JP2005509624A5 - - Google Patents
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- Publication number
- JP2005509624A5 JP2005509624A5 JP2003535800A JP2003535800A JP2005509624A5 JP 2005509624 A5 JP2005509624 A5 JP 2005509624A5 JP 2003535800 A JP2003535800 A JP 2003535800A JP 2003535800 A JP2003535800 A JP 2003535800A JP 2005509624 A5 JP2005509624 A5 JP 2005509624A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- substituted
- atom
- imino
- 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.)
- Granted
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- -1 trifluoromethylsulfenyl group Chemical group 0.000 claims 292
- 125000000217 alkyl group Chemical group 0.000 claims 157
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 86
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 79
- 125000003545 alkoxy group Chemical group 0.000 claims 74
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 71
- 125000003118 aryl group Chemical group 0.000 claims 64
- 125000003277 amino group Chemical group 0.000 claims 63
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 62
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 60
- 125000004093 cyano group Chemical group *C#N 0.000 claims 59
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 58
- 125000003282 alkyl amino group Chemical group 0.000 claims 54
- 125000004663 dialkyl amino group Chemical group 0.000 claims 53
- 229910052717 sulfur Inorganic materials 0.000 claims 49
- 125000004434 sulfur atom Chemical group 0.000 claims 49
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 45
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 43
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 42
- 125000004432 carbon atom Chemical group C* 0.000 claims 41
- 229910052801 chlorine Inorganic materials 0.000 claims 41
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 37
- 125000001153 fluoro group Chemical group F* 0.000 claims 37
- 229910052731 fluorine Inorganic materials 0.000 claims 35
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 34
- 229910052757 nitrogen Inorganic materials 0.000 claims 34
- 125000001309 chloro group Chemical group Cl* 0.000 claims 32
- 229910052760 oxygen Inorganic materials 0.000 claims 32
- 125000004430 oxygen atom Chemical group O* 0.000 claims 31
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 31
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 30
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 29
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 29
- 239000001301 oxygen Substances 0.000 claims 28
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 27
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 27
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 27
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 26
- 125000003710 aryl alkyl group Chemical group 0.000 claims 25
- 125000006413 ring segment Chemical group 0.000 claims 23
- 125000002947 alkylene group Chemical group 0.000 claims 22
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 22
- 150000001721 carbon Chemical group 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 21
- 125000001424 substituent group Chemical group 0.000 claims 20
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 19
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 19
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 18
- 229910052740 iodine Inorganic materials 0.000 claims 18
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 16
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 15
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 15
- 125000004104 aryloxy group Chemical group 0.000 claims 15
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 13
- 125000004647 alkyl sulfenyl group Chemical group 0.000 claims 13
- 125000004429 atom Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 13
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 12
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 12
- 125000005135 aryl sulfinyl group Chemical group 0.000 claims 12
- 239000000460 chlorine Substances 0.000 claims 12
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 11
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims 11
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 10
