JP2013505903A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013505903A5 JP2013505903A5 JP2012530181A JP2012530181A JP2013505903A5 JP 2013505903 A5 JP2013505903 A5 JP 2013505903A5 JP 2012530181 A JP2012530181 A JP 2012530181A JP 2012530181 A JP2012530181 A JP 2012530181A JP 2013505903 A5 JP2013505903 A5 JP 2013505903A5
- Authority
- JP
- Japan
- Prior art keywords
- trans
- ethyl
- amine
- alkyl
- pyrrolidin
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 15
- 239000012453 solvate Substances 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000001188 haloalkyl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- -1 cyano, sulfonyl Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- AELCINSCMGFISI-DTWKUNHWSA-N (1R,2S)-tranylcypromine Chemical compound N[C@@H]1C[C@H]1C1=CC=CC=C1 AELCINSCMGFISI-DTWKUNHWSA-N 0.000 claims 1
- IOOMPWILDDCJEB-JKSUJKDBSA-N (1r,2s)-2-(4-bromophenyl)-n-[2-(4-methylpiperazin-1-yl)ethyl]cyclopropan-1-amine Chemical compound C1CN(C)CCN1CCN[C@H]1[C@H](C=2C=CC(Br)=CC=2)C1 IOOMPWILDDCJEB-JKSUJKDBSA-N 0.000 claims 1
- RODXJVOOUYCESN-FCHUYYIVSA-N (1r,2s)-2-[4-(3-chlorophenyl)phenyl]-n-[2-(4-methylpiperazin-1-yl)ethyl]cyclopropan-1-amine Chemical compound C1CN(C)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(Cl)C=CC=2)C1 RODXJVOOUYCESN-FCHUYYIVSA-N 0.000 claims 1
- YFSDVCYHUDZZKO-LEWJYISDSA-N (1r,2s)-n-(2-piperazin-1-ylethyl)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropan-1-amine Chemical compound FC(F)(F)C1=CC=CC(C=2C=CC(=CC=2)[C@H]2[C@@H](C2)NCCN2CCNCC2)=C1 YFSDVCYHUDZZKO-LEWJYISDSA-N 0.000 claims 1
- NWVPJEFDOAHEEB-FCHUYYIVSA-N (1r,2s)-n-(2-piperidin-1-ylethyl)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropan-1-amine Chemical compound FC(F)(F)C1=CC=CC(C=2C=CC(=CC=2)[C@H]2[C@@H](C2)NCCN2CCCCC2)=C1 NWVPJEFDOAHEEB-FCHUYYIVSA-N 0.000 claims 1
- CDAXGWVFDQIAMH-XZOQPEGZSA-N (1r,2s)-n-[2-(4-methylpiperazin-1-yl)ethyl]-2-(4-phenylmethoxyphenyl)cyclopropan-1-amine Chemical compound C1CN(C)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 CDAXGWVFDQIAMH-XZOQPEGZSA-N 0.000 claims 1
- IQOVUPJXECOXCB-FCHUYYIVSA-N (1r,2s)-n-[2-(4-methylpiperazin-1-yl)ethyl]-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropan-1-amine Chemical compound C1CN(C)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(C=CC=2)C(F)(F)F)C1 IQOVUPJXECOXCB-FCHUYYIVSA-N 0.000 claims 1
- CFXNTRJXWJLTFH-JRGCBEDISA-N (3R)-1-[2-[[(1R,2S)-2-(4-phenoxyphenyl)cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound O(C1=CC=CC=C1)C1=CC=C(C=C1)[C@H]1[C@@H](C1)NCCN1C[C@@H](CC1)N CFXNTRJXWJLTFH-JRGCBEDISA-N 0.000 claims 1
- MCSRJIHITMDLCC-CMTIAEDTSA-N (3r)-1-[2-[[(1r,2s)-2-(3-phenyl-4-phenylmethoxyphenyl)cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=C(C(OCC=3C=CC=CC=3)=CC=2)C=2C=CC=CC=2)C1 MCSRJIHITMDLCC-CMTIAEDTSA-N 0.000 claims 1
- AJJQQTYZTNTYOE-QHAWAJNXSA-N (3r)-1-[2-[[(1r,2s)-2-[4-(3,5-dichlorophenyl)phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(Cl)C=C(Cl)C=2)C1 AJJQQTYZTNTYOE-QHAWAJNXSA-N 0.000 claims 1
- FGHLFNOKGRFXSQ-QHAWAJNXSA-N (3r)-1-[2-[[(1r,2s)-2-[4-(3-chlorophenyl)phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(Cl)C=CC=2)C1 FGHLFNOKGRFXSQ-QHAWAJNXSA-N 0.000 claims 1
- VJXLAAQFANGKTA-BAGYTPMASA-N (3r)-1-[2-[[(1r,2s)-2-[4-(3-methoxyphenyl)phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound COC1=CC=CC(C=2C=CC(=CC=2)[C@H]2[C@@H](C2)NCCN2C[C@H](N)CC2)=C1 VJXLAAQFANGKTA-BAGYTPMASA-N 0.000 claims 1
- SQQDLFIQQCVQEF-QHAWAJNXSA-N (3r)-1-[2-[[(1r,2s)-2-[4-(4-chlorophenyl)phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=CC(Cl)=CC=2)C1 SQQDLFIQQCVQEF-QHAWAJNXSA-N 0.000 claims 1
- CYSBBYYGKATUQF-BAGYTPMASA-N (3r)-1-[2-[[(1r,2s)-2-[4-[(3-bromophenyl)methoxy]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=C(Br)C=CC=3)=CC=2)C1 CYSBBYYGKATUQF-BAGYTPMASA-N 0.000 claims 1
- WSFOYBOPRZUJTA-BAGYTPMASA-N (3r)-1-[2-[[(1r,2s)-2-[4-[(4-bromophenyl)methoxy]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=CC(Br)=CC=3)=CC=2)C1 WSFOYBOPRZUJTA-BAGYTPMASA-N 0.000 claims 1
- NMMZFPBXLQKWCO-BAGYTPMASA-N (3r)-1-[2-[[(1r,2s)-2-[4-[(4-chlorophenyl)methoxy]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=CC(Cl)=CC=3)=CC=2)C1 NMMZFPBXLQKWCO-BAGYTPMASA-N 0.000 claims 1
