AU2542501A - Pyrido(2,3-d)pyrimidine-2,7-diamine kinase inhibitors - Google Patents
Pyrido(2,3-d)pyrimidine-2,7-diamine kinase inhibitors Download PDFInfo
- Publication number
- AU2542501A AU2542501A AU25425/01A AU2542501A AU2542501A AU 2542501 A AU2542501 A AU 2542501A AU 25425/01 A AU25425/01 A AU 25425/01A AU 2542501 A AU2542501 A AU 2542501A AU 2542501 A AU2542501 A AU 2542501A
- Authority
- AU
- Australia
- Prior art keywords
- urea
- pyrido
- pyrimidin
- piperazin
- phenylamino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- QRRCMVPZJCHBLQ-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine-2,7-diamine Chemical compound C1=NC(N)=NC2=NC(N)=CC=C21 QRRCMVPZJCHBLQ-UHFFFAOYSA-N 0.000 title description 3
- 229940043355 kinase inhibitor Drugs 0.000 title description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 148
- 239000004202 carbamide Substances 0.000 claims description 145
- 125000000217 alkyl group Chemical group 0.000 claims description 62
- 229910052736 halogen Inorganic materials 0.000 claims description 48
- 150000002367 halogens Chemical class 0.000 claims description 48
- -1 nitro, carboxy Chemical group 0.000 claims description 45
- 238000000034 method Methods 0.000 claims description 41
- 239000001257 hydrogen Substances 0.000 claims description 37
- 229910052739 hydrogen Inorganic materials 0.000 claims description 37
- 150000002148 esters Chemical class 0.000 claims description 31
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 29
- 125000001072 heteroaryl group Chemical group 0.000 claims description 27
- 125000000623 heterocyclic group Chemical group 0.000 claims description 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 25
- 125000003545 alkoxy group Chemical group 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 23
- 125000003118 aryl group Chemical group 0.000 claims description 23
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 22
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 19
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- 101150073031 cdk2 gene Proteins 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 125000000304 alkynyl group Chemical group 0.000 claims description 15
- 150000001408 amides Chemical class 0.000 claims description 15
- 239000000651 prodrug Substances 0.000 claims description 15
- 229940002612 prodrug Drugs 0.000 claims description 15
- 108091000080 Phosphotransferase Proteins 0.000 claims description 14
- 125000003342 alkenyl group Chemical group 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 150000002431 hydrogen Chemical class 0.000 claims description 14
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- 101100440696 Caenorhabditis elegans cor-1 gene Proteins 0.000 claims description 12
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 12
- 125000002837 carbocyclic group Chemical group 0.000 claims description 12
- 230000002401 inhibitory effect Effects 0.000 claims description 11
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 10
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- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 10
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims description 10
