JP2015523385A5 - - Google Patents
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- JP2015523385A5 JP2015523385A5 JP2015521820A JP2015521820A JP2015523385A5 JP 2015523385 A5 JP2015523385 A5 JP 2015523385A5 JP 2015521820 A JP2015521820 A JP 2015521820A JP 2015521820 A JP2015521820 A JP 2015521820A JP 2015523385 A5 JP2015523385 A5 JP 2015523385A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrocarbyl
- ring
- different
- same
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 148
- 150000001875 compounds Chemical class 0.000 claims 103
- 229910052739 hydrogen Inorganic materials 0.000 claims 86
- 229910052757 nitrogen Inorganic materials 0.000 claims 80
- 125000005842 heteroatom Chemical group 0.000 claims 74
- 239000008194 pharmaceutical composition Substances 0.000 claims 62
- 229910052799 carbon Inorganic materials 0.000 claims 60
- 229910052760 oxygen Inorganic materials 0.000 claims 48
- -1 bisulfate ion Chemical class 0.000 claims 47
- 239000001301 oxygen Substances 0.000 claims 44
- 229910052717 sulfur Inorganic materials 0.000 claims 44
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 42
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 39
- 229910052805 deuterium Inorganic materials 0.000 claims 39
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 38
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 38
- 239000011593 sulfur Substances 0.000 claims 38
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 26
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 125000004429 atom Chemical group 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 20
- 125000002950 monocyclic group Chemical group 0.000 claims 14
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical group CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 12
- 150000001408 amides Chemical class 0.000 claims 12
- 229940124530 sulfonamide Drugs 0.000 claims 12
- 150000003456 sulfonamides Chemical class 0.000 claims 12
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 150000003857 carboxamides Chemical class 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 10
- 108020001612 μ-opioid receptors Proteins 0.000 claims 9
- 150000001450 anions Chemical class 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 102000013366 Filamin Human genes 0.000 claims 4
- 108060002900 Filamin Proteins 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims 4
- 229960004127 naloxone Drugs 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 230000000638 stimulation Effects 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 3
- HPZJMUBDEAMBFI-WTNAPCKOSA-N (D-Ala(2)-mephe(4)-gly-ol(5))enkephalin Chemical compound C([C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N(C)[C@@H](CC=1C=CC=CC=1)C(=O)NCCO)C1=CC=C(O)C=C1 HPZJMUBDEAMBFI-WTNAPCKOSA-N 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
- 108700022183 Ala(2)-MePhe(4)-Gly(5)- Enkephalin Proteins 0.000 claims 2
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 229940077388 benzenesulfonate Drugs 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- MHMNJMPURVTYEJ-UHFFFAOYSA-N fluorescein-5-isothiocyanate Chemical compound O1C(=O)C2=CC(N=C=S)=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 MHMNJMPURVTYEJ-UHFFFAOYSA-N 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- XMBWDFGMSWQBCA-UHFFFAOYSA-M iodide Chemical compound [I-] XMBWDFGMSWQBCA-UHFFFAOYSA-M 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 2