- BXALQNIJQDSQKF-FPNNDXFKSA-N (3r)-1-[2-[[(1r,2s)-2-[4-[(4-phenylphenyl)methoxy]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=CC(=CC=3)C=3C=CC=CC=3)=CC=2)C1 BXALQNIJQDSQKF-FPNNDXFKSA-N 0.000 claims 1
- VAGWVWUAEASTPV-QHAWAJNXSA-N (3r)-1-[2-[[(1r,2s)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(C=CC=2)C(F)(F)F)C1 VAGWVWUAEASTPV-QHAWAJNXSA-N 0.000 claims 1
- UKGARUUHGKZAJC-CMTIAEDTSA-N (3r)-1-[2-[[(1r,2s)-2-[4-phenylmethoxy-3-[4-(trifluoromethyl)phenyl]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=C(C(OCC=3C=CC=CC=3)=CC=2)C=2C=CC(=CC=2)C(F)(F)F)C1 UKGARUUHGKZAJC-CMTIAEDTSA-N 0.000 claims 1
- NAHDAZSNDUPYRR-SLYNCCJLSA-N (3r)-1-[2-[[(1r,2s)-2-[6-(3-methoxyphenyl)pyridin-3-yl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound COC1=CC=CC(C=2N=CC(=CC=2)[C@H]2[C@@H](C2)NCCN2C[C@H](N)CC2)=C1 NAHDAZSNDUPYRR-SLYNCCJLSA-N 0.000 claims 1
- ATZFUODKLCRKOF-WSTZPKSXSA-N (3r)-1-[2-[[(1r,2s)-2-[6-(4-chlorophenyl)pyridin-3-yl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=CC(Cl)=CC=2)C1 ATZFUODKLCRKOF-WSTZPKSXSA-N 0.000 claims 1
- QFYANZUXBPAMGB-WSTZPKSXSA-N (3r)-1-[2-[[(1r,2s)-2-[6-[3-(trifluoromethyl)phenyl]pyridin-3-yl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(C=CC=2)C(F)(F)F)C1 QFYANZUXBPAMGB-WSTZPKSXSA-N 0.000 claims 1
- BZRVBWUSMRDPGM-IXDOHACOSA-N (3r)-n,n-dimethyl-1-[2-[[(1r,2s)-2-phenylcyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@H](N(C)C)CCN1CCN[C@H]1[C@H](C=2C=CC=CC=2)C1 BZRVBWUSMRDPGM-IXDOHACOSA-N 0.000 claims 1
- VAGWVWUAEASTPV-PCCBWWKXSA-N (3s)-1-[2-[[(1r,2s)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(C=CC=2)C(F)(F)F)C1 VAGWVWUAEASTPV-PCCBWWKXSA-N 0.000 claims 1
- BZRVBWUSMRDPGM-YESZJQIVSA-N (3s)-n,n-dimethyl-1-[2-[[(1r,2s)-2-phenylcyclopropyl]amino]ethyl]pyrrolidin-3-amine Chemical compound C1[C@@H](N(C)C)CCN1CCN[C@H]1[C@H](C=2C=CC=CC=2)C1 BZRVBWUSMRDPGM-YESZJQIVSA-N 0.000 claims 1
- DRMKVHQNZVCKDG-SJBAFXMYSA-N 1-cyclopropyl-n'-[(1r,2s)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropyl]ethane-1,2-diamine Chemical compound C1=CC([C@@H]2C[C@H]2NCC(N)C2CC2)=CC=C1C1=CC=CC(C(F)(F)F)=C1 DRMKVHQNZVCKDG-SJBAFXMYSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- UGWAJVCPADIRPW-AKIFATBCSA-N 4-[[4-[(1s,2r)-2-[2-[(3r)-3-aminopyrrolidin-1-yl]ethylamino]cyclopropyl]phenoxy]methyl]benzonitrile Chemical compound C1[C@H](N)CCN1CCN[C@H]1[C@H](C=2C=CC(OCC=3C=CC(=CC=3)C#N)=CC=2)C1 UGWAJVCPADIRPW-AKIFATBCSA-N 0.000 claims 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- YBIDJXFXIZRDEE-VQTJNVASSA-N N-cyclopropyl-N'-[(1R,2S)-2-(4-phenoxyphenyl)cyclopropyl]ethane-1,2-diamine Chemical compound C1(CC1)NCCN[C@H]1[C@@H](C1)C1=CC=C(C=C1)OC1=CC=CC=C1 YBIDJXFXIZRDEE-VQTJNVASSA-N 0.000 claims 1
- VHBCVESMJOJIRL-IZZNHLLZSA-N N-cyclopropyl-N'-[(1R,2S)-2-[4-(2-phenylphenyl)phenyl]cyclopropyl]ethane-1,2-diamine Chemical compound C1(=CC=C(C=C1)[C@H]1[C@@H](C1)NCCNC1CC1)C=1C(=CC=CC=1)C1=CC=CC=C1 VHBCVESMJOJIRL-IZZNHLLZSA-N 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- YPBRQNQXWALCHZ-FCHUYYIVSA-N n',n'-diethyl-n-[(1r,2s)-2-[4-[(3-fluorophenyl)methoxy]phenyl]cyclopropyl]ethane-1,2-diamine Chemical compound CCN(CC)CCN[C@@H]1C[C@H]1C(C=C1)=CC=C1OCC1=CC=CC(F)=C1 YPBRQNQXWALCHZ-FCHUYYIVSA-N 0.000 claims 1
- CUQSYDVZERBOMN-LEWJYISDSA-N n',n'-diethyl-n-[(1r,2s)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]cyclopropyl]ethane-1,2-diamine Chemical compound CCN(CC)CCN[C@@H]1C[C@H]1C1=CC=C(C=2C=C(C=CC=2)C(F)(F)F)C=C1 CUQSYDVZERBOMN-LEWJYISDSA-N 0.000 claims 1
- DVBSOEFWXFGEMP-LSDHHAIUSA-N n',n'-diethyl-n-[(1r,2s)-2-phenylcyclopropyl]ethane-1,2-diamine Chemical compound CCN(CC)CCN[C@@H]1C[C@H]1C1=CC=CC=C1 DVBSOEFWXFGEMP-LSDHHAIUSA-N 0.000 claims 1
- NBJLJFJELKATJD-UHFFFAOYSA-N n',n'-dimethyl-n-(2-phenylcyclopropyl)ethane-1,2-diamine Chemical compound CN(C)CCNC1CC1C1=CC=CC=C1 NBJLJFJELKATJD-UHFFFAOYSA-N 0.000 claims 1
- AZHJFXWZXIPIDC-KFSCXFRDSA-N n'-(2-adamantyl)-n-[(1r,2s)-2-phenylcyclopropyl]ethane-1,2-diamine Chemical compound C1([C@@H]2C[C@H]2NCCNC2C3CC4CC(C3)CC2C4)=CC=CC=C1 AZHJFXWZXIPIDC-KFSCXFRDSA-N 0.000 claims 1