- 239000011737 fluorine Substances 0.000 claims 10
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 10
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 9
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 9
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 claims 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 8
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 8
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 claims 8
- 125000005140 aralkylsulfonyl group Chemical group 0.000 claims 8
- 125000005126 aryl alkyl carbonyl amino group Chemical group 0.000 claims 8
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 8
- 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 8
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000005125 aryl alkyl amino carbonyl group Chemical group 0.000 claims 7
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 7
- 229910052794 bromium Inorganic materials 0.000 claims 7
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 7
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims 6
- 125000004103 aminoalkyl group Chemical group 0.000 claims 6
- 125000005243 carbonyl alkyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 6
- 125000004689 alkyl amino carbonyl alkyl group Chemical group 0.000 claims 5
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 5
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 5
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000004472 dialkylaminosulfonyl group Chemical group 0.000 claims 5
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 5
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 5
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 4
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 4
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims 4
- 125000005141 aryl amino sulfonyl group Chemical group 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 4
- 125000006263 dimethyl aminosulfonyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])S(*)(=O)=O 0.000 claims 4
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 4
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 4
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 4
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims 3
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 3
- 125000005278 alkyl sulfonyloxy group Chemical group 0.000 claims 3
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000001769 aryl amino group Chemical group 0.000 claims 3
- 125000005199 aryl carbonyloxy group Chemical group 0.000 claims 3
- 125000000638 benzylaminocarbonyl group Chemical group C(C1=CC=CC=C1)NC(=O)* 0.000 claims 3
- 125000001246 bromo group Chemical group Br* 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 125000004984 dialkylaminoalkoxy group Chemical group 0.000 claims 3
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 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 3
- 125000006261 methyl amino sulfonyl group Chemical group [H]N(C([H])([H])[H])S(*)(=O)=O 0.000 claims 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000005184 naphthylamino group Chemical group C1(=CC=CC2=CC=CC=C12)N* 0.000 claims 3
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 3
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 2
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims 2
- 125000004539 5-benzimidazolyl group Chemical group N1=CNC2=C1C=CC(=C2)* 0.000 claims 2
- 239000005977 Ethylene Substances 0.000 claims 2
- 125000005138 alkoxysulfonyl group Chemical group 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000006264 diethylaminomethyl group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000004464 hydroxyphenyl group Chemical group 0.000 claims 2
- 125000004537 indazol-5-yl group Chemical group N1N=CC2=CC(=CC=C12)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 1
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000004398 2-methyl-2-butyl group Chemical group CC(C)(CC)* 0.000 claims 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- CTOUNZIAEBIWAW-UHFFFAOYSA-N 3,4-dihydro-1h-quinazolin-2-one Chemical compound C1=CC=C2NC(=O)NCC2=C1 CTOUNZIAEBIWAW-UHFFFAOYSA-N 0.000 claims 1
