ZA200107252B - Pyrimidine compounds. - Google Patents

Pyrimidine compounds. Download PDF

Info

Publication number: ZA200107252B
Authority: ZA; South Africa
Prior art keywords: formula; alkyl; compound; alkoxy; acceptable salt
Prior art date: 1999-03-06

Application number

ZA200107252A

Other languages

English (en)

Inventor

Gloria Anne Breault

Stewart Russell James

Jane Elizabeth Pease

Original Assignee

Astrazeneca Ab

Priority date (The priority date 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 date listed.)

1999-03-06

Filing date

2001-08-31

Publication date

2002-12-02

2001-08-31 Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab

2002-12-02 Publication of ZA200107252B publication Critical patent/ZA200107252B/en

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150000003230 pyrimidines Chemical class 0.000 title claims abstract description 26
125000001424 substituent group Chemical group 0.000 claims abstract description 44
150000002148 esters Chemical class 0.000 claims abstract description 32
150000003839 salts Chemical class 0.000 claims abstract description 29
238000001727 in vivo Methods 0.000 claims abstract description 27
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 15
125000000623 heterocyclic group Chemical group 0.000 claims abstract description 14
125000005842 heteroatom Chemical group 0.000 claims abstract description 13
238000004519 manufacturing process Methods 0.000 claims abstract description 11
238000000034 method Methods 0.000 claims abstract description 8
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 4
-1 hydroxy, nitro, amino Chemical group 0.000 claims description 184
125000000217 alkyl group Chemical group 0.000 claims description 153
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 64
150000001875 compounds Chemical class 0.000 claims description 54
125000003545 alkoxy group Chemical group 0.000 claims description 50
229910052757 nitrogen Inorganic materials 0.000 claims description 41
SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 26
125000005843 halogen group Chemical group 0.000 claims description 23
229910052799 carbon Inorganic materials 0.000 claims description 22
229910052739 hydrogen Inorganic materials 0.000 claims description 19
229910052760 oxygen Inorganic materials 0.000 claims description 19
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 17
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 16
239000005864 Sulphur Chemical group 0.000 claims description 16
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 16
239000001301 oxygen Chemical group 0.000 claims description 16
150000001721 carbon Chemical group 0.000 claims description 15
YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 14
239000001257 hydrogen Substances 0.000 claims description 13
125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 12
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 11
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 10
125000003282 alkyl amino group Chemical group 0.000 claims description 10
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 10
125000003342 alkenyl group Chemical group 0.000 claims description 9
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 9
125000004093 cyano group Chemical group *C#N 0.000 claims description 9
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 9
241001465754 Metazoa Species 0.000 claims description 8
CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 claims description 8
HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 7
125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 7
125000004414 alkyl thio group Chemical group 0.000 claims description 7
125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 7
125000001246 bromo group Chemical group Br* 0.000 claims description 7
125000001589 carboacyl group Chemical group 0.000 claims description 7
125000001309 chloro group Chemical group Cl* 0.000 claims description 7
PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims description 7
RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims description 7
125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 6
125000000304 alkynyl group Chemical group 0.000 claims description 6
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 6
125000001072 heteroaryl group Chemical group 0.000 claims description 6
239000000203 mixture Substances 0.000 claims description 6
125000001624 naphthyl group Chemical group 0.000 claims description 6
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 5
CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 5
230000001093 anti-cancer Effects 0.000 claims description 5
125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 5
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
125000005236 alkanoylamino group Chemical group 0.000 claims description 4
125000001153 fluoro group Chemical group F* 0.000 claims description 4
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 3
125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 3
125000000753 cycloalkyl group Chemical group 0.000 claims description 3
125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 claims description 3
125000003302 alkenyloxy group Chemical group 0.000 claims description 2
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 2
125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
238000006243 chemical reaction Methods 0.000 claims 14
239000012038 nucleophile Substances 0.000 claims 6
239000000126 substance Substances 0.000 claims 5
DUYAAUVXQSMXQP-UHFFFAOYSA-N ethanethioic S-acid Chemical group CC(S)=O DUYAAUVXQSMXQP-UHFFFAOYSA-N 0.000 claims 2
125000004404 heteroalkyl group Chemical group 0.000 claims 2
125000006239 protecting group Chemical group 0.000 claims 2
229910052717 sulfur Inorganic materials 0.000 claims 2
BWNAFPYJZGFTOM-UHFFFAOYSA-N 1-(dimethylamino)-3-[4-[[4-(2,3-dimethyl-2,3-dihydroindol-1-yl)pyrimidin-2-yl]amino]phenoxy]propan-2-ol Chemical compound CC1C(C)C2=CC=CC=C2N1C(N=1)=CC=NC=1NC1=CC=C(OCC(O)CN(C)C)C=C1 BWNAFPYJZGFTOM-UHFFFAOYSA-N 0.000 claims 1
239000003085 diluting agent Substances 0.000 claims 1
238000002560 therapeutic procedure Methods 0.000 claims 1
239000002246 antineoplastic agent Substances 0.000 abstract description 2
125000004429 atom Chemical group 0.000 description 9
230000022131 cell cycle Effects 0.000 description 8
102000016621 Focal Adhesion Protein-Tyrosine Kinases Human genes 0.000 description 7
108010067715 Focal Adhesion Protein-Tyrosine Kinases Proteins 0.000 description 7
150000002431 hydrogen Chemical group 0.000 description 7
230000000694 effects Effects 0.000 description 6
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 6
206010028980 Neoplasm Diseases 0.000 description 5
125000000714 pyrimidinyl group Chemical group 0.000 description 5
BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 4
KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 4
102000016736 Cyclin Human genes 0.000 description 4
108050006400 Cyclin Proteins 0.000 description 4
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 4
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 4
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 4
125000002619 bicyclic group Chemical group 0.000 description 4
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 4
239000003112 inhibitor Substances 0.000 description 4
230000002401 inhibitory effect Effects 0.000 description 4
125000002950 monocyclic group Chemical group 0.000 description 4
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 4
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 3
108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 description 3
108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 description 3
102100036239 Cyclin-dependent kinase 2 Human genes 0.000 description 3
102100036252 Cyclin-dependent kinase 4 Human genes 0.000 description 3
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
210000004027 cell Anatomy 0.000 description 3
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 3
238000013508 migration Methods 0.000 description 3
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 3
125000004433 nitrogen atom Chemical group N* 0.000 description 3
230000035755 proliferation Effects 0.000 description 3
230000019491 signal transduction Effects 0.000 description 3
125000004607 1,2,3,4-tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 2
125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 description 2
VHMICKWLTGFITH-UHFFFAOYSA-N 2H-isoindole Chemical compound C1=CC=CC2=CNC=C21 VHMICKWLTGFITH-UHFFFAOYSA-N 0.000 description 2
108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 description 2
102100026804 Cyclin-dependent kinase 6 Human genes 0.000 description 2
ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 description 2
YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 2
BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 description 2
108700020796 Oncogene Proteins 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 2
DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 2
230000001640 apoptogenic effect Effects 0.000 description 2
IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 description 2
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
230000004663 cell proliferation Effects 0.000 description 2
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Natural products OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 2
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 2
RCCPEORTSYDPMB-UHFFFAOYSA-N hydroxy benzenecarboximidothioate Chemical compound OSC(=N)C1=CC=CC=C1 RCCPEORTSYDPMB-UHFFFAOYSA-N 0.000 description 2
125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 description 2
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 2
125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 2
125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 2
230000005012 migration Effects 0.000 description 2
229940002612 prodrug Drugs 0.000 description 2
239000000651 prodrug Substances 0.000 description 2
125000004742 propyloxycarbonyl group Chemical group 0.000 description 2
229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 description 2
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 description 2
BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 description 1
FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 description 1
ILROLYQPRYHHFG-UHFFFAOYSA-N 1-$l^{1}-oxidanylprop-2-en-1-one Chemical group [O]C(=O)C=C ILROLYQPRYHHFG-UHFFFAOYSA-N 0.000 description 1
GYMZRGMAWRJZPV-UHFFFAOYSA-N 1-(2,3-dihydro-1h-indol-5-yl)ethanone Chemical compound CC(=O)C1=CC=C2NCCC2=C1 GYMZRGMAWRJZPV-UHFFFAOYSA-N 0.000 description 1
LLAPDLPYIYKTGQ-UHFFFAOYSA-N 1-aminoethyl Chemical group C[CH]N LLAPDLPYIYKTGQ-UHFFFAOYSA-N 0.000 description 1
125000004173 1-benzimidazolyl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N1* 0.000 description 1
125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 description 1
JQCSUVJDBHJKNG-UHFFFAOYSA-N 1-methoxy-ethyl Chemical group C[CH]OC JQCSUVJDBHJKNG-UHFFFAOYSA-N 0.000 description 1
QLAXPBPKMZSIED-UHFFFAOYSA-N 1-piperazin-1-yl-3,4-dihydro-2h-quinoline Chemical compound C12=CC=CC=C2CCCN1N1CCNCC1 QLAXPBPKMZSIED-UHFFFAOYSA-N 0.000 description 1
125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 description 1
YHZODXGIMHTEJV-UHFFFAOYSA-N 1h-pyrrolo[1,2-a]imidazole Chemical compound N1C=CN2C=CC=C21 YHZODXGIMHTEJV-UHFFFAOYSA-N 0.000 description 1
NNPSOAOENINXMR-UHFFFAOYSA-N 2,3-dimethyl-2,3-dihydro-1h-indole Chemical compound C1=CC=C2C(C)C(C)NC2=C1 NNPSOAOENINXMR-UHFFFAOYSA-N 0.000 description 1
QRWRJDVVXAXGBT-UHFFFAOYSA-N 2-Methylindoline Chemical compound C1=CC=C2NC(C)CC2=C1 QRWRJDVVXAXGBT-UHFFFAOYSA-N 0.000 description 1
125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 description 1
125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 description 1
125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 description 1
125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 description 1
125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 description 1
125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 description 1
125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical compound C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 description 1
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229910052783 alkali metal Inorganic materials 0.000 description 1
229910052784 alkaline earth metal Inorganic materials 0.000 description 1
125000005115 alkyl carbamoyl group Chemical group 0.000 description 1
125000005907 alkyl ester group Chemical group 0.000 description 1
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125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 1
230000033228 biological regulation Effects 0.000 description 1
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125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
229910052791 calcium Inorganic materials 0.000 description 1
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230000006020 chronic inflammation Effects 0.000 description 1
125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 1
125000004122 cyclic group Chemical group 0.000 description 1
230000026374 cyclin catabolic process Effects 0.000 description 1
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
238000012217 deletion Methods 0.000 description 1
230000037430 deletion Effects 0.000 description 1
230000001419 dependent effect Effects 0.000 description 1
125000005117 dialkylcarbamoyl group Chemical group 0.000 description 1
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 description 1
125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 description 1
125000004914 dipropylamino group Chemical group C(CC)N(CCC)* 0.000 description 1
201000010099 disease Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000003814 drug Substances 0.000 description 1
125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 description 1
125000006534 ethyl amino methyl group Chemical group [H]N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 description 1
125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 1
230000000893 fibroproliferative effect Effects 0.000 description 1
125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
201000011066 hemangioma Diseases 0.000 description 1
125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
230000007062 hydrolysis Effects 0.000 description 1
238000006460 hydrolysis reaction Methods 0.000 description 1
125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
MBVAHHOKMIRXLP-UHFFFAOYSA-N imidazo[1,2-a]pyrazine Chemical compound C1=CN=CC2=NC=CN21 MBVAHHOKMIRXLP-UHFFFAOYSA-N 0.000 description 1
UTCSSFWDNNEEBH-UHFFFAOYSA-N imidazo[1,2-a]pyridine Chemical compound C1=CC=CC2=NC=CN21 UTCSSFWDNNEEBH-UHFFFAOYSA-N 0.000 description 1
INSWZAQOISIYDT-UHFFFAOYSA-N imidazo[1,2-a]pyrimidine Chemical compound C1=CC=NC2=NC=CN21 INSWZAQOISIYDT-UHFFFAOYSA-N 0.000 description 1
PQWQQQGKMHENOC-UHFFFAOYSA-N imidazo[1,2-c]pyrimidine Chemical compound C1=NC=CC2=NC=CN21 PQWQQQGKMHENOC-UHFFFAOYSA-N 0.000 description 1
MIFJMFOVENWQDP-UHFFFAOYSA-N imidazo[1,5-a]pyrazine Chemical compound C1=CN=CC2=CN=CN21 MIFJMFOVENWQDP-UHFFFAOYSA-N 0.000 description 1
JMANUKZDKDKBJP-UHFFFAOYSA-N imidazo[1,5-a]pyridine Chemical compound C1=CC=CC2=CN=CN21 JMANUKZDKDKBJP-UHFFFAOYSA-N 0.000 description 1
LXYHLTOJFGNEKG-UHFFFAOYSA-N imidazo[1,5-a]pyrimidine Chemical compound C1=CC=NC2=CN=CN21 LXYHLTOJFGNEKG-UHFFFAOYSA-N 0.000 description 1
MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 description 1
125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 description 1
230000005764 inhibitory process Effects 0.000 description 1
150000002485 inorganic esters Chemical class 0.000 description 1
230000003834 intracellular effect Effects 0.000 description 1
125000002346 iodo group Chemical group I* 0.000 description 1
125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
125000005956 isoquinolyl group Chemical group 0.000 description 1
CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 description 1
208000017169 kidney disease Diseases 0.000 description 1
208000032839 leukemia Diseases 0.000 description 1
159000000003 magnesium salts Chemical class 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
239000011976 maleic acid Substances 0.000 description 1
125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 description 1
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
230000002297 mitogenic effect Effects 0.000 description 1
125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 description 1
125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 1
230000007935 neutral effect Effects 0.000 description 1
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
230000003287 optical effect Effects 0.000 description 1
150000007524 organic acids Chemical class 0.000 description 1
150000007530 organic bases Chemical class 0.000 description 1
150000003014 phosphoric acid esters Chemical class 0.000 description 1
102000020233 phosphotransferase Human genes 0.000 description 1
125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
125000005633 phthalidyl group Chemical group 0.000 description 1
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 description 1
XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
TURAMGVWNUTQKH-UHFFFAOYSA-N propa-1,2-dien-1-one Chemical group C=C=C=O TURAMGVWNUTQKH-UHFFFAOYSA-N 0.000 description 1
125000006308 propyl amino group Chemical group 0.000 description 1
108060006633 protein kinase Proteins 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
102000004169 proteins and genes Human genes 0.000 description 1
125000003373 pyrazinyl group Chemical group 0.000 description 1
125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 description 1
USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 description 1
DNXIASIHZYFFRO-UHFFFAOYSA-N pyrazoline Chemical compound C1CN=NC1 DNXIASIHZYFFRO-UHFFFAOYSA-N 0.000 description 1
125000002098 pyridazinyl group Chemical group 0.000 description 1
125000004076 pyridyl group Chemical group 0.000 description 1
125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
125000005493 quinolyl group Chemical group 0.000 description 1
125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
150000003254 radicals Chemical class 0.000 description 1
210000001210 retinal vessel Anatomy 0.000 description 1
206010039073 rheumatoid arthritis Diseases 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
239000001117 sulphuric acid Substances 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
125000005505 thiomorpholino group Chemical group 0.000 description 1
229930192474 thiophene Natural products 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1
210000004881 tumor cell Anatomy 0.000 description 1
230000003827 upregulation Effects 0.000 description 1
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
229920002554 vinyl polymer Polymers 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
- C07D403/04—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
- 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
- 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