- RTPFABDYVHBIDV-VQTJNVASSA-N n'-[(1r,2s)-2-[4-(3-chlorophenyl)phenyl]cyclopropyl]-n-cyclopropylethane-1,2-diamine Chemical compound ClC1=CC=CC(C=2C=CC(=CC=2)[C@H]2[C@@H](C2)NCCNC2CC2)=C1 RTPFABDYVHBIDV-VQTJNVASSA-N 0.000 claims 1
- MHORTFLUTXEXFM-LEWJYISDSA-N n'-[(1r,2s)-2-[4-[(3-bromophenyl)methoxy]phenyl]cyclopropyl]-n-cyclopropylethane-1,2-diamine Chemical compound BrC1=CC=CC(COC=2C=CC(=CC=2)[C@H]2[C@@H](C2)NCCNC2CC2)=C1 MHORTFLUTXEXFM-LEWJYISDSA-N 0.000 claims 1
- AHXKVJVCGLFBPS-FCHUYYIVSA-N n'-[(1r,2s)-2-phenylcyclopropyl]-n-undecylethane-1,2-diamine Chemical compound CCCCCCCCCCCNCCN[C@@H]1C[C@H]1C1=CC=CC=C1 AHXKVJVCGLFBPS-FCHUYYIVSA-N 0.000 claims 1
- VFINUHQWEAVJCD-LSDHHAIUSA-N n-[2-(dimethylamino)ethyl]-n'-[(1r,2s)-2-phenylcyclopropyl]ethane-1,2-diamine Chemical compound CN(C)CCNCCN[C@@H]1C[C@H]1C1=CC=CC=C1 VFINUHQWEAVJCD-LSDHHAIUSA-N 0.000 claims 1
- VRFRQFHGEDELOY-RBUKOAKNSA-N n-cyclooctyl-n'-[(1r,2s)-2-phenylcyclopropyl]ethane-1,2-diamine Chemical compound N([C@H]1[C@@H](C1)C=1C=CC=CC=1)CCNC1CCCCCCC1 VRFRQFHGEDELOY-RBUKOAKNSA-N 0.000 claims 1
- NVBCQZQTXUJEFW-UONOGXRCSA-N n-cyclopropyl-n'-[(1r,2s)-2-phenylcyclopropyl]ethane-1,2-diamine Chemical compound C1([C@@H]2C[C@H]2NCCNC2CC2)=CC=CC=C1 NVBCQZQTXUJEFW-UONOGXRCSA-N 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical compound NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09171425.3 | 2009-09-25 | ||
| EP09171425 | 2009-09-25 | ||
| EP10150866 | 2010-01-15 | ||
| EP10150866.1 | 2010-01-15 | ||
| PCT/EP2010/055131 WO2011035941A1 (en) | 2009-09-25 | 2010-04-19 | Lysine specific demethylase-1 inhibitors and their use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013505903A JP2013505903A (ja) | 2013-02-21 |
| JP2013505903A5 true JP2013505903A5 (enExample) | 2013-06-06 |
| JP5699152B2 JP5699152B2 (ja) | 2015-04-08 |
Family
ID=42829238
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012530181A Expired - Fee Related JP5699152B2 (ja) | 2009-09-25 | 2010-04-19 | リジン特異的デメチラーゼ−１阻害剤およびその使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8859555B2 (enExample) |
| EP (1) | EP2480528B1 (enExample) |
| JP (1) | JP5699152B2 (enExample) |
| KR (1) | KR101736218B1 (enExample) |
| CN (1) | CN102639496B (enExample) |
| AU (1) | AU2010297557C1 (enExample) |
| BR (1) | BR112012006572A2 (enExample) |
| CA (1) | CA2812683C (enExample) |
| IL (1) | IL218778A (enExample) |
| MX (1) | MX338041B (enExample) |
| RU (1) | RU2602814C2 (enExample) |
| WO (1) | WO2011035941A1 (enExample) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| WO2010084160A1 (en) | 2009-01-21 | 2010-07-29 | Oryzon Genomics S.A. | Phenylcyclopropylamine derivatives and their medical use |
| JP5699152B2 (ja) | 2009-09-25 | 2015-04-08 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的デメチラーゼ−１阻害剤およびその使用 |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011106574A2 (en) * | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
| JP5868948B2 (ja) | 2010-04-19 | 2016-02-24 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的脱メチル化酵素１阻害薬およびその使用 |
| ES2564352T3 (es) * | 2010-04-20 | 2016-03-22 | Università Degli Studi Di Roma "La Sapienza" | Derivados de tranilcipromina como inhibidores de la histona-desmetilasa LSD1 y/o LSD2 |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| WO2012013728A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012045883A1 (en) * | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| EP2712315B1 (en) | 2011-02-08 | 2021-11-24 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| EP2712316A1 (en) | 2011-02-08 | 2014-04-02 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| JP5813855B2 (ja) | 2011-03-25 | 2015-11-17 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ | Ｌｓｄ１阻害剤としてのシクロプロピルアミン |
| WO2012156537A2 (en) | 2011-05-19 | 2012-11-22 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| US20140329833A1 (en) | 2011-05-19 | 2014-11-06 | Oryzon Genomics, S.A | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| CN103842332B (zh) | 2011-08-09 | 2016-08-17 | 武田药品工业株式会社 | 环丙胺化合物 |
| US9289415B2 (en) | 2011-09-01 | 2016-03-22 | The Brigham And Women's Hospital, Inc. | Treatment of cancer |