- 229940085991 phosphate ion Drugs 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 101000669447 Homo sapiens Toll-like receptor 4 Proteins 0.000 claims 1
- 102100039360 Toll-like receptor 4 Human genes 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 102000051367 mu Opioid Receptors Human genes 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 102000013498 tau Proteins Human genes 0.000 claims 1
- 108010026424 tau Proteins Proteins 0.000 claims 1
- 0 *C(BN(*)*)*OC(C1)[C@]2C1[C@@](CC1)C1CC2 Chemical compound *C(BN(*)*)*OC(C1)[C@]2C1[C@@](CC1)C1CC2 0.000 description 5
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261671235P | 2012-07-13 | 2012-07-13 | |
| US61/671,235 | 2012-07-13 | ||
| US201361789180P | 2013-03-15 | 2013-03-15 | |
| US61/789,180 | 2013-03-15 | ||
| US13/940,016 US10017736B2 (en) | 2012-07-13 | 2013-07-11 | Method of inhibiting tau phosphorylation |
| US13/940,016 | 2013-07-11 | ||
| PCT/US2013/050126 WO2014011917A2 (en) | 2012-07-13 | 2013-07-11 | A method of inhibiting tau phosphorylation |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018000198A Division JP6630374B2 (ja) | 2012-07-13 | 2018-01-04 | τリン酸化を阻害する方法 |
| JP2018189789A Division JP2019031520A (ja) | 2012-07-13 | 2018-10-05 | τリン酸化を阻害する方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015523385A JP2015523385A (ja) | 2015-08-13 |
| JP2015523385A5 true JP2015523385A5 (enExample) | 2016-09-01 |
| JP6417324B2 JP6417324B2 (ja) | 2018-11-07 |
Family
ID=49914489
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015521820A Active JP6417324B2 (ja) | 2012-07-13 | 2013-07-11 | τリン酸化を阻害する方法 |
| JP2018000198A Active JP6630374B2 (ja) | 2012-07-13 | 2018-01-04 | τリン酸化を阻害する方法 |
| JP2018189789A Pending JP2019031520A (ja) | 2012-07-13 | 2018-10-05 | τリン酸化を阻害する方法 |
| JP2021089538A Pending JP2022000421A (ja) | 2012-07-13 | 2021-05-27 | τリン酸化を阻害する方法 |
| JP2022198455A Active JP7419486B2 (ja) | 2012-07-13 | 2022-12-13 | τリン酸化を阻害する方法 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018000198A Active JP6630374B2 (ja) | 2012-07-13 | 2018-01-04 | τリン酸化を阻害する方法 |
| JP2018189789A Pending JP2019031520A (ja) | 2012-07-13 | 2018-10-05 | τリン酸化を阻害する方法 |
| JP2021089538A Pending JP2022000421A (ja) | 2012-07-13 | 2021-05-27 | τリン酸化を阻害する方法 |
| JP2022198455A Active JP7419486B2 (ja) | 2012-07-13 | 2022-12-13 | τリン酸化を阻害する方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (7) | US10017736B2 (enExample) |
| EP (1) | EP2882428B1 (enExample) |
| JP (5) | JP6417324B2 (enExample) |
| DK (1) | DK2882428T3 (enExample) |
| ES (1) | ES2716049T3 (enExample) |
| WO (1) | WO2014011917A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2872899B1 (en) * | 2012-07-13 | 2018-07-11 | Pain Therapeutics, Inc. | Alzheimer's disease assay in a living patient |
| GB201312499D0 (en) * | 2013-07-12 | 2013-08-28 | Isis Innovation | Therapeutic compounds |
| US9433604B2 (en) | 2013-10-08 | 2016-09-06 | Pain Therapeutics Inc. | Method for inhibiting growth of cancer cells |
| CN104030933A (zh) * | 2014-05-16 | 2014-09-10 | 烟台恒迪克能源科技有限公司 | 一种β-异烷醇基氨基戊酸环己胺的合成方法 |
