JP2017019839A5 - - Google Patents

Info

Publication number

JP2017019839A5

JP2017019839A5 JP2016173146A JP2016173146A JP2017019839A5 JP 2017019839 A5 JP2017019839 A5 JP 2017019839A5 JP 2016173146 A JP2016173146 A JP 2016173146A JP 2016173146 A JP2016173146 A JP 2016173146A JP 2017019839 A5 JP2017019839 A5 JP 2017019839A5

Authority

JP

Japan

Prior art keywords

pharmaceutically acceptable

composition according

composition

compound

acceptable salt

Prior art date

2016-09-05

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

• Espacenet
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• 239000000203 mixture Substances 0.000 claims description 56
• 150000001875 compounds Chemical class 0.000 claims description 38
• 150000003839 salts Chemical class 0.000 claims description 31
• 125000000217 alkyl group Chemical group 0.000 claims description 30
• 125000003118 aryl group Chemical group 0.000 claims description 16
• 125000000623 heterocyclic group Chemical group 0.000 claims description 15
• 125000001072 heteroaryl group Chemical group 0.000 claims description 14
• 210000004369 blood Anatomy 0.000 claims description 13
• 239000008280 blood Substances 0.000 claims description 13
• 229910052799 carbon Inorganic materials 0.000 claims description 12
• 125000004432 carbon atom Chemical group C* 0.000 claims description 12
• 125000001188 haloalkyl group Chemical group 0.000 claims description 12
• 125000001475 halogen functional group Chemical group 0.000 claims description 12
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
• 229910052739 hydrogen Inorganic materials 0.000 claims description 10
• 239000001257 hydrogen Substances 0.000 claims description 10
• 210000003743 erythrocyte Anatomy 0.000 claims description 9
• 125000004438 haloalkoxy group Chemical group 0.000 claims description 8
• 239000003937 drug carrier Substances 0.000 claims description 7
• 210000004027 cell Anatomy 0.000 claims description 6
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
• 125000002252 acyl group Chemical group 0.000 claims description 4
• 125000003545 alkoxy group Chemical group 0.000 claims description 4
• 125000000304 alkynyl group Chemical group 0.000 claims description 4
• -1 cyano, hydroxyl Chemical group 0.000 claims description 4
• 125000004122 cyclic group Chemical group 0.000 claims description 4
• 150000002431 hydrogen Chemical class 0.000 claims description 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
• 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 4
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
• 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 4
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
• 125000003107 substituted aryl group Chemical group 0.000 claims description 2
• 102000013009 Pyruvate Kinase Human genes 0.000 claims 2
• 108020005115 Pyruvate Kinase Proteins 0.000 claims 2
• 108700014121 Pyruvate Kinase Deficiency of Red Cells Proteins 0.000 claims 2
• 230000035772 mutation Effects 0.000 claims 2
• 230000003213 activating effect Effects 0.000 claims 1
• 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
• 238000000034 method Methods 0.000 description 30
• 239000008194 pharmaceutical composition Substances 0.000 description 7
• XOHUEYCVLUUEJJ-UHFFFAOYSA-N 2,3-Bisphosphoglyceric acid Chemical compound OP(=O)(O)OC(C(=O)O)COP(O)(O)=O XOHUEYCVLUUEJJ-UHFFFAOYSA-N 0.000 description 6
• 238000000338 in vitro Methods 0.000 description 5
• 238000001802 infusion Methods 0.000 description 4
• 238000007918 intramuscular administration Methods 0.000 description 4
• 238000007912 intraperitoneal administration Methods 0.000 description 4
• XOHUEYCVLUUEJJ-UWTATZPHSA-N 2,3-bisphospho-D-glyceric acid Chemical compound OP(=O)(O)O[C@@H](C(=O)O)COP(O)(O)=O XOHUEYCVLUUEJJ-UWTATZPHSA-N 0.000 description 2
• 102000001554 Hemoglobins Human genes 0.000 description 2
• 108010054147 Hemoglobins Proteins 0.000 description 2
• 230000032683 aging Effects 0.000 description 2
• 230000003281 allosteric effect Effects 0.000 description 2
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
• 230000015572 biosynthetic process Effects 0.000 description 2
• 239000003795 chemical substances by application Substances 0.000 description 2
• 238000010494 dissociation reaction Methods 0.000 description 2
• 230000005593 dissociations Effects 0.000 description 2
• 230000006872 improvement Effects 0.000 description 2
• 230000005764 inhibitory process Effects 0.000 description 2
• 230000003834 intracellular effect Effects 0.000 description 2
• 238000012986 modification Methods 0.000 description 2
• 230000004048 modification Effects 0.000 description 2
• 230000003647 oxidation Effects 0.000 description 2
• 238000007254 oxidation reaction Methods 0.000 description 2
• 229910052760 oxygen Inorganic materials 0.000 description 2
• 239000001301 oxygen Substances 0.000 description 2
• 238000006116 polymerization reaction Methods 0.000 description 2
• 230000000087 stabilizing effect Effects 0.000 description 2
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 2
• 230000001225 therapeutic effect Effects 0.000 description 2
• XOHUEYCVLUUEJJ-UHFFFAOYSA-I 2,3-Diphosphoglycerate Chemical compound [O-]P(=O)([O-])OC(C(=O)[O-])COP([O-])([O-])=O XOHUEYCVLUUEJJ-UHFFFAOYSA-I 0.000 description 1
• 230000004075 alteration Effects 0.000 description 1
• 230000007812 deficiency Effects 0.000 description 1
• 208000007475 hemolytic anemia Diseases 0.000 description 1
• 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
• 208000007056 sickle cell anemia Diseases 0.000 description 1