JP2022191517A5 - - Google Patents

Info

Publication number

JP2022191517A5

JP2022191517A5 JP2022172961A JP2022172961A JP2022191517A5 JP 2022191517 A5 JP2022191517 A5 JP 2022191517A5 JP 2022172961 A JP2022172961 A JP 2022172961A JP 2022172961 A JP2022172961 A JP 2022172961A JP 2022191517 A5 JP2022191517 A5 JP 2022191517A5

Authority

JP

Japan

Prior art keywords

dioxo

dihydro

isoindol

amino

dioxopiperidin

Prior art date

2022-10-28

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.)

Pending

Links

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• DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 42
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 19
• 239000008194 pharmaceutical composition Substances 0.000 claims 9
• 125000000217 alkyl group Chemical group 0.000 claims 8
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 8
• 125000005647 linker group Chemical group 0.000 claims 8
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 8
• 239000000126 substance Substances 0.000 claims 8
• 230000004481 post-translational protein modification Effects 0.000 claims 7
• -1 5-bromo-2-{[4-({1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro- 1H-isoindol-4-yl]-4,7,10-trioxa-1-azadodecane-12-yl}oxy)phenyl]amino}pyrimidin-4-yl Chemical group 0.000 claims 6
• METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 claims 6
• 229910052739 hydrogen Inorganic materials 0.000 claims 6
• 229910052760 oxygen Inorganic materials 0.000 claims 6
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
• 229910052717 sulfur Inorganic materials 0.000 claims 6
• UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 4
• 125000003118 aryl group Chemical group 0.000 claims 4
• 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 4
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 4
• 125000000623 heterocyclic group Chemical group 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• 230000000707 stereoselective effect Effects 0.000 claims 4
• 108010080146 androgen receptors Proteins 0.000 claims 3
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
• 125000000753 cycloalkyl group Chemical group 0.000 claims 3
• 102100032187 Androgen receptor Human genes 0.000 claims 2
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
• 102100038595 Estrogen receptor Human genes 0.000 claims 2
• LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
• 102100032783 Protein cereblon Human genes 0.000 claims 2
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 230000015556 catabolic process Effects 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 230000008878 coupling Effects 0.000 claims 2
• 238000010168 coupling process Methods 0.000 claims 2
• 238000005859 coupling reaction Methods 0.000 claims 2
• 238000006731 degradation reaction Methods 0.000 claims 2
• 108010038795 estrogen receptors Proteins 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 230000001939 inductive effect Effects 0.000 claims 2
• 239000003112 inhibitor Substances 0.000 claims 2
• 229920001223 polyethylene glycol Polymers 0.000 claims 2
• 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 2
• 230000018883 protein targeting Effects 0.000 claims 2
• 102000004169 proteins and genes Human genes 0.000 claims 2
• 108090000623 proteins and genes Proteins 0.000 claims 2
• 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
• 238000006467 substitution reaction Methods 0.000 claims 2
• 229960003433 thalidomide Drugs 0.000 claims 2
• QSPCDHGSGMVDJL-UHFFFAOYSA-N CC1(C)C(NC(=O)C2=CC=C(OCCCCCOCCCNC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)C=C2)C(C)(C)C1OC1=CC(Cl)=C(C=C1)C#N Chemical compound CC1(C)C(NC(=O)C2=CC=C(OCCCCCOCCCNC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)C=C2)C(C)(C)C1OC1=CC(Cl)=C(C=C1)C#N QSPCDHGSGMVDJL-UHFFFAOYSA-N 0.000 claims 1
• 108010007005 Estrogen Receptor alpha Proteins 0.000 claims 1
• 150000001204 N-oxides Chemical class 0.000 claims 1
• CRGJHGSSJCLPQU-UHFFFAOYSA-N O=C1NC(CCC1N1C(C2=CC=CC(=C2C1=O)NCCOCCOC1=CC=C(C=C1)N1C(N(C(C1(C)C)=O)C1=CC(=C(C#N)C=C1)C(F)(F)F)=S)=O)=O Chemical compound O=C1NC(CCC1N1C(C2=CC=CC(=C2C1=O)NCCOCCOC1=CC=C(C=C1)N1C(N(C(C1(C)C)=O)C1=CC(=C(C#N)C=C1)C(F)(F)F)=S)=O)=O CRGJHGSSJCLPQU-UHFFFAOYSA-N 0.000 claims 1
• 102000001307 androgen receptors Human genes 0.000 claims 1
• 239000000262 estrogen Substances 0.000 claims 1
• 229940011871 estrogen Drugs 0.000 claims 1
• 102000015694 estrogen receptors Human genes 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 150000003384 small molecules Chemical class 0.000 claims 1