| AU2012324803B9 (en) | 2011-10-20 | 2017-08-24 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
| SG11201401066PA (en) | 2011-10-20 | 2014-10-30 | Oryzon Genomics Sa | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| WO2014058071A1 (ja) | 2012-10-12 | 2014-04-17 | 武田薬品工業株式会社 | シクロプロパンアミン化合物およびその用途 |
| EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| WO2014194280A2 (en) * | 2013-05-30 | 2014-12-04 | The Board of Regents of the Nevada System of Higher Education on behalf of the University of | Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells |
| EP3030323B1 (en) | 2013-08-06 | 2019-04-24 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| US9186391B2 (en) | 2013-08-29 | 2015-11-17 | Musc Foundation For Research Development | Cyclic peptide inhibitors of lysine-specific demethylase 1 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9493450B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| PE20161573A1 (es) | 2014-02-13 | 2017-01-19 | Incyte Corp | Ciclopropilamina como inhibidor de la lsd1 |
| PE20161441A1 (es) | 2014-04-11 | 2017-01-21 | Takeda Pharmaceuticals Co | Compuesto de ciclopropanamina y sus usos |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| ES3005884T3 (en) | 2015-02-12 | 2025-03-17 | Imago Biosciences Inc | A kdm1a inhibitor and its use in therapy |
| PE20180455A1 (es) | 2015-04-03 | 2018-03-05 | Incyte Corp | Compuestos heterociclicos como inhibidores de lsd1 |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| US20180284095A1 (en) | 2015-06-12 | 2018-10-04 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| EP3307267B1 (en) | 2016-06-10 | 2019-04-10 | Oryzon Genomics, S.A. | Multiple sclerosis treatment |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| SG10202001219UA (en) | 2015-08-12 | 2020-03-30 | Incyte Corp | Salts of an lsd1 inhibitor |
| WO2017079476A1 (en) | 2015-11-05 | 2017-05-11 | Mirati Therapeutics, Inc. | Lsd1 inhibitors |
| US9809541B2 (en) | 2015-12-29 | 2017-11-07 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| CN109072195A (zh) | 2015-12-30 | 2018-12-21 | 诺华股份有限公司 | 具有增强功效的免疫效应细胞疗法 |
| MX2018011100A (es) | 2016-03-15 | 2019-01-10 | Oryzon Genomics Sa | Combinaciones de inhibidores de desmetilasa-1 especifica de lisina (lsd1) para el tratamiento de malignidades hematologicas. |
| CN120661674A (zh) | 2016-03-15 | 2025-09-19 | 奥莱松基因组股份有限公司 | 用于治疗实体瘤的lsd1抑制剂的组合 |
| US11034991B2 (en) | 2016-03-16 | 2021-06-15 | Oryzon Genomics S.A. | Methods to determine KDM1A target engagement and chemoprobes useful therefor |
| CN109414410B (zh) | 2016-04-22 | 2022-08-12 | 因赛特公司 | Lsd1抑制剂的制剂 |
| WO2018035259A1 (en) | 2016-08-16 | 2018-02-22 | Imago Biosciences, Inc. | Methods and processes for the preparation of kdm1a inhibitors |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| RU2765152C2 (ru) * | 2017-05-26 | 2022-01-26 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| CA3071804A1 (en) | 2017-08-03 | 2019-02-07 | Oryzon Genomics, S.A. | Use of a kdm1a inhibitor in the treatment of behavior alterations |
| WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
| IL279260B2 (en) | 2018-05-11 | 2024-10-01 | Imago Biosciences Inc | Kdm1a inhibitors for the treatment of disease |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| CN113631164A (zh) | 2019-03-20 | 2021-11-09 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
| HRP20260110T1 (hr) | 2019-03-20 | 2026-03-13 | Oryzon Genomics, S.A. | Vafidemstat za liječenje neagresivnih simptoma graničnog poremećaja osobnosti |
| JP2022546908A (ja) | 2019-07-05 | 2022-11-10 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法 |
| WO2021254417A1 (zh) * | 2020-06-17 | 2021-12-23 | 贝达药业股份有限公司 | 双环类化合物及其应用 |
| EP3964204A1 (en) | 2020-09-08 | 2022-03-09 | Université d'Aix-Marseille | Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues |
| MX2023011779A (es) | 2021-04-08 | 2023-11-22 | Oryzon Genomics Sa | Combinaciones de inhibidores de lsd1 para el tratamiento de canceres mieloides. |
| CN119497613A (zh) | 2022-05-09 | 2025-02-21 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗nf1-突变肿瘤的方法 |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| CN114853680A (zh) * | 2022-06-06 | 2022-08-05 | 沈阳药科大学 | 芳香六元环并咪唑类衍生物及其制备方法和应用 |
