HRP20151386T1 - Fenil aminopirimidinski spojevi i njihova primjena - Google Patents
Fenil aminopirimidinski spojevi i njihova primjena Download PDFInfo
- Publication number
- HRP20151386T1 HRP20151386T1 HRP20151386TT HRP20151386T HRP20151386T1 HR P20151386 T1 HRP20151386 T1 HR P20151386T1 HR P20151386T T HRP20151386T T HR P20151386TT HR P20151386 T HRP20151386 T HR P20151386T HR P20151386 T1 HRP20151386 T1 HR P20151386T1
- Authority
- HR
- Croatia
- Prior art keywords
- pyrimidin
- cyanomethyl
- benzamide
- morpholinophenylamino
- phenylamino
- Prior art date
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- DMEGQEWPMXDRMO-UHFFFAOYSA-N 4-phenylpyrimidin-2-amine Chemical class NC1=NC=CC(C=2C=CC=CC=2)=N1 DMEGQEWPMXDRMO-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 29
- -1 morpholino, thiomorpholinyl Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 4
- 208000037244 polycythemia vera Diseases 0.000 claims 4
- 208000003476 primary myelofibrosis Diseases 0.000 claims 4
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 3
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 230000003463 hyperproliferative effect Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033755 Neutrophilic Chronic Leukemia Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 206010028537 myelofibrosis Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- RFPTXMLFYMYJSO-UHFFFAOYSA-N 2-cyano-n-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(CC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 RFPTXMLFYMYJSO-UHFFFAOYSA-N 0.000 claims 1
- ZKNKULZWHFOBKN-UHFFFAOYSA-N 4-[2-[4-(1-benzylpiperidin-4-yl)oxyanilino]pyrimidin-4-yl]-n-(cyanomethyl)benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(OC3CCN(CC=4C=CC=CC=4)CC3)=CC=2)=N1 ZKNKULZWHFOBKN-UHFFFAOYSA-N 0.000 claims 1
- DUVAENBVORMJGM-UHFFFAOYSA-N 4-[2-[4-(4-acetylpiperazin-1-yl)anilino]pyrimidin-4-yl]-n-(cyanomethyl)benzamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=CC(C=2C=CC(=CC=2)C(=O)NCC#N)=N1 DUVAENBVORMJGM-UHFFFAOYSA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- CNXIVFUEFOVEQD-UHFFFAOYSA-N 4-methylbenzenesulfonic acid;n-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]-n-prop-2-ynylmethanesulfonamide Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.C1=CC(N(CC#C)S(=O)(=O)C)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 CNXIVFUEFOVEQD-UHFFFAOYSA-N 0.000 claims 1
- PZHBSZFJSTVJLP-UHFFFAOYSA-N 5-[[4-[4-(cyanomethylcarbamoyl)phenyl]pyrimidin-2-yl]amino]-n,n-dimethyl-2-morpholin-4-ylbenzamide Chemical compound C=1C=C(N2CCOCC2)C(C(=O)N(C)C)=CC=1NC(N=1)=NC=CC=1C1=CC=C(C(=O)NCC#N)C=C1 PZHBSZFJSTVJLP-UHFFFAOYSA-N 0.000 claims 1
- ASYUXYORMIJKGM-UHFFFAOYSA-N 5-[[4-[4-(cyanomethylcarbamoyl)phenyl]pyrimidin-2-yl]amino]-n-ethyl-2-morpholin-4-ylbenzamide Chemical compound C=1C=C(N2CCOCC2)C(C(=O)NCC)=CC=1NC(N=1)=NC=CC=1C1=CC=C(C(=O)NCC#N)C=C1 ASYUXYORMIJKGM-UHFFFAOYSA-N 0.000 claims 1
- WHAMVDHXDXVFJO-UHFFFAOYSA-N 5-[[4-[4-[cyanomethyl(methylsulfonyl)amino]phenyl]pyrimidin-2-yl]amino]-n-[2-(dimethylamino)ethyl]-2-morpholin-4-ylbenzamide Chemical compound C=1C=C(N2CCOCC2)C(C(=O)NCCN(C)C)=CC=1NC(N=1)=NC=CC=1C1=CC=C(N(CC#N)S(C)(=O)=O)C=C1 WHAMVDHXDXVFJO-UHFFFAOYSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 1
- 229940121730 Janus kinase 2 inhibitor Drugs 0.000 claims 1
