SI2961736T1 - Histone demethylase inhibitors - Google Patents
Histone demethylase inhibitors Download PDFInfo
- Publication number
- SI2961736T1 SI2961736T1 SI201430706T SI201430706T SI2961736T1 SI 2961736 T1 SI2961736 T1 SI 2961736T1 SI 201430706 T SI201430706 T SI 201430706T SI 201430706 T SI201430706 T SI 201430706T SI 2961736 T1 SI2961736 T1 SI 2961736T1
- Authority
- SI
- Slovenia
- Prior art keywords
- methyl
- amino
- pyridin
- ethyl
- dimethylamino
- Prior art date
Links
- 102000008157 Histone Demethylases Human genes 0.000 title claims abstract 4
- 108010074870 Histone Demethylases Proteins 0.000 title claims abstract 4
- 239000003112 inhibitor Substances 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 239000000203 mixture Substances 0.000 claims abstract 5
- 201000010099 disease Diseases 0.000 claims abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 3
- -1 heterocyclylene Chemical group 0.000 claims 63
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 53
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 33
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 28
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 23
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 14
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 13
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 11
- 125000004043 oxo group Chemical group O=* 0.000 claims 10
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 9
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 9
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 8
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 6
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 4
- 150000001412 amines Chemical class 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000004419 alkynylene group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 3
- 150000003254 radicals Chemical class 0.000 claims 3
- 125000003003 spiro group Chemical group 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 2
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000000732 arylene group Chemical group 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 2
- BGUWFUQJCDRPTL-UHFFFAOYSA-N pyridine-4-carbaldehyde Chemical compound O=CC1=CC=NC=C1 BGUWFUQJCDRPTL-UHFFFAOYSA-N 0.000 claims 2
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 1
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 claims 1
- YQCVBJMGLPDRHR-UHFFFAOYSA-N 2-[(3-pyrrolidin-1-ylpropylamino)methyl]pyridine-4-carbaldehyde Chemical compound O=CC1=CC=NC(CNCCCN2CCCC2)=C1 YQCVBJMGLPDRHR-UHFFFAOYSA-N 0.000 claims 1
- CDQAQUVTAFYHDI-UHFFFAOYSA-N 2-[[4-(2-cyclohexylethyliminomethyl)pyridin-2-yl]methylamino]-n-[2-(dimethylamino)ethyl]-n-ethylacetamide Chemical compound C1=NC(CNCC(=O)N(CCN(C)C)CC)=CC(C=NCCC2CCCCC2)=C1 CDQAQUVTAFYHDI-UHFFFAOYSA-N 0.000 claims 1
- BNVDTDBQVGGKHM-ONEGZZNKSA-N 2-[[[(e)-4-(dimethylamino)but-2-enyl]amino]methyl]pyridine-4-carbaldehyde Chemical compound CN(C)C\C=C\CNCC1=CC(C=O)=CC=N1 BNVDTDBQVGGKHM-ONEGZZNKSA-N 0.000 claims 1
- HHANQIRRGYANJJ-UHFFFAOYSA-N 2-[[methyl-(2-oxo-2-piperidin-1-ylethyl)amino]methyl]pyridine-4-carbaldehyde Chemical compound C=1C(C=O)=CC=NC=1CN(C)CC(=O)N1CCCCC1 HHANQIRRGYANJJ-UHFFFAOYSA-N 0.000 claims 1
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 101100240519 Caenorhabditis elegans nhr-13 gene Proteins 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- 101100203602 Hypocrea jecorina (strain QM6a) sor7 gene Proteins 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- 125000003289 ascorbyl group Chemical class [H]O[C@@]([H])(C([H])([H])O*)[C@@]1([H])OC(=O)C(O*)=C1O* 0.000 claims 1
