JP2007501804A5

JP2007501804A5 -

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Publication number: JP2007501804A5
Authority: JP; Japan
Prior art keywords: compound; alkyl; ring; substituents; optionally substituted
Prior art date: 2004-08-09
Legal status : Pending

Application number

JP2006522803A

Other languages

English (en)

Japanese (ja)

Other versions

JP2007501804A (ja

Filing date

2004-08-09

Publication date

2011-01-27

2004-08-09 Application filed filed Critical

2004-08-09 Priority claimed from PCT/US2004/025827 external-priority patent/WO2005013914A2/en

2007-02-01 Publication of JP2007501804A publication Critical patent/JP2007501804A/ja

2011-01-27 Publication of JP2007501804A5 publication Critical patent/JP2007501804A5/ja

Status Pending legal-status Critical Current

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-1 isoindol-1,3-dione-2-yl Chemical group 0.000 claims description 372
150000001875 compounds Chemical class 0.000 claims description 299
125000001424 substituent group Chemical group 0.000 claims description 131
125000000217 alkyl group Chemical group 0.000 claims description 118
125000005843 halogen group Chemical group 0.000 claims description 85
125000001931 aliphatic group Chemical group 0.000 claims description 66
125000003118 aryl group Chemical group 0.000 claims description 66
229910052739 hydrogen Inorganic materials 0.000 claims description 60
239000001257 hydrogen Substances 0.000 claims description 58
125000001072 heteroaryl group Chemical group 0.000 claims description 41
125000005842 heteroatom Chemical group 0.000 claims description 41
125000000623 heterocyclic group Chemical group 0.000 claims description 39
229910052717 sulfur Inorganic materials 0.000 claims description 39
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 35
125000002723 alicyclic group Chemical group 0.000 claims description 34
229910052760 oxygen Inorganic materials 0.000 claims description 33
125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims description 30
125000003545 alkoxy group Chemical group 0.000 claims description 27
125000004093 cyano group Chemical group *C#N 0.000 claims description 25
150000002431 hydrogen Chemical class 0.000 claims description 24
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 23
229910052757 nitrogen Inorganic materials 0.000 claims description 22
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 21
125000003342 alkenyl group Chemical group 0.000 claims description 20
125000001624 naphthyl group Chemical group 0.000 claims description 13
125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims description 13
125000004076 pyridyl group Chemical group 0.000 claims description 12
125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 8
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 7
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 7
125000002619 bicyclic group Chemical group 0.000 claims description 6
125000005322 morpholin-1-yl group Chemical group 0.000 claims description 6
125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 6
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 5
125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 5
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 5
125000000842 isoxazolyl group Chemical group 0.000 claims description 5
125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 4
239000002671 adjuvant Substances 0.000 claims description 4
CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 3
CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical group C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 claims 3
NNBZCPXTIHJBJL-UHFFFAOYSA-N decalin Chemical group C1CCCC2CCCCC21 NNBZCPXTIHJBJL-UHFFFAOYSA-N 0.000 claims 2
HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 claims 1
239000008194 pharmaceutical composition Substances 0.000 claims 1
PXXNTAGJWPJAGM-UHFFFAOYSA-N vertaline Chemical group C1C2C=3C=C(OC)C(OC)=CC=3OC(C=C3)=CC=C3CCC(=O)OC1CC1N2CCCC1 PXXNTAGJWPJAGM-UHFFFAOYSA-N 0.000 claims 1
239000000203 mixture Substances 0.000 description 72
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210000004027 cell Anatomy 0.000 description 59
ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 57
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XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 43
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125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 37
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 36
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ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 29
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WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 21
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125000002950 monocyclic group Chemical group 0.000 description 14
239000002904 solvent Substances 0.000 description 14
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239000003112 inhibitor Substances 0.000 description 13
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VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 12
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 12
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 12
125000002947 alkylene group Chemical group 0.000 description 12
ZYGHJZDHTFUPRJ-UHFFFAOYSA-N coumarin Chemical compound C1=CC=C2OC(=O)C=CC2=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 description 12
229940079593 drug Drugs 0.000 description 12
230000003287 optical effect Effects 0.000 description 12
229910052708 sodium Inorganic materials 0.000 description 12
JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 11
239000007821 HATU Substances 0.000 description 11
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LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 10
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125000005605 benzo group Chemical group 0.000 description 10
PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 10
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JNMRHUJNCSQMMB-UHFFFAOYSA-N sulfathiazole Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=NC=CS1 JNMRHUJNCSQMMB-UHFFFAOYSA-N 0.000 description 10
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LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 description 8
PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 description 8
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JP2006522803A 2003-08-08 2004-08-09 電位開口型のナトリウムチャネルのインヒビターとして有用な組成物 Pending JP2007501804A (ja)