HRP20210299T1 - Inhibitori histonske demetilaze - Google Patents
Inhibitori histonske demetilaze Download PDFInfo
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- HRP20210299T1 HRP20210299T1 HRP20210299TT HRP20210299T HRP20210299T1 HR P20210299 T1 HRP20210299 T1 HR P20210299T1 HR P20210299T T HRP20210299T T HR P20210299TT HR P20210299 T HRP20210299 T HR P20210299T HR P20210299 T1 HRP20210299 T1 HR P20210299T1
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- Prior art keywords
- optionally substituted
- aryl
- alkyl
- heteroaryl
- pharmaceutically acceptable
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- 102000008157 Histone Demethylases Human genes 0.000 title 1
- 108010074870 Histone Demethylases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000000547 substituted alkyl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000003107 substituted aryl group Chemical group 0.000 claims 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 7
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- -1 cyano, hydroxy, amino Chemical group 0.000 claims 1
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
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- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (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, ili njegov stereoizomer ili njegova farmaceutski prihvatljiva sol, naznačen time, da posjeduje strukturu formule (II):
[image]
u kojoj,
X je O ili CH2;
R6 je odabran od opcionalno supstituiranog heterociklila, opcionalno supstituiranog heterocikliloksi, opcionalno supstituiranog heterociklilalkila, opcionalno supstituiranog heterociklilalkoksi, opcionalno supstituiranog C6-C10-aril-SO2-; opcionalno supstituiranog heteroaril-S-, ili -N(R1)(R2), pri čemu R1 je vodik ili opcionalno supstituirani alkil, i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-; i
svaki od R5, R7 i R8 je neovisno odabran od sljedećih: vodik, halogen, -OH, -CN, opcionalno supstituirani C1-C6-alkil, opcionalno supstituirani C1-C6-alkoksi, opcionalno supstituirani C3-C7-karbociklil, opcionalno supstituirani C3-C7-karbocikliloksi, opcionalno supstituirani C4-C12-karbociklilalkil, opcionalno supstituirani C4-C12-karbociklilalkoksi, opcionalno supstituirani C1-C6-alkinil, opcionalno supstituirani C1-C6-alkenil, opcionalno supstituirani C6-C10-aril, opcionalno supstituirani C6-C10-ariloksi, opcionalno supstituirani C6-C10-aril-S-, opcionalno supstituirani C7-C14-aralkoksi, opcionalno supstituirani heteroaril, i opcionalno supstituirani heteroariloksi, opcionalno supstituirani heterociklil, opcionalno supstituirani heterocikliloksi, supstituirani heterociklilalkil, opcionalno supstituirani heterociklilalkoksi, opcionalno supstituirani C6-C10-aril-SO2-, opcionalno supstituirani heteroaril-S-, ili –N(R1)(R2), pri čemu R1 je vodik ili opcionalno supstituirani alkil, i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-;
uz uvjet da najmanje jedan od R5, R7 i R8 jest vodik.
2. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 1, naznačen time, da posjeduje strukturu formule (IIa):
[image]
u kojoj,
X je O ili CH2;
R6 je odabran od opcionalno supstituiranog heterociklila, opcionalno supstituiranog heterocikliloksi, opcionalno supstituiranog heterociklilalkila, opcionalno supstituiranog heterociklilalkoksi, opcionalno supstituiranog C6-C10-aril-SO2-; opcionalno supstituiranog heteroaril-S-, ili -N(R1)(R2), pri čemu R1 je vodik ili opcionalno supstituirani alkil, i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-; i
svaki od R5, R7 i R8 je neovisno odabran od sljedećih: vodik, halogen, -OH, -CN, opcionalno supstituirani C1-C6-alkil, opcionalno supstituirani C1-C6-alkoksi, opcionalno supstituirani C3-C7-karbociklil, opcionalno supstituirani C3-C7-karbocikliloksi, opcionalno supstituirani C4-C12-karbociklilalkil, opcionalno supstituirani C4-C12-karbociklilalkoksi, opcionalno supstituirani C1-C6-alkinil, opcionalno supstituirani C1-C6-alkenil, opcionalno supstituirani C6-C10-aril, opcionalno supstituirani C6-C10-ariloksi, opcionalno supstituirani C6-C10-aril-S-, opcionalno supstituirani C7-C14-aralkoksi, opcionalno supstituirani heteroaril, i opcionalno supstituirani heteroariloksi, opcionalno supstituirani heterociklil, opcionalno supstituirani heterocikliloksi, supstituirani heterociklilalkil, opcionalno supstituirani heterociklilalkoksi, opcionalno supstituirani C6-C10-aril-SO2-, opcionalno supstituirani heteroaril-S-, ili –N(R1)(R2), pri čemu R1 je vodik ili opcionalno supstituirani alkil, i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-;
uz uvjet da najmanje jedan od R5, R7 i R8 jest vodik.
3. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 2, naznačen time, da X je O, ili time, da X je CH2.
4. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 2, naznačen time, da je R5 vodik ili je R7 vodik ili je R8 vodik, ili time, da su R5, R7 i R8 vodici.
5. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 2, naznačen time, da je R6 odabran iz skupine koja se sastoji od opcionalno supstituiranog heterociklila, opcionalno supstituiranog heterocikliloksi, opcionalno supstituiranog C6-C10-aril-SO2- i opcionalno supstituiranog heteroaril-S-.
6. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 2, naznačen time, da
R6 je –N(R1)(R2), pri čemu je R1 vodik; i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-; ili
pri čemu R6 je –N(R1)(R2), dok je R1 opcionalno supstituirani alkil; i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, odabran od opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-.
7. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 4, naznačen time, da
su R5, R7 i R8 vodici i pri čemu R6 je –N(R1)(R2), gdje je R1 opcionalno supstituirani alkil; i R2 je odabran od opcionalno supstituiranog alkila, opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, odabran od opcionalno supstituiranog heteroaril-CO-, opcionalno supstituiranog cikloalkil-CO-, ili opcionalno supstituiranog alkil-CO-.
8. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 7, naznačen time, da je R2 odabran iz skupine koja se sastoji od opcionalno supstituiranog arila, opcionalno supstituiranog heteroarila, opcionalno supstituiranog heterociklila, opcionalno supstituiranog cikloalkila, opcionalno supstituiranog cikloalkilalkila, opcionalno supstituiranog aril-CO-, opcionalno supstituiranog cikloalkil-CO- i opcionalno supstituiranog alkil-CO-.
9. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 8, naznačen time, da R1 je opcionalno supstituirani C1-C3-alkil ili time, da R1 je CH3-skupina.
10. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 8, naznačen time, da je opcionalno supstituirani aril supstituiran s najmanje jednim supstituentom koji je odabran od sljedećih: opcionalno supstituirani C1-C5-alkil, opcionalno supstituirani C2-C5-alkenil, halogen, cijano, hidroksi, amino, opcionalno supstituirani C1-C5-alkoksi, opcionalno supstituirani alkilamino, opcionalno supstituirani dialkilamino, opcionalno supstituirani heterociklil, opcionalno supstituirani heteroaril, opcionalno supstituirani cikloalkil, opcionalno supstituirani cikloalkilalkil, opcionalno supstituirani cikloalkilalkoksi, ili opcionalno supstituirani cikloalkoksi.
11. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 8, naznačen time, da je opcionalno supstituirani aril supstituiran s najmanje jednim supstituentom koji je odabran od sljedećih: opcionalno supstituirani C1-C5-alkil, halogen, ili opcionalno supstituirani C1-C5-alkoksi i time, da R1 je CH3-skupina, i X je O.
12. Spoj, ili njegova farmaceutski prihvatljiva sol, prema patentnom zahtjevu 2, naznačen time, da posjeduje strukturu koja je odabrana iz skupine koju sačinjavaju:
[image]
[image]
[image]
[image]
i
[image]
13. Farmaceutski pripravak, naznačen time, da sadrži spoj formule (II) koji je definiran u patentnom zahtjevu 1, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivu pomoćnu tvar.
14. Pripravak koji sadrži formulu (II) definiranu u patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačeni time, da su za uporabu u liječenju raka.