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 9
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 9
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- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 9
- 230000001404 mediated effect Effects 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 9
- 230000002062 proliferating effect Effects 0.000 claims description 9
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 125000005842 heteroatom Chemical group 0.000 claims description 8
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- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
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- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 5
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 5
- 101150012716 CDK1 gene Proteins 0.000 claims description 4
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- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 4
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- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 3
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- RFIOZSIHFNEKFF-UHFFFAOYSA-N piperazine-1-carboxylic acid Chemical compound OC(=O)N1CCNCC1 RFIOZSIHFNEKFF-UHFFFAOYSA-N 0.000 claims description 3
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- NHOWDZOIZKMVAI-UHFFFAOYSA-N (2-chlorophenyl)(4-chlorophenyl)pyrimidin-5-ylmethanol Chemical compound C=1N=CN=CC=1C(C=1C(=CC=CC=1)Cl)(O)C1=CC=C(Cl)C=C1 NHOWDZOIZKMVAI-UHFFFAOYSA-N 0.000 claims description 2
- XMINZZZOTRYZGB-UHFFFAOYSA-N 1-(2-hydroxyethyl)-3-[2-(4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound N=1C2=NC(NC(=O)NCCO)=CC=C2C=NC=1NC(C=C1)=CC=C1N1CCNCC1 XMINZZZOTRYZGB-UHFFFAOYSA-N 0.000 claims description 2
- XFILUMCRLWWGHF-UHFFFAOYSA-N 1-(2-hydroxyethyl)-3-[5-methyl-2-(4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound N=1C=C2C(C)=CC(NC(=O)NCCO)=NC2=NC=1NC(C=C1)=CC=C1N1CCNCC1 XFILUMCRLWWGHF-UHFFFAOYSA-N 0.000 claims description 2
- ZOUYYHCVTKXASL-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)-3-chloroanilino]pyrido[2,3-d]pyrimidin-7-yl]-3-(2-hydroxyethyl)urea Chemical compound C1CN(C(=O)C)CCN1C(C(=C1)Cl)=CC=C1NC1=NC=C(C=CC(NC(=O)NCCO)=N2)C2=N1 ZOUYYHCVTKXASL-UHFFFAOYSA-N 0.000 claims description 2
- DWKOQXAXRXLTRO-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-5-methylpyrido[2,3-d]pyrimidin-7-yl]-3-(2-hydroxyethyl)urea Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(C)=CC(NC(=O)NCCO)=N2)C2=N1 DWKOQXAXRXLTRO-UHFFFAOYSA-N 0.000 claims description 2
- ROWUHEGVMUYETM-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-6-fluoropyrido[2,3-d]pyrimidin-7-yl]-3-(2-hydroxyethyl)urea Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C=C(F)C(NC(=O)NCCO)=N2)C2=N1 ROWUHEGVMUYETM-UHFFFAOYSA-N 0.000 claims description 2
- KNWWGBNAUNTSRV-UHFFFAOYSA-N 4-methylpiperazine-1-carboxylic acid Chemical compound CN1CCN(C(O)=O)CC1 KNWWGBNAUNTSRV-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 102000018233 Fibroblast Growth Factor Human genes 0.000 claims 2
- 108050007372 Fibroblast Growth Factor Proteins 0.000 claims 2
- 102000010780 Platelet-Derived Growth Factor Human genes 0.000 claims 2
