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)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (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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ID=10849022

Family Applications (1)

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

Country Status (20)

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

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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 WO PCT/GB2000/000737 patent/WO2000053595A1/en active IP Right Grant
- 2000-03-02 CA CA002366668A patent/CA2366668A1/en not_active Abandoned
- 2000-03-02 KR KR1020017011289A patent/KR100683512B1/ko not_active IP Right Cessation
- 2000-03-02 MX MXPA01008960A patent/MXPA01008960A/es active IP Right Grant
- 2000-03-02 ES ES00906531T patent/ES2200824T3/es not_active Expired - Lifetime
- 2000-03-02 DE DE60003001T patent/DE60003001T2/de 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 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 IL IL14519200A patent/IL145192A0/xx active IP Right Grant
- 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
- 2000-03-02 EP EP00906531A patent/EP1161428B1/en not_active Expired - Lifetime
- 2000-03-02 CN CNB008070679A patent/CN1227249C/zh not_active Expired - Fee Related
2001
- 2001-08-30 IL IL145192A patent/IL145192A/en not_active IP Right Cessation
- 2001-08-31 ZA ZA200107252A patent/ZA200107252B/en unknown
- 2001-09-05 NO NO20014317A patent/NO320909B1/no unknown

Also Published As

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

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