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)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

ZA200107252A 1999-03-06 2001-08-31 Pyrimidine compounds. ZA200107252B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB9905075.9A GB9905075D0 (en)	1999-03-06	1999-03-06	Chemical compounds

Publications (1)

Publication Number	Publication Date
ZA200107252B true ZA200107252B (en)	2002-12-02

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Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200107252A ZA200107252B (en)	1999-03-06	2001-08-31	Pyrimidine compounds.

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US (1)	US6716831B1 (da)
EP (1)	EP1161428B1 (da)
JP (1)	JP2002539120A (da)
KR (1)	KR100683512B1 (da)
CN (1)	CN1227249C (da)
AT (1)	ATE241617T1 (da)
AU (1)	AU754967B2 (da)
BR (1)	BR0008770A (da)
CA (1)	CA2366668A1 (da)
DE (1)	DE60003001T2 (da)
DK (1)	DK1161428T3 (da)
ES (1)	ES2200824T3 (da)
GB (1)	GB9905075D0 (da)
IL (2)	IL145192A0 (da)
MX (1)	MXPA01008960A (da)
NO (1)	NO320909B1 (da)
NZ (1)	NZ513893A (da)
PT (1)	PT1161428E (da)
WO (1)	WO2000053595A1 (da)
ZA (1)	ZA200107252B (da)

