JP2009520685A5 - - Google Patents
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- JP2009520685A5 JP2009520685A5 JP2008541110A JP2008541110A JP2009520685A5 JP 2009520685 A5 JP2009520685 A5 JP 2009520685A5 JP 2008541110 A JP2008541110 A JP 2008541110A JP 2008541110 A JP2008541110 A JP 2008541110A JP 2009520685 A5 JP2009520685 A5 JP 2009520685A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- heterocycloalkyl
- cycloalkyl
- Prior art date
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 72
- 125000003118 aryl group Chemical group 0.000 claims 70
- 125000001072 heteroaryl group Chemical group 0.000 claims 70
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 69
- 125000000753 cycloalkyl group Chemical group 0.000 claims 63
- 125000003710 aryl alkyl group Chemical group 0.000 claims 57
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 51
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 44
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 44
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 34
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 32
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 32
- 125000005843 halogen group Chemical group 0.000 claims 27
- 229910052799 carbon Inorganic materials 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 12
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 11
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000001188 haloalkyl group Chemical group 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 206010012289 Dementia Diseases 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 238000001727 in vivo Methods 0.000 claims 3
- 239000002243 precursor Substances 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- -1 (3′-methoxybiphenyl-3-yl) -1′H-spiro [cyclohexane-1,2′-quinazoline] -4′-amine trifluoroacetate Chemical compound 0.000 claims 1
- QDMVACSUPDWDLL-UHFFFAOYSA-N 1'-[3-(3-methoxyphenyl)phenyl]spiro[1h-quinazoline-2,3'-cyclohexene]-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C=2CCCC3(C=2)N=C(N)C2=CC=CC=C2N3)=C1 QDMVACSUPDWDLL-UHFFFAOYSA-N 0.000 claims 1
- ZFEGUWVJFDUVCO-UHFFFAOYSA-N 1-amino-3-(3-bromophenyl)-3-(trifluoromethyl)-4h-isoquinoline-6-carbonitrile Chemical compound C1C2=CC(C#N)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC(Br)=C1 ZFEGUWVJFDUVCO-UHFFFAOYSA-N 0.000 claims 1
- NJNNIZZZQLHDQT-UHFFFAOYSA-N 1-amino-3-(3-bromophenyl)-3-(trifluoromethyl)-4h-isoquinoline-6-carboxamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC(C(=O)N)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC(Br)=C1 NJNNIZZZQLHDQT-UHFFFAOYSA-N 0.000 claims 1
- GGANFIZMIYZCQB-UHFFFAOYSA-N 1-amino-3-[3-(3-methoxyphenyl)phenyl]-3-(trifluoromethyl)-4h-isoquinoline-6-carbonitrile;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(N=C(N)C3=CC=C(C=C3C2)C#N)C(F)(F)F)=C1 GGANFIZMIYZCQB-UHFFFAOYSA-N 0.000 claims 1
