 2003-06-11 | 2005-01-05 | Medical Enzymes Ag | Pharmazeutische Kombinationspräparate zur Krebstherapie |
| US20060276438A1 (en) | 2004-10-04 | 2006-12-07 | Natarajan Sethuraman | Prevention and treatment of influenza with glutamine antagonist agents |
| US8338607B2 (en) | 2005-10-06 | 2012-12-25 | Nippon Soda Co., Ltd. | Cyclic amine compounds and agents for pest control |
| US8465736B2 (en) | 2006-05-10 | 2013-06-18 | New Medical Enzymes Ag | Glutadon |
| TW200819437A (en) * | 2006-08-17 | 2008-05-01 | Astrazeneca Ab | Chemical compounds |
| US7638541B2 (en) * | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| TWI414523B (zh) * | 2006-12-28 | 2013-11-11 | Metabolex Inc | 用於治療糖尿病及代謝病症之雜環受體促效劑 |
| AU2008279447A1 (en) | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders |
| EA018703B1 (ru) * | 2008-04-07 | 2013-10-30 | Айрм Ллк | Соединения и композиции в качестве модуляторов активности gpr119 |
| TW200948797A (en) * | 2008-04-22 | 2009-12-01 | Daiichi Sankyo Co Ltd | 5-hydroxypyrimidine-4-carboxamide compounds |
| US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| US8536176B2 (en) | 2008-08-01 | 2013-09-17 | Nippon Chemiphar Co., Ltd. | GPR119 agonist |
| WO2010033871A2 (en) | 2008-09-18 | 2010-03-25 | The Johns Hopkins University | Compositions and methods targeting glutaminase |
| EP2350067A2 (en) * | 2008-10-16 | 2011-08-03 | Schering Corporation | Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof |
| WO2010048149A2 (en) * | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| JP2010138082A (ja) * | 2008-12-09 | 2010-06-24 | Nippon Soda Co Ltd | 環状アミン化合物またはその塩、並びに有害生物防除剤 |
| US10532034B2 (en) | 2009-03-25 | 2020-01-14 | Cornell University | Inhibition of glutaminase C |
| US20120245344A1 (en) * | 2009-08-31 | 2012-09-27 | Nippon Chemiphar Co., Ltd. | Gpr119 agonist |
| PH12012500901A1 (en) * | 2009-11-05 | 2016-08-05 | Rhizen Pharmaceuticals Sa | Novel benzopyran kinase modulators |
| ES2362770B1 (es) | 2009-12-24 | 2012-05-22 | Universidad De Sevilla | Uso de compuesto n-fenil-n'-(3-metil-2-butenil)tiourea para la elaboración de medicamentos destinados al tratamiento de la encefalopatía hepática. |
| KR20120130104A (ko) * | 2010-02-01 | 2012-11-28 | 닛뽕 케미파 가부시키가이샤 | Ｇｐｒ119 작동약 |
| US20130109643A1 (en) | 2010-05-10 | 2013-05-02 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| JP5960688B2 (ja) * | 2010-05-17 | 2016-08-02 | インコゼン セラピューティクス プライベート リミテッド | プロテインキナーゼ調節物質としての新規３，５−二置換−３ｈ−［１，２，３］トリアゾロ［４，５−ｂ］ピリジン化合物 |
| WO2012006506A1 (en) | 2010-07-09 | 2012-01-12 | Massachusetts Institute Of Technology | Metabolic gene, enzyme, and flux targets for cancer therapy |
| WO2012034123A1 (en) | 2010-09-10 | 2012-03-15 | Cornell University | Activating phosphorylation site on glutaminase c |
| JP2014094886A (ja) * | 2011-02-28 | 2014-05-22 | Nippon Chemiphar Co Ltd | Ｇｐｒ１１９作動薬 |
| 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 |
| TW201321353A (zh) | 2011-10-08 | 2013-06-01 | Novartis Ag | 胺基甲酸酯／尿素衍生物 |
| 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 |
| 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 |
| 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 |
| 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 |
-
2015
- 2015-01-05 CA CA2934700A patent/CA2934700A1/en not_active Abandoned
- 2015-01-05 WO PCT/IB2015/050076 patent/WO2015101958A2/en not_active Ceased
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- 2015-01-05 EA EA201691134A patent/EA035499B1/ru unknown
- 2015-01-05 EP EP15705095.6A patent/EP3092235A2/en not_active Withdrawn
- 2015-01-05 CN CN202010671865.6A patent/CN111892589A/zh active Pending
- 2015-01-05 CA CA2934702A patent/CA2934702A1/en not_active Abandoned
- 2015-01-05 KR KR1020167021580A patent/KR20160100407A/ko not_active Ceased
- 2015-01-05 KR KR1020167021582A patent/KR20160100408A/ko not_active Ceased
- 2015-01-05 SG SG11201605478XA patent/SG11201605478XA/en unknown
- 2015-01-05 KR KR1020227001963A patent/KR20220013017A/ko not_active Ceased
- 2015-01-05 US US14/769,365 patent/US20160297761A1/en not_active Abandoned
- 2015-01-05 ES ES15705845T patent/ES2833576T3/es active Active
- 2015-01-05 CN CN201580006698.0A patent/CN105960405B/zh not_active Expired - Fee Related
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