NO324942B1 - Hydroksamderivater, farmasoytiske preparater inneholdende disse, anvendelse av derivatene samt fregangsmate for regulering av p21 promoter - Google Patents
Hydroksamderivater, farmasoytiske preparater inneholdende disse, anvendelse av derivatene samt fregangsmate for regulering av p21 promoter Download PDFInfo
- Publication number
- NO324942B1 NO324942B1 NO20030867A NO20030867A NO324942B1 NO 324942 B1 NO324942 B1 NO 324942B1 NO 20030867 A NO20030867 A NO 20030867A NO 20030867 A NO20030867 A NO 20030867A NO 324942 B1 NO324942 B1 NO 324942B1
- Authority
- NO
- Norway
- Prior art keywords
- alkyl
- aryl
- cycloalkyl
- heteroaryl
- substituted
- Prior art date
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- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 283
- 150000001875 compounds Chemical class 0.000 claims description 117
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 101
- 125000001072 heteroaryl group Chemical group 0.000 claims description 97
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 82
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 78
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 70
- 125000000217 alkyl group Chemical group 0.000 claims description 60
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 59
- 229910052799 carbon Inorganic materials 0.000 claims description 53
- 125000002252 acyl group Chemical group 0.000 claims description 50
- 150000003839 salts Chemical class 0.000 claims description 50
- 125000001424 substituent group Chemical group 0.000 claims description 50
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims description 46
- 150000002367 halogens Chemical class 0.000 claims description 46
- -1 C 1 -C 4 alkyl Inorganic materials 0.000 claims description 45
- 229910052736 halogen Inorganic materials 0.000 claims description 45
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 38
- 229910052757 nitrogen Inorganic materials 0.000 claims description 37
- 229910052717 sulfur Inorganic materials 0.000 claims description 37
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 34
- 125000004122 cyclic group Chemical group 0.000 claims description 31
- 125000003282 alkyl amino group Chemical group 0.000 claims description 29
- 229910052760 oxygen Chemical group 0.000 claims description 27
- 125000002619 bicyclic group Chemical group 0.000 claims description 25
- 125000005842 heteroatom Chemical group 0.000 claims description 25
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 25
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 24
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 24
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 22
- 125000005429 oxyalkyl group Chemical group 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- 125000004442 acylamino group Chemical group 0.000 claims description 16
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 15
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 125000004432 carbon atom Chemical group C* 0.000 claims description 12
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 11
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 11
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 10
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 10
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims description 10
- 125000001624 naphthyl group Chemical group 0.000 claims description 10
- 150000002825 nitriles Chemical class 0.000 claims description 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 9
- 230000002062 proliferating effect Effects 0.000 claims description 9
- FPOHNWQLNRZRFC-ZHACJKMWSA-N panobinostat Chemical compound CC=1NC2=CC=CC=C2C=1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FPOHNWQLNRZRFC-ZHACJKMWSA-N 0.000 claims description 8
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- BWDQBBCUWLSASG-MDZDMXLPSA-N (e)-n-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1h-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide Chemical compound C=1NC2=CC=CC=C2C=1CCN(CCO)CC1=CC=C(\C=C\C(=O)NO)C=C1 BWDQBBCUWLSASG-MDZDMXLPSA-N 0.000 claims description 7
- ZLUZDKXBTNQWOL-MDZDMXLPSA-N (e)-n-hydroxy-3-[4-[[2-(1h-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide Chemical compound C1=CC(/C=C/C(=O)NO)=CC=C1CNCCC1=CNC2=CC=CC=C12 ZLUZDKXBTNQWOL-MDZDMXLPSA-N 0.000 claims description 6
- 239000000460 chlorine Substances 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
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- 101100135744 Caenorhabditis elegans pch-2 gene Proteins 0.000 claims description 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 5
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 5
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- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 4
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- JGTCTTGDRUHLHS-MDZDMXLPSA-N (e)-3-[4-[[2-(1-benzofuran-3-yl)ethylamino]methyl]phenyl]-n-hydroxyprop-2-enamide Chemical compound C1=CC(/C=C/C(=O)NO)=CC=C1CNCCC1=COC2=CC=CC=C12 JGTCTTGDRUHLHS-MDZDMXLPSA-N 0.000 claims description 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 3