- AMIKLZSNQVTNNN-UHFFFAOYSA-N 1-amino-3-[3-(3-methoxyphenyl)phenyl]-3-(trifluoromethyl)-4h-isoquinoline-6-carboxamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(N=C(N)C3=CC=C(C=C3C2)C(N)=O)C(F)(F)F)=C1 AMIKLZSNQVTNNN-UHFFFAOYSA-N 0.000 claims 1
- DBEQWEKSSBSANW-UHFFFAOYSA-N 1-amino-3-[3-(3-methoxyphenyl)phenyl]-3-(trifluoromethyl)-4h-isoquinoline-6-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(N=C(N)C3=CC=C(C=C3C2)C(O)=O)C(F)(F)F)=C1 DBEQWEKSSBSANW-UHFFFAOYSA-N 0.000 claims 1
- RXVNKLSJBYVTPV-UHFFFAOYSA-N 1-amino-3-phenyl-3-(trifluoromethyl)-4H-isoquinoline-6-carbonitrile hydrochloride Chemical compound Cl.C1C2=CC(C#N)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 RXVNKLSJBYVTPV-UHFFFAOYSA-N 0.000 claims 1
- IDGGKHZOFFZFNT-UHFFFAOYSA-N 1-amino-3-phenyl-3-(trifluoromethyl)-4h-isoquinoline-6-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC(C(O)=O)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 IDGGKHZOFFZFNT-UHFFFAOYSA-N 0.000 claims 1
- HICQWLMPQMJNOW-UHFFFAOYSA-N 2-(3-bromophenyl)-2-methyl-1,3-benzoxazin-4-amine Chemical compound O1C2=CC=CC=C2C(N)=NC1(C)C1=CC=CC(Br)=C1 HICQWLMPQMJNOW-UHFFFAOYSA-N 0.000 claims 1
- CVEMAFPNUJWPBK-UHFFFAOYSA-N 2-(3-bromophenyl)-2-methyl-1h-quinazolin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N1C2=CC=CC=C2C(N)=NC1(C)C1=CC=CC(Br)=C1 CVEMAFPNUJWPBK-UHFFFAOYSA-N 0.000 claims 1
- CBDCPWBARIEQJW-UHFFFAOYSA-N 2-(3-bromophenyl)-2-methyl-3h-1,3-benzoxazin-4-one Chemical compound N1C(=O)C2=CC=CC=C2OC1(C)C1=CC=CC(Br)=C1 CBDCPWBARIEQJW-UHFFFAOYSA-N 0.000 claims 1
- OBIOITWOYDDXBX-UHFFFAOYSA-N 2-(3-bromophenyl)-4-chloro-2-methyl-1,3-benzoxazine Chemical compound O1C2=CC=CC=C2C(Cl)=NC1(C)C1=CC=CC(Br)=C1 OBIOITWOYDDXBX-UHFFFAOYSA-N 0.000 claims 1
- IFKZSHQHLMNYJN-UHFFFAOYSA-N 2-(3-bromophenyl)-n-methoxy-2-methyl-1,3-benzoxazin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O1C2=CC=CC=C2C(NOC)=NC1(C)C1=CC=CC(Br)=C1 IFKZSHQHLMNYJN-UHFFFAOYSA-N 0.000 claims 1
- UANBHJOGMLSYJJ-UHFFFAOYSA-N 2-[2-(3-bromophenyl)ethyl]-2-methyl-1,3-benzoxazin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.O1C2=CC=CC=C2C(N)=NC1(C)CCC1=CC=CC(Br)=C1 UANBHJOGMLSYJJ-UHFFFAOYSA-N 0.000 claims 1
- ASJPNAGKSRTSOU-UHFFFAOYSA-N 2-[2-(3-bromophenyl)ethyl]-2-methyl-1h-quinazolin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N1C2=CC=CC=C2C(N)=NC1(C)CCC1=CC=CC(Br)=C1 ASJPNAGKSRTSOU-UHFFFAOYSA-N 0.000 claims 1
- SORJLLJWDWPORX-UHFFFAOYSA-N 2-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-1,2-dimethylquinazolin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(C)N(C4=CC=CC=C4C(N)=N3)C)C=CC=2)=C1 SORJLLJWDWPORX-UHFFFAOYSA-N 0.000 claims 1