| MA44037B1 (fr) | 2016-06-06 | 2020-03-31 | Arena Pharm Inc | Modulateurs du récepteur adrénergique bêta 3 utile dans le traitement ou la prévention de troubles associés à ceux-ci |
| KR20190096949A (ko) | 2016-10-05 | 2019-08-20 | 유니버시티 오브 피츠버그 - 오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 소분자 ampk 활성화제 |
| US12186307B2 (en) | 2019-02-13 | 2025-01-07 | Yale University | Methods of treating epilepsy |
| CN114072406B (zh) | 2019-02-21 | 2025-03-18 | 卡萨瓦科学公司 | Flna-结合化合物及其盐酸盐的固体多晶型物 |
| US12428378B2 (en) | 2019-09-10 | 2025-09-30 | University of Pittsburgh—of the Commonwealth System of Higher Education | Methods and materials for increasing level of phosphorylated AMPK protein |
| US20230045629A1 (en) * | 2020-01-15 | 2023-02-09 | National University Corporation Tokai National Higher Education And Research System | Treatment of progressive supranuclear palsy |
| AU2021376267A1 (en) * | 2020-11-03 | 2023-06-15 | Cassava Sciences, Inc. | Inhibiting an immune response mediated by one or more of tlr2, rage, ccr5, cxcr4 and cd4 |
| CN114252324B (zh) * | 2022-03-02 | 2022-05-13 | 中国人民解放军军事科学院军事医学研究院 | 一种方便使用的多孔脑片孵育装置 |
| WO2024151661A2 (en) * | 2023-01-10 | 2024-07-18 | Washington University | Methods of decreasing pathological neuroinflammation |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3723442A (en) | 1970-12-31 | 1973-03-27 | Yoshitomi Pharmaceutical | 3-oxo-1-oxa-4,8-diazaspiro(4.5)decanes |
| US4981858A (en) | 1987-08-13 | 1991-01-01 | State Of Israel, Represented By The Prime Minister's Office, Israel Institute For Biological Research | Optical isomers |
| DE3853758T2 (de) | 1987-10-05 | 1995-09-07 | Yamanouchi Pharma Co Ltd | Heterozyklische Spiroverbindungen und ihre Herstellung. |
| US5852029A (en) | 1990-04-10 | 1998-12-22 | Israel Institute For Biological Research | Aza spiro compounds acting on the cholinergic system with muscarinic agonist activity |
| US5534520A (en) | 1990-04-10 | 1996-07-09 | Fisher; Abraham | Spiro compounds containing five-membered rings |
| US5766846A (en) * | 1992-07-10 | 1998-06-16 | Athena Neurosciences | Methods of screening for compounds which inhibit soluble β-amyloid peptide production |
| AU693087B2 (en) | 1993-01-28 | 1998-06-25 | Merck & Co., Inc. | Spiro-substituted azacycles as tachykinin receptor antagonists |
| US6060469A (en) | 1995-11-23 | 2000-05-09 | Merck Sharp & Dohme Ltd. | Spiro-piperidine derivatives and their use as tachykinin antagonists |
| DK1083889T3 (da) * | 1998-06-01 | 2004-04-13 | Ortho Mcneil Pharm Inc | Tetrahydronaphthalenforbindelser og deres anvendelse til behandling af neurodegenerative sygdomme |
| DE10130020A1 (de) | 2001-06-25 | 2003-12-04 | Gruenenthal Gmbh | Substituierte 1-Oxa-2,8-diaza-spiro[4.5]dec-2-en-derivate |
| JP4356453B2 (ja) | 2001-07-23 | 2009-11-04 | 萬有製薬株式会社 | 4−オキソイミダゾリジン−2−スピロピペリジン誘導体 |
| KR101027570B1 (ko) | 2002-05-03 | 2011-04-06 | 이스라엘 인스티튜트 포 바이올로지컬 리서치 | 중추 및 말초 신경계 장애의 치료를 위한 방법 및 조성물, 및 그에 유용한 신규 화합물 |
| DE102004014304A1 (de) | 2004-03-22 | 2005-10-06 | Grünenthal GmbH | Substituierte 1,4,8- Triazaspiro[4,5]decan-2-on-Verbindungen |
| DE102004014296A1 (de) | 2004-03-22 | 2005-10-06 | Grünenthal GmbH | Substituierte 1,4,8-Triazaspiro[4.5]decan-2-on-Verbindingen |