- XTKDAFGWCDAMPY-UHFFFAOYSA-N azaperone Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CCN(C=2N=CC=CC=2)CC1 XTKDAFGWCDAMPY-UHFFFAOYSA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 150000001860 citric acid derivatives Chemical class 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- WBJINCZRORDGAQ-UHFFFAOYSA-N ethyl formate Chemical group CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 claims 1
- 235000019253 formic acid Nutrition 0.000 claims 1
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 claims 1
- UCHALCCVDSGKEA-UHFFFAOYSA-N n-[4-(diethylamino)butyl]-2,2,2-trifluoro-n-[(4-formylpyridin-2-yl)methyl]acetamide Chemical compound CCN(CC)CCCCN(C(=O)C(F)(F)F)CC1=CC(C=O)=CC=N1 UCHALCCVDSGKEA-UHFFFAOYSA-N 0.000 claims 1
- IFNHEIYJHOMOPW-UHFFFAOYSA-N n-[[2-[[[2-[2-(dimethylamino)ethyl-ethylamino]-2-oxoethyl]-(2,2,2-trifluoroacetyl)amino]methyl]pyridin-4-yl]methyl]-2,2,2-trifluoroacetamide Chemical compound CN(C)CCN(CC)C(=O)CN(C(=O)C(F)(F)F)CC1=CC(CNC(=O)C(F)(F)F)=CC=N1 IFNHEIYJHOMOPW-UHFFFAOYSA-N 0.000 claims 1
- VEZIUZPDOIYXLQ-UHFFFAOYSA-N n-methyl-n-(2-phenylethyl)acetamide Chemical compound CC(=O)N(C)CCC1=CC=CC=C1 VEZIUZPDOIYXLQ-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 150000003891 oxalate salts Chemical class 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 claims 1
- 125000006308 propyl amino group Chemical group 0.000 claims 1
- ZMANZCXQSJIPKH-UHFFFAOYSA-N triethylamine Natural products CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000008482 dysregulation Effects 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000008506 pathogenesis Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
-
- 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
-
- 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
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/06—Oxalic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/06—Oxalic acid
- C07C55/07—Salts thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/265—Citric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
- C07D213/48—Aldehydo radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/56—Amides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D307/62—Three oxygen atoms, e.g. ascorbic acid
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (9)
| 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 | ||
| DKPA201370113 | 2013-02-27 | ||
| DKPA201370115 | 2013-02-27 | ||
| US201461931126P | 2014-01-24 | 2014-01-24 | |
| EP14706607.0A EP2961736B1 (en) | 2013-02-27 | 2014-02-26 | Inhibitors of histone demethylases |
| PCT/EP2014/053674 WO2014131777A1 (en) | 2013-02-27 | 2014-02-26 | Inhibitors of histone demethylases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI2961736T1 true SI2961736T1 (en) | 2018-06-29 |
Family
ID=51427545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201430706T SI2961736T1 (en) | 2013-02-27 | 2014-02-26 | Histone demethylase inhibitors |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US9650339B2 (OSRAM) |
| EP (2) | EP3170811A1 (OSRAM) |
| JP (2) | JP6514117B2 (OSRAM) |
| KR (1) | KR102229992B1 (OSRAM) |
| CN (1) | CN105263906B (OSRAM) |
| AP (1) | AP2015008676A0 (OSRAM) |
| AU (2) | AU2014222756B2 (OSRAM) |
| BR (1) | BR112015020650A2 (OSRAM) |
| CA (1) | CA2901022C (OSRAM) |
| CL (1) | CL2015002394A1 (OSRAM) |
| CR (1) | CR20150507A (OSRAM) |
| EA (1) | EA030451B1 (OSRAM) |
| ES (1) | ES2670864T3 (OSRAM) |
| IL (1) | IL240439A0 (OSRAM) |
| MD (1) | MD20150085A2 (OSRAM) |
| MX (1) | MX2015011097A (OSRAM) |
| PE (1) | PE20151667A1 (OSRAM) |
| PH (1) | PH12015501868A1 (OSRAM) |
| PL (1) | PL2961736T3 (OSRAM) |
| SG (2) | SG11201506717UA (OSRAM) |
| SI (1) | SI2961736T1 (OSRAM) |
| TR (1) | TR201808599T4 (OSRAM) |
| WO (1) | WO2014131777A1 (OSRAM) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2015003959A (es) | 2012-10-02 | 2015-11-16 | Epitherapeutics Aps | Inhibidores de histona demetilasas. |