- IVZRBDBEWXWNCG-UHFFFAOYSA-N 2-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-2-methyl-1,3-benzoxazin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(C)N=C(N)C4=CC=CC=C4O3)C=CC=2)=C1 IVZRBDBEWXWNCG-UHFFFAOYSA-N 0.000 claims 1
- NCSVTMDNYOUHMB-UHFFFAOYSA-N 2-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-2-methyl-1h-quinazolin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(C)N=C(N)C4=CC=CC=C4N3)C=CC=2)=C1 NCSVTMDNYOUHMB-UHFFFAOYSA-N 0.000 claims 1
- YQYFQGAKNKITRN-UHFFFAOYSA-N 2-[3-(3-methoxyphenyl)phenyl]-2-methyl-1,3-benzoxazin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(C)N=C(N)C3=CC=CC=C3O2)=C1 YQYFQGAKNKITRN-UHFFFAOYSA-N 0.000 claims 1
- WAYHGSVZWAQZSE-UHFFFAOYSA-N 2-[3-(3-methoxyphenyl)phenyl]-2-methyl-1h-quinazolin-4-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(C)N=C(N)C3=CC=CC=C3N2)=C1 WAYHGSVZWAQZSE-UHFFFAOYSA-N 0.000 claims 1
- GUZQPEQUNBMUCL-UHFFFAOYSA-N 3-(3-bromophenyl)-1-ethylsulfanyl-3-methyl-4h-isoquinoline Chemical compound C1C2=CC=CC=C2C(SCC)=NC1(C)C1=CC=CC(Br)=C1 GUZQPEQUNBMUCL-UHFFFAOYSA-N 0.000 claims 1
- CDVOQPAKADWWQB-UHFFFAOYSA-N 3-(3-bromophenyl)-3,4-dihydroisoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1C1=CC=CC(Br)=C1 CDVOQPAKADWWQB-UHFFFAOYSA-N 0.000 claims 1
- HMUSTCPHRCSDBS-UHFFFAOYSA-N 3-(3-bromophenyl)-3-(trifluoromethyl)-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC(Br)=C1 HMUSTCPHRCSDBS-UHFFFAOYSA-N 0.000 claims 1
- IZGOILZIFQOLCH-UHFFFAOYSA-N 3-(3-phenylphenyl)-3,4-dihydroisoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1C(C=1)=CC=CC=1C1=CC=CC=C1 IZGOILZIFQOLCH-UHFFFAOYSA-N 0.000 claims 1
- GTMLVVUMMNMOPR-UHFFFAOYSA-N 3-[2-(3-bromophenyl)ethyl]-3-methyl-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1(C)CCC1=CC=CC(Br)=C1 GTMLVVUMMNMOPR-UHFFFAOYSA-N 0.000 claims 1
- MMSHNXHHAKRLCP-UHFFFAOYSA-N 3-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-3-methyl-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(C)N=C(N)C4=CC=CC=C4C3)C=CC=2)=C1 MMSHNXHHAKRLCP-UHFFFAOYSA-N 0.000 claims 1
- HOPNUIGTNSSOGT-UHFFFAOYSA-N 3-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-3-phenyl-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(N=C(N)C4=CC=CC=C4C3)C=3C=CC=CC=3)C=CC=2)=C1 HOPNUIGTNSSOGT-UHFFFAOYSA-N 0.000 claims 1
- YRWAUSCCJAWRNU-UHFFFAOYSA-N 3-[3-(3-methoxyphenyl)phenyl]-3,4-dihydroisoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2N=C(N)C3=CC=CC=C3C2)=C1 YRWAUSCCJAWRNU-UHFFFAOYSA-N 0.000 claims 1
- BVPXFERMHNAQCD-UHFFFAOYSA-N 3-[3-(3-methoxyphenyl)phenyl]-3-(trifluoromethyl)-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(N=C(N)C3=CC=CC=C3C2)C(F)(F)F)=C1 BVPXFERMHNAQCD-UHFFFAOYSA-N 0.000 claims 1
- XQRYHJYTPLAAOZ-UHFFFAOYSA-N 3-methyl-3-(3-phenylphenyl)-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1(C)C(C=1)=CC=CC=1C1=CC=CC=C1 XQRYHJYTPLAAOZ-UHFFFAOYSA-N 0.000 claims 1
