HRP20211610T1 - Inhibitori heterocikličke glutaminaze - Google Patents
Inhibitori heterocikličke glutaminaze Download PDFInfo
- Publication number
- HRP20211610T1 HRP20211610T1 HRP20211610TT HRP20211610T HRP20211610T1 HR P20211610 T1 HRP20211610 T1 HR P20211610T1 HR P20211610T T HRP20211610T T HR P20211610TT HR P20211610 T HRP20211610 T HR P20211610T HR P20211610 T1 HRP20211610 T1 HR P20211610T1
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- Croatia
- Prior art keywords
- cancer
- alkyl
- aryl
- cell
- heteroaryl
- Prior art date
Links
- 125000000623 heterocyclic group Chemical group 0.000 title claims 10
- 102000009127 Glutaminase Human genes 0.000 title 1
- 108010073324 Glutaminase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000003118 aryl group Chemical group 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 206010028980 Neoplasm Diseases 0.000 claims 11
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 9
- 210000003169 central nervous system Anatomy 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
- 125000004104 aryloxy group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 6
- 201000005962 mycosis fungoides Diseases 0.000 claims 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 5
- 206010025323 Lymphomas Diseases 0.000 claims 4
- 208000034578 Multiple myelomas Diseases 0.000 claims 4
- 208000007641 Pinealoma Diseases 0.000 claims 4
- 206010039491 Sarcoma Diseases 0.000 claims 4
- 208000009359 Sezary Syndrome Diseases 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 201000008968 osteosarcoma Diseases 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 208000029340 primitive neuroectodermal tumor Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 201000008271 Atypical teratoid rhabdoid tumor Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 208000021309 Germ cell tumor Diseases 0.000 claims 3
- 208000017604 Hodgkin disease Diseases 0.000 claims 3
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 3
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 3
- 208000025966 Neurological disease Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- -1 cyano, nitro, azido, sulfhydryl Chemical group 0.000 claims 3
- 208000014616 embryonal neoplasm Diseases 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 208000026278 immune system disease Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 230000003211 malignant effect Effects 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 201000005443 oral cavity cancer Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- 201000008205 supratentorial primitive neuroectodermal tumor Diseases 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 2
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- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 2
- 206010004593 Bile duct cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
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- 208000018084 Bone neoplasm Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000009798 Craniopharyngioma Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 201000008228 Ependymoblastoma Diseases 0.000 claims 2
- 206010014967 Ependymoma Diseases 0.000 claims 2
- 206010014968 Ependymoma malignant Diseases 0.000 claims 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 2
- 206010061252 Intraocular melanoma Diseases 0.000 claims 2
- 208000009164 Islet Cell Adenoma Diseases 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 2
- 206010025557 Malignant fibrous histiocytoma of bone Diseases 0.000 claims 2
- 208000000172 Medulloblastoma Diseases 0.000 claims 2
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 206010029266 Neuroendocrine carcinoma of the skin Diseases 0.000 claims 2
- 206010050487 Pinealoblastoma Diseases 0.000 claims 2
- 201000000582 Retinoblastoma Diseases 0.000 claims 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 2
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 2
- 206010046431 Urethral cancer Diseases 0.000 claims 2
- 206010046458 Urethral neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 201000005969 Uveal melanoma Diseases 0.000 claims 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims 2
- 208000011654 childhood malignant neoplasm Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 2
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims 2
- 230000004069 differentiation Effects 0.000 claims 2
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 2
- 201000010175 gallbladder cancer Diseases 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 210000000244 kidney pelvis Anatomy 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 201000008203 medulloepithelioma Diseases 0.000 claims 2
- 208000018795 nasal cavity and paranasal sinus carcinoma Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 201000002575 ocular melanoma Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Chemical group 0.000 claims 2
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- 229910052717 sulfur Chemical group 0.000 claims 2
- 239000011593 sulfur Chemical group 0.000 claims 2
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- 208000018417 undifferentiated high grade pleomorphic sarcoma of bone Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 1
