JP2013525318A5 - - Google Patents
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- Publication number
- JP2013525318A5 JP2013525318A5 JP2013505423A JP2013505423A JP2013525318A5 JP 2013525318 A5 JP2013525318 A5 JP 2013525318A5 JP 2013505423 A JP2013505423 A JP 2013505423A JP 2013505423 A JP2013505423 A JP 2013505423A JP 2013525318 A5 JP2013525318 A5 JP 2013525318A5
- Authority
- JP
- Japan
- Prior art keywords
- aminocyclopropyl
- trans
- compound
- ylcarbamate
- phenylamino
- 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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- 150000001875 compounds Chemical class 0.000 claims 27
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- -1 cycloalkylalkylamino Chemical group 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 125000006847 BOC protecting group Chemical group 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 101000619676 Drosophila melanogaster Lipid storage droplets surface-binding protein 2 Proteins 0.000 claims 2
- 101001050886 Homo sapiens Lysine-specific histone demethylase 1A Proteins 0.000 claims 2
- 101000613960 Homo sapiens Lysine-specific histone demethylase 1B Proteins 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 102100040596 Lysine-specific histone demethylase 1B Human genes 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 150000001266 acyl halides Chemical class 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 2
- 230000003796 beauty Effects 0.000 claims 2
- 150000001735 carboxylic acids Chemical class 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 150000007524 organic acids Chemical class 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- IRJRUHLVZNTFIU-UHFFFAOYSA-N C(CCCC(N)N)CCCO Chemical compound C(CCCC(N)N)CCCO IRJRUHLVZNTFIU-UHFFFAOYSA-N 0.000 claims 1
- 208000009889 Herpes Simplex Diseases 0.000 claims 1
- 108010074870 Histone Demethylases Proteins 0.000 claims 1
- 102000008157 Histone Demethylases Human genes 0.000 claims 1
- 102100024985 Lysine-specific histone demethylase 1A Human genes 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 241000700584 Simplexvirus Species 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- BBFSSGWGPSUYCK-XAGPSQNTSA-N [1-[4-[(1S,2R)-2-aminocyclopropyl]anilino]-1-oxo-3-phenylpropan-2-yl]-[(4-bromophenyl)methyl]carbamic acid Chemical compound N[C@@H]1C[C@H]1c1ccc(NC(=O)C(Cc2ccccc2)N(Cc2ccc(Br)cc2)C(O)=O)cc1 BBFSSGWGPSUYCK-XAGPSQNTSA-N 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- WHQIXYSISIAXMR-ZXABPTRBSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]-n-methylanilino]-1-oxo-3-phenylpropan-2-yl]carbamate Chemical compound C=1C=C([C@H]2[C@@H](C2)N)C=CC=1N(C)C(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WHQIXYSISIAXMR-ZXABPTRBSA-N 0.000 claims 1
- ASLBWLIVSCJXGE-VXLAJHQFSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-1-oxo-3,3-diphenylpropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(C(C=1C=CC=CC=1)C=1C=CC=CC=1)NC(=O)OCC1=CC=CC=C1 ASLBWLIVSCJXGE-VXLAJHQFSA-N 0.000 claims 1
- HDVDLEPVLVTECB-XAGPSQNTSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-1-oxo-3-phenylpropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 HDVDLEPVLVTECB-XAGPSQNTSA-N 0.000 claims 1
- QLBXSMSHSPUCHK-ZXABPTRBSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-1-oxo-4-phenylbutan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CCC1=CC=CC=C1 QLBXSMSHSPUCHK-ZXABPTRBSA-N 0.000 claims 1