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- RRHGJUQNOFWUDK-UHFFFAOYSA-N Isoprene Chemical compound CC(=C)C=C RRHGJUQNOFWUDK-UHFFFAOYSA-N 0.000 claims 1
- 229920001774 Perfluoroether Polymers 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000004849 alkoxymethyl group Chemical group 0.000 claims 1
- 125000005094 alkyl carbonyl amino alkyl group Chemical group 0.000 claims 1
- 125000005154 alkyl sulfonyl amino alkyl group Chemical group 0.000 claims 1
- 125000005133 alkynyloxy group Chemical group 0.000 claims 1
- 125000004467 aryl imino group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 125000000043 benzamido group Chemical group [H]N([*])C(=O)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- YXVFYQXJAXKLAK-UHFFFAOYSA-N biphenyl-4-ol Chemical group C1=CC(O)=CC=C1C1=CC=CC=C1 YXVFYQXJAXKLAK-UHFFFAOYSA-N 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 150000001804 chlorine Chemical group 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000004992 haloalkylamino group Chemical group 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 claims 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 0 C*(C)C*(*)c1nc(N(*)*)c(*)cn1 Chemical compound C*(C)C*(*)c1nc(N(*)*)c(*)cn1 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33014501P | 2001-10-17 | 2001-10-17 | |
| PCT/EP2002/011453 WO2003032997A1 (de) | 2001-10-17 | 2002-10-14 | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005509624A JP2005509624A (ja) | 2005-04-14 |
| JP2005509624A5 true JP2005509624A5 (enExample) | 2006-01-05 |
| JP4460292B2 JP4460292B2 (ja) | 2010-05-12 |
Family
ID=23288491
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003535800A Expired - Lifetime JP4460292B2 (ja) | 2001-10-17 | 2002-10-14 | ピリミジン誘導体、これらの化合物を含む医薬組成物、その使用及びその調製方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US7173028B2 (enExample) |
| EP (3) | EP2090571B1 (enExample) |
| JP (1) | JP4460292B2 (enExample) |
| AT (1) | ATE407678T1 (enExample) |
| CA (1) | CA2463989C (enExample) |
| CY (1) | CY1110442T1 (enExample) |
| DE (1) | DE50212771D1 (enExample) |
| DK (1) | DK1438053T3 (enExample) |
| ES (1) | ES2314106T3 (enExample) |
| PT (1) | PT1438053E (enExample) |
| UY (1) | UY27487A1 (enExample) |
| WO (1) | WO2003032997A1 (enExample) |
Families Citing this family (135)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002312933B2 (en) | 2001-05-29 | 2007-12-06 | Schering Ag | CDK inhibiting pyrimidines, production thereof and their use as medicaments |
| CA2451128A1 (en) | 2001-06-26 | 2003-01-09 | Bristol-Myers Squibb Company | N-heterocyclic inhibitors of tnf-alpha expression |
| DK1438053T3 (da) * | 2001-10-17 | 2008-12-08 | Boehringer Ingelheim Pharma | Pyrimidinderivater, lægemiddel indeholdende disse forbindelser, deres anvendelse og fremgangsmåder til deres fremstilling |
| DK1442024T3 (da) * | 2001-11-01 | 2008-06-30 | Janssen Pharmaceutica Nv | Aminobenzamidderivater som glycogensystasekinase 3 beta-inhibitorer |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| PL373043A1 (en) | 2002-03-26 | 2005-08-08 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| AU2003231231A1 (en) * | 2002-05-06 | 2003-11-11 | Bayer Pharmaceuticals Corporation | Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders |
| EA009789B1 (ru) * | 2002-07-05 | 2008-04-28 | Таргасепт, Инк. | N-арилдиазаспирациклические соединения и способы их получения и применения |
| BR0313059B8 (pt) | 2002-07-29 | 2021-07-27 | Rigel Pharmaceuticals | composto, e, composição farmacêutica |
| JP4619786B2 (ja) * | 2002-08-29 | 2011-01-26 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 炎症性、アレルギー性及び増殖性疾患の治療において糖質コルチコイドミメティックスとして使用するための３−（スルホンアミドエチル）−インドール誘導体 |
| KR20050084027A (ko) * | 2002-11-28 | 2005-08-26 | 쉐링 악티엔게젤샤프트 | Ｃｈｋ-, ｐｄｋ- 및 ａｋｔ-억제성 피리미딘, 그의제조방법 및 약제로서의 그의 용도 |
| UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| EA013248B1 (ru) * | 2002-12-20 | 2010-04-30 | Пфайзер Продактс Инк. | Производные пиримидина для лечения патологического роста клеток |
| US7109337B2 (en) | 2002-12-20 | 2006-09-19 | Pfizer Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| DE602004022633D1 (de) * | 2003-01-30 | 2009-10-01 | Boehringer Ingelheim Pharma | 2,4-diaminopyrimidinderivate, die sich als inhibitoren von pkc-theta eignen |