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- 101150020251 NR13 gene Proteins 0.000 claims description 3
- 125000004532 benzofuran-3-yl group Chemical group O1C=C(C2=C1C=CC=C2)* 0.000 claims description 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 3
- 229910052794 bromium Inorganic materials 0.000 claims description 3
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims description 3
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- 230000001105 regulatory effect Effects 0.000 claims description 3
- 229920006395 saturated elastomer Polymers 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 210000004962 mammalian cell Anatomy 0.000 claims description 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims 18
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
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- 238000006722 reduction reaction Methods 0.000 description 1
- 201000002793 renal fibrosis Diseases 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 239000013037 reversible inhibitor Substances 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000013207 serial dilution Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- VPZRWNZGLKXFOE-UHFFFAOYSA-M sodium phenylbutyrate Chemical compound [Na+].[O-]C(=O)CCCC1=CC=CC=C1 VPZRWNZGLKXFOE-UHFFFAOYSA-M 0.000 description 1
- 229960002232 sodium phenylbutyrate Drugs 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000036262 stenosis Effects 0.000 description 1
- 208000037804 stenosis Diseases 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- MFPWEWYKQYMWRO-UHFFFAOYSA-N tert-butyl carboxy carbonate Chemical compound CC(C)(C)OC(=O)OC(O)=O MFPWEWYKQYMWRO-UHFFFAOYSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical class C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 229930185603 trichostatin Natural products 0.000 description 1
- 230000004565 tumor cell growth Effects 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 208000037964 urogenital cancer Diseases 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
- C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
- C07D209/16—Tryptamines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- 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
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D403/02—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
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D405/02—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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Structural Engineering (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Inorganic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Materials Engineering (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Furan Compounds (AREA)
- Pyrane Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
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| US22994300P | 2000-09-01 | 2000-09-01 | |
| US29223201P | 2001-05-18 | 2001-05-18 | |
| PCT/EP2001/010037 WO2002022577A2 (en) | 2000-09-01 | 2001-08-30 | Hydroxamate derivatives useful as deacetylase inhibitors |
Publications (3)
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| NO20030867L NO20030867L (no) | 2003-02-25 |
| NO20030867D0 NO20030867D0 (no) | 2003-02-25 |
| NO324942B1 true NO324942B1 (no) | 2008-01-07 |
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| NO20030867A NO324942B1 (no) | 2000-09-01 | 2003-02-25 | Hydroksamderivater, farmasoytiske preparater inneholdende disse, anvendelse av derivatene samt fregangsmate for regulering av p21 promoter |
| NO2015026C NO2015026I2 (no) | 2000-09-01 | 2015-12-10 | panobinostat eller et farmasøytisk akseptabelt salt derav |
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| NO2015026C NO2015026I2 (no) | 2000-09-01 | 2015-12-10 | panobinostat eller et farmasøytisk akseptabelt salt derav |
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| EP (2) | EP1870399A1 (cs) |
| JP (1) | JP4012819B2 (cs) |
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| AU (2) | AU8212901A (cs) |
| BE (1) | BE2015C062I2 (cs) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US6777217B1 (en) | 1996-03-26 | 2004-08-17 | President And Fellows Of Harvard College | Histone deacetylases, and uses related thereto |
| US6822267B1 (en) * | 1997-08-20 | 2004-11-23 | Advantest Corporation | Signal transmission circuit, CMOS semiconductor device, and circuit board |
| KR20100035666A (ko) | 1999-11-23 | 2010-04-05 | 메틸진 인크. | 히스톤 디아세틸라제의 억제제 |
| US20030129724A1 (en) | 2000-03-03 | 2003-07-10 | Grozinger Christina M. | Class II human histone deacetylases, and uses related thereto |
| PE20020354A1 (es) * | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| DE60115279T2 (de) | 2000-09-29 | 2006-12-28 | Topotarget Uk Ltd., Abingdon | Carbaminsäurederivate enthaltend eine amidgruppe als hdac-inhibitoren |