- 108010038512 Platelet-Derived Growth Factor Proteins 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 229940126864 fibroblast growth factor Drugs 0.000 claims 2
- JYSYXVGVSGEKJX-UHFFFAOYSA-N 1-[2-(3-chloro-4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-yl]-3-(2-hydroxyethyl)urea Chemical compound N=1C2=NC(NC(=O)NCCO)=CC=C2C=NC=1NC(C=C1Cl)=CC=C1N1CCNCC1 JYSYXVGVSGEKJX-UHFFFAOYSA-N 0.000 claims 1
- CSHJWZUPBIECMW-UHFFFAOYSA-N 1-[2-(dimethylamino)ethyl]-3-[2-(4-fluoroanilino)pyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound N=1C2=NC(NC(=O)NCCN(C)C)=CC=C2C=NC=1NC1=CC=C(F)C=C1 CSHJWZUPBIECMW-UHFFFAOYSA-N 0.000 claims 1
- MPKZVSBVKJFRCB-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-yl]-3-ethylurea Chemical compound N=1C2=NC(NC(=O)NCC)=CC=C2C=NC=1NC(C=C1)=CC=C1N1CCN(C(C)=O)CC1 MPKZVSBVKJFRCB-UHFFFAOYSA-N 0.000 claims 1
- BMTGASBFAFZLBO-UHFFFAOYSA-N 1-cyclohexyl-3-[2-[4-(3,3-dimethylpiperazin-1-yl)anilino]-6-fluoropyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound C1CNC(C)(C)CN1C(C=C1)=CC=C1NC1=NC=C(C=C(F)C(NC(=O)NC2CCCCC2)=N2)C2=N1 BMTGASBFAFZLBO-UHFFFAOYSA-N 0.000 claims 1
- ZTIAGQKFXYSPQF-KDURUIRLSA-N 1-cyclohexyl-3-[2-[4-[(3s,5r)-3,5-dimethylpiperazin-1-yl]anilino]-6-methylpyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound C1[C@@H](C)N[C@@H](C)CN1C(C=C1)=CC=C1NC1=NC=C(C=C(C)C(NC(=O)NC2CCCCC2)=N2)C2=N1 ZTIAGQKFXYSPQF-KDURUIRLSA-N 0.000 claims 1
- CZKTXARZWICZDX-IYBDPMFKSA-N 1-cyclopropyl-3-[2-[4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]anilino]-6-methylpyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound C1[C@@H](C)N[C@@H](C)CN1C(C=C1)=CC=C1NC1=NC=C(C=C(C)C(NC(=O)NC2CC2)=N2)C2=N1 CZKTXARZWICZDX-IYBDPMFKSA-N 0.000 claims 1
- PMFGZMVIXFORHF-UHFFFAOYSA-N 1-ethyl-3-[2-(4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound N=1C2=NC(NC(=O)NCC)=CC=C2C=NC=1NC(C=C1)=CC=C1N1CCNCC1 PMFGZMVIXFORHF-UHFFFAOYSA-N 0.000 claims 1
- MEPIXWYYOTZYNT-UHFFFAOYSA-N 1-ethyl-3-[5-methyl-2-(4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-yl]urea Chemical compound N=1C2=NC(NC(=O)NCC)=CC(C)=C2C=NC=1NC(C=C1)=CC=C1N1CCNCC1 MEPIXWYYOTZYNT-UHFFFAOYSA-N 0.000 claims 1
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- QESQUIMEUZZKIO-KDURUIRLSA-N tert-butyl (2s,6r)-4-[4-[[7-(tert-butylcarbamoylamino)pyrido[2,3-d]pyrimidin-2-yl]amino]phenyl]-2,6-dimethylpiperazine-1-carboxylate Chemical group C1[C@@H](C)N(C(=O)OC(C)(C)C)[C@@H](C)CN1C(C=C1)=CC=C1NC1=NC=C(C=CC(NC(=O)NC(C)(C)C)=N2)C2=N1 QESQUIMEUZZKIO-KDURUIRLSA-N 0.000 description 1
- RBOGBIZGALIITO-UHFFFAOYSA-N tert-butyl 2,6-dimethylpiperazine-1-carboxylate Chemical compound CC1CNCC(C)N1C(=O)OC(C)(C)C RBOGBIZGALIITO-UHFFFAOYSA-N 0.000 description 1
- QUKABSSPBMVPRN-UHFFFAOYSA-N tert-butyl 4-(4-aminophenyl)-2,2-dimethylpiperazine-1-carboxylate Chemical compound C1C(C)(C)N(C(=O)OC(C)(C)C)CCN1C1=CC=C(N)C=C1 QUKABSSPBMVPRN-UHFFFAOYSA-N 0.000 description 1
- OSBIEGRZGZRSBF-UHFFFAOYSA-N tert-butyl 4-[4-[(5-acetyl-4-aminopyrimidin-2-yl)amino]phenyl]piperazine-1-carboxylate Chemical compound N1=C(N)C(C(=O)C)=CN=C1NC1=CC=C(N2CCN(CC2)C(=O)OC(C)(C)C)C=C1 OSBIEGRZGZRSBF-UHFFFAOYSA-N 0.000 description 1