| DE602004021472D1 (en) * | 2003-02-20 | 2009-07-23 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| GB0311274D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| WO2005005424A1 (en) * | 2003-07-02 | 2005-01-20 | TEVA Gyógyszergyár Részvénytársaság | Aztreonam l-lysine and methods for the preparation thereof |
| CN102358738A (zh) | 2003-07-30 | 2012-02-22 | 里格尔药品股份有限公司 | 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途 |
| EP1663991B1 (en) * | 2003-09-05 | 2007-01-10 | Pfizer Products Inc. | Selective synthesis of cf3-substituted pyrimidines |
| UY28526A1 (es) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos |
| ATE414701T1 (de) * | 2003-10-03 | 2008-12-15 | Boehringer Ingelheim Pharma | Fluoreszenzsonden zur verwendung bei einem bindungsassay auf proteinkinaseinhibitoren |
| AU2004313928A1 (en) * | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| WO2005061519A1 (en) | 2003-12-19 | 2005-07-07 | Takeda San Diego, Inc. | Kinase inhibitors |
| US7795272B2 (en) | 2004-03-13 | 2010-09-14 | Boehringer Ingelheim Pharmaceutical, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof |
| US7456176B2 (en) * | 2004-04-08 | 2008-11-25 | Targegen, Inc. | Benzotriazine inhibitors of kinases |
| US20060205945A1 (en) * | 2004-05-14 | 2006-09-14 | Pfizer Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| WO2005111016A1 (en) | 2004-05-14 | 2005-11-24 | Pfizer Products Inc. | Pyrimidine derivatives for the treatment of abnormal cell growth |
| WO2005111022A1 (en) * | 2004-05-14 | 2005-11-24 | Pfizer Products Inc. | Pyrimidines derivatives for the treatment of abnormal cell growth |
| MXPA06011658A (es) | 2004-05-14 | 2006-12-14 | Pfizer Prod Inc | Derivados de pirimidina para el tratamiento del crecimiento celular anormal. |
| US7754714B2 (en) | 2004-05-18 | 2010-07-13 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| WO2006014482A1 (en) * | 2004-07-08 | 2006-02-09 | Boehringer Ingelheim Pharmaceuticals, Inc. | Pyrimidine derivatives useful as inhibitors of pkc-theta |
| US7550598B2 (en) | 2004-08-18 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| DE602005023333D1 (de) | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| JP5095409B2 (ja) | 2004-11-24 | 2012-12-12 | ライジェル ファーマシューティカルズ， インコーポレイテッド | スピロ２，４−ピリミジンジアミン化合物およびその使用 |
| US7635711B2 (en) | 2004-12-27 | 2009-12-22 | Boehringer-Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| JP4801096B2 (ja) * | 2005-01-19 | 2011-10-26 | ライジェル ファーマシューティカルズ， インコーポレイテッド | ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 |
| US20060270694A1 (en) * | 2005-05-03 | 2006-11-30 | Rigel Pharmaceuticals, Inc. | JAK kinase inhibitors and their uses |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP1904457B1 (en) | 2005-06-08 | 2017-09-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP1741709A1 (en) * | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals |
| US20070032514A1 (en) * | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| JP4653842B2 (ja) | 2006-02-17 | 2011-03-16 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 自己免疫疾患を治療または予防するための２，４−ピリミジンジアミン化合物 |
| JP2009528295A (ja) | 2006-02-24 | 2009-08-06 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｊａｋ経路の阻害のための組成物および方法 |
| KR20090023698A (ko) * | 2006-06-15 | 2009-03-05 | 베링거 인겔하임 인터내셔날 게엠베하 | 2-아닐리노-4-아미노알킬렌아미노피리미딘 |
| EP2054392A2 (en) | 2006-06-15 | 2009-05-06 | Boehringer Ingelheim International GmbH | 2-anilino-4-(heterocyclic)amino-pyrimidines as inhibitors of protein kinase c-alpha |
| US8258129B2 (en) | 2006-07-06 | 2012-09-04 | Boehringer Ingelheim International Gmbh | 4-heterocycloalkylpyri(mi)dines, process for the preparation thereof and their use as medicaments |
| SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
| ES2555803T3 (es) | 2006-10-23 | 2016-01-08 | Cephalon, Inc. | Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met |
| MX2009005264A (es) | 2006-12-06 | 2009-05-28 | Boehringer Ingelheim Int | Mimeticos de glucocorticoides, metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos. |
| CA2673184A1 (en) | 2006-12-22 | 2008-07-03 | Boehringer Ingelheim International Gmbh | New compounds |
| EP2121633A2 (en) * | 2007-02-12 | 2009-11-25 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| US8252803B2 (en) * | 2007-02-12 | 2012-08-28 | Merck Sharp & Dohme Corp. | Piperidine derivatives |