| CN120529900A (zh) | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
| CN116284214A (zh) * | 2023-03-09 | 2023-06-23 | 郑州大学 | 二肽类化合物及其制备方法和应用 |
Family Cites Families (125)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3106578A (en) | 1960-09-16 | 1963-10-08 | Smith Kline French Lab | Nu-phenethyl-2-phenylcyclopropylamine derivatives |
| US3365458A (en) | 1964-06-23 | 1968-01-23 | Aldrich Chem Co Inc | N-aryl-n'-cyclopropyl-ethylene diamine derivatives |
| US3532749A (en) | 1965-05-11 | 1970-10-06 | Aldrich Chem Co Inc | N'-propargyl-n**2-cyclopropyl-ethylenediamines and the salts thereof |
| US3471522A (en) | 1967-09-29 | 1969-10-07 | Aldrich Chem Co Inc | N-cyclopropyl-n'-furfuryl-n'-methyl ethylene diamines |
| US3532712A (en) | 1967-09-29 | 1970-10-06 | Aldrich Chem Co Inc | N'-cyclopropyl ethylenediamine derivatives |
| US3654306A (en) | 1970-01-26 | 1972-04-04 | Robins Co Inc A H | 5-azaspiro(2.4)heptane-4 6-diones |
| US3758684A (en) | 1971-09-07 | 1973-09-11 | Burroughs Wellcome Co | Treating dna virus infections with amino purine derivatives |
| US4530901A (en) | 1980-01-08 | 1985-07-23 | Biogen N.V. | Recombinant DNA molecules and their use in producing human interferon-like polypeptides |
| US4409243A (en) | 1981-11-09 | 1983-10-11 | Julian Lieb | Treatment of auto-immune and inflammatory diseases |
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| GB9311282D0 (en) | 1993-06-01 | 1993-07-21 | Rhone Poulenc Rorer Ltd | New compositions of matter |
| CN1147459C (zh) | 1994-10-21 | 2004-04-28 | Nps药物有限公司 | 钙受体活性化合物 |
| US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
| US20040132820A1 (en) | 1996-02-15 | 2004-07-08 | Jean Gosselin | Agents with leukotriene B4-like antiviral (DNA) and anti-neoplastic activities |
| GB9615730D0 (en) | 1996-07-26 | 1996-09-04 | Medical Res Council | Anti-viral agent 1 |
| US5961987A (en) | 1996-10-31 | 1999-10-05 | University Of Iowa Research Foundation | Ocular protein stimulants |
| DE19647615A1 (de) | 1996-11-18 | 1998-05-20 | Bayer Ag | Verfahren zur Herstellung von Cyclopropylaminen |
| AR017014A1 (es) | 1997-07-22 | 2001-08-22 | Astrazeneca Ab | Compuestos de triazolo [4,5-d]pirimidina, composiciones farmaceuticas, uso de los mismos para preparar medicamentos y procesos para la preparacionde dichos compuestos |
| SE9702772D0 (sv) | 1997-07-22 | 1997-07-22 | Astra Pharma Prod | Novel compounds |
| AU1631699A (en) | 1997-12-18 | 1999-07-05 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
| US6809120B1 (en) | 1998-01-13 | 2004-10-26 | University Of Saskatchewan Technologies Inc. | Composition containing propargylamine for enhancing cancer therapy |
| DK1071752T3 (da) | 1998-04-21 | 2003-10-20 | Micromet Ag | CD19xCD3-specifikke polypeptider og anvendelsen deraf |
| SE9802206D0 (sv) | 1998-06-22 | 1998-06-22 | Astra Pharma Inc | Novel compounds |
| TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
| MY132006A (en) | 2000-05-26 | 2007-09-28 | Schering Corp | ADENOSINE A2a RECEPTOR ANTAGONISTS |
| JP2001354563A (ja) | 2000-06-09 | 2001-12-25 | Sankyo Co Ltd | 置換ベンジルアミン類を含有する医薬 |
| US8519005B2 (en) | 2000-07-27 | 2013-08-27 | Thomas N. Thomas | Compositions and methods to prevent toxicity of antiinflammatory agents and enhance their efficacy |
| EP1193268A1 (en) | 2000-09-27 | 2002-04-03 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases |
| JP2004531506A (ja) | 2001-03-29 | 2004-10-14 | ブリストル−マイヤーズ スクイブ カンパニー | 選択的なセロトニン再取り込みインヒビターとしてのシクロプロピルインドール誘導体 |
| DE10123163A1 (de) | 2001-05-09 | 2003-01-16 | Gruenenthal Gmbh | Substituierte Cyclohexan-1,4-diaminderivate |
| US20030008844A1 (en) | 2001-05-17 | 2003-01-09 | Keryx Biopharmaceuticals, Inc. | Use of sulodexide for the treatment of inflammatory bowel disease |
| US7544675B2 (en) | 2002-04-18 | 2009-06-09 | Ucb, S.A. | Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| JP4901102B2 (ja) | 2002-05-03 | 2012-03-21 | エクセリクシス， インク． | プロテインキナーゼモジュレーターおよびその使用方法 |
| AU2003273179A1 (en) | 2002-05-10 | 2003-12-12 | Bristol-Myers Squibb Company | 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors |
| US6951961B2 (en) | 2002-05-17 | 2005-10-04 | Marina Nikolaevna Protopopova | Methods of use and compositions for the diagnosis and treatment of infectious disease |
| US7456222B2 (en) * | 2002-05-17 | 2008-11-25 | Sequella, Inc. | Anti tubercular drug: compositions and methods |
| US20040033986A1 (en) | 2002-05-17 | 2004-02-19 | Protopopova Marina Nikolaevna | Anti tubercular drug: compositions and methods |
| EP1506172B1 (en) | 2002-05-20 | 2011-03-30 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| US7611704B2 (en) | 2002-07-15 | 2009-11-03 | Board Of Regents, The University Of Texas System | Compositions and methods for treating viral infections using antibodies and immunoconjugates to aminophospholipids |
| SE0202539D0 (sv) | 2002-08-27 | 2002-08-27 | Astrazeneca Ab | Compounds |
| ATE384724T1 (de) | 2002-12-13 | 2008-02-15 | Smithkline Beecham Corp | Cyclopropylverbindungen als ccr5 antagonisten |
| SG2012000667A (en) | 2003-01-08 | 2015-03-30 | Univ Washington | Antibacterial agents |
| US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| GB0303439D0 (en) | 2003-02-14 | 2003-03-19 | Pfizer Ltd | Antiparasitic terpene alkaloids |
| US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| ATE446752T1 (de) | 2003-04-24 | 2009-11-15 | Merck & Co Inc | Hemmer der akt aktivität |
| US7265246B2 (en) | 2003-07-03 | 2007-09-04 | Eli Lilly And Company | Indane derivates as muscarinic receptor agonists |
| EP1670787B1 (en) | 2003-09-11 | 2012-05-30 | iTherX Pharma, Inc. | Cytokine inhibitors |
| ATE551997T1 (de) | 2003-09-12 | 2012-04-15 | Merck Serono Sa | Sulfonamid-derivate zur behandlung von diabetes |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| CN1871008A (zh) | 2003-10-21 | 2006-11-29 | 默克公司 | 用于治疗神经病变性疼痛的三唑并－哒嗪化合物和它们的衍生物 |
| US7026339B2 (en) | 2003-11-07 | 2006-04-11 | Fan Yang | Inhibitors of HCV NS5B polymerase |
| DE602004026629D1 (de) | 2003-12-15 | 2010-05-27 | Japan Tobacco Inc | Cyclopropanderivate und ihre pharmazeutische verwendung |
| CA2551944A1 (en) | 2003-12-15 | 2005-06-30 | Almirall Prodesfarma Ag | 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
| ZA200605247B (en) | 2003-12-15 | 2007-10-31 | Japan Tobacco Inc | N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof |
| US7399825B2 (en) | 2003-12-24 | 2008-07-15 | Lipps Binie V | Synthetic peptide, inhibitor to DNA viruses |
| MXPA06012449A (es) | 2004-04-26 | 2007-01-17 | Pfizer | Inhibidores de la enzima integrasa de vih. |
| US20090275099A1 (en) | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| DE102004057594A1 (de) | 2004-11-29 | 2006-06-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substitueirte Pteridine zur Behandlung von entzündlichen Erkrankungen |
| WO2006071608A2 (en) | 2004-12-16 | 2006-07-06 | President And Fellows Of Harvard College | Histone demethylation mediated by the nuclear amine oxidase homolog lsd1 |
| ATE476970T1 (de) | 2005-02-18 | 2010-08-15 | Universitaetsklinikum Freiburg | Kontrolle der androgen rezeptor-abhängigen gen expression durch hemmung der aminoxidase aktivität der lysin spezifischen demethylase (lsd1) |
| US20060275366A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Controlled-release formulation |
| US7273882B2 (en) | 2005-06-21 | 2007-09-25 | Bristol-Myers Squibb Company | Aminoacetamide acyl guanidines as β-secretase inhibitors |
| EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
| KR101294467B1 (ko) | 2005-07-25 | 2013-09-09 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규 거대고리형 억제제 |
| CN101410367A (zh) | 2005-08-10 | 2009-04-15 | 约翰·霍普金斯大学 | 多胺用在抗寄生虫与抗癌治疗学以及作为赖氨酸-特异性脱甲基酶抑制剂 |
| US20090203750A1 (en) | 2005-08-24 | 2009-08-13 | Alan Kozikowski | 5-HT2C Receptor Agonists as Anorectic Agents |
| GB0517740D0 (en) * | 2005-08-31 | 2005-10-12 | Novartis Ag | Organic compounds |
| TW200745067A (en) | 2006-03-14 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
| DE602007003343D1 (de) | 2006-05-18 | 2009-12-31 | Syngenta Ltd | Neue mikrobiozide |
| US8198301B2 (en) | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
| EP2521786B1 (en) | 2006-07-20 | 2015-06-24 | Vical Incorporated | Compositions for vaccinating against hsv-2 |