- 206010028561 Myeloid metaplasia Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 208000005485 Thrombocytosis Diseases 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000005907 alkyl ester group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000005251 aryl acyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000002843 carboxylic acid group Chemical group 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical compound [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000003106 haloaryl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- ZVHNDZWQTBEVRY-UHFFFAOYSA-N momelotinib Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 ZVHNDZWQTBEVRY-UHFFFAOYSA-N 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- XRZVCGWERZVRNT-UHFFFAOYSA-N n-(2-cyanopropan-2-yl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(=O)NC(C)(C)C#N)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 XRZVCGWERZVRNT-UHFFFAOYSA-N 0.000 claims 1
- HSQKKTMYEWBKDJ-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-(3-fluoro-4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound C=1C=C(N2CCOCC2)C(F)=CC=1NC(N=1)=NC=CC=1C1=CC=C(C(=O)NCC#N)C=C1 HSQKKTMYEWBKDJ-UHFFFAOYSA-N 0.000 claims 1
- BMUQBXPJHZHPET-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-(3-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=C(C=CC=2)N2CCOCC2)=N1 BMUQBXPJHZHPET-UHFFFAOYSA-N 0.000 claims 1
- FBGQWQKPPNXFPL-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-(4-iodoanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(I)=CC=C1NC1=NC=CC(C=2C=CC(=CC=2)C(=O)NCC#N)=N1 FBGQWQKPPNXFPL-UHFFFAOYSA-N 0.000 claims 1
- YPYLBOZLGZWTBR-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-(4-piperidin-4-yloxyanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(OC3CCNCC3)=CC=2)=N1 YPYLBOZLGZWTBR-UHFFFAOYSA-N 0.000 claims 1
- XHATTZDUUOAKGZ-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[(6-morpholin-4-ylpyridin-3-yl)amino]pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=NC(=CC=2)N2CCOCC2)=N1 XHATTZDUUOAKGZ-UHFFFAOYSA-N 0.000 claims 1
- WGYLKXSLEVYOED-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[3-(propoxymethyl)anilino]pyrimidin-4-yl]benzamide Chemical compound CCCOCC1=CC=CC(NC=2N=C(C=CN=2)C=2C=CC(=CC=2)C(=O)NCC#N)=C1 WGYLKXSLEVYOED-UHFFFAOYSA-N 0.000 claims 1
- NVWVHHYJMKVMCA-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(1-ethylpiperidin-4-yl)oxyanilino]pyrimidin-4-yl]benzamide Chemical compound C1CN(CC)CCC1OC(C=C1)=CC=C1NC1=NC=CC(C=2C=CC(=CC=2)C(=O)NCC#N)=N1 NVWVHHYJMKVMCA-UHFFFAOYSA-N 0.000 claims 1
- VEQFDJWBJMBHQL-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(2-morpholin-4-ylethoxy)anilino]pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(OCCN3CCOCC3)=CC=2)=N1 VEQFDJWBJMBHQL-UHFFFAOYSA-N 0.000 claims 1
- PUUSPGBLECGIDO-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(3-hydroxypiperidin-1-yl)anilino]-5-methylpyrimidin-4-yl]benzamide Chemical compound N1=C(C=2C=CC(=CC=2)C(=O)NCC#N)C(C)=CN=C1NC(C=C1)=CC=C1N1CCCC(O)C1 PUUSPGBLECGIDO-UHFFFAOYSA-N 0.000 claims 1
- WKWZJQKWLBPCFA-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(4-hydroxypiperidin-1-yl)anilino]-5-methylpyrimidin-4-yl]benzamide Chemical compound N1=C(C=2C=CC(=CC=2)C(=O)NCC#N)C(C)=CN=C1NC(C=C1)=CC=C1N1CCC(O)CC1 WKWZJQKWLBPCFA-UHFFFAOYSA-N 0.000 claims 1
- ZPHRKMIVEXOWDD-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(4-hydroxypiperidin-1-yl)anilino]pyrimidin-4-yl]benzamide Chemical compound C1CC(O)CCN1C(C=C1)=CC=C1NC1=NC=CC(C=2C=CC(=CC=2)C(=O)NCC#N)=N1 ZPHRKMIVEXOWDD-UHFFFAOYSA-N 0.000 claims 1
- JWNVJLOTJWLIAA-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]benzamide Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1NC1=NC=CC(C=2C=CC(=CC=2)C(=O)NCC#N)=N1 JWNVJLOTJWLIAA-UHFFFAOYSA-N 0.000 claims 1
- ZGWDWXIWRGKYHA-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(NCC#N)=O)=CC=C1C1=CC=NC(NC=2C=CC(CN3CCOCC3)=CC=2)=N1 ZGWDWXIWRGKYHA-UHFFFAOYSA-N 0.000 claims 1