Families Citing this family (218)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6632820B1 (en)	1998-08-29	2003-10-14	Astrazeneca Ab	Pyrimidine compounds
ATE342892T1 (de)	1998-08-29	2006-11-15	Astrazeneca Ab	Pyrimidine verbindungen
GB9828511D0 (en)	1998-12-24	1999-02-17	Zeneca Ltd	Chemical compounds
GB9905075D0 (en)	1999-03-06	1999-04-28	Zeneca Ltd	Chemical compounds
GB9907658D0 (en)	1999-04-06	1999-05-26	Zeneca Ltd	Chemical compounds
WO2001000213A1 (en) *	1999-06-30	2001-01-04	Merck & Co., Inc.	Src kinase inhibitor compounds
GB9919778D0 (en)	1999-08-21	1999-10-27	Zeneca Ltd	Chemical compounds
MXPA02003436A (es)	1999-10-07	2002-08-20	Amgen Inc	Inhibidores de triazina cinasa.
US7101869B2 (en)	1999-11-30	2006-09-05	Pfizer Inc.	2,4-diaminopyrimidine compounds useful as immunosuppressants
MXPA02005350A (es) *	1999-11-30	2002-12-11	Pfizer Prod Inc	Compuestos de 2,4-diamino pirimidina utiles como supresores de inmunidad.
AU3704101A (en) *	2000-02-17	2001-08-27	Amgen Inc	Kinase inhibitors
GB0004890D0 (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
GB0004886D0 (en)	2000-03-01	2000-04-19	Astrazeneca Uk Ltd	Chemical compounds
GB0004887D0 (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
GB0016877D0 (en)	2000-07-11	2000-08-30	Astrazeneca Ab	Chemical compounds
GB0021726D0 (en)	2000-09-05	2000-10-18	Astrazeneca Ab	Chemical compounds
US6989385B2 (en) *	2000-12-21	2006-01-24	Vertex Pharmaceuticals Incorporated	Pyrazole compounds useful as protein kinase inhibitors
BR0116452A (pt)	2000-12-21	2003-09-30	Glaxo Group Ltd	Composto, composição farmacêutica, uso de um composto
BR0209774A (pt) *	2001-05-29	2004-06-01	Schering Ag	Pirimidinas inibidoras de cdk, sua preparação e aplicação como medicamento
DE10212098A1 (de) *	2002-03-11	2003-10-23	Schering Ag	CDK inhibitorische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
GB0113041D0 (en)	2001-05-30	2001-07-18	Astrazeneca Ab	Chemical compounds
US7115617B2 (en)	2001-08-22	2006-10-03	Amgen Inc.	Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en)	2001-08-22	2005-09-06	Amgen Inc.	Substituted pyrimidinyl derivatives and methods of use
ATE407678T1 (de)	2001-10-17	2008-09-15	Boehringer Ingelheim Pharma	Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
WO2003032994A2 (de)	2001-10-17	2003-04-24	Boehringer Ingelheim Pharma Gmbh & Co. Kg	5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
WO2003047516A2 (en) *	2001-11-30	2003-06-12	Synta Pharmaceuticals Corporation	Pyrimidine compounds
GB0205693D0 (en)	2002-03-09	2002-04-24	Astrazeneca Ab	Chemical compounds
GB0205690D0 (en)	2002-03-09	2002-04-24	Astrazeneca Ab	Chemical compounds
GB0205688D0 (en) *	2002-03-09	2002-04-24	Astrazeneca Ab	Chemical compounds
US7442697B2 (en)	2002-03-09	2008-10-28	Astrazeneca Ab	4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity
GB0311274D0 (en) *	2003-05-16	2003-06-18	Astrazeneca Ab	Chemical compounds
GB0311276D0 (en)	2003-05-16	2003-06-18	Astrazeneca Ab	Chemical compounds
DE10349423A1 (de)	2003-10-16	2005-06-16	Schering Ag	Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
TW200528101A (en)	2004-02-03	2005-09-01	Astrazeneca Ab	Chemical compounds
EP1598343A1 (de) *	2004-05-19	2005-11-23	Boehringer Ingelheim International GmbH	2-Arylaminopyrimidine als PLK Inhibitoren
MX2007007272A (es) *	2004-12-17	2007-07-11	Astrazeneca Ab	4-(4-imidazol-4-il)pirimidin-2-ilamino)benzamidas como inhibidores de cdk.
US7563781B2 (en) *	2005-01-14	2009-07-21	Janssen Pharmaceutica Nv	Triazolopyrimidine derivatives
SI1853588T1 (sl)	2005-02-16	2008-10-31	Astrazeneca Ab	Kemične spojine
PL1879573T3 (pl)	2005-05-10	2013-05-31	Incyte Holdings Corp	Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
US20080287437A1 (en)	2005-05-16	2008-11-20	Astrazeneca Ab	Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
US8193206B2 (en)	2005-06-14	2012-06-05	Taigen Biotechnology Co., Ltd.	Pyrimidine compounds
NZ564222A (en) *	2005-06-14	2011-10-28	Taigen Biotechnology Co Ltd	Pyrimidine compounds
JP4278172B2 (ja) *	2005-07-30	2009-06-10	アストラゼネカアクチボラグ	増殖性疾患の治療において使用するためのイミダゾリル−ピリミジン化合物
CA2621261C (en)	2005-09-22	2014-05-20	Incyte Corporation	Azepine inhibitors of janus kinases
AR056556A1 (es) *	2005-09-30	2007-10-10	Astrazeneca Ab	Imidazo(1,2-a)piridina con actividad antiproliferacion celular
JP2009513615A (ja)	2005-10-28	2009-04-02	アストラゼネカアクチボラグ	癌の治療においてチロシンキナーゼ阻害剤として使用するための４−（３−アミノピラゾール）ピリミジン誘導体
SG10202003901UA (en)	2005-12-13	2020-05-28	Incyte Holdings Corp	Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
CN101563336A (zh) *	2006-03-16	2009-10-21	诺瓦提斯公司	用于治疗特别是黑素瘤的杂环有机化合物
TW200811169A (en) *	2006-05-26	2008-03-01	Astrazeneca Ab	Chemical compounds
CA2654670A1 (en) *	2006-07-06	2008-01-10	Boehringer Ingelheim International Gmbh	New compounds
CA2673038C (en)	2006-12-22	2015-12-15	Incyte Corporation	Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
UA99459C2 (en)	2007-05-04	2012-08-27	Астразенека Аб	9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
CL2008001709A1 (es)	2007-06-13	2008-11-03	Incyte Corp	Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20150036210A (ko)	2007-06-13	2015-04-07	인사이트 코포레이션	야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
US7989465B2 (en)	2007-10-19	2011-08-02	Avila Therapeutics, Inc.	4,6-disubstituted pyrimidines useful as kinase inhibitors
TWI552752B (zh)	2007-10-19	2016-10-11	賽基艾維洛米斯研究股份有限公司	雜芳基化合物及其用途
UA104849C2 (uk)	2007-11-16	2014-03-25	Інсайт Корпорейшн	4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
HUE029767T2 (en)	2008-03-11	2017-04-28	Incyte Holdings Corp	JAK inhibitor azetidine and cyclobutane derivatives
US8063058B2 (en)	2008-04-16	2011-11-22	Portola Pharmaceuticals, Inc.	Inhibitors of syk and JAK protein kinases
US8138339B2 (en)	2008-04-16	2012-03-20	Portola Pharmaceuticals, Inc.	Inhibitors of protein kinases
DK2268635T3 (da)	2008-04-21	2015-09-14	Taigen Biotechnology Co Ltd	Heterocykliske forbindelser
AU2009238590A1 (en) *	2008-04-22	2009-10-29	Portola Pharmaceuticals, Inc.	Inhibitors of protein kinases
EP2274288A2 (en)	2008-04-24	2011-01-19	Incyte Corporation	Macrocyclic compounds and their use as kinase inhibitors
JP5465720B2 (ja)	2008-07-08	2014-04-09	インサイト・コーポレイション	インドールアミン２，３−ジオキシゲナーゼの阻害剤としての１，２，５−オキサジアゾール
CL2009001884A1 (es)	2008-10-02	2010-05-14	Incyte Holdings Corp	Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
WO2010085246A1 (en) *	2009-01-21	2010-07-29	Praecis Pharmaceuticals Inc	2,4-diamino-1,3,5-triazine and 4, 6-diamino-pyrimidine derivatives and their use as aggrecanase inhibitors
WO2010085597A1 (en)	2009-01-23	2010-07-29	Incyte Corporation	Macrocyclic compounds and their use as kinase inhibitors
AR076794A1 (es)	2009-05-22	2011-07-06	Incyte Corp	Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl)	2009-05-22	2019-11-29	Incyte Holdings Corp	3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
KR101763656B1 (ko)	2009-06-29	2017-08-01	인사이트 홀딩스 코포레이션	Ｐｉ3ｋ 저해물질로서의 피리미디논
TW201113285A (en)	2009-09-01	2011-04-16	Incyte Corp	Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru)	2009-10-09	2015-06-30	Инсайт Корпорейшн	ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
US8759359B2 (en)	2009-12-18	2014-06-24	Incyte Corporation	Substituted heteroaryl fused derivatives as PI3K inhibitors
TW201130842A (en)	2009-12-18	2011-09-16	Incyte Corp	Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
JP5858434B2 (ja)	2010-02-18	2016-02-10	インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅＨｏｌｄｉｎｇｓＣｏｒｐｏｒａｔｉｏｎ	Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
