JP2016509047A5 - - Google Patents
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- JP2016509047A5 JP2016509047A5 JP2015558495A JP2015558495A JP2016509047A5 JP 2016509047 A5 JP2016509047 A5 JP 2016509047A5 JP 2015558495 A JP2015558495 A JP 2015558495A JP 2015558495 A JP2015558495 A JP 2015558495A JP 2016509047 A5 JP2016509047 A5 JP 2016509047A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- alkyl
- heteroaryl
- aryl
- alkynyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 225
- 125000000304 alkynyl group Chemical group 0.000 claims description 175
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 171
- 125000003342 alkenyl group Chemical group 0.000 claims description 162
- 125000001072 heteroaryl group Chemical group 0.000 claims description 145
- 125000000623 heterocyclic group Chemical group 0.000 claims description 145
- 125000003118 aryl group Chemical group 0.000 claims description 141
- 229910052799 carbon Inorganic materials 0.000 claims description 95
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 81
- 229910052739 hydrogen Inorganic materials 0.000 claims description 81
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 74
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 64
- 150000001875 compounds Chemical class 0.000 claims description 56
- 125000003545 alkoxy group Chemical group 0.000 claims description 45
- 125000004043 oxo group Chemical group O=* 0.000 claims description 42
- 229910052736 halogen Inorganic materials 0.000 claims description 36
- 150000002367 halogens Chemical class 0.000 claims description 36
- 239000000203 mixture Substances 0.000 claims description 35
- -1 heterocyclylene Chemical group 0.000 claims description 34
- 125000002947 alkylene group Chemical group 0.000 claims description 29
- 125000004104 aryloxy group Chemical group 0.000 claims description 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 27
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 27
- 239000000651 prodrug Substances 0.000 claims description 25
- 229940002612 prodrug Drugs 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 25
- 239000012453 solvate Substances 0.000 claims description 25
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 23
- 125000004419 alkynylene group Chemical group 0.000 claims description 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 18
- 125000004450 alkenylene group Chemical group 0.000 claims description 18
- 125000000732 arylene group Chemical group 0.000 claims description 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 18
- 125000005549 heteroarylene group Chemical group 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims description 18
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 17
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims description 17
- 125000004122 cyclic group Chemical group 0.000 claims description 16
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 14
- 125000003003 spiro group Chemical group 0.000 claims description 11
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 238000006467 substitution reaction Methods 0.000 claims description 9
- 230000001419 dependent effect Effects 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 229940072107 ascorbate Drugs 0.000 claims description 2
- 235000010323 ascorbic acid Nutrition 0.000 claims description 2
- 239000011668 ascorbic acid Substances 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 7
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 2
- 0 **N(*)Cc1nccc(*)c1 Chemical compound **N(*)Cc1nccc(*)c1 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361770058P | 2013-02-27 | 2013-02-27 | |
