JP2018044008A5 - - Google Patents
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- Publication number
- JP2018044008A5 JP2018044008A5 JP2017243651A JP2017243651A JP2018044008A5 JP 2018044008 A5 JP2018044008 A5 JP 2018044008A5 JP 2017243651 A JP2017243651 A JP 2017243651A JP 2017243651 A JP2017243651 A JP 2017243651A JP 2018044008 A5 JP2018044008 A5 JP 2018044008A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- ethyl
- pyrimidin
- chloro
- pyrazolo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 38
- 150000003839 salts Chemical class 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 22
- 125000005843 halogen group Chemical group 0.000 claims 18
- -1 —OH Chemical group 0.000 claims 18
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical group FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 13
- 102000038030 PI3Ks Human genes 0.000 claims 12
- 108091007960 PI3Ks Proteins 0.000 claims 12
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000006601 (C1-C3) alkylcarbamyl group Chemical group 0.000 claims 6
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 5
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 3
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- CEECNMYKERBUGO-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 CEECNMYKERBUGO-UHFFFAOYSA-N 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- RYYHOGBWUDOVBW-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 RYYHOGBWUDOVBW-UHFFFAOYSA-N 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- YGGWPDLYLUHWIQ-UHFFFAOYSA-N n,n-dimethylpyridine-2-carboxamide Chemical compound CN(C)C(=O)C1=CC=CC=N1 YGGWPDLYLUHWIQ-UHFFFAOYSA-N 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006599 (C1-C3) alkylaminocarbonylamino group Chemical group 0.000 claims 1
- 125000006597 (C1-C3) alkylcarbonylamino group Chemical group 0.000 claims 1
- 125000006595 (C1-C3) alkylsulfinyl group Chemical group 0.000 claims 1
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims 1
- 125000006602 (C1-C3) alkylsulfonylamino group Chemical group 0.000 claims 1
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- VBCPGZBXELQVJW-UHFFFAOYSA-N 1-[1-[3-(6-aminopyridin-3-yl)-5-chloro-2-methoxy-4-methylphenyl]ethyl]-3-methylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(N)N=C1 VBCPGZBXELQVJW-UHFFFAOYSA-N 0.000 claims 1
- VZCBKGOVKCOFDS-UHFFFAOYSA-N 2-[5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]pyridin-2-yl]oxyethanol Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(OCCO)N=C1 VZCBKGOVKCOFDS-UHFFFAOYSA-N 0.000 claims 1
- UXTGQWWQMSXIHY-UHFFFAOYSA-N 2-[[5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]pyridin-2-yl]amino]ethanol Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(NCCO)N=C1 UXTGQWWQMSXIHY-UHFFFAOYSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- DZTKLUFVTZFHFJ-UHFFFAOYSA-N 3-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-N,N-dimethylpyridine-2-carboxamide Chemical compound NC1=C2C(=NC=N1)N(N=C2C)C(C)C=2C(=C(C(=C(C2)Cl)C)C=2C(=NC=CC2)C(=O)N(C)C)OC DZTKLUFVTZFHFJ-UHFFFAOYSA-N 0.000 claims 1
- VJJSELYTDOGDNE-UHFFFAOYSA-N 4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n-(2-hydroxyethyl)-n-methylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=NC(C(=O)N(C)CCO)=C1 VJJSELYTDOGDNE-UHFFFAOYSA-N 0.000 claims 1
- JAOSUCRDSSWHBL-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-cyanopyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C#N)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 JAOSUCRDSSWHBL-UHFFFAOYSA-N 0.000 claims 1