EP3354652B1 (en)	2010-03-10	2020-05-06	Incyte Holdings Corporation	Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP2558463A1 (en)	2010-04-14	2013-02-20	Incyte Corporation	Fused derivatives as i3 inhibitors
PE20130216A1 (es)	2010-05-21	2013-02-27	Incyte Corp	Formulacion topica para un inhibidor de jak
WO2011163195A1 (en)	2010-06-21	2011-12-29	Incyte Corporation	Fused pyrrole derivatives as pi3k inhibitors
PE20140146A1 (es)	2010-11-19	2014-02-06	Incyte Corp	Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US9034884B2 (en)	2010-11-19	2015-05-19	Incyte Corporation	Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
EP3660016A1 (en)	2010-12-20	2020-06-03	Incyte Holdings Corporation	N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US20130324532A1 (en)	2011-02-17	2013-12-05	Cancer Therapeutics Crc Pty Limited	Fak inhibitors
US9174946B2 (en)	2011-02-17	2015-11-03	Cancer Therapeutics Crc Pty Ltd	Selective FAK inhibitors
ES2547916T3 (es)	2011-02-18	2015-10-09	Novartis Pharma Ag	Terapia de combinación de inhibidores de mTOR/JAK
US9108984B2 (en)	2011-03-14	2015-08-18	Incyte Corporation	Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en)	2011-03-25	2012-10-04	Incyte Corporation	Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
CN103797010B (zh)	2011-06-20	2016-02-24	因塞特控股公司	作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
EP2741747A1 (en)	2011-08-10	2014-06-18	Novartis Pharma AG	JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh)	2011-08-18	2013-04-01	Incyte Corp	作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
PT3513793T (pt)	2011-09-02	2021-05-10	Incyte Holdings Corp	Heterociclilaminas como inibidores de pi3k
UA111854C2 (uk)	2011-09-07	2016-06-24	Інсайт Холдінгс Корпорейшн	Способи і проміжні сполуки для отримання інгібіторів jak
MX363551B (es)	2011-11-23	2019-03-27	Portola Pharmaceuticals Inc Star	Compuestos derivados de pirazina como inhibidores de cinasa.
WO2013146963A1 (ja) *	2012-03-28	2013-10-03	武田薬品工業株式会社	複素環化合物
AR090548A1 (es)	2012-04-02	2014-11-19	Incyte Corp	Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TW201406761A (zh)	2012-05-18	2014-02-16	Incyte Corp	做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
RS58514B1 (sr)	2012-06-13	2019-04-30	Incyte Holdings Corp	Supstituisana triciklična jedinjenja kao inhibitori fgfr
TWI646099B (zh)	2012-11-01	2019-01-01	英塞特控股公司	作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
PH12020551186B1 (en)	2012-11-15	2024-03-20	Incyte Holdings Corp	Sustained-release dosage forms of ruxolitinib
NZ746607A (en) *	2012-11-21	2019-11-29	Ptc Therapeutics Inc	Substituted reverse pyrimidine bmi-1 inhibitors
TWI687220B (zh)	2013-03-01	2020-03-11	美商英塞特控股公司	吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
RS62867B1 (sr)	2013-03-06	2022-02-28	Incyte Holdings Corp	Postupci i intermedijeri za dobijanje inhibitora jak
PH12015502383B1 (en)	2013-04-19	2023-02-03	Incyte Holdings Corp	Bicyclic heterocycles as fgfr inhibitors
HUE033587T2 (hu)	2013-05-17	2017-12-28	Incyte Corp	Bipirazol-származékok mint JAK inhibitorok
SMT202000315T1 (it)	2013-08-07	2020-07-08	Incyte Corp	Forme di dosaggio a rilascio prolungato per un inibitore di jak1
CA2921568A1 (en)	2013-08-20	2015-02-25	Incyte Corporation	Survival benefit in patients with solid tumors with elevated c-reactive protein levels
KR20160136323A (ko)	2014-02-28	2016-11-29	인사이트 코포레이션	골수형성이상증후군 치료용 jak1 억제제
SI3129021T1 (sl)	2014-04-08	2021-07-30	Incyte Corporation	Zdravljenje malignosti B-celic s kombinacijo zaviralcev JAK in PI3K
MA39987A (fr)	2014-04-30	2017-03-08	Incyte Corp	Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
US9498467B2 (en)	2014-05-30	2016-11-22	Incyte Corporation	Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2015191677A1 (en)	2014-06-11	2015-12-17	Incyte Corporation	Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016130501A1 (en)	2015-02-09	2016-08-18	Incyte Corporation	Aza-heteroaryl compounds as pi3k-gamma inhibitors
TWI712601B (zh)	2015-02-20	2020-12-11	美商英塞特公司	作為fgfr抑制劑之雙環雜環
MA41551A (fr)	2015-02-20	2017-12-26	Incyte Corp	Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG10201907576SA (en)	2015-02-27	2019-09-27	Incyte Corp	Salts of pi3k inhibitor and processes for their preparation
US9732097B2 (en)	2015-05-11	2017-08-15	Incyte Corporation	Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US20160362424A1 (en)	2015-05-11	2016-12-15	Incyte Corporation	Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
US9988401B2 (en)	2015-05-11	2018-06-05	Incyte Corporation	Crystalline forms of a PI3K inhibitor
PT3371190T (pt)	2015-11-06	2022-07-08	Incyte Corp	Compostos heterocíclicos como inibidores de pi3k-gamma
US20170190689A1 (en)	2016-01-05	2017-07-06	Incyte Corporation	Pyridine and pyridimine compounds as pi3k-gamma inhibitors
TWI726968B (zh)	2016-01-07	2021-05-11	開曼群島商Ｃｓ醫藥技術公司	Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
WO2017119732A1 (en)	2016-01-08	2017-07-13	Samsung Electronics Co., Ltd.	Electronic device and operating method thereof
US11753626B2 (en)	2016-03-09	2023-09-12	Beijing Percans Oncology Co., Ltd.	Tumor cell suspension cultures and related methods
US10138248B2 (en)	2016-06-24	2018-11-27	Incyte Corporation	Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
AR111960A1 (es)	2017-05-26	2019-09-04	Incyte Corp	Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR102717072B1 (ko)	2017-10-18	2024-10-15	인사이트 코포레이션	Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
CN107987054B (zh) *	2017-11-28	2020-05-19	四川大学	一种cdk2抑制剂
WO2019113487A1 (en)	2017-12-08	2019-06-13	Incyte Corporation	Low dose combination therapy for treatment of myeloproliferative neoplasms
US11306079B2 (en)	2017-12-21	2022-04-19	Incyte Corporation	3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
SG11202007164UA (en)	2018-01-30	2020-08-28	Incyte Corp	Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR102925957B1 (ko)	2018-02-16	2026-02-11	인사이트 코포레이션	사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
TWI877770B (zh)	2018-02-27	2025-03-21	美商英塞特公司	作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶
BR112020018094A2 (pt)	2018-03-08	2020-12-22	Incyte Corporation	Compostos de aminopirazina diol como inibidores de pi3k-¿
SMT202400306T1 (it)	2018-03-30	2024-09-16	Incyte Corp	Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
US11220510B2 (en)	2018-04-09	2022-01-11	Incyte Corporation	Pyrrole tricyclic compounds as A2A / A2B inhibitors
AU2019262579B2 (en)	2018-05-04	2024-09-12	Incyte Corporation	Salts of an FGFR inhibitor
HRP20241288T1 (hr)	2018-05-04	2024-12-06	Incyte Corporation	Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
EP3810610A1 (en)	2018-05-18	2021-04-28	Incyte Corporation	Fused pyrimidine derivatives as a2a / a2b inhibitors
JP7570235B2 (ja)	2018-05-25	2024-10-21	インサイト・コーポレイション	Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物
SG11202011680YA (en)	2018-06-01	2020-12-30	Incyte Corp	Dosing regimen for the treatment of pi3k related disorders
US11046658B2 (en)	2018-07-02	2021-06-29	Incyte Corporation	Aminopyrazine derivatives as PI3K-γ inhibitors
WO2020010197A1 (en)	2018-07-05	2020-01-09	Incyte Corporation	Fused pyrazine derivatives as a2a / a2b inhibitors
US11008344B2 (en)	2018-07-31	2021-05-18	Incyte Corporation	Tricyclic heteroaryl compounds as STING activators
WO2020028566A1 (en)	2018-07-31	2020-02-06	Incyte Corporation	Heteroaryl amide compounds as sting activators