| AP2009005010A0 (en) | 2007-04-18 | 2009-10-31 | Pfizer Prod Inc | Sulfonyl amide derivatives for the treatment of abnormal cell growth |
| KR101294731B1 (ko) * | 2007-06-04 | 2013-08-16 | 삼성디스플레이 주식회사 | 어레이 기판, 이를 갖는 표시패널 및 이의 제조방법 |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| WO2009071535A1 (en) * | 2007-12-03 | 2009-06-11 | Boehringer Ingelheim International Gmbh | Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation |
| CA2708262A1 (en) * | 2007-12-07 | 2009-06-18 | Elan Pharmaceuticals, Inc. | Methods and compositions for treating liquid tumors |
| US20100056524A1 (en) * | 2008-04-02 | 2010-03-04 | Mciver Edward Giles | Compound |
| ATE541846T1 (de) | 2008-06-06 | 2012-02-15 | Boehringer Ingelheim Int | Glucocorticoidmimetika, verfahren zu deren herstellung, pharmazeutische zusammensetzungen und anwendungen davon |
| WO2010024430A1 (ja) | 2008-09-01 | 2010-03-04 | アステラス製薬株式会社 | 2,4-ジアミノピリミジン化合物 |
| KR20110049905A (ko) * | 2008-09-03 | 2011-05-12 | 바이엘 크롭사이언스 아게 | 4-알킬-치환된 디아미노피리미딘 |
| CN102203080A (zh) * | 2008-09-03 | 2011-09-28 | 拜尔农作物科学股份公司 | 作为杀菌剂的杂环取代的苯胺基嘧啶 |
| EP2179992A1 (de) | 2008-10-21 | 2010-04-28 | Bayer Schering Pharma Aktiengesellschaft | Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| EP2179993A1 (de) | 2008-10-21 | 2010-04-28 | Bayer Schering Pharma Aktiengesellschaft | Sulfoxidsubstituierte Anilinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| TW201024281A (en) * | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
| AR074210A1 (es) | 2008-11-24 | 2010-12-29 | Boehringer Ingelheim Int | Derivados de pirimidina como inhibidores de ptk2-quinasa |
| US8952014B2 (en) | 2008-12-19 | 2015-02-10 | Boehringer Ingelheim International Gmbh | Pyrimidine derivatives which are CGRP—antagonists |
| JP5815411B2 (ja) | 2008-12-30 | 2015-11-17 | ライジェル ファーマシューティカルズ， インコーポレイテッド | ピリミジンジアミンキナーゼ阻害剤 |
| JP5658685B2 (ja) * | 2009-01-14 | 2015-01-28 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 炎症性障害の治療のための２，４−ピリミジンジアミン化合物 |
| ES2635504T3 (es) | 2009-01-21 | 2017-10-04 | Rigel Pharmaceuticals, Inc. | Derivados de N2-(3-piridilo o fenil)-N4-(4-piperidil)-2,4-pirimidinadiamina útiles en el tratamiento de enfermedades inflamatorias, toimmunitarias o proliferativas |
| PL2395983T3 (pl) | 2009-02-13 | 2020-09-07 | Boehringer Ingelheim International Gmbh | Kompozycja farmaceutyczna zawierająca inhibitor sglt2, inhibitor dpp-iv i ewentualnie dalszy środek przeciwcukrzycowy oraz jej zastosowania |
| US20110071158A1 (en) * | 2009-03-18 | 2011-03-24 | Boehringer Ingelheim International Gmbh | New compounds |
| JP2012525403A (ja) * | 2009-04-28 | 2012-10-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ＰＫＣθ阻害薬による免疫学的疾患のＥＸ−ＶＩＶＯ治療 |
| US8410126B2 (en) * | 2009-05-29 | 2013-04-02 | Boehringer Ingelheim International Gmbh | Pyrimidine inhibitors of PKTK2 |
| CA2768543C (en) * | 2009-07-28 | 2017-06-20 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
| JP5539518B2 (ja) | 2009-08-14 | 2014-07-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ２−アミノ−５−トリフルオロメチルピリミジン誘導体の位置選択的調製 |
| US8466155B2 (en) | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| US20110130415A1 (en) | 2009-12-01 | 2011-06-02 | Rajinder Singh | Protein kinase c inhibitors and uses thereof |
| JP2013519732A (ja) | 2010-02-17 | 2013-05-30 | アムジエン・インコーポレーテツド | 疼痛治療のためのナトリウムチャンネル阻害薬としてのアリールカルボキサミド誘導体 |
| ES2365960B1 (es) * | 2010-03-31 | 2012-06-04 | Palobiofarma, S.L | Nuevos antagonistas de los receptores de adenosina. |
| TWI513694B (zh) | 2010-05-11 | 2015-12-21 | Amgen Inc | 抑制間變性淋巴瘤激酶的嘧啶化合物 |
| AU2011255218B2 (en) | 2010-05-21 | 2015-03-12 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| BR112012029647A2 (pt) | 2010-05-21 | 2016-08-02 | Chemilia Ab | novos derivados de pirimidinas |
| US8354420B2 (en) * | 2010-06-04 | 2013-01-15 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 inhibitors |
| DE102010034699A1 (de) * | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidinderivate |
| SI2638031T1 (en) | 2010-11-10 | 2018-02-28 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as LRRK2 modulators |
| JP5959537B2 (ja) | 2011-01-28 | 2016-08-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換ピリジニル−ピリミジン及び医薬としてのその使用 |