- RRSCRMHZMWUSFN-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-cyclopropylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3CC3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 RRSCRMHZMWUSFN-UHFFFAOYSA-N 0.000 claims 1
- LWRCOZZUEDSSRB-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-ethylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(CC)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 LWRCOZZUEDSSRB-UHFFFAOYSA-N 0.000 claims 1
- MICRYOZLKDGIIJ-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-iodopyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(I)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 MICRYOZLKDGIIJ-UHFFFAOYSA-N 0.000 claims 1
- OFKSVBCPWKARPM-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-(2,2-difluoroethoxy)-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound N1=C(C)C2=C(N)N=CN=C2N1C(C)C(C=1OCC(F)F)=CC(Cl)=C(C)C=1C1=CC=C(C(=O)N(C)C)N=C1 OFKSVBCPWKARPM-UHFFFAOYSA-N 0.000 claims 1
- SPDKDKKGRGWOLC-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n-methylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)NC)N=C1 SPDKDKKGRGWOLC-UHFFFAOYSA-N 0.000 claims 1
- ONBNCONPECJPDM-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n-methylpyridine-2-carboxamide Chemical compound C1=NC(C(=O)NC)=CC=C1C1=C(C)C(Cl)=CC(C(C)N2C3=NC=NC(N)=C3C(C)=N2)=C1OC ONBNCONPECJPDM-UHFFFAOYSA-N 0.000 claims 1
- MRVLFHBXSHLHOL-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-methylpyrazolo[4,3-c]pyridin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=CC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 MRVLFHBXSHLHOL-UHFFFAOYSA-N 0.000 claims 1
- POXLGQURDCNRHS-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=NC=CC=3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 POXLGQURDCNRHS-UHFFFAOYSA-N 0.000 claims 1
- YXXAZOUQFXBZTQ-UHFFFAOYSA-N 5-[3-[1-(4-amino-3-pyridin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=CN=CC=3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 YXXAZOUQFXBZTQ-UHFFFAOYSA-N 0.000 claims 1
- NHMULOGKNRTRLR-UHFFFAOYSA-N 5-[3-[1-(4-amino-5-methylpyrrolo[2,3-d]pyrimidin-7-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=C2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 NHMULOGKNRTRLR-UHFFFAOYSA-N 0.000 claims 1
- MKJFFPOJZAUGHO-UHFFFAOYSA-N 5-[3-[1-(4-amino-5-oxopyrido[2,3-d]pyrimidin-8-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(=O)C=C2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 MKJFFPOJZAUGHO-UHFFFAOYSA-N 0.000 claims 1
- MYTVYESWXXZGCZ-UHFFFAOYSA-N 5-[3-[1-(4-amino-5-oxopyrido[2,3-d]pyrimidin-8-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(=O)C=C2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 MYTVYESWXXZGCZ-UHFFFAOYSA-N 0.000 claims 1
- KBNSWEWQWKDWCH-UHFFFAOYSA-N 5-[3-[1-(4-amino-5-oxopyrido[2,3-d]pyrimidin-8-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n-methylpyridine-2-carboxamide Chemical compound C1=NC(C(=O)NC)=CC=C1C1=C(C)C(Cl)=CC(C(C)N2C3=NC=NC(N)=C3C(=O)C=C2)=C1OC KBNSWEWQWKDWCH-UHFFFAOYSA-N 0.000 claims 1
- RCULREUPLKRTQM-UHFFFAOYSA-N 5-[3-[1-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C=C2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 RCULREUPLKRTQM-UHFFFAOYSA-N 0.000 claims 1
- NCKZBAHNOUNLOC-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(1-methylpyrazol-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3=NN(C)C=C3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 NCKZBAHNOUNLOC-UHFFFAOYSA-N 0.000 claims 1
- YUPRTAQNMSAZLS-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(1-methylpyrazol-4-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3=CN(C)N=C3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 YUPRTAQNMSAZLS-UHFFFAOYSA-N 0.000 claims 1