| US201361770067P | 2013-02-27 | 2013-02-27 | |
| US201361770065P | 2013-02-27 | 2013-02-27 | |
| DKPA201370114 | 2013-02-27 | ||
| DKPA201370114 | 2013-02-27 | ||
| US61/770,065 | 2013-02-27 | ||
| US61/770,058 | 2013-02-27 | ||
| DKPA201370113 | 2013-02-27 | ||
| DKPA201370115 | 2013-02-27 | ||
| DKPA201370115 | 2013-02-27 | ||
| DKPA201370113 | 2013-02-27 | ||
| US61/770,067 | 2013-02-27 | ||
| US201461931126P | 2014-01-24 | 2014-01-24 | |
| US61/931,126 | 2014-01-24 | ||
| PCT/EP2014/053674 WO2014131777A1 (en) | 2013-02-27 | 2014-02-26 | Inhibitors of histone demethylases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018082444A Division JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | ヒストン脱メチル化酵素の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016509047A JP2016509047A (ja) | 2016-03-24 |
| JP2016509047A5 true JP2016509047A5 (enExample) | 2017-03-30 |
| JP6514117B2 JP6514117B2 (ja) | 2019-05-15 |
Family
ID=51427545
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015558495A Active JP6514117B2 (ja) | 2013-02-27 | 2014-02-26 | ヒストン脱メチル化酵素の阻害剤 |
| JP2018082444A Withdrawn JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | ヒストン脱メチル化酵素の阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018082444A Withdrawn JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | ヒストン脱メチル化酵素の阻害剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US9650339B2 (enExample) |
| EP (2) | EP2961736B1 (enExample) |
| JP (2) | JP6514117B2 (enExample) |
| KR (1) | KR102229992B1 (enExample) |
| CN (1) | CN105263906B (enExample) |
| AP (1) | AP2015008676A0 (enExample) |
| AU (2) | AU2014222756B2 (enExample) |
| BR (1) | BR112015020650A2 (enExample) |
| CA (1) | CA2901022C (enExample) |
| CL (1) | CL2015002394A1 (enExample) |
| CR (1) | CR20150507A (enExample) |
| EA (1) | EA030451B1 (enExample) |
| ES (1) | ES2670864T3 (enExample) |
| IL (1) | IL240439A0 (enExample) |
| MD (1) | MD20150085A2 (enExample) |
| MX (1) | MX2015011097A (enExample) |
| PE (1) | PE20151667A1 (enExample) |
| PH (1) | PH12015501868A1 (enExample) |
| PL (1) | PL2961736T3 (enExample) |
| SG (2) | SG10201707027SA (enExample) |
| SI (1) | SI2961736T1 (enExample) |
| TR (1) | TR201808599T4 (enExample) |
| WO (1) | WO2014131777A1 (enExample) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MD20150043A2 (ro) | 2012-10-02 | 2015-08-31 | Epitherapeutics Aps | Inhibitori ai histon-demetilazelor |
| PE20151667A1 (es) | 2013-02-27 | 2015-11-27 | Epitherapeutics Aps | Inhibidores de histona desmetilasas |
| WO2015153498A1 (en) * | 2014-03-31 | 2015-10-08 | Epitherapeutics, Aps | Inhibitors of histone demethylases |
| SG11201701182VA (en) | 2014-08-27 | 2017-03-30 | Gilead Sciences Inc | Compounds and methods for inhibiting histone demethylases |
| EP3212647B1 (en) | 2014-10-29 | 2019-04-03 | Dong-A ST Co., Ltd. | Novel pyridopyrimidinone compounds for modulating the catalytic activity of histone lysine demethylases (kdms) |
| EP3283076A1 (en) * | 2015-04-14 | 2018-02-21 | Gilead Sciences, Inc. | Methods of treating hepatitis b virus |
| WO2017099829A1 (en) * | 2015-12-11 | 2017-06-15 | The General Hospital Corporation | Compositions and methods for treating drug-tolerant glioblastoma |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| SG11201809893WA (en) | 2016-05-27 | 2018-12-28 | Gilead Sciences Inc | Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| EP3507288B1 (en) | 2016-09-02 | 2020-08-26 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| AU2017318601B2 (en) | 2016-09-02 | 2020-09-03 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| US10662416B2 (en) | 2016-10-14 | 2020-05-26 | Precision Biosciences, Inc. | Engineered meganucleases specific for recognition sequences in the hepatitis B virus genome |
