ES2565243T3 - Inhibidores de histona desacetilasa - Google Patents
Inhibidores de histona desacetilasa Download PDFInfo
- Publication number
- ES2565243T3 ES2565243T3 ES08733559.2T ES08733559T ES2565243T3 ES 2565243 T3 ES2565243 T3 ES 2565243T3 ES 08733559 T ES08733559 T ES 08733559T ES 2565243 T3 ES2565243 T3 ES 2565243T3
- Authority
- ES
- Spain
- Prior art keywords
- phenyl
- aminophenylcarbamoyl
- pyrrolidin
- ylcarbamate
- hydrocarbyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 229940121372 histone deacetylase inhibitor Drugs 0.000 title 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 31
- 239000000203 mixture Substances 0.000 claims abstract description 17
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims abstract 21
- -1 di-alkylamino Chemical group 0.000 claims description 15
- 125000001424 substituent group Chemical group 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
- 102000003964 Histone deacetylase Human genes 0.000 claims description 4
- 108090000353 Histone deacetylase Proteins 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000003282 alkyl amino group Chemical group 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- VSEUPAAPIVKGEP-INIZCTEOSA-N 2-methoxyethyl n-[(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl]carbamate Chemical compound C1[C@@H](NC(=O)OCCOC)CCN1C1=CC=C(C(=O)NC=2C(=CC=CC=2)N)C=C1 VSEUPAAPIVKGEP-INIZCTEOSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- UDSLGDKSJDZFLT-KRWDZBQOSA-N 2-(dimethylamino)ethyl n-[(3s)-1-[4-[(2-aminophenyl)carbamoyl]phenyl]pyrrolidin-3-yl]carbamate Chemical compound C1[C@@H](NC(=O)OCCN(C)C)CCN1C1=CC=C(C(=O)NC=2C(=CC=CC=2)N)C=C1 UDSLGDKSJDZFLT-KRWDZBQOSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- RUZLIIJDZBWWSA-INIZCTEOSA-N methyl 2-[[(1s)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoate Chemical group COC(=O)C1=CC=CC=C1N[C@@H](C)C1=CC(C)=CN2C(=O)C=C(N3CCOCC3)N=C12 RUZLIIJDZBWWSA-INIZCTEOSA-N 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 abstract description 10
- 239000012453 solvate Substances 0.000 abstract description 9
- 150000001204 N-oxides Chemical class 0.000 abstract description 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract description 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 4
- 125000000732 arylene group Chemical group 0.000 abstract description 3
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 27
- 238000005481 NMR spectroscopy Methods 0.000 description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 12
- 210000004027 cell Anatomy 0.000 description 10
- 230000000694 effects Effects 0.000 description 9
- 239000000651 prodrug Substances 0.000 description 8
- 229940002612 prodrug Drugs 0.000 description 8
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 6
- 125000004122 cyclic group Chemical group 0.000 description 6
- JAEIBKXSIXOLOL-UHFFFAOYSA-N pyrrolidin-1-ium-3-carboxylate Chemical compound OC(=O)C1CCNC1 JAEIBKXSIXOLOL-UHFFFAOYSA-N 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000000872 buffer Substances 0.000 description 4
- 238000012512 characterization method Methods 0.000 description 4
- KFTZCNLLRKFMQH-UHFFFAOYSA-N pyrrolidin-3-ylcarbamic acid Chemical compound OC(=O)NC1CCNC1 KFTZCNLLRKFMQH-UHFFFAOYSA-N 0.000 description 4
- 238000005160 1H NMR spectroscopy Methods 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
- 125000003118 aryl group Chemical group 0.000 description 3
- 229910052736 halogen Inorganic materials 0.000 description 3
- 150000002367 halogens Chemical class 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 description 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- HEDRZPFGACZZDS-MICDWDOJSA-N Trichloro(2H)methane Chemical compound [2H]C(Cl)(Cl)Cl HEDRZPFGACZZDS-MICDWDOJSA-N 0.000 description 2
- 125000004442 acylamino group Chemical group 0.000 description 2