- PWUUIKXPHXIFIT-UHFFFAOYSA-N tert-butyl 4-[4-[(7-amino-5-methylpyrido[2,3-d]pyrimidin-2-yl)amino]phenyl]piperazine-1-carboxylate Chemical group N=1C=C2C(C)=CC(N)=NC2=NC=1NC(C=C1)=CC=C1N1CCN(C(=O)OC(C)(C)C)CC1 PWUUIKXPHXIFIT-UHFFFAOYSA-N 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- CBXCPBUEXACCNR-UHFFFAOYSA-N tetraethylammonium Chemical compound CC[N+](CC)(CC)CC CBXCPBUEXACCNR-UHFFFAOYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- XJDNKRIXUMDJCW-UHFFFAOYSA-J titanium tetrachloride Chemical compound Cl[Ti](Cl)(Cl)Cl XJDNKRIXUMDJCW-UHFFFAOYSA-J 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 230000026683 transduction Effects 0.000 description 1
- 238000010361 transduction Methods 0.000 description 1
- 125000004665 trialkylsilyl group Chemical group 0.000 description 1
- 125000006000 trichloroethyl group Chemical group 0.000 description 1
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 231100000588 tumorigenic Toxicity 0.000 description 1
- 230000000381 tumorigenic effect Effects 0.000 description 1
- 208000010576 undifferentiated carcinoma Diseases 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 208000010570 urinary bladder carcinoma Diseases 0.000 description 1
- 229940070710 valerate Drugs 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000011345 viscous material Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
- 229910000166 zirconium phosphate Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17826100P | 2000-01-25 | 2000-01-25 | |
US60178261 | 2000-01-25 | ||
PCT/IB2001/000069 WO2001055147A1 (en) | 2000-01-25 | 2001-01-23 | PYRIDO[2,3-d]PYRIMIDINE-2,7-DIAMINE KINASE INHIBITORS |
Publications (1)
Publication Number | Publication Date |
---|---|
AU2542501A true AU2542501A (en) | 2001-08-07 |
Family
ID=22651853
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AU25425/01A Abandoned AU2542501A (en) | 2000-01-25 | 2001-01-23 | Pyrido(2,3-d)pyrimidine-2,7-diamine kinase inhibitors |
Country Status (34)
Country | Link |
---|---|
EP (1) | EP1254137A1 (es) |
JP (1) | JP4047010B2 (es) |
KR (1) | KR20020065939A (es) |
CN (1) | CN1395578A (es) |
AP (1) | AP2002002586A0 (es) |
AR (1) | AR030044A1 (es) |
AU (1) | AU2542501A (es) |
BG (1) | BG106850A (es) |
BR (1) | BR0107751A (es) |
CA (1) | CA2397961C (es) |
CO (1) | CO5261549A1 (es) |
CR (1) | CR6706A (es) |
CZ (1) | CZ20022475A3 (es) |
DZ (1) | DZ3266A1 (es) |
EA (1) | EA200200643A1 (es) |
EE (1) | EE200200405A (es) |
GT (1) | GT200100016A (es) |
HN (1) | HN2001000013A (es) |
HU (1) | HUP0204141A3 (es) |
IL (1) | IL150545A0 (es) |
IS (1) | IS6443A (es) |
MA (1) | MA26868A1 (es) |
MX (1) | MXPA02007221A (es) |
NO (1) | NO20023527L (es) |
OA (1) | OA12161A (es) |
PA (1) | PA8510701A1 (es) |
PE (1) | PE20011066A1 (es) |
PL (1) | PL356802A1 (es) |
SK (1) | SK10632002A3 (es) |
SV (1) | SV2002000294A (es) |
TN (1) | TNSN01014A1 (es) |
WO (1) | WO2001055147A1 (es) |
YU (1) | YU50402A (es) |
ZA (1) | ZA200205879B (es) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7235551B2 (en) | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
AU2002246855B2 (en) | 2000-10-23 | 2005-12-22 | Smithkline Beecham Corporation | Novel compounds |
PE20030008A1 (es) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | Inhibidores duales de pde 7 y pde 4 |
