EA006654B1

EA006654B1 - Лечение нарушений центральной нервной системы с использованием антагонистов оксидазы d-аминокислот и d-аспартатоксидазы

Лечение нарушений центральной нервной системы с использованием антагонистов оксидазы d-аминокислот и d-аспартатоксидазы Download PDF

Info

Publication number: EA006654B1
Authority: EA; Eurasian Patent Office
Prior art keywords: alkyl; substituted; polypeptide; compound; halogen
Prior art date: 2001-01-16

Application number

EA200300807A

Other languages

English (en)

Russian (ru)

Other versions

EA200300807A1 (ru

Inventor

Даниель Коэн

Илья Чумаков

Original Assignee

Женсет С. А.

Priority date

2001-01-16

Filing date

2002-01-15

Publication date

2006-02-24

2002-01-15 Application filed by Женсет С. А. filed Critical Женсет С. А.

2004-08-26 Publication of EA200300807A1 publication Critical patent/EA200300807A1/ru

2006-02-24 Publication of EA006654B1 publication Critical patent/EA006654B1/ru

Links

239000005557 antagonist Substances 0.000 title claims abstract description 122
238000011282 treatment Methods 0.000 title claims description 54
108010070357 D-Aspartate Oxidase Proteins 0.000 title abstract 2
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108010003989 D-amino-acid oxidase Proteins 0.000 title abstract 2
102100039462 D-aspartate oxidase Human genes 0.000 title abstract 2
239000000203 mixture Substances 0.000 claims abstract description 346
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230000000694 effects Effects 0.000 claims description 171
229940024606 amino acid Drugs 0.000 claims description 140
150000001413 amino acids Chemical group 0.000 claims description 117
239000012634 fragment Substances 0.000 claims description 112
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238000012360 testing method Methods 0.000 claims description 73
229910052736 halogen Inorganic materials 0.000 claims description 68
150000002367 halogens Chemical class 0.000 claims description 68
125000000623 heterocyclic group Chemical group 0.000 claims description 62
125000000217 alkyl group Chemical group 0.000 claims description 60
230000000295 complement effect Effects 0.000 claims description 56
-1 phenoxy, benzyloxy, amino Chemical group 0.000 claims description 56
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 55
125000005842 heteroatom Chemical group 0.000 claims description 51
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 50
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 49
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229910052760 oxygen Inorganic materials 0.000 claims description 42
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238000006731 degradation reaction Methods 0.000 claims description 26
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BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims description 22
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UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims description 21
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229910052717 sulfur Inorganic materials 0.000 claims description 19
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HRXJCQXGAHSUJC-UHFFFAOYSA-N 3,4-dehydrothiomorpholine-3-carboxylic acid Chemical compound OC(=O)C1=NCCSC1 HRXJCQXGAHSUJC-UHFFFAOYSA-N 0.000 claims description 18
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238000012216 screening Methods 0.000 claims description 17
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NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 16
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UXWAJSLYHVAVKJ-UHFFFAOYSA-N 2-hydrazinyl-2-oxoacetic acid Chemical compound NNC(=O)C(O)=O UXWAJSLYHVAVKJ-UHFFFAOYSA-N 0.000 claims description 14
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125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
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OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
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XJUQJVUYGRTQGI-SCSAIBSYSA-N cystathionine ketimine Chemical compound OC(=O)[C@H]1CCSCC(C(O)=O)=N1 XJUQJVUYGRTQGI-SCSAIBSYSA-N 0.000 claims description 3
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125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
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MHRLWUPLSHYLOK-UHFFFAOYSA-N thiomorpholine-3,5-dicarboxylic acid Chemical compound OC(=O)C1CSCC(C(O)=O)N1 MHRLWUPLSHYLOK-UHFFFAOYSA-N 0.000 claims description 3
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