| US20130324532A1 (en) * | 2011-02-17 | 2013-12-05 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
| AU2012216894B2 (en) * | 2011-02-17 | 2016-07-14 | Cancer Therapeutics Crc Pty Limited | Selective FAK inhibitors |
| UY33937A (es) | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
| JP5886411B2 (ja) | 2011-03-24 | 2016-03-16 | ノビガ・リサーチ・エービーＮｏｖｉｇａ Ｒｅｓｅａｒｃｈ ＡＢ | 新規のピリミジン誘導体 |
| EP2751093A1 (en) | 2011-08-29 | 2014-07-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| LT2785711T (lt) * | 2011-11-29 | 2016-10-25 | F.Hoffmann-La Roche Ag | 2-(fenil arba pirid-3-il)aminopirimidino dariniai kaip kinazės lrrk2 moduliatoriai skirti parkinsono ligos gydymui |
| CA2852609C (en) * | 2011-11-29 | 2020-03-10 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as lrrk2 modulators |
| AR089182A1 (es) * | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| CN104736533B (zh) | 2012-08-17 | 2016-12-07 | 癌症治疗合作研究中心有限公司 | Vegfr3抑制剂 |
| AU2013302319A1 (en) | 2012-08-17 | 2015-02-26 | Cancer Therapeutics Crc Pty Limited | VEGFR3 inhibitors |
| US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| CN104903312B (zh) * | 2013-10-07 | 2019-01-29 | 卡德门企业有限公司 | Rho激酶抑制剂 |
| BR112016008080B1 (pt) * | 2013-10-16 | 2021-02-23 | Fujifilm Corporation | sal de ácido carboxílico ou um sal de ácido mineral, cristal de succinato, cristal de fumarato e composição farmacêutica |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| EP3094629B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| JP6517319B2 (ja) | 2014-03-28 | 2019-05-22 | キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーＣａｌｉｔｏｒ Ｓｃｉｅｎｃｅｓ， Ｌｌｃ | 置換されたヘテロアリール化合物および使用方法 |
| RU2016141934A (ru) * | 2014-04-04 | 2018-05-07 | Сирос Фармасьютикалз, Инк. | Ингибиторы циклин-зависимой киназы 7 (cdk7) |
| CN107072995B (zh) | 2014-08-22 | 2020-02-21 | 富士胶片株式会社 | 用于处置flt3突变阳性癌的医药组合物、突变型flt3抑制剂以及这些的应用 |
| WO2016205304A1 (en) * | 2015-06-16 | 2016-12-22 | Signal Pharmaceuticals, Llc | Methods of treatment using substituted diaminopyrimidyl compounds |
| JP6878316B2 (ja) | 2015-06-19 | 2021-05-26 | ノバルティス アーゲー | Ｓｈｐ２の活性を阻害するための化合物および組成物 |
| ES2741746T3 (es) | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| US10287266B2 (en) | 2015-06-19 | 2019-05-14 | Novartis Ag | Compounds and compositions for inhibiting the activity of SHP2 |
| JP6412471B2 (ja) | 2015-07-15 | 2018-10-24 | 富士フイルム株式会社 | 含窒素複素環化合物の製造方法およびその中間体 |
| DE102017112612A1 (de) * | 2016-06-10 | 2017-12-14 | Hitachi High-Tech Science Corporation | Flüssigkeitschromatograph und Verfahren zum Korrigieren von Schwankungen eines Detektorausgabewerts des Flüssigkeitschromatographen |
| AU2017283769B2 (en) | 2016-06-14 | 2019-08-15 | Novartis Ag | Compounds and compositions for inhibiting the activity of SHP2 |
| KR101876514B1 (ko) * | 2016-11-08 | 2018-07-10 | 한국화학연구원 | 신규한 피리미딘화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암 및 염증질환의 예방 또는 치료용 약학적 조성물 |
| EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
| US10590136B2 (en) * | 2017-10-04 | 2020-03-17 | Celgene Corporation | Processes for the preparation of cis-4-[2-{[(3S,4R)-3-fluorooxan-4-yl]amino}-8-(2,4,6-trichloroanilino)-9H-purin-9-yl]-1-methylcyclohexane-1-carboxamide |
| BR112021022105A2 (pt) * | 2019-05-05 | 2021-12-28 | Qilu Regor Therapeutics Inc | Inibidores de cdk |
| EP3966206B1 (en) | 2019-05-10 | 2023-08-09 | Deciphera Pharmaceuticals, LLC | Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| EP3966207B1 (en) * | 2019-05-10 | 2023-11-01 | Deciphera Pharmaceuticals, LLC | Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| JP7626722B2 (ja) * | 2019-06-17 | 2025-02-04 | デシフェラ・ファーマシューティカルズ，エルエルシー | アミノピリミジンアミドオートファジー阻害剤およびその使用方法 |
| CN111187220B (zh) * | 2020-01-19 | 2022-08-02 | 郑州大学 | 含席夫碱结构单元的三氟甲基嘧啶类衍生物及其制备方法和用途 |
| CN111646978B (zh) * | 2020-06-11 | 2021-12-21 | 浙江大学 | N2-取代烷氧芳环-2-氨基嘧啶类衍生物及应用 |
| CN111732548B (zh) * | 2020-06-11 | 2022-06-17 | 浙江大学 | N2-氨甲酰芳环-2-氨基嘧啶类衍生物及其医药用途 |
| KR20230117416A (ko) * | 2021-01-18 | 2023-08-08 | 하이노바 파마슈티컬스 인코포레이티드 | 아미노피리미딘계 fak 억제제 화합물의 합성 방법 |
| WO2022214869A2 (en) * | 2021-04-07 | 2022-10-13 | Lifearc | Ulk1/2 inhibitors and their use thereof |
| WO2023122723A1 (en) | 2021-12-23 | 2023-06-29 | The Broad Institute, Inc. | Panels and methods for diagnosing and treating lung cancer |