| TWI820984B (zh) | 2017-01-31 | 2023-11-01 | 美商基利科學股份有限公司 | 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型 |
| JOP20180008A1 (ar) | 2017-02-02 | 2019-01-30 | Gilead Sciences Inc | مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| WO2018222831A1 (en) * | 2017-05-31 | 2018-12-06 | The Children's Medical Center Corporation | TARGETING LYSINE DEMETHYLASES (KDMs) AS A THERAPEUTIC STRATEGY FOR DIFFUSE LARGE B-CELL LYMPHOMA |
| AU2018328308A1 (en) | 2017-09-06 | 2020-04-16 | Translational Drug Development, Llc | Aminobenzimidazole derivatives, treatments, and methods of inhibiting histone deacetylase |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| KR102492187B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드 |
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| TWI796596B (zh) | 2018-02-13 | 2023-03-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
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| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| US20190359645A1 (en) | 2018-05-03 | 2019-11-28 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide |
| MX2021000100A (es) | 2018-07-13 | 2021-03-25 | Gilead Sciences Inc | Inhibidores de muerte programada-1 (pd-1)/ ligando de muerte programada 1 (pd-l1). |
| WO2020028097A1 (en) | 2018-08-01 | 2020-02-06 | Gilead Sciences, Inc. | Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid |
| CA3106548A1 (en) * | 2018-08-06 | 2020-02-13 | Dana-Farber Cancer Institute, Inc. | Histone demethylase 5 inhibitors and uses thereof |
| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| HRP20240541T1 (hr) | 2018-10-31 | 2024-07-05 | Gilead Sciences, Inc. | Supstituirani spojevi 6-azabenzimidazola kao inhibitori hpk1 |
| CN109852662B (zh) * | 2018-12-25 | 2021-02-19 | 华南农业大学 | 组蛋白甲基化H3K4me3在猪卵巢颗粒细胞中的应用 |
| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| DK3934757T3 (da) | 2019-03-07 | 2023-04-17 | Inst Of Organic Chemistry And Biochemistry Ascr V V I | 2'3'-cykliske dinukleotider og prodrugs deraf |
| AU2020231115B2 (en) | 2019-03-07 | 2025-02-20 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| TWI751516B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TW202212339A (zh) | 2019-04-17 | 2022-04-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| KR102776925B1 (ko) | 2019-06-25 | 2025-03-11 | 길리애드 사이언시즈, 인코포레이티드 | Flt3l-fc 융합 단백질 및 사용 방법 |
| WO2021011891A1 (en) | 2019-07-18 | 2021-01-21 | Gilead Sciences, Inc. | Long-acting formulations of tenofovir alafenamide |
| WO2021034804A1 (en) | 2019-08-19 | 2021-02-25 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| FI4037708T3 (fi) | 2019-09-30 | 2024-10-31 | Gilead Sciences Inc | Hbv-rokotteita ja menetelmiä, hbv:n hoitamiseksi |
| EP4567109A3 (en) | 2019-12-06 | 2025-09-17 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome |
| US11718637B2 (en) | 2020-03-20 | 2023-08-08 | Gilead Sciences, Inc. | Prodrugs of 4′-C-substituted-2-halo-2′- deoxyadenosine nucleosides and methods of making and using the same |
| EP4192474B1 (en) | 2020-08-07 | 2025-09-10 | Gilead Sciences, Inc. | Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use |
| TW202406932A (zh) | 2020-10-22 | 2024-02-16 | 美商基利科學股份有限公司 | 介白素2-Fc融合蛋白及使用方法 |
| TW202310852A (zh) | 2021-05-13 | 2023-03-16 | 美商基利科學股份有限公司 | ＴＬＲ８調節化合物及抗ＨＢＶ ｓｉＲＮＡ療法之組合 |