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- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
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- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 206010073360 Appendix cancer Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010006143 Brain stem glioma Diseases 0.000 claims 1
- 206010007275 Carcinoid tumour Diseases 0.000 claims 1
- 206010007279 Carcinoid tumour of the gastrointestinal tract Diseases 0.000 claims 1
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- 208000011231 Crohn disease Diseases 0.000 claims 1
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- 208000017259 Extragonadal germ cell tumor Diseases 0.000 claims 1
- 206010053717 Fibrous histiocytoma Diseases 0.000 claims 1
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
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- 208000009329 Graft vs Host 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
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 201000005099 Langerhans cell histiocytosis Diseases 0.000 claims 1
- 206010061523 Lip and/or oral cavity cancer Diseases 0.000 claims 1
- 206010073099 Lobular breast carcinoma in situ Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
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- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
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- 229910019142 PO4 Inorganic materials 0.000 claims 1
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- 206010061332 Paraganglion neoplasm Diseases 0.000 claims 1
- 208000000821 Parathyroid Neoplasms Diseases 0.000 claims 1
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- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
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- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
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- 201000004810 Vascular dementia Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 208000020990 adrenal cortex carcinoma Diseases 0.000 claims 1
- 208000007128 adrenocortical carcinoma Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001409 amidines Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
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- 230000001394 metastastic effect Effects 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- AWIJRPNMLHPLNC-UHFFFAOYSA-N methanethioic s-acid Chemical group SC=O AWIJRPNMLHPLNC-UHFFFAOYSA-N 0.000 claims 1
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical group [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Chemical group 0.000 claims 1
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical group [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 1
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical group [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 1
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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
- C07D417/02—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
-
- 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
- C07D417/14—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)
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| US201361824434P | 2013-05-17 | 2013-05-17 | |
| EP13855039.7A EP2920168B1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic glutaminase inhibitors |
| PCT/US2013/070277 WO2014078645A1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic glutaminase inhibitors |
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| Publication Number | Publication Date |
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| HRP20211610T1 true HRP20211610T1 (hr) | 2022-02-04 |
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| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| JP6275153B2 (ja) | 2012-11-16 | 2018-02-07 | 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 | ヘテロ環式グルタミナーゼ阻害剤 |
| CA2892817A1 (en) * | 2012-12-03 | 2014-06-12 | Calithera Biosciences Inc. | Treatment of cancer with heterocyclic inhibitors of glutaminase |
| EP3092235A2 (en) | 2014-01-06 | 2016-11-16 | Rhizen Pharmaceuticals S.A. | Novel inhibitors of glutaminase |
| MX2016014143A (es) * | 2014-04-30 | 2017-02-15 | Pfizer | Derivados de diheterociclo enlazado a cicloalquilo. |
| GB201409624D0 (en) | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| AU2015274361B2 (en) * | 2014-06-13 | 2020-11-05 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| 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 |
| CN107074805B (zh) | 2014-07-03 | 2021-02-26 | 德州大学系统董事会 | 用于治疗疾病的gls1抑制剂 |
| WO2016007647A1 (en) * | 2014-07-09 | 2016-01-14 | The Johns Hopkins University | Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy |
| EA037738B1 (ru) * | 2014-08-07 | 2021-05-17 | Калитера Байосайенсиз, Инк. | Кристаллические формы ингибиторов глутаминазы |
| JP6768693B2 (ja) * | 2015-03-30 | 2020-10-14 | 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投与する方法 |
| US10441587B2 (en) * | 2015-04-06 | 2019-10-15 | Calithera Biosciences, Inc. | Treatment of lung cancer with inhibitors of glutaminase |