| US20080161324A1 (en) | 2006-09-14 | 2008-07-03 | Johansen Lisa M | Compositions and methods for treatment of viral diseases |
| WO2008127734A2 (en) | 2007-04-13 | 2008-10-23 | The Johns Hopkins University | Lysine-specific demethylase inhibitors |
| US7906513B2 (en) | 2007-04-26 | 2011-03-15 | Enanta Pharmaceuticals, Inc. | Hydrazide-containing hepatitis C serine protease inhibitors |
| JP5140154B2 (ja) | 2007-06-27 | 2013-02-06 | アストラゼネカ・アクチエボラーグ | ピラジノン誘導体および肺疾患の処置におけるそれらの使用 |
| US20090176778A1 (en) | 2007-08-10 | 2009-07-09 | Franz Ulrich Schmitz | Certain nitrogen containing bicyclic chemical entities for treating viral infections |
| CN104628654A (zh) | 2007-09-17 | 2015-05-20 | 艾伯维巴哈马有限公司 | 抗感染嘧啶及其用途 |
| US20100016262A1 (en) | 2007-10-18 | 2010-01-21 | Yale University | Compositions and methods for reducing hepatotoxicity associated with drug administration and treating non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and associated cirrhosis |
| CA2702469A1 (en) | 2007-10-19 | 2009-04-23 | Boehringer Ingelheim International Gmbh | Ccr10 antagonists |
| KR20100109934A (ko) | 2007-12-26 | 2010-10-11 | 시오노기세야쿠 가부시키가이샤 | 글리코펩티드 항생 물질 배당화 유도체 |
| WO2009109991A2 (en) | 2008-01-23 | 2009-09-11 | Sun Pharma Advanced Research Company Ltd., | Novel hydrazide containing tyrosine kinase inhibitors |
| CA2713998A1 (en) | 2008-01-28 | 2009-08-06 | Janssen Pharmaceutica N.V. | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of.beta.-secretase (bace) |
| CA2718723C (en) | 2008-03-19 | 2018-05-08 | Aurimmed Pharma, Inc. | Novel compounds advantageous in the treatment of central nervous system diseases and disorders |
| MX2010010407A (es) | 2008-03-27 | 2010-10-25 | Gruenenthal Gmbh | Derivados de 4-aminociclohexanos sustituidos. |
| EP2321283B1 (en) | 2008-04-16 | 2016-07-13 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors |
| WO2009153197A1 (en) | 2008-06-18 | 2009-12-23 | F. Hoffmann-La Roche Ag | Halo-substituted pyrimidodiazepines as plkl inhibitors |
| EP2317992A2 (en) | 2008-07-24 | 2011-05-11 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Preventing or treating viral infection using an inhibitor of the lsd1 protein, a mao inhibitor or an inhibitor of lsd1 and a mao inhibitor |
| CA2732320C (en) | 2008-08-01 | 2017-08-29 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
| US8048887B2 (en) | 2008-09-11 | 2011-11-01 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis C |
| WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| WO2010084160A1 (en) | 2009-01-21 | 2010-07-29 | Oryzon Genomics S.A. | Phenylcyclopropylamine derivatives and their medical use |
| WO2010085749A2 (en) | 2009-01-23 | 2010-07-29 | Northwestern University | Potent and selective neuronal nitric oxide synthase inhibitors with improved membrane permeability |
| CN102427731B (zh) | 2009-02-27 | 2015-05-13 | 英安塔制药有限公司 | 丙型肝炎病毒抑制剂 |
| JP5659224B2 (ja) | 2009-05-15 | 2015-01-28 | ノバルティス アーゲー | アルドステロンシンターゼ阻害剤としてのアリールピリジン |
| US8389580B2 (en) | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| WO2010143582A1 (ja) | 2009-06-11 | 2010-12-16 | 公立大学法人名古屋市立大学 | フェニルシクロプロピルアミン誘導体及びlsd1阻害剤 |
| US9708255B2 (en) | 2009-08-18 | 2017-07-18 | Robert A. Casero | (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| EP2475254A4 (en) | 2009-09-11 | 2013-05-22 | Enanta Pharm Inc | HEPATITIS C-VIRUS HEMMER |
| JP5699152B2 (ja) | 2009-09-25 | 2015-04-08 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的デメチラーゼ−１阻害剤およびその使用 |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011057262A2 (en) | 2009-11-09 | 2011-05-12 | Evolva Inc. | Treatment of infections with tp receptor antagonists |
| WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| US9186337B2 (en) | 2010-02-24 | 2015-11-17 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae |
| US20130197088A1 (en) | 2010-03-12 | 2013-08-01 | Robert A. Casero, JR. | Compositions and Methods for Combinations of Oligoamines with 2-Difluoromethylornithine (DFMO) |
| JP5868948B2 (ja) | 2010-04-19 | 2016-02-24 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的脱メチル化酵素１阻害薬およびその使用 |
