JP2013505903A5 - - Google Patents
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- 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
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- 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 | 2009-09-25 | ||
| EP09171425.3 | 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 (https=) | 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 (https=) |
| EP (1) | EP2480528B1 (https=) |
| JP (1) | JP5699152B2 (https=) |
| KR (1) | KR101736218B1 (https=) |
| CN (1) | CN102639496B (https=) |
| AU (1) | AU2010297557C1 (https=) |
| BR (1) | BR112012006572A2 (https=) |
| CA (1) | CA2812683C (https=) |
| IL (1) | IL218778A (https=) |
| MX (1) | MX338041B (https=) |
| RU (1) | RU2602814C2 (https=) |
| WO (1) | WO2011035941A1 (https=) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | 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 |
| RU2602814C2 (ru) | 2009-09-25 | 2016-11-20 | Оризон Дженомикс С.А. | Лизинспецифические ингибиторы деметилазы-1 и их применение |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | 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 |
| WO2011106573A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| RS55348B1 (sr) | 2010-04-19 | 2017-03-31 | Oryzon Gnomics S A | Inhibitori lizin specifične demetilaze-1 i njihova upotreba |
| CN102985402B (zh) * | 2010-04-20 | 2015-04-29 | 罗马大学 | 反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 |
| WO2012013728A1 (en) * | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
| EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| US9061966B2 (en) * | 2010-10-08 | 2015-06-23 | 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 |
| WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| EA023143B1 (ru) | 2011-03-25 | 2016-04-29 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Замещенный циклопропиламин в качестве ингибитора lsd1 |
| US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| EP2741741A2 (en) | 2011-05-19 | 2014-06-18 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| KR20140052018A (ko) | 2011-08-09 | 2014-05-02 | 다케다 야쿠힌 고교 가부시키가이샤 | 시클로프로판아민 화합물 |
| US9289415B2 (en) | 2011-09-01 | 2016-03-22 | The Brigham And Women's Hospital, Inc. | Treatment of cancer |
| RU2668952C2 (ru) * | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
| MX356344B (es) * | 2011-10-20 | 2018-05-23 | Oryzon Genomics Sa | Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1. |
| CN105051005B (zh) * | 2012-10-12 | 2017-06-13 | 武田药品工业株式会社 | 环丙胺化合物及其用途 |
| EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| EP3003301B1 (en) * | 2013-05-30 | 2021-02-24 | Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas | Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells |
| ES2734209T3 (es) | 2013-08-06 | 2019-12-04 | Imago Biosciences Inc | Inhibidores de KDM1A para el tratamiento de enfermedades |
| US9186391B2 (en) | 2013-08-29 | 2015-11-17 | Musc Foundation For Research Development | Cyclic peptide inhibitors of lysine-specific demethylase 1 |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| AR099994A1 (es) | 2014-04-11 | 2016-08-31 | Takeda Pharmaceuticals Co | Compuesto de ciclopropanamina y sus usos |
| WO2016007722A1 (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 |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| PL3256218T3 (pl) | 2015-02-12 | 2025-03-31 | Imago Biosciences Inc. | Inhibitor kdm1a i jego zastosowanie w terapii |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| CA2987876A1 (en) | 2015-06-12 | 2016-12-15 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| JP6916795B2 (ja) | 2015-12-29 | 2021-08-11 | ミラティ セラピューティクス， インコーポレイテッド | Ｌｓｄ１阻害剤 |