| CN117355531A (zh) | 2021-06-23 | 2024-01-05 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| CN117480155A (zh) | 2021-06-23 | 2024-01-30 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| US11999733B2 (en) | 2021-06-23 | 2024-06-04 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240244A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection |
| WO2025240243A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1524747A (en) | 1976-05-11 | 1978-09-13 | Ici Ltd | Polypeptide |
| LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
| GB8327256D0 (en) | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| AU3732889A (en) * | 1988-11-11 | 1990-05-28 | Banyu Pharmaceutical Co., Ltd. | Substituted allylamine derivatives, process for their preparation and their use |
| JPH03173865A (ja) * | 1988-11-11 | 1991-07-29 | Banyu Pharmaceut Co Ltd | 置換アリルアミン誘導体、その製造法及びその用途 |
| US5010099A (en) | 1989-08-11 | 1991-04-23 | Harbor Branch Oceanographic Institution, Inc. | Discodermolide compounds, compositions containing same and method of preparation and use |
| US5843901A (en) | 1995-06-07 | 1998-12-01 | Advanced Research & Technology Institute | LHRH antagonist peptides |
| AU716610B2 (en) | 1996-08-30 | 2000-03-02 | Novartis Ag | Method for producing epothilones, and intermediate products obtained during the production process |
| DE69724269T2 (de) | 1996-09-06 | 2004-06-09 | Obducat Ab | Verfahren für das anisotrope ätzen von strukturen in leitende materialien |
| US5874438A (en) | 1996-10-11 | 1999-02-23 | Bayer Aktiengesellschaft | 2,2'-bridged bis-2,4-diaminoquinazolines |
| US5756517A (en) * | 1996-10-25 | 1998-05-26 | Bayer Aktiengesellschaft | Use of bisquinoline compounds in the treatment of cerebral disorders |
| DK1367057T3 (da) | 1996-11-18 | 2009-01-19 | Biotechnolog Forschung Gmbh | Epothiloner E og F |
| US6441186B1 (en) | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
| GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| CA2322157C (en) | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| EP1135470A2 (en) | 1998-11-20 | 2001-09-26 | Kosan Biosciences, Inc. | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| KR20050044407A (ko) * | 2001-11-08 | 2005-05-12 | 엘란 파마슈티칼스, 인크. | N,n'-치환-1,3-디아미노-2-히드록시프로판 유도체 |
| PL230179B1 (pl) | 2002-03-13 | 2018-09-28 | Array Biopharma Inc | N3 Alkilowane pochodne benzoimidazolu, kompozycja je zawierająca oraz ich zastosowanie do wytwarzania leku do leczenia zaburzeń hiperproliferacyjnych |
| WO2006129842A1 (ja) * | 2005-06-01 | 2006-12-07 | Banyu Pharmaceutical Co., Ltd. | オーロラa選択的阻害作用を有する新規アミノピリジン誘導体 |
| US20080021024A1 (en) | 2006-06-29 | 2008-01-24 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors |
| SA109300195B1 (ar) | 2008-03-28 | 2013-04-20 | Astrazeneca Ab | تركيبة صيدلانية جديدة مضادة للسرطان |
| JP2012507556A (ja) | 2008-10-29 | 2012-03-29 | サートリス ファーマシューティカルズ， インコーポレイテッド | サーチュインモジュレーターとしてのピリジン、二環式ピリジンおよび関連するアナログ |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| AU2010279359A1 (en) | 2009-08-07 | 2012-02-16 | The Wistar Institute | Compositions containing JARID1B inhibitors and methods for treating cancer |
| SI2545045T1 (sl) | 2010-03-10 | 2016-05-31 | Incyte Holdings Corporation | Derivati piperidin-4-ila kot zaviralci JAK1 |
| US9365553B2 (en) | 2010-05-27 | 2016-06-14 | Aska Pharmaceutical Co., Ltd. | Heterocyclic compound and H1 receptor antagonist |
| WO2012007007A1 (en) | 2010-07-15 | 2012-01-19 | Epitherapeutics Aps | Inhibitors of hdme |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| GB201112607D0 (en) | 2011-07-22 | 2011-09-07 | Glaxo Group Ltd | Novel compounds |
| WO2012071469A2 (en) * | 2010-11-23 | 2012-05-31 | Nevada Cancer Institute | Histone demethylase inhibitors and uses thereof for treatment o f cancer |