- 125000003368 amide group Chemical group 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 239000011550 stock solution Substances 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- FBFNMTGUOBUGFQ-UHFFFAOYSA-M 2-(2,5-diphenyltetrazol-1-ium-1-yl)-4,5-dimethyl-1,3-thiazole;bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=C(C=2C=CC=CC=2)N=NN1C1=CC=CC=C1 FBFNMTGUOBUGFQ-UHFFFAOYSA-M 0.000 description 1
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 description 1
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- OKKJLVBELUTLKV-MZCSYVLQSA-N Deuterated methanol Chemical compound [2H]OC([2H])([2H])[2H] OKKJLVBELUTLKV-MZCSYVLQSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 239000007995 HEPES buffer Substances 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 description 1
- 125000001769 aryl amino group Chemical group 0.000 description 1
- 125000005129 aryl carbonyl group Chemical group 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 210000004748 cultured cell Anatomy 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 239000006193 liquid solution Substances 0.000 description 1
- 239000006194 liquid suspension Substances 0.000 description 1
- 229910001629 magnesium chloride Inorganic materials 0.000 description 1
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 description 1
- 125000004957 naphthylene group Chemical group 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000011537 solubilization buffer Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000000565 sulfonamide group Chemical group 0.000 description 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- SUTRDULVNIPNLW-SFHVURJKSA-N tert-butyl n-[(2s)-6-acetamido-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxohexan-2-yl]carbamate Chemical group CC1=CC(=O)OC2=CC(NC(=O)[C@@H](NC(=O)OC(C)(C)C)CCCCNC(=O)C)=CC=C21 SUTRDULVNIPNLW-SFHVURJKSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
Classifications
-
- 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
- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90673307P | 2007-03-13 | 2007-03-13 | |
| US906733P | 2007-03-13 | ||
| US12/043,450 US8030344B2 (en) | 2007-03-13 | 2008-03-06 | Inhibitors of histone deacetylase |
| US43450 | 2008-03-06 | ||
| PCT/CA2008/000455 WO2008109994A1 (en) | 2007-03-13 | 2008-03-12 | Inhibitors of histone deacetylase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2565243T3 true ES2565243T3 (es) | 2016-04-01 |
Family
ID=39758948
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08733559.2T Active ES2565243T3 (es) | 2007-03-13 | 2008-03-12 | Inhibidores de histona desacetilasa |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8030344B2 (enExample) |
| EP (1) | EP2134680B1 (enExample) |
| JP (2) | JP2010520893A (enExample) |
| KR (2) | KR20150080025A (enExample) |
| CN (1) | CN101679239B (enExample) |
| CA (1) | CA2680467C (enExample) |
| ES (1) | ES2565243T3 (enExample) |
| TW (1) | TWI549676B (enExample) |
| WO (1) | WO2008109994A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8030344B2 (en) * | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CA2703718A1 (en) * | 2007-11-02 | 2009-05-07 | Tammy Mallais | Inhibitors of histone deacetylase |
| US9265734B2 (en) | 2008-09-03 | 2016-02-23 | Biomarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors |
| AU2010215524A1 (en) * | 2009-02-23 | 2011-06-30 | F. Hoffmann-La Roche Ag | Novel ortho-aminoamides for the treatment of cancer |
| WO2011053876A1 (en) | 2009-10-30 | 2011-05-05 | Massachusetts Institute Of Technology | The use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders |
| US20130310379A1 (en) * | 2010-11-19 | 2013-11-21 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| WO2012118782A1 (en) | 2011-02-28 | 2012-09-07 | Repligen Corporation | Histone deacetylase inhibitors |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| CN102775368B (zh) * | 2011-05-10 | 2016-08-17 | 上海驺虞医药科技有限公司 | 一类噻唑类化合物及其制备方法和用途 |