| AU2016382512A1 (en) | 2015-12-30 | 2018-07-12 | Novartis Ag | Immune effector cell therapies with enhanced efficacy |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| CN109462980B (zh) | 2016-03-15 | 2022-02-08 | 奥莱松基因组股份有限公司 | 用于治疗血液恶性肿瘤的lsd1抑制剂的组合 |
| WO2017158136A1 (en) | 2016-03-16 | 2017-09-21 | Oryzon Genomics, S.A. | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| JP6999574B2 (ja) | 2016-04-22 | 2022-01-18 | インサイト・コーポレイション | Ｌｓｄ１阻害剤の製剤 |
| RS58951B1 (sr) | 2016-06-10 | 2019-08-30 | Oryzon Genomics Sa | Lečenje multiple skleroze |
| 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 |
| CN110740991B (zh) * | 2017-05-26 | 2023-07-04 | 大鹏药品工业株式会社 | 新型联苯化合物或其盐 |
| MX2020001323A (es) | 2017-08-03 | 2020-03-20 | Oryzon Genomics Sa | Metodos para tratar alteraciones del comportamiento. |
| WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
| BR112021001066A2 (pt) | 2018-05-11 | 2021-04-20 | Imago Biosciences, Inc. | composto, método de tratamento de uma doença mediada por kdm1a, método de tratamento de uma doença mediada por globina, composição farmacêutica; método de inibição de kdm1a, método para obter um efeito em um paciente, e método para inibir pelo menos uma função de kdm1a |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| ES3053813T3 (en) | 2019-03-20 | 2026-01-26 | Oryzon Genomics Sa | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
| CN115667190B (zh) * | 2020-06-17 | 2024-10-11 | 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 |
| JP2024513260A (ja) | 2021-04-08 | 2024-03-22 | オリゾン ジェノミックス ソシエダッド アノニマ | 骨髄癌処置のためのｌｓｄ１阻害剤の組み合わせ |
| JP2025516648A (ja) | 2022-05-09 | 2025-05-30 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｌｓｄ１阻害薬を用いるｎｆ１変異腫瘍の治療法 |
| CN119546292A (zh) | 2022-05-09 | 2025-02-28 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法 |
| 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 |
| US6211244B1 (en) | 1994-10-21 | 2001-04-03 | Nps Pharmaceuticals, Inc. | Calcium receptor-active compounds |
| 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 |
| CZ302070B6 (cs) | 1998-04-21 | 2010-09-29 | Micromet Ag | Jednoretezcový multifunkcní polypeptid, polynukleotid, vektor obsahující tento polynukleotid, bunka transfekovaná tímto polynukleotidem, prostredek obsahující tento polypeptid, polynukleotid nebo vektor a jejich použití a zpusob identifikace aktiváto |
| 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 |
| SI1283839T1 (https=) | 2000-05-26 | 2005-08-31 | Schering Corp | |
| 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 |
| EP1499598A1 (en) | 2002-04-18 | 2005-01-26 | 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 |
| EP1501514B1 (en) | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7312214B2 (en) | 2002-05-10 | 2007-12-25 | Bristol-Myers Squibb Company | 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors |
| US20040033986A1 (en) | 2002-05-17 | 2004-02-19 | Protopopova Marina Nikolaevna | Anti tubercular drug: compositions and methods |
| 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 |
| ES2361011T3 (es) | 2002-05-20 | 2011-06-13 | Bristol-Myers Squibb Company | Inhibidores del virus de la hepatitis c. |
| 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 |
| US7569579B2 (en) | 2002-12-13 | 2009-08-04 | Smithkline Beecham Corporation | Cyclopropyl compounds as ccr5 antagonists |
| CA2851462A1 (en) | 2003-01-08 | 2004-07-29 | University Of 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 |
| CN1809536A (zh) | 2003-04-24 | 2006-07-26 | 麦克公司 | Akt活性抑制剂 |
| CA2529036A1 (en) | 2003-07-03 | 2005-02-03 | Eli Lilly And Company | Indane derivates as muscarinic receptor agonists |
| US7749999B2 (en) | 2003-09-11 | 2010-07-06 | Itherx Pharmaceuticals, Inc. | Alpha-ketoamides and derivatives thereof |