CR20250050A (es)	2018-09-05	2025-03-19	Incyte Corp	Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en)	2018-10-11	2021-07-20	Incyte Corporation	Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020102216A1 (en)	2018-11-13	2020-05-22	Incyte Corporation	Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102150A1 (en)	2018-11-13	2020-05-22	Incyte Corporation	Heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en)	2018-11-13	2020-05-22	Incyte Corporation	Heterocyclic derivatives as pi3k inhibitors
US11596692B1 (en)	2018-11-21	2023-03-07	Incyte Corporation	PD-L1/STING conjugates and methods of use
WO2020146237A1 (en)	2019-01-07	2020-07-16	Incyte Corporation	Heteroaryl amide compounds as sting activators
TWI829857B (zh)	2019-01-29	2024-01-21	美商英塞特公司	作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
PH12021551976A1 (en)	2019-02-15	2022-07-04	Incyte Corp	Cyclin-dependent kinase 2 biomarkers and uses thereof
US11384083B2 (en)	2019-02-15	2022-07-12	Incyte Corporation	Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh)	2019-03-05	2021-01-01	美商英塞特公司	作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
US11628162B2 (en)	2019-03-08	2023-04-18	Incyte Corporation	Methods of treating cancer with an FGFR inhibitor
WO2020205560A1 (en)	2019-03-29	2020-10-08	Incyte Corporation	Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en)	2019-05-01	2020-11-05	Incyte Corporation	N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en)	2019-05-01	2022-09-20	Incyte Corporation	Tricyclic amine compounds as CDK2 inhibitors
JP7532511B2 (ja)	2019-06-10	2024-08-13	インサイト・コーポレイション	Ｊａｋ阻害剤による尋常性白斑の局所治療
US11591329B2 (en)	2019-07-09	2023-02-28	Incyte Corporation	Bicyclic heterocycles as FGFR inhibitors
KR20220044527A (ko)	2019-08-01	2022-04-08	인사이트 코포레이션	Ido 억제제의 투여 요법
CA3150681A1 (en)	2019-08-14	2021-02-18	Incyte Corporation	Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
PE20230372A1 (es)	2019-08-26	2023-03-06	Incyte Corp	Triazolopirimidinas como inhibidores de a2a/a2b
WO2021067374A1 (en)	2019-10-01	2021-04-08	Incyte Corporation	Bicyclic heterocycles as fgfr inhibitors
US11851426B2 (en)	2019-10-11	2023-12-26	Incyte Corporation	Bicyclic amines as CDK2 inhibitors
CA3157361A1 (en)	2019-10-14	2021-04-22	Incyte Corporation	Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en)	2019-10-16	2021-04-22	Incyte Corporation	Bicyclic heterocycles as fgfr inhibitors
JP7518900B2 (ja)	2019-10-16	2024-07-18	インサイト・コーポレイション	皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用
US11992490B2 (en)	2019-10-16	2024-05-28	Incyte Corporation	Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
CA3163875A1 (en)	2019-12-04	2021-06-10	Incyte Corporation	Tricyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja)	2019-12-04	2026-03-18	インサイト・コーポレイション	Ｆｇｆｒ阻害剤の誘導体
US12012409B2 (en)	2020-01-15	2024-06-18	Incyte Corporation	Bicyclic heterocycles as FGFR inhibitors
WO2021178779A1 (en)	2020-03-06	2021-09-10	Incyte Corporation	Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
AU2021254794A1 (en)	2020-04-16	2022-12-15	Incyte Corporation	Fused tricyclic KRAS inhibitors
US11739102B2 (en)	2020-05-13	2023-08-29	Incyte Corporation	Fused pyrimidine compounds as KRAS inhibitors
MX2022015221A (es)	2020-06-02	2023-03-08	Incyte Corp	Procesos para preparar un inhibidor de cinasa jano 1 (jak1).
US11833155B2 (en)	2020-06-03	2023-12-05	Incyte Corporation	Combination therapy for treatment of myeloproliferative neoplasms
US11999752B2 (en)	2020-08-28	2024-06-04	Incyte Corporation	Vinyl imidazole compounds as inhibitors of KRAS
WO2022061351A1 (en)	2020-09-16	2022-03-24	Incyte Corporation	Topical treatment of vitiligo
US11767320B2 (en)	2020-10-02	2023-09-26	Incyte Corporation	Bicyclic dione compounds as inhibitors of KRAS
CN112390760B (zh) *	2020-10-15	2022-07-29	北京师范大学	靶向fak的化合物及其制备方法和应用
CA3204374A1 (en)	2020-12-08	2022-06-16	Incyte Corporation	Jak1 pathway inhibitors for the treatment of vitiligo
WO2022155941A1 (en)	2021-01-25	2022-07-28	Qilu Regor Therapeutics Inc.	Cdk2 inhibitors
WO2022206888A1 (en)	2021-03-31	2022-10-06	Qilu Regor Therapeutics Inc.	Cdk2 inhibitors and use thereof
WO2022221170A1 (en)	2021-04-12	2022-10-20	Incyte Corporation	Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
UA129643C2 (uk)	2021-05-03	2025-06-18	Інсайт Корпорейшн	Інгібітори шляху jak1 для лікування вузлуватого свербця
US11939331B2 (en)	2021-06-09	2024-03-26	Incyte Corporation	Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en)	2021-06-09	2022-12-15	Incyte Corporation	Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en)	2021-06-21	2024-05-14	Incyte Corporation	Bicyclic pyrazolyl amines as CDK2 inhibitors
MX2024000357A (es)	2021-07-07	2024-02-12	Incyte Corp	Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras).
WO2023287896A1 (en)	2021-07-14	2023-01-19	Incyte Corporation	Tricyclic compounds as inhibitors of kras
US12441742B2 (en)	2021-08-31	2025-10-14	Incyte Corporation	Naphthyridine compounds as inhibitors of KRAS
WO2023049697A1 (en)	2021-09-21	2023-03-30	Incyte Corporation	Hetero-tricyclic compounds as inhibitors of kras
CA3234375A1 (en)	2021-10-01	2023-04-06	Incyte Corporation	Pyrazoloquinoline kras inhibitors
CA3235146A1 (en)	2021-10-14	2023-04-20	Incyte Corporation	Quinoline compounds as inhibitors of kras
MX2024006113A (es)	2021-11-22	2024-07-29	Incyte Corp	Terapia de combinación que comprende un inhibidor del receptor del factor de crecimiento de fibroblastos (fgfr) y un inhibidor del sarcoma de rata de kirsten (kras).
WO2023102184A1 (en)	2021-12-03	2023-06-08	Incyte Corporation	Bicyclic amine compounds as cdk12 inhibitors
US11976073B2 (en)	2021-12-10	2024-05-07	Incyte Corporation	Bicyclic amines as CDK2 inhibitors
US12084453B2 (en)	2021-12-10	2024-09-10	Incyte Corporation	Bicyclic amines as CDK12 inhibitors
EP4452982A1 (en)	2021-12-22	2024-10-30	Incyte Corporation	Salts and solid forms of an fgfr inhibitor and processes of preparing thereof
WO2023116884A1 (en)	2021-12-24	2023-06-29	Qilu Regor Therapeutics Inc.	Cdk2 inhibitors and use thereof
WO2023168686A1 (en)	2022-03-11	2023-09-14	Qilu Regor Therapeutics Inc.	Substituted cyclopentanes as cdk2 inhibitors
JP2025512710A (ja)	2022-03-07	2025-04-22	インサイト・コーポレイション	Ｃｄｋ２阻害剤の固体形態、塩、ならびに調製プロセス
AU2023293093A1 (en)	2022-06-14	2025-01-02	Incyte Corporation	Solid forms of a jak inhibitor and process of preparing the same
AR129675A1 (es)	2022-06-22	2024-09-18	Incyte Corp	Inhibidores de cdk12 de aminas biciclicas
US20240101557A1 (en)	2022-07-11	2024-03-28	Incyte Corporation	Fused tricyclic compounds as inhibitors of kras g12v mutants
JP2025527297A (ja)	2022-08-05	2025-08-20	インサイト・コーポレイション	Ｊａｋ阻害剤を使用した蕁麻疹の処置
US20240390340A1 (en)	2023-04-18	2024-11-28	Incyte Corporation	Pyrrolidine kras inhibitors
CR20250500A (es)	2023-04-18	2026-01-12	Incyte Corp	Inhibidores de kras de 2-azabiciclo [2.2.1] heptano
WO2024254245A1 (en)	2023-06-09	2024-12-12	Incyte Corporation	Bicyclic amines as cdk2 inhibitors
WO2025096738A1 (en)	2023-11-01	2025-05-08	Incyte Corporation	Kras inhibitors
US20250195536A1 (en)	2023-12-13	2025-06-19	Incyte Corporation	Bicyclooctane kras inhibitors
US20260053743A1 (en)	2024-08-26	2026-02-26	Incyte Corporation	Topical skin formulations of a pharmaceutically acceptable salt of ruxolitinib
US20260069605A1 (en)	2024-09-11	2026-03-12	Incyte Corporation	Kras inhibitors
US20260098044A1 (en)	2024-10-04	2026-04-09	Incyte Corporation	Tricyclic heteroaryl compounds as inhibitors of tyk2 and/or jak1