- SLEODHBJUISKGK-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(1H-pyrazol-4-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-N,N-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3=CNN=C3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 SLEODHBJUISKGK-UHFFFAOYSA-N 0.000 claims 1
- LQXVADVQSDQOEW-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(1h-pyrazol-5-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3=NNC=C3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 LQXVADVQSDQOEW-UHFFFAOYSA-N 0.000 claims 1
- RPANFZBTBQXCEP-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(2-aminopyrimidin-5-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=NC(N)=NC=3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 RPANFZBTBQXCEP-UHFFFAOYSA-N 0.000 claims 1
- COEMEMLQEMXAPG-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(3-fluorophenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=C(F)C=CC=3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 COEMEMLQEMXAPG-UHFFFAOYSA-N 0.000 claims 1
- FTBLQBUNWWAOJJ-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(4-fluorophenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=CC(F)=CC=3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 FTBLQBUNWWAOJJ-UHFFFAOYSA-N 0.000 claims 1
- DUXSSDXCLZIENR-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(5-cyanopyridin-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=C(C=NC=3)C#N)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 DUXSSDXCLZIENR-UHFFFAOYSA-N 0.000 claims 1
- PFCWFOYSXIUQJD-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(difluoromethyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C(F)F)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 PFCWFOYSXIUQJD-UHFFFAOYSA-N 0.000 claims 1
- XVIFKEIMNFEGHE-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(fluoromethyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(CF)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 XVIFKEIMNFEGHE-UHFFFAOYSA-N 0.000 claims 1
- OIQDMTOTTQKSIQ-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(hydroxymethyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(CO)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 OIQDMTOTTQKSIQ-UHFFFAOYSA-N 0.000 claims 1
- RJLOXSYBHFJOBP-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-(methylaminomethyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(CNC)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 RJLOXSYBHFJOBP-UHFFFAOYSA-N 0.000 claims 1
- IDJOZOUOJMRPMD-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-[(dimethylamino)methyl]pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(CN(C)C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 IDJOZOUOJMRPMD-UHFFFAOYSA-N 0.000 claims 1
- LODIZXIHZIZZJF-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-[1-(2-hydroxyethyl)pyrazol-4-yl]pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C3=CN(CCO)N=C3)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 LODIZXIHZIZZJF-UHFFFAOYSA-N 0.000 claims 1
- MJPPETLGDRBERR-UHFFFAOYSA-N 5-[3-[1-[4-amino-3-[5-(dimethylcarbamoyl)pyridin-3-yl]pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-5-chloro-2-ethoxy-6-methylphenyl]-n,n-dimethylpyridine-2-carboxamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C=3C=C(C=NC=3)C(=O)N(C)C)=N2)C=C(Cl)C(C)=C1C1=CC=C(C(=O)N(C)C)N=C1 MJPPETLGDRBERR-UHFFFAOYSA-N 0.000 claims 1
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Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