| AU2004271741A1 (en) | 2003-09-12 | 2005-03-24 | Laboratoires Serono Sa | Sulfonamide derivatives for the treatment of 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 |
| EP1677799A4 (en) | 2003-10-21 | 2008-09-10 | Merck & Co Inc | TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF FOR THE TREATMENT OF NEUROPATHIC PAIN |
| US7026339B2 (en) | 2003-11-07 | 2006-04-11 | Fan Yang | Inhibitors of HCV NS5B polymerase |
| JP2007514003A (ja) | 2003-12-15 | 2007-05-31 | アルミラル プロデスファルマ アーゲー | アデノシン受容体アンタゴニストとしての２，６−ビスヘテロアリール−４−アミノピリミジン |
| JP2007516982A (ja) | 2003-12-15 | 2007-06-28 | 日本たばこ産業株式会社 | シクロプロパン化合物及びその医薬用途 |
| KR20060109937A (ko) | 2003-12-15 | 2006-10-23 | 니뽄 다바코 산교 가부시키가이샤 | Ｎ-치환-ｎ-술포닐아미노시클로프로판 화합물 및 그의약제학적 용도 |
| US7399825B2 (en) | 2003-12-24 | 2008-07-15 | Lipps Binie V | Synthetic peptide, inhibitor to DNA viruses |
| WO2005103003A2 (en) | 2004-04-26 | 2005-11-03 | Pfizer Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
| 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 |
| ATE554184T1 (de) | 2004-12-16 | 2012-05-15 | Harvard College | Durch das nukleäre aminoxidase-homolog lsd1 vermittelte histondemethylierung |
| DE602005022826D1 (de) | 2005-02-18 | 2010-09-23 | 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 |
| AU2006276246B2 (en) | 2005-07-25 | 2012-09-27 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis C virus replication |
| CA2619005A1 (en) | 2005-08-10 | 2007-02-22 | Johns Hopkins University | Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors |
| WO2007025144A1 (en) | 2005-08-24 | 2007-03-01 | University Of Illinois - Chicago | 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 |
| GT200700041A (es) | 2006-05-18 | 2008-02-05 | Nuevos microbiocidas | |
| 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 |
| EP2170848B1 (en) | 2007-06-27 | 2014-10-22 | AstraZeneca AB | Pyrazinone derivatives and their use in the treatment of lung diseases |
| WO2009023179A2 (en) | 2007-08-10 | 2009-02-19 | Genelabs Technologies, Inc. | Nitrogen containing bicyclic chemical entities for treating viral infections |
| SI2368882T1 (sl) | 2007-09-17 | 2015-02-27 | Abbvie Bahamas Ltd. | Antiinfekcijski pirimidini in njihove uporabe |
| 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 |
| CN101959900A (zh) | 2007-12-26 | 2011-01-26 | 盐野义制药株式会社 | 糖肽类抗生素糖基化衍生物 |
| WO2009109991A2 (en) | 2008-01-23 | 2009-09-11 | Sun Pharma Advanced Research Company Ltd., | Novel hydrazide containing tyrosine kinase inhibitors |
| US8076358B2 (en) | 2008-01-28 | 2011-12-13 | Janssen Pharmaceutica Nv | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| RU2010142655A (ru) | 2008-03-19 | 2012-04-27 | Ауриммед Фарма, Инк. (Us) | Соединение, пригодное для лечения болезней и нарушений центральной нервной системы, и способ его получения |
| ES2464102T3 (es) | 2008-03-27 | 2014-05-30 | Grünenthal GmbH | Derivados de 4-aminociclohexano sustituidos |
| WO2010014921A2 (en) | 2008-08-01 | 2010-02-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
| EA024109B1 (ru) | 2008-04-16 | 2016-08-31 | Портола Фармасьютиклз, Инк. | Ингибиторы протеинкиназ |
| JP2011527667A (ja) | 2008-06-18 | 2011-11-04 | 武田薬品工業株式会社 | ハロ置換ピリミドジアゼピン |
| WO2010011845A2 (en) | 2008-07-24 | 2010-01-28 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Methods of preventing or treating viral infection or reactivation after latency in a host using inhibitors of the lsd1 protein |
| US8048887B2 (en) | 2008-09-11 | 2011-11-01 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis C |
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | 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 |
