MXPA03010255A - Ligandos heterobiciclicos de proteinas de union a fk-506. - Google Patents

Info

Publication number

MXPA03010255A

MXPA03010255A MXPA03010255A MXPA03010255A MXPA03010255A MX PA03010255 A MXPA03010255 A MX PA03010255A MX PA03010255 A MXPA03010255 A MX PA03010255A MX PA03010255 A MXPA03010255 A MX PA03010255A MX PA03010255 A MXPA03010255 A MX PA03010255A

Authority

MX

Mexico

Prior art keywords

compound

mmol

pharmaceutically acceptable

substituted

product

Prior art date

2001-05-10

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• 239000003446 ligand Substances 0.000 title description 2
• 150000001875 compounds Chemical class 0.000 claims abstract description 582
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• 208000025966 Neurological disease Diseases 0.000 claims abstract description 6
• 229910052739 hydrogen Inorganic materials 0.000 claims description 176
• -1 dimethoxymethyl Chemical group 0.000 claims description 92
• 150000003839 salts Chemical class 0.000 claims description 58
• 125000000217 alkyl group Chemical group 0.000 claims description 40
• 239000002207 metabolite Substances 0.000 claims description 37
• 239000001257 hydrogen Substances 0.000 claims description 31
• 239000012453 solvate Substances 0.000 claims description 30
• 239000000651 prodrug Substances 0.000 claims description 29
• 229940002612 prodrug Drugs 0.000 claims description 29
• 125000001072 heteroaryl group Chemical group 0.000 claims description 25
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
• 125000003118 aryl group Chemical group 0.000 claims description 20
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 20
• 229910052799 carbon Inorganic materials 0.000 claims description 17
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 17
• 229910052760 oxygen Inorganic materials 0.000 claims description 17
• 239000008194 pharmaceutical composition Substances 0.000 claims description 16
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 15
• 229910052757 nitrogen Inorganic materials 0.000 claims description 15
• 239000001301 oxygen Substances 0.000 claims description 15
• 150000001412 amines Chemical class 0.000 claims description 14
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
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• 125000003545 alkoxy group Chemical group 0.000 claims description 10
• 125000000623 heterocyclic group Chemical group 0.000 claims description 10
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• 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims description 9
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• 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
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• 125000001917 2,4-dinitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1*)[N+]([O-])=O)[N+]([O-])=O 0.000 claims description 2
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• 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 2
• 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 claims description 2
• GMPKIPWJBDOURN-UHFFFAOYSA-N Methoxyamine Chemical compound CON GMPKIPWJBDOURN-UHFFFAOYSA-N 0.000 claims description 2
• KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims description 2
• 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 2
• 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 2
• 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
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• 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 claims 1
• 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims 1
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• OKTJSMMVPCPJKN-NJFSPNSNSA-N Carbon-14 Chemical compound [14C] OKTJSMMVPCPJKN-NJFSPNSNSA-N 0.000 claims 1
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• 108091011114 FK506 binding proteins Proteins 0.000 abstract description 21
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• KTSZYXNHBVWNNV-UHFFFAOYSA-N 1,2-diazabicyclo[3.3.1]nonane Chemical class C1CNN2CCCC1C2 KTSZYXNHBVWNNV-UHFFFAOYSA-N 0.000 abstract 1
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