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4946956A (en)	1988-09-21	1990-08-07	Uniroyal Chemical Company, Inc.	Arylenediamine substituted pyrimidines
HU206337B (en)	1988-12-29	1992-10-28	Mitsui Petrochemical Ind	Process for producing pyrimidine derivatives and pharmaceutical compositions
US4983608A (en)	1989-09-05	1991-01-08	Hoechst-Roussell Pharmaceuticals, Inc.	N-substituted-4-pyrimidinamines and pyrimidinediamines
GB9012592D0 (en)	1990-06-06	1990-07-25	Smithkline Beecham Intercredit	Compounds
SG64322A1 (en)	1991-05-10	1999-04-27	Rhone Poulenc Rorer Int	Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5516775A (en)	1992-08-31	1996-05-14	Ciba-Geigy Corporation	Further use of pyrimidine derivatives
KR100262254B1 (ko)	1992-10-05	2000-07-15	나카히로 마오미	피리미딘 화합물
WO1995009851A1 (en)	1993-10-01	1995-04-13	Ciba-Geigy Ag	Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
US5543520A (en)	1993-10-01	1996-08-06	Ciba-Geigy Corporation	Pyrimidine derivatives
WO1995009847A1 (en)	1993-10-01	1995-04-13	Ciba-Geigy Ag	Pyrimidineamine derivatives and processes for the preparation thereof
PT672041E (pt)	1993-10-01	2002-04-29	Novartis Ag	Derivados da piridina farmacologicamente activos e processos para a sua preparacao
GB9325217D0 (en)	1993-12-09	1994-02-09	Zeneca Ltd	Pyrimidine derivatives
JP2896532B2 (ja)	1994-08-13	1999-05-31	ユーハンコーポレーション	新規なピリミジン誘導体およびその製造方法
DE69630214T2 (de)	1995-03-10	2004-07-15	Berlex Laboratories, Inc., Richmond	Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
IL118544A (en)	1995-06-07	2001-08-08	Smithkline Beecham Corp	History of imidazole, the process for their preparation and the pharmaceutical preparations containing them
US5739143A (en)	1995-06-07	1998-04-14	Smithkline Beecham Corporation	Imidazole compounds and compositions
GB9523675D0 (en)	1995-11-20	1996-01-24	Celltech Therapeutics Ltd	Chemical compounds
EP0889888A4 (en)	1996-03-25	2003-01-08	Smithkline Beecham Corp	NEW TREATMENT OF LESIONS IN THE CENTRAL NERVOUS SYSTEM
ES2239357T3 (es)	1996-06-10	2005-09-16	MERCK & CO., INC.	Imidazoles sustituidos que tienen actividad inhibidora de citoquinas.
GB9619284D0 (en)	1996-09-16	1996-10-30	Celltech Therapeutics Ltd	Chemical compounds
AU5147598A (en)	1996-10-17	1998-05-11	Smithkline Beecham Corporation	Methods for reversibly inhibiting myelopoiesis in mammalian tissue
GB9622363D0 (en)	1996-10-28	1997-01-08	Celltech Therapeutics Ltd	Chemical compounds
ZA9711092B (en)	1996-12-11	1999-07-22	Smithkline Beecham Corp	Novel compounds.
WO1998033798A2 (en)	1997-02-05	1998-08-06	Warner Lambert Company	Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
DE19710435A1 (de)	1997-03-13	1998-09-17	Hoechst Ag	Verwendung von Pyrimidinderivaten zur Prävention von Krebs allein oder in Kombination mit anderen therapeutischen Maßnahmen
GB9705361D0 (en)	1997-03-14	1997-04-30	Celltech Therapeutics Ltd	Chemical compounds
JP2002501532A (ja)	1997-05-30	2002-01-15	メルクエンドカンパニーインコーポレーテッド	新規血管形成阻害薬
DE69835518T2 (de)	1997-06-12	2007-08-09	Aventis Pharma Ltd., West Malling	Imidazolyl-cyclische acetale
TW517055B (en)	1997-07-02	2003-01-11	Smithkline Beecham Corp	Novel substituted imidazole compounds
EP1021173A1 (en)	1997-10-10	2000-07-26	Imperial College Innovations Limited	Use of csaid?tm compounds for the management of uterine contractions
EP1054004B1 (en)	1997-12-15	2008-07-16	Astellas Pharma Inc.	Novel pyrimidine-5-carboxamide derivatives
AU1924699A (en)	1997-12-19	1999-07-12	Smithkline Beecham Corporation	Compounds of heteroaryl substituted imidazole, their pharmaceutical compositionsand uses
EA002973B1 (ru)	1998-03-27	2002-12-26	Янссен Фармацевтика Н.В.	Производные пиримидина в качестве ингибиторов репликации вируса иммунодефицита человека
ATE342892T1 (de)	1998-08-29	2006-11-15	Astrazeneca Ab	Pyrimidine verbindungen
US6632820B1 (en)	1998-08-29	2003-10-14	Astrazeneca Ab	Pyrimidine compounds
ES2253930T3 (es)	1998-09-18	2006-06-01	ABBOTT GMBH & CO. KG	4-aminopirrolopirimidinas como inhibidores de quinasa.
ID29028A (id)	1998-09-18	2001-07-26	Basf Ag	Pirolopirimidina sebagai penghambat protein kinase
WO2000025780A1 (en)	1998-10-29	2000-05-11	Bristol-Myers Squibb Company	Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
AU6476599A (en)	1998-11-03	2000-05-22	Novartis Ag	Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles
HK1044334A1 (zh)	1999-02-01	2002-10-18	Cv治疗公司	依赖细胞周期蛋白的激酶2和IκB-α的嘌呤抑制剂
GB9903762D0 (en)	1999-02-18	1999-04-14	Novartis Ag	Organic compounds
GB9905075D0 (en)	1999-03-06	1999-04-28	Zeneca Ltd	Chemical compounds
US6627633B2 (en)	1999-03-17	2003-09-30	Albany Molecular Research, Inc.	6-substituted biaryl purine derivatives as potent cyclin/CDK inhibitors and antiproliferative agents
GB9907658D0 (en)	1999-04-06	1999-05-26	Zeneca Ltd	Chemical compounds
GB9914258D0 (en)	1999-06-18	1999-08-18	Celltech Therapeutics Ltd	Chemical compounds
GB9919778D0 (en)	1999-08-21	1999-10-27	Zeneca Ltd	Chemical compounds
GB9924862D0 (en)	1999-10-20	1999-12-22	Celltech Therapeutics Ltd	Chemical compounds
AU7922900A (en)	1999-10-27	2001-05-08	Novartis Ag	Thiazole and imidazo (4,5-b) pyridine compounds and their pharmaceutical use
GB0004890D0 (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
GB0004886D0 (en)	2000-03-01	2000-04-19	Astrazeneca Uk Ltd	Chemical compounds
GB0004887D0 (en)	2000-03-01	2000-04-19	Astrazeneca Uk Ltd	Chemical compounds