| WO2024099225A1 (zh) * | 2022-11-08 | 2024-05-16 | 微境生物医药科技(上海)有限公司 | Ulk抑制剂 |
| WO2024243485A1 (en) * | 2023-05-25 | 2024-11-28 | Odyssey Therapeutics, Inc. | Cdk2 inhibitors and uses thereof |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2055900A (en) | 1935-03-11 | 1936-09-29 | Daisy Mfg Co | Toy gun |
| US2152960A (en) | 1935-05-28 | 1939-04-04 | Soc Of Chemical Ind | Process for the manufacture of cyclohexanols |
| US2723975A (en) | 1952-04-03 | 1955-11-15 | Nepera Chemical Co Inc | 2, 4-di-piperidino-5-benzylpyrimidine |
| DE1249282B (enExample) | 1960-11-01 | |||
| FR2358148A1 (fr) | 1976-07-12 | 1978-02-10 | Dick Pr | Derives de 2,4-diaminopyrimidines et leur mise en solution en association avec des sulfamides |
| DE2709634A1 (de) | 1977-03-05 | 1978-09-07 | Basf Ag | Benzylpyrimidine, verfahren zu ihrer herstellung und diese enthaltende arzneimittel |
| DE2730467A1 (de) | 1977-07-06 | 1979-01-18 | Basf Ag | Benzylpyrimidine, verfahren zu ihrer herstellung und diese enthaltende arzneimittel |
| DE2756370A1 (de) * | 1977-12-17 | 1979-06-21 | Noell Gmbh | Kombinierter greifer in einem kernreaktor |
| US4255568A (en) | 1979-04-18 | 1981-03-10 | American Home Products Corporation | 2H-Pyrimido[4,5-d][1,3]oxazine-2,4(1H)-dione derivatives |
| US4215216A (en) | 1979-04-18 | 1980-07-29 | American Home Products Corporation | 7,8-Dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]pyrimidine-6-carboxylic acid derivatives |
| US4301281A (en) | 1979-04-18 | 1981-11-17 | American Home Products Corporation | 7,8-Dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]-pyrimidine-6-carboxylic acid amides |
| US4245094A (en) | 1980-01-28 | 1981-01-13 | American Home Products Corporation | 5-Amino-2,8-dialkyl-7,8-dihydro-7-oxo-pyrido-[2,3-d]pyrimidine-6 carboxylic acid derivatives |
| FR2502152A1 (fr) | 1981-03-20 | 1982-09-24 | Panmedica Laboratoires | Nouveaux derives solubles n2 substitues de la diamino-2,4-benzyl-5-pyrimidines, leur procede de preparation et medicaments les contenant |
| JPS6253973A (ja) | 1985-09-02 | 1987-03-09 | Mitsui Toatsu Chem Inc | ハロゲノチオシアノピリミジン誘導体、その製造法および農園芸用殺菌剤 |
| HU206337B (en) | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
| JPH03127790A (ja) | 1989-10-11 | 1991-05-30 | Morishita Pharmaceut Co Ltd | Ｎ―（１ｈ―テトラゾール―５―イル）―２―アニリノ―５―ピリミジンカルボキシアミド類及びその合成中間体 |
| GB9012592D0 (en) | 1990-06-06 | 1990-07-25 | Smithkline Beecham Intercredit | Compounds |
| DE4029650A1 (de) | 1990-09-19 | 1992-03-26 | Hoechst Ag | 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide |
| US5491234A (en) | 1992-03-30 | 1996-02-13 | Pfizer Inc. | Pyrimidine derivatives for enhancing antitumor activity |
| GB9212673D0 (en) | 1992-06-15 | 1992-07-29 | Celltech Ltd | Chemical compounds |
| US5620981A (en) | 1995-05-03 | 1997-04-15 | Warner-Lambert Company | Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6498163B1 (en) | 1997-02-05 | 2002-12-24 | Warner-Lambert Company | Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation |
| US6440965B1 (en) | 1997-10-15 | 2002-08-27 | Krenitsky Pharmaceuticals, Inc. | Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system |
| JP2002503662A (ja) | 1998-02-17 | 2002-02-05 | テュラリク インコーポレイテッド | 抗ウイルス性ピリミジン誘導体 |
| ES2361146T3 (es) | 1998-03-27 | 2011-06-14 | Janssen Pharmaceutica Nv | Derivados de la piramidina inhibitatoria de vih. |
| AU751573C (en) * | 1998-03-27 | 2003-10-09 | Janssen Pharmaceutica N.V. | HIV inhibiting pyrimidine derivatives |
| US6632820B1 (en) | 1998-08-29 | 2003-10-14 | Astrazeneca Ab | Pyrimidine compounds |
| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| DE19851421A1 (de) * | 1998-11-07 | 2000-05-11 | Boehringer Ingelheim Pharma | Neue Pyrimidine, deren Herstellung und Verwendung |
| JP3635238B2 (ja) | 1998-11-10 | 2005-04-06 | 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 | Ｈｉｖの複製を阻害するピリミジン類 |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| GB9905075D0 (en) * | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| AU5636900A (en) * | 1999-06-30 | 2001-01-31 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| KR20020027649A (ko) | 1999-09-15 | 2002-04-13 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 카이나제 억제제로서의 프테리딘온 |
