CA2891667A1 - Heterocyclic glutaminase inhibitors - Google Patents
Heterocyclic glutaminase inhibitors Download PDFInfo
- Publication number
- CA2891667A1 CA2891667A1 CA2891667A CA2891667A CA2891667A1 CA 2891667 A1 CA2891667 A1 CA 2891667A1 CA 2891667 A CA2891667 A CA 2891667A CA 2891667 A CA2891667 A CA 2891667A CA 2891667 A1 CA2891667 A1 CA 2891667A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- compound
- arylalkyl
- aryl
- heteroaryl
- 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.)
- Abandoned
Links
- 125000000623 heterocyclic group Chemical group 0.000 title claims description 56
- 108010073324 Glutaminase Proteins 0.000 title abstract description 42
- 102000009127 Glutaminase Human genes 0.000 title abstract description 42
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- 150000001875 compounds Chemical class 0.000 claims abstract description 288
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- 208000026278 immune system disease Diseases 0.000 claims abstract description 7
- 230000001900 immune effect Effects 0.000 claims abstract description 5
- 125000003118 aryl group Chemical group 0.000 claims description 99
- 125000000217 alkyl group Chemical group 0.000 claims description 97
- 238000000034 method Methods 0.000 claims description 95
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 83
- 125000001072 heteroaryl group Chemical group 0.000 claims description 80
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- 125000003545 alkoxy group Chemical group 0.000 claims description 60
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- -1 CH2NHCH2 Chemical group 0.000 claims description 52
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 52
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 50
- 239000008194 pharmaceutical composition Substances 0.000 claims description 49
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- 125000003342 alkenyl group Chemical group 0.000 claims description 38
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Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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)
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- 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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| US201261727195P | 2012-11-16 | 2012-11-16 | |
| US61/727,195 | 2012-11-16 | ||
| US201361824434P | 2013-05-17 | 2013-05-17 | |
| US61/824,434 | 2013-05-17 | ||
| PCT/US2013/070277 WO2014078645A1 (en) | 2012-11-16 | 2013-11-15 | Heterocyclic glutaminase inhibitors |
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| CA2891667A1 true CA2891667A1 (en) | 2014-05-22 |
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| PT2920168T (pt) | 2012-11-16 | 2021-10-18 | Calithera Biosciences Inc | Inibidores heterocíclicos de glutaminase |
| SG11201504184PA (en) * | 2012-12-03 | 2015-06-29 | Calithera Biosciences Inc | Treatment of cancer with heterocyclic inhibitors of glutaminase |
| CA2934702A1 (en) | 2014-01-06 | 2015-07-09 | Rhizen Pharmaceuticals Sa | Inhibitors of glutaminase |
| WO2015166373A1 (en) * | 2014-04-30 | 2015-11-05 | 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 |
| EA036001B1 (ru) * | 2014-06-13 | 2020-09-11 | Калитера Байосайенсиз, Инк. | Комбинация эрлотиниба и ингибитора глутаминазы для лечения рака легких |
| US20160002248A1 (en) * | 2014-07-03 | 2016-01-07 | Board Of Regents, The University Of Texas System | Gls1 inhibitors for treating disease |
| EP3164195B1 (en) * | 2014-07-03 | 2022-06-15 | Board of Regents, The University of Texas System | Glutaminase inhibitor therapy |
| 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 |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| EP3277276B1 (en) * | 2015-03-30 | 2020-11-04 | Calithera Biosciences, Inc. | Methods of administering glutaminase inhibitors |
| SG11201708153XA (en) | 2015-04-06 | 2017-11-29 | 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 |
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