- UNSMGVCQMIQVKA-UHFFFAOYSA-N 3-methyl-5-trimethylsilylthiophene-2-carbonitrile Chemical compound CC=1C=C([Si](C)(C)C)SC=1C#N UNSMGVCQMIQVKA-UHFFFAOYSA-N 0.000 claims 1
- RTJBVUVZUZULEL-UHFFFAOYSA-N 3-phenyl-3-(trifluoromethyl)-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 RTJBVUVZUZULEL-UHFFFAOYSA-N 0.000 claims 1
- KSNHYZMGOLDAAD-UHFFFAOYSA-N 3-phenyl-6-(2h-tetrazol-5-yl)-3-(trifluoromethyl)-4h-isoquinolin-1-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C=1C=C2C(N)=NC(C(F)(F)F)(C=3C=CC=CC=3)CC2=CC=1C1=NN=NN1 KSNHYZMGOLDAAD-UHFFFAOYSA-N 0.000 claims 1
- OVYSOCDQHHFLLW-UHFFFAOYSA-N 4-amino-2-[2-(3-bromophenyl)ethyl]-2-methyl-1h-quinazoline-7-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N1C2=CC(C(O)=O)=CC=C2C(N)=NC1(C)CCC1=CC=CC(Br)=C1 OVYSOCDQHHFLLW-UHFFFAOYSA-N 0.000 claims 1
- YYZVPIDGLYBUAJ-UHFFFAOYSA-N 4-amino-2-[2-[3-(3-methoxyphenyl)phenyl]ethyl]-2-methyl-1h-quinazoline-7-carboxylic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(CCC3(C)N=C(N)C4=CC=C(C=C4N3)C(O)=O)C=CC=2)=C1 YYZVPIDGLYBUAJ-UHFFFAOYSA-N 0.000 claims 1
- XHKQMNMOWLESNO-UHFFFAOYSA-N 5-(3-bromophenyl)-2-trimethylsilyl-4,5-dihydrothieno[2,3-c]pyridin-7-amine Chemical compound N1=C(N)C=2SC([Si](C)(C)C)=CC=2CC1C1=CC=CC(Br)=C1 XHKQMNMOWLESNO-UHFFFAOYSA-N 0.000 claims 1
- IGMQUPUPIVTFBY-UHFFFAOYSA-N 5-(3-bromophenyl)-4,5-dihydrothieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C=2C=CSC=2C(N)=NC1C1=CC=CC(Br)=C1 IGMQUPUPIVTFBY-UHFFFAOYSA-N 0.000 claims 1
- FDRKMWYKESHPNS-UHFFFAOYSA-N 5-(3-bromophenyl)-5-(trifluoromethyl)-2-trimethylsilyl-4h-thieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N1=C(N)C=2SC([Si](C)(C)C)=CC=2CC1(C(F)(F)F)C1=CC=CC(Br)=C1 FDRKMWYKESHPNS-UHFFFAOYSA-N 0.000 claims 1
- JENRFFTXYHALCY-UHFFFAOYSA-N 5-(3-bromophenyl)-5-(trifluoromethyl)-4h-thieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C=2C=CSC=2C(N)=NC1(C(F)(F)F)C1=CC=CC(Br)=C1 JENRFFTXYHALCY-UHFFFAOYSA-N 0.000 claims 1
- SZIYTRZVMUIROZ-UHFFFAOYSA-N 5-[3-(3-methoxyphenyl)phenyl]-4,5-dihydrothieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2N=C(N)C=3SC=CC=3C2)=C1 SZIYTRZVMUIROZ-UHFFFAOYSA-N 0.000 claims 1
- GAHWLYOYDYMKPM-UHFFFAOYSA-N 5-[3-(3-methoxyphenyl)phenyl]-5-(trifluoromethyl)-4h-thieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.COC1=CC=CC(C=2C=C(C=CC=2)C2(N=C(N)C=3SC=CC=3C2)C(F)(F)F)=C1 GAHWLYOYDYMKPM-UHFFFAOYSA-N 0.000 claims 1
- OCHYFOFDNRHDRX-UHFFFAOYSA-N 5-phenyl-5-(trifluoromethyl)-2-trimethylsilyl-4h-thieno[2,3-c]pyridin-7-amine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N1=C(N)C=2SC([Si](C)(C)C)=CC=2CC1(C(F)(F)F)C1=CC=CC=C1 OCHYFOFDNRHDRX-UHFFFAOYSA-N 0.000 claims 1