| CA2796504A1 (en) | 2010-04-20 | 2011-10-27 | Actavis Group Ptc Ehf | Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates |
| ES2564352T3 (es) | 2010-04-20 | 2016-03-22 | Università Degli Studi Di Roma "La Sapienza" | Derivados de tranilcipromina como inhibidores de la histona-desmetilasa LSD1 y/o LSD2 |
| RU2013103794A (ru) | 2010-06-30 | 2014-08-10 | Актавис Груп Птс Ехф | Новые способы получения производных фенилциклопропиламина и их применение для получения тикагрелора |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| WO2012013728A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
| WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| EP2712316A1 (en) | 2011-02-08 | 2014-04-02 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| EP2712315B1 (en) | 2011-02-08 | 2021-11-24 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| JP5813855B2 (ja) | 2011-03-25 | 2015-11-17 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ | Ｌｓｄ１阻害剤としてのシクロプロピルアミン |
| US20140329833A1 (en) | 2011-05-19 | 2014-11-06 | Oryzon Genomics, S.A | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| WO2012156537A2 (en) | 2011-05-19 | 2012-11-22 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| SG11201401066PA (en) | 2011-10-20 | 2014-10-30 | Oryzon Genomics Sa | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| AU2012324803B9 (en) | 2011-10-20 | 2017-08-24 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
-
2010
- 2010-04-19 JP JP2012530181A patent/JP5699152B2/ja not_active Expired - Fee Related
- 2010-04-19 CN CN201080053636.2A patent/CN102639496B/zh not_active Expired - Fee Related
- 2010-04-19 CA CA2812683A patent/CA2812683C/en not_active Expired - Fee Related
- 2010-04-19 EP EP10720278.0A patent/EP2480528B1/en not_active Not-in-force
- 2010-04-19 MX MX2012003499A patent/MX338041B/es active IP Right Grant
- 2010-04-19 AU AU2010297557A patent/AU2010297557C1/en not_active Ceased
- 2010-04-19 WO PCT/EP2010/055131 patent/WO2011035941A1/en not_active Ceased
- 2010-04-19 US US13/497,994 patent/US8859555B2/en not_active Expired - Fee Related
- 2010-04-19 BR BR112012006572A patent/BR112012006572A2/pt not_active IP Right Cessation
- 2010-04-19 KR KR1020127010672A patent/KR101736218B1/ko not_active Expired - Fee Related
- 2010-04-19 RU RU2012116584/04A patent/RU2602814C2/ru not_active IP Right Cessation
-
2012
- 2012-03-22 IL IL218778A patent/IL218778A/en not_active IP Right Cessation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013505903A5 (enExample) | ||
| RU2012116584A (ru) | Лизинспецифические ингибиторы деметилазы-1 и их применение | |
| RU2404164C2 (ru) | Производные пиридин-3-карбоксамида в качестве обратных агонистов св1 | |
| JP2022185107A5 (enExample) | ||
| JP2020503297A5 (enExample) | ||
| RU2014145856A (ru) | Азотсодержащее гетероциклическое соединение или его соль | |
| NZ703941A (en) | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases | |
| JP2015502335A5 (enExample) | ||
| JP2015517981A5 (enExample) | ||
| JP2022043059A5 (enExample) | ||
| JP2019505541A5 (enExample) | ||
| RU2007148217A (ru) | Получение производных n-фенил-2-пиримидинамина | |
| JP2020503299A5 (enExample) | ||
| IL264982B (en) | Hetero(aryl)cyclopropylamine compounds as lsd1 inhibitors | |
| RU2013108702A (ru) | Ингибиторы деметилазы lsd1 на основе арилциклопропиламина и их применение в медицине | |
| PE20140836A1 (es) | Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide | |
| JP2006515858A5 (enExample) | ||
| HRP20140884T1 (hr) | Derivati fenoksipiridinilamida i njihova primjena u lijeäśenju bolesnih stanja posredovanih inhibitorima pde4 | |
| RU2006126974A (ru) | Амидное производное и лекарственное средство | |
| NZ591226A (en) | Benzoic acid amides, production thereof, and use thereof as medicaments | |
| AR089134A1 (es) | Arilos y heteroarilos biciclicos inhibidores de los canales de sodio | |
| NZ601655A (en) | Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof | |
| RU2015143675A (ru) | Ship1 модуляторы и относящиеся к ним способы | |
| HRP20120656T1 (hr) | Derivati indazolil amida za liječenje poremećaja posredovanih glukokortikoidnim receptorom | |
| JP2016523923A5 (enExample) |