HRP20171609T1 - Inhibitori histon demetilaze - Google Patents
Inhibitori histon demetilaze Download PDFInfo
- Publication number
- HRP20171609T1 HRP20171609T1 HRP20171609TT HRP20171609T HRP20171609T1 HR P20171609 T1 HRP20171609 T1 HR P20171609T1 HR P20171609T T HRP20171609T T HR P20171609TT HR P20171609 T HRP20171609 T HR P20171609T HR P20171609 T1 HRP20171609 T1 HR P20171609T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- heterocyclyl
- compound according
- heteroaryl
- carbocyclyl
- Prior art date
Links
- 102000008157 Histone Demethylases Human genes 0.000 title claims 3
- 108010074870 Histone Demethylases Proteins 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000004452 carbocyclyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 4
- 101100295738 Gallus gallus COR3 gene Proteins 0.000 claims 3
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000001769 aryl amino group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
Claims (15)
1. Spoj Formule (I), ili njegova farmaceutski prihvatljiva sol,
[image]
pri tome, X je alkil, ili-L-R1;
L je jedna veza, ili C1-C6 alkilen;
R1 je karbociklil, aril, heterociklil ili heteroaril;
Y je vodik ili
[image]
i R2je alkil, heterociklil, heterociklilalkil, ili karbociklilalkil.
2. Spoj sukladno patentnom zahtjevu 1, naznačeno time što je X alkil i alkil je jedan C1-C6 alkil.
3. Spoj sukladno patentnom zahtjevu 2, naznačeno time što je alkil supstituiran s najmanje jednim od fluoro, hidroksi, alkoksi, ariloksi, amino, alkilamino, arilamino, diakilamino, -NHCOR3, -NHCO2R3, -NHCONHR3, -N(R4)COR3, N(R4)CO2R3, -N(R4)CONHR3, -N(R4)CON(R4)R3, -NHSO2R3, -NR4SO2R3, -CONH2, -CONHR3, -CON(R3)2, -COR3, -SO2NH2, -SO2NHR3, -SO2N(R3)2, ili -SO2R3, pri tome je svaki R3 neovisno odabran iz alkila, arila, heteroarila, karbociklila ili heterociklila, a svaki R4 je alkil.
4. Spoj sukladno patentnom zahtjevu 1, naznačeno time što je L veza; poželjno, naznačeno time što je R1 aril.
5. Spoj sukladno patentnom zahtjevu 4, naznačeno time što je aril jedna fenil skupina.
6. Spoj sukladno patentnom zahtjevu 5, naznačeno time što je fenil supstituiran s najmanje jednim halogenom, alkilom, hidroksi, alkoksi, ariloksi, amino, alkilamino, arilamino, diakilamino, arilom, heteroarilom, karbociklilom, heterociklilom, -NHCOR3, -NHCO2R3, -NHCONHR3, -N(R4)COR3, -N(R4)CO2R3, -N(R4)CONHR3, -N(R4)CON(R4)R3, -NHSO2R3, -NR4SO2R3, -CONH2, -CONHR3, -CON(R3)2, -COR3, -SO2NH2 , -SO2NHR3, -SO2N(R3)2 ili -SO2R3, gde je svaki R3 neovisno odabrana iz alkila, arila, heteroarila, karbociklila ili heterociklila, a svaki R4 je alkil.
7. Spoj sukladno patentnom zahtjevu 6, naznačeno time što je heteroaril skupina odabrana iz benzimidazolila, benzofuranila, furanila, izotiazolila, imidazolila, indazolila, indolila, izoksazolila, oksazolila, pirolila, pirazolila, piridinila, pirazinila, pirimidinila, piridazinila, tiazolila ili tiofenila.
8. Spoj sukladno patentnom zahtjevu 6, naznačeno time što je heteroaril skupina supstituirana s najmanje jednim halogenom, alkilom, skupinama hidroksi, alkoksi, ariloksi, amino, alkilamino, arilamino, diakilamino, -NHCOR3, -NHCO2RJ, -NHCONHR3, -N(R4)COR3, N(R4)CO2R3, -N(R4)CONHR3, -N(R4)CON(R4)R3, -NHSO2R3, -NR4SO2R3, -CONH2, -CONHR3, -CON(R3)2, -COR3, -SO2NH2, -SO2NHR3, -SO2N(R3)2, -SO2R3, gde je svaki R3 neovisno odabrani iz alkila, arila, heteroarila, karbociklila ili heterociklila, a svaki R4 je alkil.
9. Spoj sukladno patentnom zahtjevu 6, naznačeno time što je heteroaril grupa supstituirana sa skupinom odabranom iz arila, heteroarila, karbociklila, heterociklila, ili pirazolila koji ima strukturu:
[image]
pri tome je R5 skupina odabrana iz alkila, karbociklila, heterociklila, karbociklilalkila, heterociklilalkila, aralkila ili heteroarilalkila.
10. Spoj sukladno patentnom zahtjevu 9, naznačeno time, što je R3 skupina jedan C1-C6 alkil, opcijski supstituirana s najmanje jednom skupinom odabranom iz hidroksi, C1-C4 alkoksi, amino, C1-C4 alkilamino, C1-C4 diakilamino, piperidinil, pirolidinil ili morfolinil; ili naznačeno time, što je R3 jedan heterociklil odabran iz 4-tetrahidropiranila, 1-morfolinila, ili 4-piperdinila koji ima strukturu:
[image]
pri tome je R6 -COR7, -CO2R7, -CONHR7, ili -SO2R7, gdje je svaki R7 neovisno odabran iz alkila, arila, heteroarila, karbociklila, ili heterociklila.