| KR101411889B1 (ko) | 2009-02-27 | 2014-06-27 | 이난타 파마슈티칼스, 인코포레이티드 | Ｃ형 간염 바이러스 억제제 |
| HRP20140371T1 (hr) | 2009-05-15 | 2014-05-23 | Novartis Ag | Arilpiridini kao inhibitori sinteze aldosterona |
| 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 |
| JPWO2010143582A1 (ja) | 2009-06-11 | 2012-11-22 | 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 |
| EP2467359A4 (en) | 2009-08-18 | 2013-01-09 | Univ Johns Hopkins | (BIS-) UREA- AND (BIS-) THIOMINE COMPOUNDS AS EPIGENE MODULATORS OF THE LYSINE-SPECIFIC DEMETHYLASE 1 AND METHODS OF DISEASE TREATMENT THEREWITH |
| EP2475254A4 (en) | 2009-09-11 | 2013-05-22 | Enanta Pharm Inc | HEPATITIS C-VIRUS HEMMER |
| RU2602814C2 (ru) | 2009-09-25 | 2016-11-20 | Оризон Дженомикс С.А. | Лизинспецифические ингибиторы деметилазы-1 и их применение |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | 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 |
| WO2011106573A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011113005A2 (en) | 2010-03-12 | 2011-09-15 | The Johns Hopkins University | Compositions and methods for combinations of oligoamines with 2-difluoromethylornithine (dfmo) |
| RS55348B1 (sr) | 2010-04-19 | 2017-03-31 | Oryzon Gnomics S A | Inhibitori lizin specifične demetilaze-1 i njihova upotreba |
| CN102985402B (zh) | 2010-04-20 | 2015-04-29 | 罗马大学 | 反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 |
| CA2796504A1 (en) | 2010-04-20 | 2011-10-27 | Actavis Group Ptc Ehf | Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates |
| WO2012001531A2 (en) | 2010-06-30 | 2012-01-05 | Actavis Group Ptc Ehf | Novel processes for the preparation of phenylcyclopropylamine derivatives and use thereof for preparing ticagrelor |
| EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | 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 |
| US9527805B2 (en) | 2010-09-10 | 2016-12-27 | Robert A. Casero | 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 |
| US9061966B2 (en) | 2010-10-08 | 2015-06-23 | 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 |
| WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| EA023143B1 (ru) | 2011-03-25 | 2016-04-29 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Замещенный циклопропиламин в качестве ингибитора lsd1 |
| EP2741741A2 (en) | 2011-05-19 | 2014-06-18 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| RU2668952C2 (ru) | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
| MX356344B (es) | 2011-10-20 | 2018-05-23 | Oryzon Genomics Sa | Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1. |
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2010
- 2010-04-19 RU RU2012116584/04A patent/RU2602814C2/ru not_active IP Right Cessation
- 2010-04-19 WO PCT/EP2010/055131 patent/WO2011035941A1/en not_active Ceased
- 2010-04-19 JP JP2012530181A patent/JP5699152B2/ja not_active Expired - Fee Related
- 2010-04-19 AU AU2010297557A patent/AU2010297557C1/en not_active Ceased
- 2010-04-19 EP EP10720278.0A patent/EP2480528B1/en not_active Not-in-force
- 2010-04-19 CN CN201080053636.2A patent/CN102639496B/zh not_active Expired - Fee Related
- 2010-04-19 US US13/497,994 patent/US8859555B2/en not_active Expired - Fee Related
- 2010-04-19 MX MX2012003499A patent/MX338041B/es active IP Right Grant
- 2010-04-19 CA CA2812683A patent/CA2812683C/en not_active Expired - Fee Related
- 2010-04-19 KR KR1020127010672A patent/KR101736218B1/ko not_active Expired - Fee Related
- 2010-04-19 BR BR112012006572A patent/BR112012006572A2/pt not_active IP Right Cessation
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2012
- 2012-03-22 IL IL218778A patent/IL218778A/en not_active IP Right Cessation
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