| EP3316887B1 (en) | 2015-06-30 | 2020-04-08 | Board of Regents, The University of Texas System | Gls1 inhibitors for treating disease |
| WO2017062354A1 (en) | 2015-10-05 | 2017-04-13 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors and immuno-oncology agents |
| 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 |
| US10150753B2 (en) | 2015-12-22 | 2018-12-11 | Board Of Regents, The University Of Texas System | Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyrdin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide |
| CN109982703A (zh) | 2016-08-25 | 2019-07-05 | 卡利泰拉生物科技公司 | 用谷氨酰胺酶抑制剂的组合疗法 |
| WO2018039544A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| US20180055825A1 (en) * | 2016-08-25 | 2018-03-01 | Yu Liang | Treatment of cancer with inhibitors of glutaminase |
| 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 |
| JP7361687B2 (ja) | 2017-10-18 | 2023-10-16 | ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム | グルタミナーゼ阻害薬療法 |
| 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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| GB9217295D0 (en) | 1992-08-14 | 1992-09-30 | Wellcome Found | Controlled released tablets |
| 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 |
| US5358970A (en) | 1993-08-12 | 1994-10-25 | Burroughs Wellcome Co. | Pharmaceutical composition containing bupropion hydrochloride and a stabilizer |
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| US8889112B2 (en) | 1999-09-16 | 2014-11-18 | Ocularis Pharma, Llc | Ophthalmic formulations including selective alpha 1 antagonists |
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| FI20115876A0 (fi) | 2011-09-06 | 2011-09-06 | Turun Yliopisto | Yhdistelmähoito |
| RS59705B1 (sr) * | 2011-11-21 | 2020-01-31 | Calithera Biosciences Inc | Heterociklični inhibitori glutaminaze |
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| JP6275153B2 (ja) | 2012-11-16 | 2018-02-07 | 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 | ヘテロ環式グルタミナーゼ阻害剤 |
| MX369691B (es) | 2012-11-21 | 2019-11-19 | Agios Pharmaceuticals Inc | Inhibidores de glutaminasa y métodos de empleo. |
| US9029531B2 (en) | 2012-11-22 | 2015-05-12 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| CA2892817A1 (en) | 2012-12-03 | 2014-06-12 | Calithera Biosciences Inc. | Treatment of cancer with heterocyclic inhibitors of glutaminase |
| WO2015061432A1 (en) | 2013-10-25 | 2015-04-30 | Calithera Biosciences, Inc. | Treatment of viral infections with inhibitors of glutaminase |
| WO2015138902A1 (en) | 2014-03-14 | 2015-09-17 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| AU2015274361B2 (en) | 2014-06-13 | 2020-11-05 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| EA037738B1 (ru) | 2014-08-07 | 2021-05-17 | Калитера Байосайенсиз, Инк. | Кристаллические формы ингибиторов глутаминазы |
| JP6768693B2 (ja) | 2015-03-30 | 2020-10-14 | 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投与する方法 |
| US10441587B2 (en) | 2015-04-06 | 2019-10-15 | Calithera Biosciences, Inc. | Treatment of lung cancer with inhibitors of glutaminase |
| WO2017062354A1 (en) | 2015-10-05 | 2017-04-13 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors and immuno-oncology agents |
| WO2018039544A1 (en) | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| JP2020510032A (ja) | 2017-03-10 | 2020-04-02 | 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 |
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2013
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- 2013-11-15 AU AU2013344560A patent/AU2013344560B2/en active Active
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- 2013-11-15 LT LTEPPCT/US2013/070277T patent/LT2920168T/lt unknown
- 2013-11-15 CA CA2891667A patent/CA2891667A1/en not_active Abandoned
- 2013-11-15 CN CN201380069950.3A patent/CN105051041B/zh active Active
- 2013-11-15 SI SI201331934T patent/SI2920168T1/sl unknown
- 2013-11-15 SM SM20210589T patent/SMT202100589T1/it unknown
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- 2013-11-15 EP EP13855039.7A patent/EP2920168B1/en active Active
- 2013-11-15 DK DK13855039.7T patent/DK2920168T3/da active
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- 2013-11-15 RS RS20211273A patent/RS62447B1/sr unknown
- 2013-11-15 PL PL13855039T patent/PL2920168T3/pl unknown
- 2013-11-15 EA EA201590941A patent/EA029707B1/ru not_active IP Right Cessation
- 2013-11-15 WO PCT/US2013/070277 patent/WO2014078645A1/en not_active Ceased
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- 2013-11-15 HR HRP20211610TT patent/HRP20211610T1/hr unknown
- 2013-11-15 MX MX2015005963A patent/MX381260B/es unknown
- 2013-11-15 PT PT138550397T patent/PT2920168T/pt unknown
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- 2013-11-15 SG SG11201503720SA patent/SG11201503720SA/en unknown
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2015
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2016
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2020
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2021
- 2021-10-19 CY CY20211100905T patent/CY1125279T1/el unknown
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