| US8759359B2 (en) * | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| AR079529A1 (es) | 2009-12-18 | 2012-02-01 | Incyte Corp | Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| AR087760A1 (es) | 2011-09-02 | 2014-04-16 | Incyte Corp | Heterociclilaminas como inhibidores de pi3k |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| MX348290B (es) | 2012-06-04 | 2017-06-05 | Pharmacyclics Llc | Formas cristalinas de un inhibidor de tirosina quinasa de bruton. |
| JP6434416B2 (ja) | 2012-11-08 | 2018-12-05 | ライゼン・ファーマシューティカルズ・エスアー | ＰＤＥ４阻害剤とＰＩ３δ阻害剤または二重ＰＩ３δ−γキナーゼ阻害剤とを含有する薬学的組成物 |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| TW201932456A (zh) | 2013-01-15 | 2019-08-16 | 美商英塞特控股公司 | 適用作pim激酶抑制劑之噻唑甲醯胺及吡啶甲醯胺化合物 |
| TW202214254A (zh) * | 2013-03-01 | 2022-04-16 | 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 |
| MX2016002367A (es) | 2013-08-23 | 2016-10-28 | Incyte Corp | Compuestos de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim. |
| EP3102194A1 (en) * | 2014-02-03 | 2016-12-14 | Quadriga Biosciences, Inc. | Beta-substituted gamma-amino acids and analogs as chemotherapeutic agents |
| SG11201606351VA (en) | 2014-02-03 | 2016-09-29 | Quadriga Biosciences Inc | Beta-substituted beta-amino acids and analogs as chemotherapeutic agents |
| EA202191009A1 (ru) | 2014-04-08 | 2021-08-31 | Инсайт Корпорейшн | Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9586949B2 (en) | 2015-02-09 | 2017-03-07 | Incyte Corporation | Aza-heteroaryl compounds as PI3K-gamma inhibitors |
| PT3831833T (pt) | 2015-02-27 | 2023-02-06 | Incyte Corp | Processos para a preparação de um inibidor pi3k |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| JP6793401B2 (ja) * | 2015-03-11 | 2020-12-02 | 国立研究開発法人理化学研究所 | 難治性白血病治療薬 |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| WO2016183071A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Hetero-tricyclic compounds and their use for the treatment of cancer |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| US9783487B2 (en) | 2015-08-03 | 2017-10-10 | Quadriga Biosciences, Inc. | Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| TWI824309B (zh) | 2015-11-06 | 2023-12-01 | 美商英塞特公司 | 作為PI3K-γ抑制劑之雜環化合物 |
| ES2995198T3 (en) | 2016-01-05 | 2025-02-07 | Incyte Corp | Pyridine compounds as pi3k-gamma inhibitors |
| HUE064656T2 (hu) | 2016-03-28 | 2024-04-28 | Incyte Corp | Pirrolotriazin vegyületek mint TAM inhibitorok |
| WO2017223414A1 (en) | 2016-06-24 | 2017-12-28 | Incyte Corporation | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS |
| KR102739325B1 (ko) | 2017-09-27 | 2024-12-09 | 인사이트 코포레이션 | Tam 억제제로서 유용한 피롤로트리아진 유도체의 염 |
| BR112020007593A2 (pt) | 2017-10-18 | 2020-09-24 | Incyte Corporation | derivados de imidazol condensados substituídos por grupos hidróxi terciários como inibidores de pi3k-gama |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| CR20200464A (es) | 2018-03-08 | 2021-04-14 | Incyte Corp | Compuestos diólicos de aminopirazina como inhibidores de pi3k-y |
| KR102884803B1 (ko) | 2018-06-01 | 2025-11-12 | 인사이트 코포레이션 | Pi3k 관련 장애의 치료를 위한 투여 요법 |
| ES3031110T3 (en) | 2018-06-29 | 2025-07-04 | Incyte Corp | Formulations of an axl/mer inhibitor |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| 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 |
| WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
| JP2021008453A (ja) | 2019-07-02 | 2021-01-28 | エフェクター・セラピューティクス，インコーポレーテッド | 翻訳阻害剤およびその使用 |
| US20210253582A1 (en) * | 2020-02-06 | 2021-08-19 | Incyte Corporation | Salts and solid forms and processes of preparing a pi3k inhibitor |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| JP2023551519A (ja) | 2020-11-30 | 2023-12-08 | インサイト・コーポレイション | 抗ｃｄ１９抗体とパルサクリシブの組み合わせ療法 |