1999
- 1999-03-06 GB GBGB9905075.9A patent/GB9905075D0/en not_active Ceased
2000
- 2000-03-02 PT PT00906531T patent/PT1161428E/pt unknown
- 2000-03-02 CN CNB008070679A patent/CN1227249C/zh not_active Expired - Fee Related
- 2000-03-02 NZ NZ513893A patent/NZ513893A/xx unknown
- 2000-03-02 JP JP2000604033A patent/JP2002539120A/ja active Pending
- 2000-03-02 CA CA002366668A patent/CA2366668A1/en not_active Abandoned
- 2000-03-02 DK DK00906531T patent/DK1161428T3/da active
- 2000-03-02 AT AT00906531T patent/ATE241617T1/de not_active IP Right Cessation
- 2000-03-02 BR BR0008770-0A patent/BR0008770A/pt not_active Application Discontinuation
- 2000-03-02 KR KR1020017011289A patent/KR100683512B1/ko not_active Expired - Fee Related
- 2000-03-02 MX MXPA01008960A patent/MXPA01008960A/es active IP Right Grant
- 2000-03-02 WO PCT/GB2000/000737 patent/WO2000053595A1/en not_active Ceased
- 2000-03-02 EP EP00906531A patent/EP1161428B1/en not_active Expired - Lifetime
- 2000-03-02 DE DE60003001T patent/DE60003001T2/de not_active Expired - Fee Related
- 2000-03-02 IL IL14519200A patent/IL145192A0/xx active IP Right Grant
- 2000-03-02 ES ES00906531T patent/ES2200824T3/es not_active Expired - Lifetime
- 2000-03-02 AU AU28187/00A patent/AU754967B2/en not_active Ceased
- 2000-03-02 US US09/914,788 patent/US6716831B1/en not_active Expired - Fee Related
2001
- 2001-08-30 IL IL145192A patent/IL145192A/en not_active IP Right Cessation
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- 2001-09-05 NO NO20014317A patent/NO320909B1/no unknown