| ES2283315T3 (es) | 1999-09-16 | 2007-11-01 | Tanabe Seiyaku Co., Ltd. | Compuestos ciclicos de 6 miembros que contienen nitrogeno aromatico. |
| DE60025837T2 (de) | 1999-09-24 | 2006-11-02 | Janssen Pharmaceutica N.V. | Antivirale feste dispersionen |
| ATE314362T1 (de) | 1999-10-12 | 2006-01-15 | Takeda Pharmaceutical | Pyrimidin-5-carboximidverbindungen, verfahren zur herstellung derselben und deren verwendung |
| AU1407401A (en) | 1999-11-09 | 2001-06-06 | Jozsef Mandzsu | Method and apparatus for producing the male component of a separable fastener, the product produced in this manner and the system containing this product |
| CZ20022521A3 (cs) | 2000-01-27 | 2003-02-12 | Warner-Lambert Company | Pyridopyrimidinonové deriváty pro léčení neurodegenerativních onemocnění |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004886D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0007371D0 (en) | 2000-03-28 | 2000-05-17 | Astrazeneca Uk Ltd | Chemical compounds |
| US7273868B2 (en) | 2000-04-28 | 2007-09-25 | Tanabe Seiyaku Co., Ltd. | Pyrazine derivatives |
| KR100711042B1 (ko) | 2000-04-28 | 2007-04-24 | 다나베 세이야꾸 가부시키가이샤 | 환상 화합물 |
| US20080027037A1 (en) | 2000-04-28 | 2008-01-31 | Tanabe Seiyaku Co., Ltd. | Cyclic compounds |
| US7034019B2 (en) | 2000-05-08 | 2006-04-25 | Janssen Pharmaceutica N.V. | Prodrugs of HIV replication inhibiting pyrimidines |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| ES2556946T3 (es) | 2000-12-21 | 2016-01-21 | Novartis Ag | Pirimidinaminas como moduladores de la angiogénesis |
| EP1361879A1 (en) | 2001-02-20 | 2003-11-19 | Bristol-Myers Squibb Company | 2,4-disubstituted pyrimidine-5-carboxamide derivatives as kcnq potassium channel modulators |
| DE10212098A1 (de) | 2002-03-11 | 2003-10-23 | Schering Ag | CDK inhibitorische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| DE10127581A1 (de) | 2001-05-29 | 2003-01-02 | Schering Ag | CDK inhibitorische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| AU2002312933B2 (en) * | 2001-05-29 | 2007-12-06 | Schering Ag | CDK inhibiting pyrimidines, production thereof and their use as medicaments |
| JP3918048B2 (ja) | 2001-07-03 | 2007-05-23 | 独立行政法人産業技術総合研究所 | 低級アルケンの製造方法 |
| WO2003040141A1 (en) * | 2001-09-28 | 2003-05-15 | Bayer Pharmaceuticals Corporation | Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders |
| EP1453516A2 (de) * | 2001-10-17 | 2004-09-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren |
| DK1438053T3 (da) | 2001-10-17 | 2008-12-08 | Boehringer Ingelheim Pharma | Pyrimidinderivater, lægemiddel indeholdende disse forbindelser, deres anvendelse og fremgangsmåder til deres fremstilling |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| AU2003220968A1 (en) | 2002-03-28 | 2003-10-13 | Kyowa Hakko Kogyo Co., Ltd. | Anti-inflammatory agent |
| DE602004022633D1 (de) | 2003-01-30 | 2009-10-01 | Boehringer Ingelheim Pharma | 2,4-diaminopyrimidinderivate, die sich als inhibitoren von pkc-theta eignen |
-
2002
- 2002-10-14 DK DK02774710T patent/DK1438053T3/da active
- 2002-10-14 EP EP08163784A patent/EP2090571B1/de not_active Expired - Lifetime
- 2002-10-14 AT AT02774710T patent/ATE407678T1/de active
- 2002-10-14 JP JP2003535800A patent/JP4460292B2/ja not_active Expired - Lifetime
- 2002-10-14 WO PCT/EP2002/011453 patent/WO2003032997A1/de not_active Ceased
- 2002-10-14 DE DE50212771T patent/DE50212771D1/de not_active Expired - Lifetime
- 2002-10-14 PT PT02774710T patent/PT1438053E/pt unknown
- 2002-10-14 UY UY27487A patent/UY27487A1/es not_active Application Discontinuation
- 2002-10-14 EP EP02774710A patent/EP1438053B1/de not_active Expired - Lifetime
- 2002-10-14 EP EP10178604A patent/EP2332924A1/de not_active Withdrawn
- 2002-10-14 CA CA2463989A patent/CA2463989C/en not_active Expired - Lifetime
- 2002-10-14 ES ES02774710T patent/ES2314106T3/es not_active Expired - Lifetime
- 2002-10-16 US US10/271,763 patent/US7173028B2/en not_active Expired - Lifetime
-
2005
- 2005-12-21 US US11/313,380 patent/US7709480B2/en not_active Expired - Lifetime
-
2008
- 2008-12-02 CY CY20081101391T patent/CY1110442T1/el unknown
-
2010
- 2010-02-24 US US12/711,364 patent/US8420630B2/en not_active Expired - Fee Related
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