15. Pripravak koji je definiran u patentnom zahtjevu 14, za uporabu u liječenju raka, naznačen time, da se rak odabire iz skupine koja se sastoji od raka prostate, raka dojke, raka mokraćnog mjehura, raka pluća ili melanoma.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462017201P | 2014-06-25 | 2014-06-25 | |
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| PE20151417A1 (es) | 2012-12-21 | 2015-10-10 | Quanticel Pharmaceuticals Inc | Inhibidores de histona desmetilasa |
| US9242968B2 (en) | 2014-06-25 | 2016-01-26 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| US10030017B2 (en) | 2014-09-17 | 2018-07-24 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| EP3453710B1 (en) | 2014-09-17 | 2022-09-21 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| JP6883913B2 (ja) * | 2015-12-28 | 2021-06-09 | 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 |
| WO2017161012A1 (en) * | 2016-03-15 | 2017-09-21 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| WO2018183370A2 (en) | 2017-03-30 | 2018-10-04 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| CN109825551B (zh) * | 2019-02-21 | 2022-08-02 | 深圳大学 | 一种评价组蛋白赖氨酸去甲基转移酶活性的方法 |
| CN111679072B (zh) * | 2020-06-15 | 2022-04-29 | 温州医科大学 | Kdm6b蛋白在乳腺癌预后评估试剂盒、诊断试剂盒中的应用 |
| AU2022254741A1 (en) * | 2021-04-09 | 2023-11-16 | Celgene Corporation | Treatment of cancer with kdm4 inhibitors |
| AU2022331536A1 (en) * | 2021-08-18 | 2024-02-22 | Celgene Corporation | Process for preparing histone demethylase inhibitors |
| WO2023122221A1 (en) * | 2021-12-23 | 2023-06-29 | Tachyon Therapeutics, Inc. | Pharmaceutical formulations comprising 3-({[(4r)-7-{methyl[4-(propan-2-yl)phenyl]amino}-3,4-dihydro-2h-l-benzopyran-4-yl]methyl}amino)pyridine-4-carboxylic acid |
| WO2023240253A2 (en) | 2022-06-10 | 2023-12-14 | Forward Therapeutics, Inc. | Modulators of tnf-alpha activity |
| WO2023250480A1 (en) * | 2022-06-23 | 2023-12-28 | The Cleveland Clinic Foundation | 3-βHSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOF |
| WO2024064734A1 (en) * | 2022-09-21 | 2024-03-28 | Celgene Corporation | Crystalline forms of 3-({[(4r)-7-{methyl[4-(propan-2- yl)phenyl]amino}-3,4-dihydro-2h-l-benzopyran-4- yl]methyl}amino)pyridine-4-carboxylic acid l-lysine salt, a histone demethylase inhibitor |
| CN115974647A (zh) * | 2022-12-05 | 2023-04-18 | 江苏宏邦化工科技有限公司 | 以四氢-4-甲基-2-苯基-2h-吡喃-4-醇为原料制备苯乐戊醇的方法 |
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| CN101851173A (zh) * | 2001-09-14 | 2010-10-06 | 梅特希尔基因公司 | 组蛋白脱乙酰化酶抑制剂 |
| UA89035C2 (ru) | 2003-12-03 | 2009-12-25 | Лео Фарма А/С | Эфиры гидроксамовых кислот и их фармацевтическое применение |
| DE102004039876A1 (de) | 2004-06-23 | 2006-01-26 | Lanxess Deutschland Gmbh | Herstellung von fluorierten 1,3-Benzodioxanen |
| AR059733A1 (es) | 2006-03-07 | 2008-04-23 | Smithkline Beecham Corp | Compuesto derivado de glicina n- sustituida con heteroaromaticos bicicicos, composicion farmaceutica que lo comprende, uso para preparar un medicamento para tratar la anemia y proceso para su preparacion |
| AU2007234843B2 (en) * | 2006-04-07 | 2013-07-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US7898712B2 (en) | 2008-06-27 | 2011-03-01 | Lockheed Martin Corporation | Risley integrated steering module |
| GB201112607D0 (en) | 2011-07-22 | 2011-09-07 | Glaxo Group Ltd | Novel compounds |
| EP2712655B1 (en) * | 2011-04-28 | 2019-12-18 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
| WO2013143597A1 (en) * | 2012-03-29 | 2013-10-03 | Glaxo Group Limited | Demethylase enzymes inhibitors |
| WO2014089368A1 (en) | 2012-12-05 | 2014-06-12 | Bio-Rad Laboratories, Inc | Methods for polymerase chain reaction copy number variation assays |
| US9604961B2 (en) | 2012-12-06 | 2017-03-28 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| EP2934145B1 (en) * | 2012-12-19 | 2017-11-15 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| PE20151417A1 (es) * | 2012-12-21 | 2015-10-10 | Quanticel Pharmaceuticals Inc | Inhibidores de histona desmetilasa |
| US9242968B2 (en) | 2014-06-25 | 2016-01-26 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| WO2018183370A2 (en) * | 2017-03-30 | 2018-10-04 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
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