- MTRYTBUOCQFRLH-XAGPSQNTSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-(4-bromophenyl)-1-oxopropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1=CC=C(Br)C=C1 MTRYTBUOCQFRLH-XAGPSQNTSA-N 0.000 claims 1
- PBWBVFCDMWLZOQ-ZXABPTRBSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]carbamate Chemical compound C1=CC(OC)=CC=C1CC(C(=O)NC=1C=CC(=CC=1)[C@H]1[C@@H](C1)N)NC(=O)OCC1=CC=CC=C1 PBWBVFCDMWLZOQ-ZXABPTRBSA-N 0.000 claims 1
- MXXUWNXLDQSFIG-XAGPSQNTSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-cyclohexyl-1-oxopropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1CCCCC1 MXXUWNXLDQSFIG-XAGPSQNTSA-N 0.000 claims 1
- DDNLQJBLMBTXLP-ABZYKWASSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-methyl-1-oxobutan-2-yl]carbamate Chemical compound C=1C=C([C@H]2[C@@H](C2)N)C=CC=1NC(=O)C(C(C)C)NC(=O)OCC1=CC=CC=C1 DDNLQJBLMBTXLP-ABZYKWASSA-N 0.000 claims 1
- MXIJEHVOYGTOKM-MDEZFMAYSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-naphthalen-1-yl-1-oxopropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC2=CC=CC=C12 MXIJEHVOYGTOKM-MDEZFMAYSA-N 0.000 claims 1
- QGICAEAHSKDUIT-MDEZFMAYSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CC1=CC=C(C=CC=C2)C2=C1 QGICAEAHSKDUIT-MDEZFMAYSA-N 0.000 claims 1
- MEUKJABSFDBHKI-LHJLODMPSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-4-(1-benzothiophen-3-yl)-1-oxobutan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CCC1=CSC2=CC=CC=C12 MEUKJABSFDBHKI-LHJLODMPSA-N 0.000 claims 1
- ZODMCOGPPKFWDE-QDSWCARHSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-4-(1h-indol-3-yl)-1-oxobutan-2-yl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)OCC=1C=CC=CC=1)CCC1=CNC2=CC=CC=C12 ZODMCOGPPKFWDE-QDSWCARHSA-N 0.000 claims 1
- DSONMQMFFYCVKT-MCOCGALXSA-N benzyl n-[1-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-4-methyl-1-oxopentan-2-yl]carbamate Chemical compound C=1C=C([C@H]2[C@@H](C2)N)C=CC=1NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 DSONMQMFFYCVKT-MCOCGALXSA-N 0.000 claims 1
- PQSQVGJMIYHPAM-ZVTBYLAHSA-N benzyl n-[2-[4-[(1s,2r)-2-aminocyclopropyl]anilino]-2-oxo-1-phenylethyl]carbamate Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(C=1C=CC=CC=1)NC(=O)OCC1=CC=CC=C1 PQSQVGJMIYHPAM-ZVTBYLAHSA-N 0.000 claims 1
- 230000024245 cell differentiation Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- PILDZWLLMBHVDL-XAGPSQNTSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]-2-(benzylcarbamoylamino)-3-phenylpropanamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C(NC(=O)NCC=1C=CC=CC=1)CC1=CC=CC=C1 PILDZWLLMBHVDL-XAGPSQNTSA-N 0.000 claims 1
- FBTOJOKQMRQDTN-JKSUJKDBSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]-2-phenylacetamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)CC1=CC=CC=C1 FBTOJOKQMRQDTN-JKSUJKDBSA-N 0.000 claims 1
- HNKLJSLPSPDIEF-LEWJYISDSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]-4-phenylbenzamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C1=CC=C(C=2C=CC=CC=2)C=C1 HNKLJSLPSPDIEF-LEWJYISDSA-N 0.000 claims 1
- FFYGOYSNGFPHEN-LSDHHAIUSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]benzamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C1=CC=CC=C1 FFYGOYSNGFPHEN-LSDHHAIUSA-N 0.000 claims 1
- KIXMLGAJOIZMLU-RBUKOAKNSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]naphthalene-1-carboxamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C1=CC=CC2=CC=CC=C12 KIXMLGAJOIZMLU-RBUKOAKNSA-N 0.000 claims 1