| ES2670864T3 (es) | 2013-02-27 | 2018-06-01 | Gilead Sciences, Inc. | Inhibidores de histonas desmetilasas |
| AR099890A1 (es) * | 2014-03-31 | 2016-08-24 | Epitherapeutics Aps | Inhibidores de histona demetilasas |
| MX2017002451A (es) | 2014-08-27 | 2017-05-23 | Gilead Sciences Inc | Compuestos y metodos para inhibir histona desmetilasas. |
| MX2017005346A (es) | 2014-10-29 | 2017-08-02 | Dong A St Co Ltd | Nuevos compuestos de piridopirimidinona para modular la actividad catalitica de histona lisina desmetilasas (kdm). |
| AU2016250099A1 (en) * | 2015-04-14 | 2017-10-12 | 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 |
| EP3463469B1 (en) | 2016-05-27 | 2023-12-13 | Gilead Sciences, Inc. | Combination of ledipasvir and sofosbuvir for use in the treatment of hepatitis b virus infections in humans |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| AU2017318601B2 (en) | 2016-09-02 | 2020-09-03 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| KR20230010826A (ko) | 2016-10-14 | 2023-01-19 | 프리시젼 바이오사이언시스 인코포레이티드 | B형 간염 바이러스 게놈 내의 인식 서열에 대해 특이적인 조작된 메가뉴클레아제 |
| TW202510891A (zh) | 2017-01-31 | 2025-03-16 | 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 |
| US20200155526A1 (en) * | 2017-05-31 | 2020-05-21 | 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 |
| US10966999B2 (en) | 2017-12-20 | 2021-04-06 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| 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 |
| WO2019154261A1 (zh) * | 2018-02-09 | 2019-08-15 | 南京明德新药研发股份有限公司 | 与kmd5通路相关的吡啶衍生物 |
| JP7062792B2 (ja) | 2018-02-13 | 2022-05-06 | 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 |
| CA3091142C (en) | 2018-02-26 | 2023-04-11 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| US10870691B2 (en) | 2018-04-05 | 2020-12-22 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis B virus protein X |
| 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 |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
| US11142750B2 (en) | 2018-04-12 | 2021-10-12 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome |
| EP3781556B1 (en) | 2018-04-19 | 2025-06-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| 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 |
| CN118221646A (zh) | 2018-07-13 | 2024-06-21 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| 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 |
| JP2021534084A (ja) * | 2018-08-06 | 2021-12-09 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | ヒストンデメチラーゼ５阻害剤およびその使用 |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| MX2021005047A (es) | 2018-10-31 | 2021-09-08 | Gilead Sciences Inc | Compuestos de 6-azabenzimidazol sustituidos como inhibidores de hpk1. |
| CN117105933A (zh) | 2018-10-31 | 2023-11-24 | 吉利德科学公司 | 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物 |
| 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 |
| US11766447B2 (en) | 2019-03-07 | 2023-09-26 | 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 |
| 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 |
| 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 |
| TWI826690B (zh) | 2019-05-23 | 2023-12-21 | 美商基利科學股份有限公司 | 經取代之烯吲哚酮化物及其用途 |
| PE20220231A1 (es) | 2019-06-25 | 2022-02-07 | Gilead Sciences Inc | Proteinas de fusion flt3l-fc y metodos de uso |
| WO2021011891A1 (en) | 2019-07-18 | 2021-01-21 | Gilead Sciences, Inc. | Long-acting formulations of tenofovir alafenamide |
| US20220296619A1 (en) | 2019-08-19 | 2022-09-22 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| EP4458975A3 (en) | 2019-09-30 | 2025-02-12 | Gilead Sciences, Inc. | Hbv vaccines and methods treating hbv |
| EP4069729B1 (en) | 2019-12-06 | 2025-01-22 | Precision BioSciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome |
| AR121620A1 (es) | 2020-03-20 | 2022-06-22 | Gilead Sciences Inc | Profármacos de nucleósidos 4-c-sustituidos-2-halo-2-deoxiadenosina y métodos de preparación y uso de los mismos |
| US12110305B2 (en) | 2020-08-07 | 2024-10-08 | Gilead Sciences, Inc. | Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use |
| TWI815194B (zh) | 2020-10-22 | 2023-09-11 | 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 |
| AU2022274607A1 (en) | 2021-05-13 | 2023-11-16 | Gilead Sciences, Inc. | COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS |
| WO2022271659A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| JP7686086B2 (ja) | 2021-06-23 | 2025-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリエルコール（ｄｉａｃｙｌｇｌｙｅｒｃｏｌ）キナーゼ調節化合物 |
| WO2022271684A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| 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 |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240243A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus |
| WO2025240242A1 (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 |
| NZ334821A (en) | 1996-08-30 | 2000-12-22 | Novartis Ag | Method for producing epothilones |
| 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 |
| CN100344627C (zh) | 1996-11-18 | 2007-10-24 | 生物技术研究有限公司(Gbf) | 埃坡霉素c、其制备方法以及作为细胞抑制剂和植物保护剂的应用 |
| 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 |
| ATE307123T1 (de) | 1998-02-25 | 2005-11-15 | Sloan Kettering Inst Cancer | Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen |
| 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) |
| EA200400648A1 (ru) * | 2001-11-08 | 2005-04-28 | Элан Фармасьютикалз, Инк. | N, n'-замещенные производные 1,3-диамино-2-гидроксипропана |
| CA2478374C (en) | 2002-03-13 | 2009-01-06 | Eli M. Wallace | N3 alkylated benzimidazole derivatives as mek inhibitors |
| 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 |
| WO2008002671A2 (en) | 2006-06-29 | 2008-01-03 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors |
| SA109300195B1 (ar) | 2008-03-28 | 2013-04-20 | Astrazeneca Ab | تركيبة صيدلانية جديدة مضادة للسرطان |
| MX2011004553A (es) | 2008-10-29 | 2011-07-20 | Sirtris Pharmaceuticals Inc | Piridina, piridina biciclica y analogos relacionados como moduladores de sirtuina. |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| WO2011017583A1 (en) | 2009-08-07 | 2011-02-10 | The Wistar Institute | Compositions containing jarid1b inhibitors and methods for treating cancer |
| PH12015502575A1 (en) | 2010-03-10 | 2017-04-24 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| US9365553B2 (en) | 2010-05-27 | 2016-06-14 | Aska Pharmaceutical Co., Ltd. | Heterocyclic compound and H1 receptor antagonist |
| WO2012007008A1 (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 |
| PE20141322A1 (es) | 2011-03-25 | 2014-10-05 | Glaxosmithkline Intellectual Property (N 2) Limited | Ciclopropilaminas como inhibidores de desmetilasa 1 especifica de lisina |
| 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 |
| MX2015003959A (es) | 2012-10-02 | 2015-11-16 | Epitherapeutics Aps | Inhibidores de histona demetilasas. |
| ES2834959T3 (es) | 2012-12-06 | 2021-06-21 | Celgene Quanticel Res Inc | Inhibidores de histona desmetilasa |
| US9617242B2 (en) | 2012-12-19 | 2017-04-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| HK1210611A1 (en) | 2012-12-21 | 2016-04-29 | Quanticel Pharmaceuticals Inc | Histone demethylase inhibitors |
| ES2670864T3 (es) | 2013-02-27 | 2018-06-01 | Gilead Sciences, Inc. | Inhibidores de histonas desmetilasas |
| HRP20171609T1 (hr) | 2013-03-15 | 2017-12-15 | Quanticel Pharmaceuticals Inc | Inhibitori histon demetilaze |
| US9505767B2 (en) | 2013-09-05 | 2016-11-29 | Genentech, Inc. | Pyrazolo[1,5-A]pyrimidin-7(4H)-onehistone demethylase inhibitors |
| AR099890A1 (es) | 2014-03-31 | 2016-08-24 | Epitherapeutics Aps | Inhibidores de histona demetilasas |