11. Spoj sukladno patentnom zahtjevu 1, pri tome je L jedan C1-C6 alkilen, opcijski jedan C1-C4 alkilen; i R1 je fenil, jedan 3- do 7- člani karbociklil, jedan 5- ili 6-člani heteroaril, ili jedan 4- do 6-člani heterociklil koji sadrži kisik.
12. Spoj sukladno patentnom zahtjevu 1, pri tome je Y
[image]
i R2 je alkil, heterociklil, heterociklilalkil, karbociklilalkil; pri tome je navedeni alkil metil ili C2-C4 alkil i pri tome je navedeni alkil opcijski supstituiran s najmanje jednim hidroksi, alkoksi, amino, alkilamino, diakilamino ili fluoro supstituentom; pri tome je navedeni heterociklil opcijski jedan 4- do 6-člani heterociklil koji sadrži kisik ili dušik; pri tome je navedeni heterociklilalkil opcijski C1-C3 alkilen, ili jedan 4- do 6-člani heterociklil koji sadrži kisik ili dušik; i pri čemu se navedeni karbociklilalkil opcijski sastoji od C1-C3 alkilena ili jednog 3- do 7-članog karbociklila.
13. Farmaceutski pripravak koji sadrži spoj sukladno bilo kojem od patentnih zahtjeva 1 do 12.
14. Spoj sukladno bilo kojem od patentnih zahjteva 1 do 12 ili pripravak sukladno patentnom zahtjevu 13, za liječenje karcinoma.
15. Postupak in vitro za inhibiranje enzima histon demetilaze koji obuhvaća dovođenje u dodir enzima histon demetilaze sa spojem u skladu s bilo kojim od patentnih zahtjeva 1 do 12.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361791406P | 2013-03-15 | 2013-03-15 | |
| PCT/US2014/024998 WO2014151106A1 (en) | 2013-03-15 | 2014-03-12 | Histone demethylase inhibitors |
| EP14768099.5A EP2970211B1 (en) | 2013-03-15 | 2014-03-12 | Histone demethylase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20171609T1 true HRP20171609T1 (hr) | 2017-12-15 |
Family
ID=51580888
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171609TT HRP20171609T1 (hr) | 2013-03-15 | 2017-10-23 | Inhibitori histon demetilaze |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9994562B2 (hr) |
| EP (1) | EP2970211B1 (hr) |
| JP (1) | JP6332654B2 (hr) |
| AU (1) | AU2014235280B2 (hr) |
| CA (1) | CA2903465A1 (hr) |
| CY (1) | CY1119476T1 (hr) |
| DK (1) | DK2970211T3 (hr) |
| ES (1) | ES2644828T3 (hr) |
| HR (1) | HRP20171609T1 (hr) |
| HU (1) | HUE034906T2 (hr) |
| LT (1) | LT2970211T (hr) |
| PL (1) | PL2970211T3 (hr) |
| PT (1) | PT2970211T (hr) |
| RS (1) | RS56561B1 (hr) |
| SI (1) | SI2970211T1 (hr) |
| WO (1) | WO2014151106A1 (hr) |
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| JP2023536663A (ja) | 2020-08-07 | 2023-08-28 | ギリアード サイエンシーズ， インコーポレイテッド | ホスホンアミドヌクレオチド類似体のプロドラッグ及びその薬学的使用 |
| 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 |
| TW202348237A (zh) | 2021-05-13 | 2023-12-16 | 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 |
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| WO2022271677A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
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| WO2022271659A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
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| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
| HRP970371A2 (en) * | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| WO2003078427A1 (en) | 2002-03-15 | 2003-09-25 | Vertex Pharmaceuticals, Inc. | Azolylaminoazines as inhibitors of protein kinases |
| AR045697A1 (es) * | 2003-07-14 | 2005-11-09 | Arena Pharm Inc | Aril y heteroaril derivados fusionados como moduladores del metabolismo y la prevencion y tratamiento de trastornos relacionados con el mismo |
| JP2008510823A (ja) | 2004-08-23 | 2008-04-10 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性阻害剤 |
| US20110319409A1 (en) * | 2010-06-23 | 2011-12-29 | Cox Christopher D | 7-aza-quinazoline pde10 inhibitors |
| GB201112607D0 (en) * | 2011-07-22 | 2011-09-07 | Glaxo Group Ltd | Novel compounds |
| WO2014151106A1 (en) | 2013-03-15 | 2014-09-25 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| AU2015317806A1 (en) | 2014-09-17 | 2017-04-13 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
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- 2014-03-12 PT PT147680995T patent/PT2970211T/pt unknown
- 2014-03-12 HU HUE14768099A patent/HUE034906T2/hu unknown
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2017
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| SI2970211T1 (sl) | 2017-12-29 |
| CA2903465A1 (en) | 2014-09-25 |
| US9994562B2 (en) | 2018-06-12 |
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| HUE034906T2 (hu) | 2018-03-28 |
| PL2970211T3 (pl) | 2018-01-31 |
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| EP2970211A1 (en) | 2016-01-20 |
| JP6332654B2 (ja) | 2018-05-30 |
| US20160039808A1 (en) | 2016-02-11 |
| EP2970211A4 (en) | 2016-08-03 |
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| US10526327B2 (en) | 2020-01-07 |
| AU2014235280A1 (en) | 2015-09-17 |
| LT2970211T (lt) | 2017-10-25 |
| CY1119476T1 (el) | 2018-03-07 |
| DK2970211T3 (en) | 2017-10-16 |
| RS56561B1 (sr) | 2018-02-28 |
| ES2644828T3 (es) | 2017-11-30 |
| EP2970211B1 (en) | 2017-07-26 |
| AU2014235280B2 (en) | 2017-08-31 |
| US20180319793A1 (en) | 2018-11-08 |
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