- FHEJLZAZDQKARO-RBUKOAKNSA-N n-[4-[(1s,2r)-2-aminocyclopropyl]phenyl]naphthalene-2-carboxamide Chemical compound N[C@@H]1C[C@H]1C(C=C1)=CC=C1NC(=O)C1=CC=C(C=CC=C2)C2=C1 FHEJLZAZDQKARO-RBUKOAKNSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32595210P | 2010-04-20 | 2010-04-20 | |
| US61/325,952 | 2010-04-20 | ||
| PCT/EP2011/055990 WO2011131576A1 (en) | 2010-04-20 | 2011-04-15 | Tranylcypromine derivatives as inhibitors of histone demethylase lsd1 and/or lsd2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013525318A JP2013525318A (ja) | 2013-06-20 |
| JP2013525318A5 true JP2013525318A5 (cg-RX-API-DMAC10.html) | 2014-05-29 |
| JP5934184B2 JP5934184B2 (ja) | 2016-06-15 |
Family
ID=43929076
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013505423A Active JP5934184B2 (ja) | 2010-04-20 | 2011-04-15 | ヒストンデメチラーゼｌｓｄ１及び／又はｌｓｄ２の阻害剤としてのトラニルシプロミン誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8765820B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP2560949B1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP5934184B2 (cg-RX-API-DMAC10.html) |
| CN (1) | CN102985402B (cg-RX-API-DMAC10.html) |
| AU (1) | AU2011244478B2 (cg-RX-API-DMAC10.html) |
| BR (1) | BR112012027062B8 (cg-RX-API-DMAC10.html) |
| CA (1) | CA2797011C (cg-RX-API-DMAC10.html) |
| EA (1) | EA022459B1 (cg-RX-API-DMAC10.html) |
| ES (1) | ES2564352T3 (cg-RX-API-DMAC10.html) |
| PL (1) | PL2560949T3 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2011131576A1 (cg-RX-API-DMAC10.html) |
| ZA (1) | ZA201207856B (cg-RX-API-DMAC10.html) |
Families Citing this family (80)
| 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 |
| KR101736218B1 (ko) | 2009-09-25 | 2017-05-16 | 오리존 지노믹스 에스.에이. | 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도 |
| WO2011042217A1 (en) | 2009-10-09 | 2011-04-14 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011106106A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011106105A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| 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 |
| EP3375775A1 (en) | 2010-07-29 | 2018-09-19 | 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 |
| 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 |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | 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 |
| EP2741741A2 (en) | 2011-05-19 | 2014-06-18 | 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 |
| JP6111195B2 (ja) * | 2011-08-09 | 2017-04-05 | 武田薬品工業株式会社 | シクロプロパンアミン化合物 |
| IL264982B (en) | 2011-10-20 | 2022-08-01 | Oryzon Genomics Sa | Hetero(aryl)cyclopropylamine compounds as lsd1 inhibitors |
| US9487512B2 (en) | 2011-10-20 | 2016-11-08 | Oryzon Genomics S.A. | (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
| CA2887598A1 (en) | 2012-10-12 | 2014-04-17 | Takeda Pharmaceutical Company Limited | Cyclopropanamine compound and use thereof |
| EP2740474A1 (en) * | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| CN105592888A (zh) | 2013-08-06 | 2016-05-18 | 伊美格生物科学公司 | 用于治疗疾病的kdm1a抑制剂 |
| SG10201806849WA (en) | 2014-02-13 | 2018-09-27 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| CN106488915B (zh) | 2014-02-13 | 2020-10-02 | 因赛特公司 | 作为lsd1抑制剂的环丙胺 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| TWI669291B (zh) | 2014-04-11 | 2019-08-21 | 日商武田藥品工業股份有限公司 | 環丙胺化合物及其用途 |
| MX375102B (es) * | 2014-05-30 | 2025-03-06 | Ieo St Europeo Di Oncologia S R L | Compuestos de ciclopropilamina como inhibidores de histona demetilasa |