| EP2780014A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| DK2970139T3 (en) | 2013-03-15 | 2018-08-13 | Biomarin Pharm Inc | HDAC inhibitors |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3033334A1 (en) | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| US9274117B2 (en) * | 2013-12-21 | 2016-03-01 | Catholic University Industry Academic | Use of SIRT7 as novel cancer therapy target and method for treating cancer using the same |
| US9636298B2 (en) | 2014-01-17 | 2017-05-02 | Methylgene Inc. | Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs |
| GB201501870D0 (en) * | 2015-02-04 | 2015-03-18 | Cancer Rec Tech Ltd | Autotaxin inhibitors |
| EP3317253A1 (en) * | 2015-07-02 | 2018-05-09 | BioMarin Pharmaceutical Inc. | Histone deacetylase inhibtors |
| US10577350B2 (en) | 2015-08-28 | 2020-03-03 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide |
| WO2018075598A1 (en) | 2016-10-19 | 2018-04-26 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of ezh2 |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2754286A (en) | 1951-10-15 | 1956-07-10 | Du Pont | Aldehydes and their acetals |
| CH431764A (de) | 1959-05-06 | 1967-03-15 | Sandoz Ag | Verfahren zur Herstellung metallhaltiger Reaktivfarbstoffe |
| US3263924A (en) | 1963-09-13 | 1966-08-02 | Dole Valve Co | Heating and cooling zone valve |
| WO1986005779A1 (en) | 1985-04-03 | 1986-10-09 | Yamanouchi Pharmaceutical Co., Ltd. | Phenylene derivatives |
| US5149797A (en) | 1990-02-15 | 1992-09-22 | The Worcester Foundation For Experimental Biology | Method of site-specific alteration of rna and production of encoded polypeptides |
| US5332750A (en) | 1991-09-04 | 1994-07-26 | Merck Patent Gesellschaft Mit Beschrankter Haftung | 1,2-dihydro-2-oxopyridines |
| US5652355A (en) | 1992-07-23 | 1997-07-29 | Worcester Foundation For Experimental Biology | Hybrid oligonucleotide phosphorothioates |
| DE19510957A1 (de) | 1995-03-25 | 1996-09-26 | Huels Chemische Werke Ag | Eingedickter Bodenverfestiger, sowie diesen enthaltende verpackte Fertigmischung für Bodenbehandlungen |
| US6174905B1 (en) | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
| US6794392B1 (en) | 1996-09-30 | 2004-09-21 | Schering Aktiengesellschaft | Cell differentiation inducer |
| JP4105451B2 (ja) | 1996-09-30 | 2008-06-25 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 分化誘導剤 |
| US6034251A (en) | 1997-11-07 | 2000-03-07 | Schering Corporation | Phenyl-alkyl-imidazoles |
| US5905084A (en) * | 1997-11-14 | 1999-05-18 | Eli Lilly And Company | 5-HTIF -agonists effective in treating migraine |
| JPH11318492A (ja) | 1998-03-09 | 1999-11-24 | Aisin Seiki Co Ltd | 蛍光発生性基質を含有する組成物 |
| JPH11269146A (ja) | 1998-03-24 | 1999-10-05 | Mitsui Chem Inc | 分化誘導剤 |
| JP4405602B2 (ja) | 1998-04-16 | 2010-01-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | ヒストン脱アセチル化酵素阻害剤 |
| JP2000256194A (ja) | 1999-01-06 | 2000-09-19 | Mitsui Chemicals Inc | 核内レセプタ作動薬およびその効果増強剤 |
| US6653309B1 (en) | 1999-04-26 | 2003-11-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of IMPDH enzyme technical field of the invention |
| CA2366408A1 (en) | 1999-05-03 | 2000-11-30 | Methylgene, Inc. | Inhibition of histone deacetylase |
| JP4360660B2 (ja) | 1999-11-09 | 2009-11-11 | 三井化学株式会社 | モノアシルフェニレンジアミン誘導体の精製法 |
| US6541661B1 (en) | 1999-11-23 | 2003-04-01 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US20040087798A1 (en) | 2000-03-14 | 2004-05-06 | Akira Yamada | Novel amide compounds |
| CA2404002A1 (en) | 2000-03-24 | 2001-09-27 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| CA2434601A1 (en) | 2001-01-12 | 2002-09-12 | Methylgene, Inc. | Methods for specifically inhibiting histone deacetylase-4 |
| US6897220B2 (en) | 2001-09-14 | 2005-05-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US7868204B2 (en) | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| BR0212510A (pt) | 2001-09-14 | 2004-08-24 | Methylgene Inc | Inibidor de histona desacetilase, composto e composição |
| WO2003066579A2 (en) * | 2002-02-07 | 2003-08-14 | Axys Pharmaceuticals | Novel bicyclic hydroxamates as inhibitors of histone deacetylase |