ATE370952T1 (de) | 2002-04-19 | 2007-09-15 | Smithkline Beecham Corp | Neue verbindungen |
BR0316680A (pt) * | 2002-11-28 | 2005-10-18 | Schering Ag | Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos |
US7157455B2 (en) * | 2003-02-10 | 2007-01-02 | Hoffmann-La Roche Inc. | 4-Aminopyrimidine-5-one derivatives |
TW200502236A (en) * | 2003-03-28 | 2005-01-16 | Hoffmann La Roche | Novel pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents |
FR2873118B1 (fr) | 2004-07-15 | 2007-11-23 | Sanofi Synthelabo | Derives de pyrido-pyrimidine, leur application en therapeutique |
CN101014600A (zh) * | 2004-09-21 | 2007-08-08 | 霍夫曼-拉罗奇有限公司 | 用作蛋白激酶抑制剂的6-(2-烷基-苯基)-吡啶并[2,3-d]嘧啶类 |
WO2006104917A2 (en) | 2005-03-25 | 2006-10-05 | Glaxo Group Limited | Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1h)-one derivatives |
JP2008535822A (ja) | 2005-03-25 | 2008-09-04 | グラクソ グループ リミテッド | 新規化合物 |
AR053346A1 (es) | 2005-03-25 | 2007-05-02 | Glaxo Group Ltd | Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38 |
TW200724142A (en) | 2005-03-25 | 2007-07-01 | Glaxo Group Ltd | Novel compounds |
FR2887882B1 (fr) * | 2005-07-01 | 2007-09-07 | Sanofi Aventis Sa | Derives de pyrido[2,3-d] pyrimidine, leur preparation, leur application en therapeutique |
BRPI0613604A2 (pt) * | 2005-07-21 | 2011-01-18 | Hoffmann La Roche | compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por inibidores de ptp-1b, e utilização dos compostos |
ES2351939T3 (es) * | 2005-08-09 | 2011-02-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteínas cinasas. |
FR2896246B1 (fr) | 2006-01-13 | 2008-08-15 | Sanofi Aventis Sa | Derives de pyrido-pyrimidone, leur preparation, leur application en therapeutique. |
EP1914234A1 (en) | 2006-10-16 | 2008-04-23 | GPC Biotech Inc. | Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors |
JO2985B1 (ar) | 2006-12-20 | 2016-09-05 | Takeda Pharmaceuticals Co | مثبطات كينازmapk/erk |
FR2910813B1 (fr) * | 2006-12-28 | 2009-02-06 | Sanofi Aventis Sa | Nouvelle utilisation therapeutique pour le traitement des leucemies |
EP2112150B1 (en) | 2008-04-22 | 2013-10-16 | Forma Therapeutics, Inc. | Improved raf inhibitors |
MX2011005720A (es) * | 2008-12-01 | 2011-06-17 | Merck Patent Gmbh | Pirido [4,3-d] pirimidinas 2,5-diamino sustituidas como inhibidores de autotaxina contra cancer. |
GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
WO2014151682A1 (en) * | 2013-03-14 | 2014-09-25 | Icahn School Of Medicine At Mount Sinai | Pyrimidine compounds as kinase inhibitors |
GB201403536D0 (en) | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
KR101671404B1 (ko) * | 2014-09-02 | 2016-11-02 | 한국원자력의학원 | 항암 효과, 방사선 병용치료 효과 및 당뇨병 치료 효과를 갖는 피리미딘 유도체 및 이의 의학적 용도 |
CN107286180B (zh) * | 2016-04-11 | 2019-07-02 | 上海勋和医药科技有限公司 | 杂代吡啶并嘧啶酮衍生物作为cdk抑制剂及其应用 |
GB201709840D0 (en) | 2017-06-20 | 2017-08-02 | Inst Of Cancer Research: Royal Cancer Hospital | Methods and medical uses |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GEP20012444B (en) * | 1994-11-14 | 2001-05-25 | Warner Lambert Company Us | 6-Aryl Pyrido[2,3-d]Pyrimidines and Naphthyridines, Pharmaceutical Composition on Their Basis and Application for Inhibiting Cellular Proliferation |