- SDEDLQGWJHWNGN-UHFFFAOYSA-N n-(cyanomethyl)-4-[2-[4-morpholin-4-yl-3-(trifluoromethyl)anilino]pyrimidin-4-yl]benzamide Chemical compound C=1C=C(N2CCOCC2)C(C(F)(F)F)=CC=1NC(N=1)=NC=CC=1C1=CC=C(C(=O)NCC#N)C=C1 SDEDLQGWJHWNGN-UHFFFAOYSA-N 0.000 claims 1
- PKEOFNLYKBPOQT-UHFFFAOYSA-N n-(cyanomethyl)-4-[5-methyl-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound N1=C(C=2C=CC(=CC=2)C(=O)NCC#N)C(C)=CN=C1NC(C=C1)=CC=C1N1CCOCC1 PKEOFNLYKBPOQT-UHFFFAOYSA-N 0.000 claims 1
- USAVSBDYEWUWKW-UHFFFAOYSA-N n-(cyanomethyl)-n-[4-[2-(3-cyano-4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]methanesulfonamide Chemical compound C1=CC(N(CC#N)S(=O)(=O)C)=CC=C1C1=CC=NC(NC=2C=C(C(N3CCOCC3)=CC=2)C#N)=N1 USAVSBDYEWUWKW-UHFFFAOYSA-N 0.000 claims 1
- OTLWDDOQHXMLOB-UHFFFAOYSA-N n-(cyanomethyl)-n-[4-[2-(3-fluoro-4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]methanesulfonamide Chemical compound C1=CC(N(CC#N)S(=O)(=O)C)=CC=C1C1=CC=NC(NC=2C=C(F)C(N3CCOCC3)=CC=2)=N1 OTLWDDOQHXMLOB-UHFFFAOYSA-N 0.000 claims 1
- YABPIKWVPZXBHT-UHFFFAOYSA-N n-(cyanomethyl)-n-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]methanesulfonamide Chemical compound C1=CC(N(CC#N)S(=O)(=O)C)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 YABPIKWVPZXBHT-UHFFFAOYSA-N 0.000 claims 1
- XVTDFRXZCMFKMJ-UHFFFAOYSA-N n-(cyanomethyl)-n-[4-[2-[4-morpholin-4-yl-3-(trifluoromethyl)anilino]pyrimidin-4-yl]phenyl]methanesulfonamide Chemical compound C1=CC(N(CC#N)S(=O)(=O)C)=CC=C1C1=CC=NC(NC=2C=C(C(N3CCOCC3)=CC=2)C(F)(F)F)=N1 XVTDFRXZCMFKMJ-UHFFFAOYSA-N 0.000 claims 1
- VOMQGBZTOWNIRU-UHFFFAOYSA-N n-(cyanomethyl)-n-methyl-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(=O)N(CC#N)C)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 VOMQGBZTOWNIRU-UHFFFAOYSA-N 0.000 claims 1
- SHACBZUITUQKQA-UHFFFAOYSA-N n-[2-(cyanomethylamino)-2-oxoethyl]-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide Chemical compound C1=CC(C(=O)NCC(=O)NCC#N)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCOCC2)=N1 SHACBZUITUQKQA-UHFFFAOYSA-N 0.000 claims 1
- RAANDBXCGYFDRL-UHFFFAOYSA-N n-tert-butyl-5-[[4-[4-(cyanomethylcarbamoyl)phenyl]pyrimidin-2-yl]amino]-2-morpholin-4-ylbenzamide Chemical compound C=1C=C(N2CCOCC2)C(C(=O)NC(C)(C)C)=CC=1NC(N=1)=NC=CC=1C1=CC=C(C(=O)NCC#N)C=C1 RAANDBXCGYFDRL-UHFFFAOYSA-N 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 229920001184 polypeptide Chemical group 0.000 claims 1
- 108090000765 processed proteins & peptides Chemical group 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
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Claims (18)
1. Spoj formule Ib
[image]
u kome je
Z je nezavisno odabrano od N i CH;
R1 je nezavisno odabran od H, halogena, OH, CONHR2, CON(R2)2, CF3, R2OR2, CN, morfolino, tiomorfolinila, tiomorfolino-1,1-dioksida, supstituiranog ili nesupstituiranog piperidinila, supstituiranog ili nesupstituiranog piperazinila, imidazolila, supstituiranog ili nesupstituiranog pirolidinila i C1-4alkilena u kome su atomi ugljika po izboru zamijenjeni sa NRY i/ili O supstituiranim sa morfolinom, tiomorfolinilom, tiomorfolino-1, 1-dioksidom, supstituiranim ili nesupstituiranim piperidinilom, supstituiranim ili nesupstituiranim piperazinilom, imidazolilom ili supstituiranim ili nesupstituiranim pirolidinilom;
R2 je supstituiran ili nesupstituiran sa C1-4alkil;
RY je H ili supstituiran ili nesupstituiran C1-4alkil;
R8 je RXCN;
RX je supstituiran ili nesupstituiran C1-4alkilen u kome do 2 atoma ugljika mogu biti po izboru zamijenjena sa CO, NS2R, NRY, CONRY, SOL, SO2 ili O;
R11 je H ili C1-4alkil,
U kome su supstituti odabrani iz grupe koja se sastoji od C1-4 alkil, C3-6 cikloalkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkilaril, aril, heterociklil, halo, haloaril, haloheterociklil, hidroksi, C1-4 alkoksi, ariloksi, karboksi, amino, C1-6alkilacil, arilacil, heterociklilacil, acilamino, aciloksi, C1-6alkilsulfenil, arilsulfonil i ciano;