| MY140390A (en) | 2002-03-13 | 2009-12-31 | Janssen Pharmaceutica Nv | Sulfonylamino-derivatives as novel inhibitors of histone deacetylase |
| MXPA04007775A (es) | 2002-03-13 | 2004-10-15 | Janssen Pharmaceutica Nv | Derivados de sulfonilo como novedosos inhibidores de la histona desacetilasa. |
| PL212089B1 (pl) | 2002-03-13 | 2012-08-31 | Janssen Pharmaceutica Nv | Związki heterocykliczne jako inhibitory deacetylazy histonowej, kompozycja farmaceutyczna je zawierająca, ich zastosowanie, sposób wytwarzania, sposób wykrywania lub identyfikacji HDAC oraz kompozycja |
| ES2307909T3 (es) | 2002-03-13 | 2008-12-01 | Janssen Pharmaceutica Nv | Derivados de piperazinil, piperidinil y morfolinil como nuevos inhidbidores de la histona deacetilasa. |
| JP4648628B2 (ja) | 2002-03-13 | 2011-03-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒストンデアセチラーゼの新規な阻害剤としてのカルボニルアミノ誘導体 |
| EP2161255A1 (en) | 2002-03-14 | 2010-03-10 | Nippon Soda Co., Ltd. | Phenolic Compound and Recording Material Using the Same |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| US20040072770A1 (en) | 2002-07-03 | 2004-04-15 | Besterman Jeffrey M. | Methods for specifically inhibiting histone deacetylase-7 and 8 |
| CA2501265A1 (en) | 2002-10-17 | 2004-04-29 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| TW200505902A (en) | 2003-03-20 | 2005-02-16 | Schering Corp | Cannabinoid receptor ligands |
| JP4809228B2 (ja) | 2003-09-24 | 2011-11-09 | メチルジーン インコーポレイテッド | ヒストンデアセチラーゼの阻害剤 |
| US7253204B2 (en) | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| WO2005092899A1 (en) | 2004-03-26 | 2005-10-06 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CA2581356A1 (en) | 2004-09-22 | 2006-03-22 | Methylgene Inc. | Histone deacetylase whole cell enzyme assay |
| WO2006066133A2 (en) * | 2004-12-16 | 2006-06-22 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| JP4853824B2 (ja) * | 2005-01-20 | 2012-01-11 | アステラス製薬株式会社 | キノロン誘導体を有効成分とする医薬組成物 |
| AU2006240258A1 (en) * | 2005-04-20 | 2006-11-02 | Merck Sharp & Dohme Corp. | Benzothiophene derivatives |
| JP2008540574A (ja) | 2005-05-11 | 2008-11-20 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
| ES2553178T3 (es) * | 2005-05-18 | 2015-12-04 | Janssen Pharmaceutica N.V. | Derivados sustituidos de aminopropenil piperidina o morfolina como nuevos inhibidores de histona deacetilasa |
| WO2007011626A2 (en) * | 2005-07-14 | 2007-01-25 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| WO2007055942A2 (en) * | 2005-11-03 | 2007-05-18 | Merck & Co., Inc. | Substituted nicotinamide compounds |
| AR057579A1 (es) * | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
| JP2009525955A (ja) | 2006-01-13 | 2009-07-16 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
| WO2007118137A1 (en) | 2006-04-07 | 2007-10-18 | Methylgene Inc. | Benzamide derivatives as inhibitors of histone deacetylase |
| US8030344B2 (en) * | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
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- 2008-03-12 KR KR1020157016812A patent/KR20150080025A/ko not_active Ceased
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| EP2134680A1 (en) | 2009-12-23 |
| HK1142597A1 (en) | 2010-12-10 |
| JP2010520893A (ja) | 2010-06-17 |
| TW200848015A (en) | 2008-12-16 |
| US20110212965A1 (en) | 2011-09-01 |
| JP2014159417A (ja) | 2014-09-04 |
| CN101679239B (zh) | 2014-12-10 |
| US20080227826A1 (en) | 2008-09-18 |
| CA2680467A1 (en) | 2008-09-18 |
| KR20150080025A (ko) | 2015-07-08 |
| KR101678611B1 (ko) | 2016-11-22 |
| JP5885311B2 (ja) | 2016-03-15 |
| US8030344B2 (en) | 2011-10-04 |
| CA2680467C (en) | 2016-11-08 |
| EP2134680A4 (en) | 2012-03-07 |
| EP2134680B1 (en) | 2016-01-13 |
| WO2008109994A1 (en) | 2008-09-18 |
| US8354445B2 (en) | 2013-01-15 |
| KR20090119004A (ko) | 2009-11-18 |
| TWI549676B (zh) | 2016-09-21 |
| CN101679239A (zh) | 2010-03-24 |
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