| CA2566445C (en) * | 2004-05-12 | 2016-02-02 | The Government Of The United States As Represented By The Secretary, Department Of Health And Human Services | Methods related to the treatment of neurodegenerative and inflammatory conditions |
| DE102005030051A1 (de) | 2005-06-27 | 2006-12-28 | Grünenthal GmbH | Substituierte 1-Oxa-3,8-diazaspiro[4,5]-decan-2-on-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| AR057579A1 (es) | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
| US20100280057A1 (en) * | 2009-05-04 | 2010-11-04 | Lindsay Burns Barbier | Novel analgesic that binds filamin a |
| US8614324B2 (en) | 2008-10-31 | 2013-12-24 | Pain Therapeutics, Inc. | Filamin A binding anti-inflammatory and analgesic |
| US8653068B2 (en) | 2009-10-30 | 2014-02-18 | Pain Therapeutics, Inc. | Filamin A binding anti-inflammatory and analgesic |
| US8722851B2 (en) | 2007-11-02 | 2014-05-13 | Pain Therapeutics, Inc. | Analgesia with minimal tolerance and dependence by a mu opioid receptor agonist that also binds filamin A |
| US8580808B2 (en) | 2009-10-30 | 2013-11-12 | Pain Therapeutic, Inc. | Filamin A-binding anti-inflammatory analgesic |
| AU2009308702B2 (en) * | 2008-10-31 | 2015-05-28 | Pain Therapeutics, Inc. | Filamin A binding anti-inflammatory and analgesic |
| US20100279997A1 (en) | 2009-05-04 | 2010-11-04 | Lindsay Burns Barbier | Analgesic that binds filamin a |
| US20100279996A1 (en) | 2009-05-04 | 2010-11-04 | Lindsay Burns Barbier | Novel analgesic that binds filamin a |
| CN102361876B (zh) | 2009-01-26 | 2015-02-04 | 以色列生物研究所 | 二环杂环螺环化合物 |
| US20100280061A1 (en) | 2009-05-04 | 2010-11-04 | Lindsay Burns Barbier | Novel analgesic that binds filamin a |
| TWI374662B (en) * | 2009-05-18 | 2012-10-11 | Novatek Microelectronics Corp | Image processing circuit and method thereof |
| US8580809B2 (en) | 2009-10-30 | 2013-11-12 | Pain Therapeutics, Inc. | Filamin A-binding anti-inflammatory analgesic |
| WO2014028755A1 (en) * | 2012-08-16 | 2014-02-20 | Pain Therapeutics, Inc. | Benzazocine-ring compound inhibition of tau hyperphosphorylation |
-
2013
- 2013-07-11 DK DK13816713.5T patent/DK2882428T3/en active
- 2013-07-11 ES ES13816713T patent/ES2716049T3/es active Active
- 2013-07-11 WO PCT/US2013/050126 patent/WO2014011917A2/en not_active Ceased
- 2013-07-11 US US13/940,016 patent/US10017736B2/en active Active
- 2013-07-11 JP JP2015521820A patent/JP6417324B2/ja active Active
- 2013-07-11 EP EP13816713.5A patent/EP2882428B1/en active Active
-
2018
- 2018-01-04 JP JP2018000198A patent/JP6630374B2/ja active Active
- 2018-07-09 US US16/030,494 patent/US10760052B2/en active Active
- 2018-10-05 JP JP2018189789A patent/JP2019031520A/ja active Pending
-
2020
- 2020-08-28 US US17/006,338 patent/US11661580B2/en active Active
-
2021
- 2021-05-27 JP JP2021089538A patent/JP2022000421A/ja active Pending
- 2021-08-20 US US17/408,038 patent/US20210389298A1/en not_active Abandoned
-
2022
- 2022-12-13 JP JP2022198455A patent/JP7419486B2/ja active Active
-
2023
- 2023-05-24 US US18/323,075 patent/US20240117306A1/en not_active Abandoned
-
2024
- 2024-11-21 US US18/955,938 patent/US20250163372A1/en active Pending
- 2024-11-21 US US18/955,937 patent/US20250092361A1/en active Pending
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