- UIRYHPCELAYYKQ-UHFFFAOYSA-N 5-phenyl-5-(trifluoromethyl)-4h-thieno[2,3-c]pyridin-7-amine Chemical compound C1C=2C=CSC=2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 UIRYHPCELAYYKQ-UHFFFAOYSA-N 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010036631 Presenile dementia Diseases 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 230000003412 degenerative effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- KMSJFRPNIYWPMV-UHFFFAOYSA-N n-[[1-amino-3-phenyl-3-(trifluoromethyl)-4h-isoquinolin-6-yl]methyl]acetamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC(CNC(=O)C)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 KMSJFRPNIYWPMV-UHFFFAOYSA-N 0.000 claims 1
- UMTXFOGGWYZSOA-UHFFFAOYSA-N n-[[1-amino-3-phenyl-3-(trifluoromethyl)-4h-isoquinolin-6-yl]methyl]methanesulfonamide;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1C2=CC(CNS(=O)(=O)C)=CC=C2C(N)=NC1(C(F)(F)F)C1=CC=CC=C1 UMTXFOGGWYZSOA-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73732705P | 2005-11-15 | 2005-11-15 | |
| PCT/SE2006/001283 WO2007058583A2 (en) | 2005-11-15 | 2006-11-13 | Novel 2-amino-heterocycles useful in the treatment of abeta-related pathologies |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009520685A JP2009520685A (ja) | 2009-05-28 |
| JP2009520685A5 true JP2009520685A5 (cg-RX-API-DMAC10.html) | 2010-01-07 |
Family
ID=38049090
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008541110A Pending JP2009520685A (ja) | 2005-11-15 | 2006-11-13 | 化合物およびそれらの使用ｉｖ |
Country Status (15)
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US8722708B2 (en) | 2005-06-14 | 2014-05-13 | Merck Sharp & Dohme Inc. | Substituted isoindolines as aspartyl protease inhibitors |
| AU2006259572A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
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2006
- 2006-11-08 TW TW095141352A patent/TW200804290A/zh unknown
- 2006-11-13 CN CNA2006800511195A patent/CN101360714A/zh active Pending
- 2006-11-13 CA CA002629831A patent/CA2629831A1/en not_active Abandoned
- 2006-11-13 WO PCT/SE2006/001283 patent/WO2007058583A2/en not_active Ceased
- 2006-11-13 EP EP06813006A patent/EP1957462A4/en not_active Withdrawn
- 2006-11-13 AU AU2006316256A patent/AU2006316256A1/en not_active Abandoned
- 2006-11-13 BR BRPI0618607-6A patent/BRPI0618607A2/pt not_active IP Right Cessation
- 2006-11-13 US US12/093,631 patent/US20080293709A1/en not_active Abandoned
- 2006-11-13 KR KR1020087014418A patent/KR20080070744A/ko not_active Withdrawn
- 2006-11-13 AR ARP060104956A patent/AR056217A1/es not_active Application Discontinuation
- 2006-11-13 JP JP2008541110A patent/JP2009520685A/ja active Pending
- 2006-11-14 UY UY29919A patent/UY29919A1/es not_active Application Discontinuation
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2008
- 2008-04-27 IL IL191057A patent/IL191057A0/en unknown
- 2008-05-06 ZA ZA200803859A patent/ZA200803859B/xx unknown
- 2008-06-03 NO NO20082481A patent/NO20082481L/no not_active Application Discontinuation