ili njegov enantiomer, njegov prolijek ili njegova farmaceutski prihvatljiva sol, gdje su prolijekovi odabrani od:
• spojevi u kojima su aminokiselinski ostatak, ili polipeptidni lanac od dva ili više aminokiselinskih ostataka kovalentno vezani peptidnom vezom za slobodnu amino, hidroksi ili karboksilnu grupu spomenutog spojevi formule Ib;
• spojevi u kojima su karbonat, karbamat, amid ili alkil estar kovalentno vezani za slobodnu amino, amido, hidroksi grupu ili grupu karboksilne kiseline spomenutog spojevi formule Ib preko karbonilnog ugljika bočnog lanca prolijeka; i
• spojevi u kojima je slobodni hidroksil spomenutog spojevi formule Ib pridružen preko veze fosfor-kisik za fosfatni derivat spojevi (kao što je kiselina, sol ili kiselina, ili estar).
2. Spoj prema patentnom zahtjevu 1 gdje R1 je morfolino.
3. Spoj prema patentnom zahtjevu 1 ili patentnom zahtjevu 2 gdje Z je CH.
4. Spoj prema patentnom zahtjevu 1 odabrano od:
N-(cianometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida;
N-(2-cianopropan-2-il)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(3-morfolinofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-tiomorfblinofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-jodofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida;
N-(cianometil)-4-(2-(4-(morfolinometil)fenilamino)pirimidin-4-il)benzamida;
N-(2-(cianometilamino)-2-oksoetil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-(4-metilpiperazin-1-il)fenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-(3-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida;
4-(2-(4-(1-benzilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida;
N-(cianometil)-4-(2-(6-morfolinopiridin-3-ilamino)pirimidin-4-il)benzamida;
4-(2-(4-(4-acetilpiperazin-1-il)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida;
N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(prop-2-inil)metansulfonamid tozilata;
N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-(piperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida;
5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N,N-dimetil-2-morfolinobenzamida;
N-terc-butil-5-(4-(4-(cianometilkarbamoil)fenil) pirimidin-2-ilamino)-2-morfolinobenzamida;
5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N-etil-2-morfolinobenzamida;
N-(cianometil)-4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)benzamida;
5-(4-(4-(N-(cianometil)metilsulfonamido)fenil)pirimidin-2-ilamino)-N-(2-(dimetilamino)etil)-2-morfolinobenzamida;
N-(cianometil)-N-(4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)fenil)metansulfonamida;
N-(cianometil)-4-(2-(3-(propoksimetil)fenilamino)pirimidin-4-il)benzamida;
4-(2-(3-(aliloksimetil)-4-morfolinofenilamino)pirimidin-4-il)-N-(cianometil)benzamida;
N-(cianometil)-4-(2-(4-(1-etilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-N-(4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida;
N-(4-(2-(3-ciano-4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(cianometil)metansulfonamida;
2-ciano-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)acetamida;
N-(cianometil)-4-(2-(4-(2-morfolinoetoksi)fenilamino)pirimidin-4-il)benzamida;
N-(cianometil)-4-(2-{[4-(1,1-diokso-1λ6,4-tiomorpholin-4-il)fenil]amino}pirimidin-4-il)benzamida;
N-(cianometil)-4-[2-({4-[(1,1-diokso-1λ6,4-tiomorfolin-4-il)metil]fenil}amino)pirimidin-4-il]benzamida;
N-(cianometil)-N-metil-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; i
N-(cianometil)-4-(5-metil-2-(4-morfolinofenilamino)pirimidin-4-il)benzamida.