| WO2022115120A1 (en) | 2020-11-30 | 2022-06-02 | Incyte Corporation | Combination therapy with an anti-cd19 antibody and parsaclisib |
| WO2023114369A2 (en) | 2021-12-16 | 2023-06-22 | Incyte Corporation | Topical formulations of pi3k-delta inhibitors |
| WO2024220380A2 (en) * | 2023-04-16 | 2024-10-24 | Totus Medicines Inc. | Pi3k assays and probe compounds therein |
| US11958832B1 (en) | 2023-10-12 | 2024-04-16 | King Faisal University | 2-alkoxy[4,3:6,3-terpyridine]-3-carbonitriles as antimicrobial compounds |
Family Cites Families (302)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3169967A (en) | 1957-11-14 | 1965-02-16 | Ciba Geigy Corp | Methyl o-lower alkanoyl-reserpates |
| US3037980A (en) | 1955-08-18 | 1962-06-05 | Burroughs Wellcome Co | Pyrrolopyrimidine vasodilators and method of making them |
| DE1770420U (de) | 1958-02-27 | 1958-07-17 | Tara Union G M B H | Blumentopf aus kunststoff. |
| US3506643A (en) | 1966-12-09 | 1970-04-14 | Max Thiel | N**6-aralkyl-adenosine derivatives |
| DE2139107A1 (de) | 1971-08-04 | 1973-02-15 | Merck Patent Gmbh | Heterocyclisch substituierte adenosinverbindungen |
| US3814251A (en) | 1972-08-09 | 1974-06-04 | Sperry Rand Corp | Power transmission |
| US3962443A (en) | 1972-08-14 | 1976-06-08 | Dainippon Pharmaceutical Co., Ltd. | Antibacterial pharmaceutical compositions and processes for preparation thereof |
| DE2248232A1 (de) | 1972-10-02 | 1974-04-11 | Basf Ag | 4-thiopyrimido eckige klammer auf 4,5-d eckige klammer zu pyrimidine |
| AR204003A1 (es) | 1973-04-03 | 1975-11-12 | Dainippon Pharmaceutical Co | Procedimiento para preparar compuestos derivados del acido 2-(1-piperazinil)-5-oxopirido-(2,3-d)pirimidino-6-carboxilico y sus sales farmaceuticamente aceptables |
| US3936454A (en) | 1973-08-14 | 1976-02-03 | Warner-Lambert Company | 5-Amino-4-chloro-6-(substituted amino)-pyrimidines |
| US3862189A (en) | 1973-08-14 | 1975-01-21 | Warner Lambert Co | Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents |
| DK3375A (cg-RX-API-DMAC10.html) | 1974-01-25 | 1975-09-15 | Ciba Geigy Ag | |
| JPS587626B2 (ja) | 1974-02-13 | 1983-02-10 | 大日本製薬株式会社 | ナフチリジン オヨビ キノリンユウドウタイノセイホウ |
| JPS50111080U (cg-RX-API-DMAC10.html) | 1974-02-21 | 1975-09-10 | ||
| JPS5625234Y2 (cg-RX-API-DMAC10.html) | 1976-01-17 | 1981-06-15 | ||
| JPS5359663A (en) | 1976-11-09 | 1978-05-29 | Sumitomo Chem Co Ltd | 2-halogeno methyl indole derivatives and process for praparation of the same |
| JPS52106897A (en) | 1977-01-10 | 1977-09-07 | Dainippon Pharmaceut Co Ltd | Synthesis of piperazine derivatives |
| JPS5392767A (en) | 1977-01-27 | 1978-08-15 | Sumitomo Chem Co Ltd | Preparation of 2-phthalimidomethylindole derivatives |
| JPS5625234A (en) | 1979-08-02 | 1981-03-11 | Hitachi Denshi Ltd | Dropout display system |
| JPS56123981U (cg-RX-API-DMAC10.html) | 1980-02-20 | 1981-09-21 | ||
| JPS56123981A (en) | 1981-02-23 | 1981-09-29 | Dainippon Pharmaceut Co Ltd | Preparation of 1,4-disubstituted piperazine |
| JPS5883698A (ja) | 1981-11-13 | 1983-05-19 | Takeda Chem Ind Ltd | キノン化合物およびその製造法 |
| JPS5883698U (ja) | 1981-11-27 | 1983-06-06 | 石川島播磨重工業株式会社 | 熱交換器 |
| JPS58162949A (ja) | 1982-03-20 | 1983-09-27 | Konishiroku Photo Ind Co Ltd | ハロゲン化銀カラ−写真感光材料 |
| JPS6067709U (ja) | 1983-10-14 | 1985-05-14 | 三洋電機株式会社 | ヘア−ドライヤ− |
| JPS60140373U (ja) | 1984-02-28 | 1985-09-17 | 東洋ハ−ネス株式会社 | ワイヤハ−ネスのア−ス構造 |
| JPS6190153A (ja) | 1984-10-09 | 1986-05-08 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料の処理方法 |
| JPS6263591U (cg-RX-API-DMAC10.html) | 1985-06-29 | 1987-04-20 | ||