IL115256A0 (en) * | 1994-11-14 | 1995-12-31 | Warner Lambert Co | 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use |
US5620981A (en) * | 1995-05-03 | 1997-04-15 | Warner-Lambert Company | Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation |
DE69939168D1 (de) * | 1998-05-26 | 2008-09-04 | Warner Lambert Co | Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung |
-
2001
- 2001-01-23 HU HU0204141A patent/HUP0204141A3/hu unknown
- 2001-01-23 AP APAP/P/2002/002586A patent/AP2002002586A0/en unknown
- 2001-01-23 BR BR0107751-1A patent/BR0107751A/pt not_active IP Right Cessation
- 2001-01-23 CZ CZ20022475A patent/CZ20022475A3/cs unknown
- 2001-01-23 AU AU25425/01A patent/AU2542501A/en not_active Abandoned
- 2001-01-23 IL IL15054501A patent/IL150545A0/xx unknown
- 2001-01-23 PL PL01356802A patent/PL356802A1/xx not_active Application Discontinuation
- 2001-01-23 EP EP01900591A patent/EP1254137A1/en not_active Withdrawn
- 2001-01-23 GT GT200100016A patent/GT200100016A/es unknown
- 2001-01-23 CN CN01804048A patent/CN1395578A/zh active Pending
- 2001-01-23 JP JP2001561006A patent/JP4047010B2/ja not_active Expired - Fee Related
- 2001-01-23 MX MXPA02007221A patent/MXPA02007221A/es not_active Application Discontinuation
- 2001-01-23 KR KR1020027009516A patent/KR20020065939A/ko not_active Application Discontinuation
- 2001-01-23 AR ARP010100285A patent/AR030044A1/es not_active Application Discontinuation
- 2001-01-23 EA EA200200643A patent/EA200200643A1/ru unknown
- 2001-01-23 YU YU50402A patent/YU50402A/sh unknown
- 2001-01-23 OA OA1200200213A patent/OA12161A/en unknown
- 2001-01-23 WO PCT/IB2001/000069 patent/WO2001055147A1/en not_active Application Discontinuation
- 2001-01-23 SK SK1063-2002A patent/SK10632002A3/sk not_active Application Discontinuation
- 2001-01-23 CA CA002397961A patent/CA2397961C/en not_active Expired - Fee Related
- 2001-01-23 EE EEP200200405A patent/EE200200405A/xx unknown
- 2001-01-23 PE PE2001000072A patent/PE20011066A1/es not_active Application Discontinuation
- 2001-01-23 DZ DZ013266A patent/DZ3266A1/fr active
- 2001-01-23 PA PA20018510701A patent/PA8510701A1/es unknown
- 2001-01-24 TN TNTNSN01014A patent/TNSN01014A1/fr unknown
- 2001-01-24 CO CO01005268A patent/CO5261549A1/es not_active Application Discontinuation
- 2001-01-24 SV SV2001000294A patent/SV2002000294A/es not_active Application Discontinuation
- 2001-01-24 HN HN2001000013A patent/HN2001000013A/es unknown
-
2002
- 2002-06-20 BG BG106850A patent/BG106850A/bg unknown
- 2002-06-25 IS IS6443A patent/IS6443A/is unknown
- 2002-07-17 CR CR6706A patent/CR6706A/es not_active Application Discontinuation
- 2002-07-22 MA MA26736A patent/MA26868A1/fr unknown
- 2002-07-23 ZA ZA200205879A patent/ZA200205879B/en unknown
- 2002-07-24 NO NO20023527A patent/NO20023527L/no not_active Application Discontinuation
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Legal Events
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MK6 | Application lapsed section 142(2)(f)/reg. 8.3(3) - pct applic. not entering national phase | ||
TH | Corrigenda |
Free format text: IN VOL 16, NO 5, PAGE(S) 912-919 UNDER THE HEADING APPLICATIONS LAPSED, REFUSED OR WITHDRAWN PLEASE DELETE ALL REFERENCE TO APPLICATION NO. 18549/00, 25425/01 AND 31890/01 |