i njihove farmaceutsko prihvatljive soli.
5. Spoj prema patentnom zahtjevu 1 koje je
[image]
ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema zahtjevu 5 koje je hidrohloridna sol slijedećeg spojevi
[image]
7. Spoj prema patentnom zahtjevu 1 koje je
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, gdje je spoj kinazni inhibitor.
9. Spoj prema patentnom zahtjevu 8, prema kome je kinazni inhibitor JAK2 inhibitor.
10. Proces za pripremu spojevi formule Ib prema patentnom zahtjevu 1, koji sadrži korak vezivanja spojevi formule II
[image]
gdje je
R11 definiran u patentnom zahtjevu 1 i X je klor koji je zatim konvertiran u jod prije vezivanja sa spojevima koja su označena formulama III i IV.
[image]
pri čemu su
Z, R1 i R8 definirani kao što je u patentnom zahtjevu 1; i M je B ili metal.
11. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9, i farmaceutski prihvatljivi nosač.
12. Implant koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili farmaceutska kompozicija prema patentnom zahtjevu 11 za primjenu u metodi liječenja bolesti povezanih sa kinazom, gdje spomenuta metoda uključuje davanje efektivne količine spomenutog spoja ili farmaceutske kompozicije subjektu kod koga postoji takva potreba.
14. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 13, gdje je bolest povezana sa kinazom imunološka ili inflamatorna bolest, bolest hiperproliferacije, virusno oboljenje, bolest metabolizma, ili vaskularno oboljenje.
15. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje su imunološko ili inflamatorno oboljenje presađeni organ.
16. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje je hiperproliferativno oboljenje rak ili mijeloproliferativna bolest.
17. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 16 gdje je hiperproliferativna bolest mijeloproliferativna bolest odabrana iz grupe koja se sastoji od slijedećih bolesti: policitemija vera (PV), primarna mijelofibroza, trombocitemija, esencijalna trombocitemija (ET), agnoneična mijeloidna metaplazija (AMM), idiopatska mijelofibroza (IMF), hronična mijeloidna leukemija (CML), sistemska mastocistoza (SM), hronična neutrofilna leukemija (CNL), mijelodisplazni sindrom (MDS) i sistemska bolest masnih ćelija (SMCD).
18. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 17, gdje je mijeloproliferativna bolest odabrana iz grupe koju čine policitemija vera (PV), primarna mijelofibroza, trombocitemija, i esencijalna trombocitemija (ET).
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US1625207P | 2007-12-21 | 2007-12-21 | |
PCT/AU2008/000339 WO2008109943A1 (en) | 2007-03-12 | 2008-03-12 | Phenyl amino pyrimidine compounds and uses thereof |
EP08714386.3A EP2152701B1 (en) | 2007-03-12 | 2008-03-12 | Phenyl amino pyrimidine compounds and uses thereof |
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- 2008-03-12 WO PCT/AU2008/000339 patent/WO2008109943A1/en active Application Filing
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- 2008-03-12 JP JP2009552972A patent/JP2010520892A/ja not_active Withdrawn
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- 2008-03-12 EP EP08714386.3A patent/EP2152701B1/en active Active
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- 2008-03-12 KR KR1020097021274A patent/KR101566840B1/ko active IP Right Grant
- 2008-03-12 KR KR1020157009274A patent/KR20150043565A/ko active Search and Examination
- 2008-03-12 HU HUE08714386A patent/HUE029188T2/en unknown
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2009
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2011
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