| EP2949648A1 (en) | 2014-05-30 | 2015-12-02 | IEO - Istituto Europeo di Oncologia Srl | Cyclopropylamine derivatives as histone demethylase inhibitors |
| SG11201700007YA (en) * | 2014-07-03 | 2017-01-27 | Celgene Quanticel Res Inc | Inhibitors of lysine specific demethylase-1 |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| CN112125901A (zh) | 2014-09-05 | 2020-12-25 | 赛尔基因昆蒂赛尔研究公司 | 赖氨酸特异性脱甲基酶-1的抑制剂 |
| EP2993175A1 (en) | 2014-09-05 | 2016-03-09 | IEO - Istituto Europeo di Oncologia Srl | Thienopyrroles as histone demethylase inhibitors |
| ES2973286T3 (es) * | 2014-11-26 | 2024-06-19 | St Europeo Di Oncologia S R L | Modelos de trastornos del desarrollo neurológico basados en la reprogramación y usos de los mismos |
| CN107438593B (zh) * | 2015-01-30 | 2020-10-30 | 基因泰克公司 | 治疗化合物及其用途 |
| EP4559902A3 (en) | 2015-02-12 | 2025-08-20 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| US9944647B2 (en) | 2015-04-03 | 2018-04-17 | Incyte Corporation | Heterocyclic compounds as LSD1 inhibitors |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| MX2017015922A (es) | 2015-06-12 | 2018-12-11 | Oryzon Genomics Sa | Biomarcadores asociados con inhibidores de lsd1 y usos de los mismos. |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| UA126277C2 (uk) | 2015-08-12 | 2022-09-14 | Інсайт Корпорейшн | Солі інгібітору lsd1 |
| KR102204748B1 (ko) | 2015-11-27 | 2021-01-19 | 다이호야쿠힌고교 가부시키가이샤 | 신규 비페닐 화합물 또는 그의 염 |
| WO2017097865A1 (en) * | 2015-12-07 | 2017-06-15 | Istituto Europeo Di Oncologia | Combination of caloric restriction (cr) or igf1/insulin receptor inhibitor with lsd1 inhibitor |
| EP3429571B1 (en) | 2016-03-15 | 2025-10-08 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| KR102646126B1 (ko) | 2016-03-15 | 2024-03-11 | 오리존 지노믹스 에스.에이. | 혈액 악성 종양의 치료를 위한 lsd1 억제제의 조합물 |
| JP2019512546A (ja) | 2016-03-16 | 2019-05-16 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ |
| BR112018071585B1 (pt) | 2016-04-22 | 2024-01-02 | Incyte Corporation | Formulações de um inibidor de lsd1, seus usos e método de preparação das mesmas |
| EP3246330A1 (en) | 2016-05-18 | 2017-11-22 | Istituto Europeo di Oncologia S.r.l. | Imidazoles as histone demethylase inhibitors |
| CA2988220C (en) | 2016-06-10 | 2021-03-02 | Oryzon Genomics, S.A. | Methods of treating multiple sclerosis |
| US11390590B2 (en) | 2016-08-16 | 2022-07-19 | Imago Biosciences, Inc. | Methods and processes for the preparation of KDM1A inhibitors |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| WO2018197583A1 (en) | 2017-04-26 | 2018-11-01 | Istituto Europeo Di Oncologia | Use of a combinational therapy of lsd1 inhibitors with p21 activators in the treatment of cancer |
| EP3632443B1 (en) * | 2017-05-26 | 2023-06-07 | Taiho Pharmaceutical Co., Ltd. | Anti-tumor effect potentiator using a biphenyl compound |
| KR102361918B1 (ko) | 2017-05-26 | 2022-02-14 | 다이호야쿠힌고교 가부시키가이샤 | 신규 비페닐 화합물 또는 그의 염 |
| MA50518A (fr) | 2017-05-31 | 2020-09-09 | Taiho Pharmaceutical Co Ltd | Méthode de prédiction de l'effet thérapeutique d'un inhibiteur de lsd1 en fonction de l'expression d'insm1 |
| BR112020000827A2 (pt) | 2017-08-03 | 2020-07-21 | Oryzon Genomics, S.A. | métodos de tratamento de alterações de comportamento |
| EP3668877B1 (en) | 2017-08-18 | 2024-05-01 | Istituto Europeo di Oncologia S.r.l. | Indole derivatives as histone demethylase inhibitors |
| WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
| US11685782B2 (en) | 2017-10-23 | 2023-06-27 | Children's Medical Center Corporation | Methods of treating cancer using LSD1 inhibitors in combination with immunotherapy |
| AU2019265022B2 (en) | 2018-05-11 | 2024-08-15 | Imago Biosciences, Inc. | KDM1A inhibitors for the treatment of disease |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| WO2020052647A1 (zh) * | 2018-09-13 | 2020-03-19 | 南京明德新药研发有限公司 | 作为lsd1抑制剂的杂螺环类化合物及其应用 |
| PH12021552251A1 (en) | 2019-03-20 | 2022-07-25 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| JP7535797B2 (ja) | 2019-03-20 | 2024-08-19 | オリソン ヘノミクス，ソシエダ アノニマ | 化合物バフィデムスタット（ｖａｆｉｄｅｍｓｔａｔ）などｋｄｍ１ａ阻害剤を使用した注意欠陥多動性障害の処置方法 |
| WO2021004610A1 (en) | 2019-07-05 | 2021-01-14 | Oryzon Genomics, S.A. | Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors |
| CA3157404A1 (en) | 2019-11-13 | 2021-05-20 | Taiho Pharmaceutical Co., Ltd. | Novel salt of terphenyl compound |
| IT202000007873A1 (it) | 2020-04-14 | 2021-10-14 | St Europeo Di Oncologia S R L | Molecole per uso nel trattamento delle infezioni virali |
| CN111454252B (zh) * | 2020-05-13 | 2021-06-11 | 郑州大学 | 含芳环/芳杂环-三氮唑-亚甲基-tcp衍生物及其制备方法和应用 |
| CN113880766B (zh) * | 2020-07-04 | 2023-10-31 | 成都先导药物开发股份有限公司 | 一种免疫调节剂 |
| KR20220027555A (ko) | 2020-08-27 | 2022-03-08 | 재단법인대구경북과학기술원 | 트라닐시프로민을 유효성분으로 포함하는 신경염증성 질환의 예방 또는 치료용 약학적 조성물 |
| 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 |
| WO2022058405A2 (en) | 2020-09-16 | 2022-03-24 | Ifom - Istituto Firc Di Oncologia Molecolare | Histone deacetylase inhibitors and uses thereof |
| CN113750095B (zh) * | 2021-03-10 | 2023-07-04 | 中国医学科学院医药生物技术研究所 | 含有环丙基骨架的化合物在制备治疗和/或预防冠状病毒感染药物中的应用 |
| BR112023020554A2 (pt) | 2021-04-08 | 2023-12-05 | Oryzon Genomics Sa | Combinações de inibidores de lsd1 para o tratamento de cânceres mieloides |
| JP2025516647A (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阻害薬を用いる悪性末梢神経鞘腫（ｍｐｎｓｔ）の治療法 |
| 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 |
| EP4622635A1 (en) | 2022-11-24 | 2025-10-01 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9311282D0 (en) * | 1993-06-01 | 1993-07-21 | Rhone Poulenc Rorer Ltd | New compositions of matter |
| JP2000507575A (ja) * | 1996-03-29 | 2000-06-20 | ジー．ディー．サール アンド カンパニー | シクロプロピルアルカノイック酸誘導体 |
| US20020052370A1 (en) * | 2000-07-06 | 2002-05-02 | Barber Christopher Gordon | Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase |
| WO2005007614A1 (en) * | 2003-07-03 | 2005-01-27 | The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 | Monoamine oxidase inhibitors |
| US7276608B2 (en) * | 2003-07-11 | 2007-10-02 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as cannabinoid receptor modulators |
| TW200528455A (en) * | 2003-12-19 | 2005-09-01 | Bristol Myers Squibb Co | Azabicyclic heterocycles as cannabinoid receptor modulators |
| EP1693062A3 (en) * | 2005-02-18 | 2007-12-12 | Universitätsklinikum Freiburg | Androgen receptor-dependent gene expression control |
| GB0705656D0 (en) * | 2007-03-23 | 2007-05-02 | Addex Pharmaceuticals Sa | Novel compounds E1 |
| 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 |
| 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 |
| 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 |
| KR101736218B1 (ko) | 2009-09-25 | 2017-05-16 | 오리존 지노믹스 에스.에이. | 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도 |
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