Also Published As

Publication number	Publication date
ATE241617T1 (de)	2003-06-15
KR100683512B1 (ko)	2007-02-16
AU754967B2 (en)	2002-11-28
CN1227249C (zh)	2005-11-16
EP1161428B1 (en)	2003-05-28
DE60003001T2 (de)	2004-05-06
JP2002539120A (ja)	2002-11-19
GB9905075D0 (en)	1999-04-28
WO2000053595A1 (en)	2000-09-14
AU2818700A (en)	2000-09-28
DK1161428T3 (da)	2003-09-15
NZ513893A (en)	2004-03-26
US6716831B1 (en)	2004-04-06
IL145192A0 (en)	2002-06-30
ES2200824T3 (es)	2004-03-16
CA2366668A1 (en)	2000-09-14
CN1349528A (zh)	2002-05-15
IL145192A (en)	2007-06-17
NO20014317D0 (no)	2001-09-05
NO320909B1 (no)	2006-02-13
NO20014317L (no)	2001-11-01
EP1161428A1 (en)	2001-12-12
PT1161428E (pt)	2003-10-31
DE60003001D1 (en)	2003-07-03
MXPA01008960A (es)	2002-04-24
KR20010102502A (ko)	2001-11-15
BR0008770A (pt)	2002-01-08

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CA2407593C (en)	2011-01-11	Fused heteroaryl derivatives
ZA200309165B (en)	2005-03-10	2-anilino-pyrimidine derivatives as cyclin dependent kinase inhibitors.
NZ537394A (en)	2006-12-22	Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
PT97827B (pt)	1998-10-30	Processo para a preparacao de 5-aril-pirimidinas substituidas
AU2004235915B2 (en)	2010-08-05	6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines
BG63245B1 (bg)	2001-07-31	Бициклични съединения, способни да инхибират тирозин кинази на рецепторно семейство на епидермалниярастежен фактор
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