-
2014
- 2014-02-26 ES ES14706607.0T patent/ES2670864T3/es active Active
- 2014-02-26 EP EP16197497.7A patent/EP3170811A1/en not_active Withdrawn
- 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 MX MX2015011097A patent/MX2015011097A/es unknown
- 2014-02-26 AU AU2014222756A patent/AU2014222756B2/en active Active
- 2014-02-26 PL PL14706607T patent/PL2961736T3/pl unknown
- 2014-02-26 US US14/381,556 patent/US9650339B2/en active Active
- 2014-02-26 SI SI201430706T patent/SI2961736T1/en unknown
- 2014-02-26 TR TR2018/08599T patent/TR201808599T4/tr unknown
- 2014-02-26 AP AP2015008676A patent/AP2015008676A0/xx unknown
- 2014-02-26 EA EA201591382A patent/EA030451B1/ru not_active IP Right Cessation
- 2014-02-26 KR KR1020157026738A patent/KR102229992B1/ko active Active
- 2014-02-26 JP JP2015558495A patent/JP6514117B2/ja active Active
- 2014-02-26 SG SG11201506717UA patent/SG11201506717UA/en unknown
- 2014-02-26 BR BR112015020650A patent/BR112015020650A2/pt not_active Application Discontinuation
- 2014-02-26 MD MDA20150085A patent/MD20150085A2/ro not_active Application Discontinuation
- 2014-02-26 SG SG10201707027SA patent/SG10201707027SA/en unknown
- 2014-02-26 WO PCT/EP2014/053674 patent/WO2014131777A1/en not_active Ceased
- 2014-02-26 EP EP14706607.0A patent/EP2961736B1/en active Active
- 2014-02-26 CA CA2901022A patent/CA2901022C/en active Active
- 2014-08-28 US US14/472,065 patent/US9221801B2/en active Active
-
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
-
2018
- 2018-04-23 JP JP2018082444A patent/JP2018127486A/ja not_active Withdrawn
- 2018-07-13 AU AU2018205204A patent/AU2018205204A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| SI2961736T1 (en) | Histone demethylase inhibitors | |
| RU2013108641A (ru) | Способ лечения офтальмологических заболеваний с использованием соединений ингибиторов киназы в пролекарственных формах | |
| RU2328486C2 (ru) | Производные 2-пиридона в качестве ингибиторов нейтрофильной эластазы | |
| RU2336275C2 (ru) | Пиримидопроизводные, характеризующиеся антипролиферативной активностью, и фармацевтическая композиция | |
| JP2010531345A5 (OSRAM) | ||
| RU2403247C2 (ru) | Модуляторы никотиновых ацетилхолиновых рецепторов альфа 7 и их терапевтические применения | |
| RU2430923C2 (ru) | Тиазолилдигидрохиназолины | |
| HRP20170217T1 (hr) | Fuzinirani heterociklički spojevi kao inhibitori protein kinaze | |
| RU2014105624A (ru) | Соединения индазола, способ их применения и фармацевтическая композиция | |
| RU2005110061A (ru) | Замещенные пиперазины, (1,4)-диазепины и 2,5-диазабицикло(2,2,1)гептаны в качестве н1-и/или н3-антагонистов гистамина или обратных н3-антагонистов гистамина | |
| RU2005111225A (ru) | Производные триазаспиро[5.5]ундекана и лекарственные средства, содержащие их в качестве активного ингредиента | |
| JP2016521273A5 (OSRAM) | ||
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| RU2008108898A (ru) | Соединения и композиции в качестве ингибиторов протеинкиназы | |
| RU2003110577A (ru) | Гетероциклические соединения, связывающиеся с хемокиновыми рецепторами | |
| RU2004104625A (ru) | Аналоги простагландинов в качестве агонистов рецептора ep4 | |
| RU2008112691A (ru) | Азотсодержащее гетероциклическое соединение и его фармацевтическое применение | |
| RU2010126105A (ru) | Производные пиридина, замещенные гетероциклическим кольцом и фосфоноксиметильной группой, и содержащие их противогрибковые средства | |
| JP2007513915A5 (OSRAM) | ||
| RU2008120850A (ru) | Соединения и композиции в качестве ингибиторов протеинкиназ | |
| RU2006101541A (ru) | Производные пиперазина и способ их применения | |
| RU2012130929A (ru) | Гетероциклические соединения в качестве ингибиторов янус-киназы | |
| JP2020511536A5 (OSRAM) | ||
| JP2021500332A5 (OSRAM) | ||
| JP2015502371A5 (OSRAM) |