| US7312247B2 (en) * | 2001-03-27 | 2007-12-25 | Errant Gene Therapeutics, Llc | Histone deacetylase inhibitors |
| EP2269609A3 (en) | 2001-10-16 | 2012-07-11 | Sloan-Kettering Institute for Cancer Research | Treatment of neurodegenerative diseases and cancer of the brain with SAHA |
| US7402603B2 (en) * | 2001-11-06 | 2008-07-22 | Novartis Ag | Cyclooxygenase-2 inhibitor/histone deacetylase inhibitor combination |
| EP2266552A3 (en) | 2002-03-04 | 2011-03-02 | Merck HDAC Research, LLC | Methods of inducing terminal differentiation |
| US7148257B2 (en) | 2002-03-04 | 2006-12-12 | Merck Hdac Research, Llc | Methods of treating mesothelioma with suberoylanilide hydroxamic acid |
| US7456219B2 (en) | 2002-03-04 | 2008-11-25 | Merck Hdac Research, Llc | Polymorphs of suberoylanilide hydroxamic acid |
| JP4606027B2 (ja) | 2002-04-03 | 2011-01-05 | トポターゲット ユーケー リミテッド | Ｈｄａｃ阻害剤としてのピペラジン結合を有するカルバミン酸化合物 |
| US7495022B2 (en) | 2002-04-11 | 2009-02-24 | Sk Chemicals Co., Ltd. | α,β-unsaturated hydroxamic acid derivatives and their use as histone deacetylase inhibitors |
| WO2003088954A1 (en) * | 2002-04-15 | 2003-10-30 | Sloan-Kettering Institute For Cancer Research | Combination therapy for the treatment of cancer |
| EP2179745A1 (en) * | 2002-06-10 | 2010-04-28 | Novartis AG | Combinations comprising epothilones and pharmaceutical uses thereof |
| US20050272647A1 (en) * | 2002-08-20 | 2005-12-08 | Noboru Yamaji | Arthrodial cartilage extracellular matrix degradation inhibitor |
| CN1681505A (zh) * | 2002-09-13 | 2005-10-12 | 弗吉尼亚州立大学 | 用于治疗白血病的а ) N－{ 5－[ 4－( 4－甲基－哌嗪－1－基－甲基)－苯甲酰氨基]－2－甲基苯基}－4－( 3－吡啶基 ) －2－嘧啶－胺和b )组蛋白脱乙酰基酶抑制剂的组合 |
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7250514B1 (en) | 2002-10-21 | 2007-07-31 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| WO2004046107A1 (en) * | 2002-11-19 | 2004-06-03 | Takeda Pharmaceutical Company Limited | Indole derivatives as somatostatin agonists or antagonists |
| WO2004052292A2 (en) | 2002-12-06 | 2004-06-24 | University Of South Florida | Histone deacetylase inhibitor enhancement of trail-induced apoptosis |
| TW200418806A (en) * | 2003-01-13 | 2004-10-01 | Fujisawa Pharmaceutical Co | HDAC inhibitor |
| EP1583736A1 (en) | 2003-01-17 | 2005-10-12 | TopoTarget UK Limited | Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors |
| AU2003900587A0 (en) * | 2003-02-11 | 2003-02-27 | Fujisawa Pharmaceutical Co., Ltd. | Hdac inhibitor |
| AU2003900608A0 (en) * | 2003-02-11 | 2003-02-27 | Fujisawa Pharmaceutical Co., Ltd. | Hdac inhibitor |
| US7652036B2 (en) | 2003-02-25 | 2010-01-26 | Topotarget Uk Limited | Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors |
| US7375228B2 (en) | 2003-03-17 | 2008-05-20 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| EP1628651A2 (en) * | 2003-05-21 | 2006-03-01 | Novartis AG | Combination of histone deacetylase inhibitors with chemotherapeutic agents |
| WO2005011598A2 (en) | 2003-07-31 | 2005-02-10 | University Of South Florida | Leukemia treatment method and composition |
| JP2007501775A (ja) * | 2003-08-07 | 2007-02-01 | ノバルティス アクチエンゲゼルシャフト | 免疫抑制剤としてのヒストンデアセチラーゼ阻害剤 |
| MXPA06001524A (es) | 2003-08-08 | 2006-05-15 | Novartis Ag | Combinaciones que comprenden estaurosporinas. |
| NZ545935A (en) | 2003-08-26 | 2009-02-28 | Merck Hdac Res Llc | Method of treating cancer with HDAC inhibitors |
| AU2004270150C1 (en) | 2003-08-29 | 2011-07-14 | Merck Hdac Research, Llc | Combination methods of treating cancer |
| CN100455564C (zh) * | 2003-09-12 | 2009-01-28 | 深圳微芯生物科技有限责任公司 | 组蛋白去乙酰化酶抑制剂及其药用制剂的制备和应用 |
| BRPI0414506A (pt) * | 2003-09-18 | 2006-11-07 | Novartis Ag | combinação de um inibidor de histona desacetilase com um ligante de receptor de morte |
| SI1673349T1 (sl) * | 2003-09-22 | 2010-10-29 | S Bio Pte Ltd | Derivati benzimidazola: priprava in farmacevtske uporabe |
| CA2539766C (en) | 2003-09-22 | 2013-07-02 | S*Bio Pte Ltd | Benzimidazole derivates: preparation and pharmaceutical applications |
| US20080085902A1 (en) * | 2003-09-23 | 2008-04-10 | Guido Bold | Combination Of A Vegf Receptor Inhibitor Or With A Chemotherapeutic Agent |
| EP1682538A4 (en) * | 2003-10-27 | 2009-05-27 | S Bio Pte Ltd | BIARYL-ASSOCIATED HYDROXAMATE: PREPARATION AND PHARMACEUTICAL APPLICATIONS |
| WO2005055928A2 (en) | 2003-12-02 | 2005-06-23 | The Ohio State University Research Foundation | Zn2+ -chelating motif-tethered short -chain fatty acids as a novel class of histone deacetylase inhibitors |
| EP1541549A1 (en) * | 2003-12-12 | 2005-06-15 | Exonhit Therapeutics S.A. | Tricyclic hydroxamate and benzaminde derivatives, compositions and methods |
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- 2015-12-14 CY CY2015053C patent/CY2015053I1/el unknown
- 2015-12-16 HU HUS1500068C patent/HUS1500068I1/hu unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995031977A1 (en) * | 1994-05-19 | 1995-11-30 | Sloan-Kettering Institute For Cancer Research | Novel potent inducers of terminal differentiation and methods of use thereof |
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