| 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 |
| BR112014003382B1 (pt) * | 2011-08-15 | 2022-03-15 | University Of Utah Research Foundation | Análogos de (e)-n-(1-feniletilideno) benzo-hidrazida substituída como inibidores de histona desmetilase e composições farmacêuticas compreendendo-os |
| CN102585150B (zh) | 2012-02-01 | 2013-09-04 | 嘉兴学院 | 织物涂饰用阴离子水性聚氨酯分散体的制备方法 |
| WO2013123411A1 (en) | 2012-02-17 | 2013-08-22 | Board Of Regents, The University Of Texas System | Methods for diagnosing and treating cancer |
| MD20150043A2 (ro) | 2012-10-02 | 2015-08-31 | Epitherapeutics Aps | Inhibitori ai histon-demetilazelor |
| EP3763367A1 (en) | 2012-12-06 | 2021-01-13 | Celgene Quanticel Research, Inc. | Pyridine-pyrazole derivatives as histone demethylase inhibitors |
| PL2934145T3 (pl) | 2012-12-19 | 2018-04-30 | Celgene Quanticel Research, Inc. | Inhibitory demetylazy histonowej |
| US11639333B2 (en) | 2012-12-21 | 2023-05-02 | Celgene Quanticel Research, Inc | Histone demethylase inhibitors |
| PE20151667A1 (es) | 2013-02-27 | 2015-11-27 | Epitherapeutics Aps | Inhibidores de histona desmetilasas |
| JP6332654B2 (ja) | 2013-03-15 | 2018-05-30 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
| WO2015035062A1 (en) | 2013-09-05 | 2015-03-12 | Genentech, Inc. | Antiproliferative compounds |
| WO2015153498A1 (en) | 2014-03-31 | 2015-10-08 | Epitherapeutics, Aps | Inhibitors of histone demethylases |
-
2014
- 2014-02-26 PE PE2015001818A patent/PE20151667A1/es not_active Application Discontinuation
- 2014-02-26 CN CN201480010601.9A patent/CN105263906B/zh active Active
- 2014-02-26 JP JP2015558495A patent/JP6514117B2/ja active Active
- 2014-02-26 AU AU2014222756A patent/AU2014222756B2/en active Active
- 2014-02-26 SG SG10201707027SA patent/SG10201707027SA/en unknown
- 2014-02-26 MD MDA20150085A patent/MD20150085A2/ro not_active Application Discontinuation
- 2014-02-26 PL PL14706607T patent/PL2961736T3/pl unknown
- 2014-02-26 AP AP2015008676A patent/AP2015008676A0/xx unknown
- 2014-02-26 WO PCT/EP2014/053674 patent/WO2014131777A1/en not_active Ceased
- 2014-02-26 EA EA201591382A patent/EA030451B1/ru not_active IP Right Cessation
- 2014-02-26 US US14/381,556 patent/US9650339B2/en active Active
- 2014-02-26 KR KR1020157026738A patent/KR102229992B1/ko active Active
- 2014-02-26 EP EP14706607.0A patent/EP2961736B1/en active Active
- 2014-02-26 BR BR112015020650A patent/BR112015020650A2/pt not_active Application Discontinuation
- 2014-02-26 MX MX2015011097A patent/MX2015011097A/es unknown
- 2014-02-26 ES ES14706607.0T patent/ES2670864T3/es active Active
- 2014-02-26 SI SI201430706T patent/SI2961736T1/en unknown
- 2014-02-26 CA CA2901022A patent/CA2901022C/en active Active
- 2014-02-26 EP EP16197497.7A patent/EP3170811A1/en not_active Withdrawn
- 2014-02-26 SG SG11201506717UA patent/SG11201506717UA/en unknown
- 2014-02-26 TR TR2018/08599T patent/TR201808599T4/tr unknown
- 2014-08-28 US US14/472,065 patent/US9221801B2/en active Active
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2015
- 2015-08-09 IL IL240439A patent/IL240439A0/en unknown
- 2015-08-25 PH PH12015501868A patent/PH12015501868A1/en unknown
- 2015-08-26 CL CL2015002394A patent/CL2015002394A1/es unknown
- 2015-09-24 CR CR20150507A patent/CR20150507A/es unknown
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2018
- 2018-04-23 JP JP2018082444A patent/JP2018127486A/ja not_active Withdrawn
- 2018-07-13 AU AU2018205204A patent/AU2018205204A1/en not_active Abandoned
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