| JPS62103640A (ja) | 1985-07-18 | 1987-05-14 | Fuji Photo Film Co Ltd | ハロゲン化銀カラ−写真感光材料 |
| JPS635783Y2 (cg-RX-API-DMAC10.html) | 1985-10-17 | 1988-02-17 | ||
| JPS62103640U (cg-RX-API-DMAC10.html) | 1985-12-18 | 1987-07-02 | ||
| JPH07119970B2 (ja) | 1986-04-18 | 1995-12-20 | 富士写真フイルム株式会社 | 画像形成方法 |
| JPS6310746A (ja) | 1986-07-01 | 1988-01-18 | Tanabe Seiyaku Co Ltd | ナフタレン誘導体 |
| CA1324609C (en) | 1986-07-30 | 1993-11-23 | Eastman Kodak Company | Photographic element and process |
| JPS6427257U (cg-RX-API-DMAC10.html) | 1987-08-11 | 1989-02-16 | ||
| US4861701A (en) | 1987-10-05 | 1989-08-29 | Eastman Kodak Company | Photographic element and process comprising a compound which comprises two timing groups in sequence |
| AT388372B (de) | 1987-10-08 | 1989-06-12 | Tanabe Seiyaku Co | Neue naphthalinderivate und sie enthaltende pharmazeutika |
| JPH01250316A (ja) | 1987-12-28 | 1989-10-05 | Tanabe Seiyaku Co Ltd | 抗脂血剤 |
| EP0364598A4 (en) | 1988-03-02 | 1992-01-15 | Yoshitomi Pharmaceutical Industries, Ltd. | 3,4-dihydrothieno 2,3-d¨pyrimidine compounds and pharmaceutical application thereof |
| US5208250A (en) | 1988-05-25 | 1993-05-04 | Warner-Lambert Company | Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents |
| JPH054831Y2 (cg-RX-API-DMAC10.html) | 1988-11-22 | 1993-02-08 | ||
| DK0482208T3 (da) | 1990-04-25 | 2000-09-18 | Nissan Chemical Ind Ltd | Pyridazinonderivat |
| SU1712359A1 (ru) | 1990-05-07 | 1992-02-15 | Уфимский Нефтяной Институт | Гидрохлорид 8 @ -гидроксихинолинового эфира 8-гидроксихинолин-7-карбоновой кислоты, в качестве бактерицида дл подавлени сульфатвосстанавливающих бактерий и культур РSеUDомоNаS и АRтнRовастеR |
| DE69129389T2 (de) | 1990-06-28 | 1998-10-08 | Fuji Photo Film Co Ltd | Photographische Silberhalogenidmaterialien |
| EP0481614A1 (en) | 1990-10-01 | 1992-04-22 | Merck & Co. Inc. | Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists |
| JPH04190232A (ja) | 1990-11-26 | 1992-07-08 | Fuji Photo Film Co Ltd | ハロゲン化銀カラー写真感光材料 |
| US5480883A (en) | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| AU1625192A (en) | 1991-05-31 | 1992-12-03 | Zeneca Limited | Heterocyclic derivatives |
| JP3108483B2 (ja) | 1991-09-30 | 2000-11-13 | 日清製粉株式会社 | インドール誘導体およびこれを有効成分とする抗潰瘍薬 |
| HUT64064A (en) | 1992-02-13 | 1993-11-29 | Chinoin Gyogyszer Es Vegyeszet | Process for producing puyrido/1,2-a/pyrimidine derivatives and pharmaceutical compositions comprising same as active ingredient |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| WO1993022291A1 (en) | 1992-04-24 | 1993-11-11 | E.I. Du Pont De Nemours And Company | Arthropodicidal and fungicidal aminopyrimidines |
| TW229140B (cg-RX-API-DMAC10.html) | 1992-06-05 | 1994-09-01 | Shell Internat Res Schappej B V | |
| FR2714907B1 (fr) | 1994-01-07 | 1996-03-29 | Union Pharma Scient Appl | Nouveaux dérivés de l'Adénosine, leurs procédés de préparation, compositions pharmaceutiques les contenant. |
| US6342501B1 (en) | 1994-02-25 | 2002-01-29 | The Regents Of The University Of Michigan | Pyrrolo[2,3-d] pyrimidines as antiviral agents |
| JPH0987282A (ja) | 1995-09-21 | 1997-03-31 | Kyowa Hakko Kogyo Co Ltd | チアゾール誘導体 |
| JPH09176162A (ja) | 1995-12-22 | 1997-07-08 | Toubishi Yakuhin Kogyo Kk | チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物 |
| JPH09176116A (ja) | 1995-12-27 | 1997-07-08 | Toray Ind Inc | 複素環誘導体およびその医薬用途 |
| JPH1025294A (ja) | 1996-03-26 | 1998-01-27 | Akira Matsuda | 縮合ヘテロ環誘導体、その製造法及びそれを含有する悪性腫瘍治療剤 |
| EP0934307B1 (en) | 1996-06-19 | 2011-04-27 | Aventis Pharma Limited | Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase |
| EP0882727B9 (en) | 1996-07-03 | 2005-06-15 | Sumitomo Pharmaceuticals Company, Limited | Novel purine derivatives |
| US5866702A (en) | 1996-08-02 | 1999-02-02 | Cv Therapeutics, Incorporation | Purine inhibitors of cyclin dependent kinase 2 |
| US6630496B1 (en) | 1996-08-26 | 2003-10-07 | Genetics Institute Llc | Inhibitors of phospholipase enzymes |
| JPH10231297A (ja) | 1997-02-20 | 1998-09-02 | Japan Energy Corp | 新規なアデニン−１−ｎ−オキシド誘導体およびその医薬用途 |
| KR100540046B1 (ko) | 1997-11-12 | 2006-01-10 | 미쓰비시 가가꾸 가부시키가이샤 | 퓨린유도체 및 이를 유효성분으로 함유하는 의약 |
| TW572758B (en) | 1997-12-22 | 2004-01-21 | Sumitomo Pharma | Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives |
| BR9909242A (pt) | 1998-02-25 | 2000-11-14 | Genetics Inst | Inibidores de fosfolipase a2 |
| SK12742000A3 (sk) | 1998-02-25 | 2001-05-10 | Genetics Institute, Inc. | Inhibítory fosfolipázových enzýmov, farmaceutický prostriedok s ich obsahom a ich použitie |
| US6828344B1 (en) | 1998-02-25 | 2004-12-07 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
| US6479487B1 (en) | 1998-02-26 | 2002-11-12 | Aventis Pharmaceuticals Inc. | 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines |
| TR200003206T2 (tr) | 1998-05-04 | 2001-07-23 | Zentaris Ag | İndol türevleri ve patolojik hücre çoğalmasının neden olduğu habis hastalıklar ve diğer hastalıkların tedavisinde kullanımları. |
| US6673797B1 (en) | 1998-05-26 | 2004-01-06 | Chugai Seiyaku Kabushiki Kaisha | Heterocyclic indole derivatives and mono- or diazaindole derivatives |
| JP3997651B2 (ja) | 1998-06-24 | 2007-10-24 | コニカミノルタホールディングス株式会社 | 新規色素及び画像記録材料及び感熱転写材料及びインクジェット記録液 |
| BR9912938B1 (pt) | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
| DE69913712T2 (de) | 1998-08-25 | 2004-10-07 | Uab Res Foundation Birmingham | Inhibitoren der bakteriellen nad synthetase |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| NZ513371A (en) | 1999-02-01 | 2003-08-29 | Cv Therapeutics Inc | 2,6,9 trisubstituted purine inhibitors of cyclin dependant kinase 2 and IkappaB-alpha |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| JP2000281654A (ja) | 1999-03-26 | 2000-10-10 | Tanabe Seiyaku Co Ltd | イソキノリン誘導体 |
| DE19932571A1 (de) | 1999-07-13 | 2001-01-18 | Clariant Gmbh | Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse |
| JP2001151771A (ja) | 1999-09-10 | 2001-06-05 | Kyowa Hakko Kogyo Co Ltd | 含窒素芳香族複素環誘導体 |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US6436965B1 (en) | 2000-03-02 | 2002-08-20 | Merck Frosst Canada & Co. | PDE IV inhibiting amides, compositions and methods of treatment |
| EP1138328A1 (en) | 2000-03-29 | 2001-10-04 | Eli Lilly And Company Limited | Naphthalene derivatives as CNS drugs |
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| NZ522783A (en) | 2000-06-28 | 2004-07-30 | Smithkline Beecham P | Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant |
| CN1331340A (zh) | 2000-06-30 | 2002-01-16 | 上海博德基因开发有限公司 | 一种新的多肽——人拓扑异构酶12.1和编码这种多肽的多核苷酸 |
| CN1186326C (zh) | 2000-07-05 | 2005-01-26 | 山之内制药株式会社 | 丙－1,3－二酮衍生物 |
| FR2814073B1 (fr) | 2000-09-21 | 2005-06-24 | Yang Ji Chemical Company Ltd | Composition pharmaceutique antifongique et/ou antiparasitaire et nouveaux derives de l'indole a titre de principes actifs d'une telle composition |
| DOP2002000334A (es) | 2001-02-14 | 2002-08-30 | Warner Lambert Co | Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz |
| SE0100568D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| IL157638A0 (en) | 2001-03-01 | 2004-03-28 | Shionogi & Co | Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity |
| UA76977C2 (en) | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
| EP1372643A1 (en) | 2001-03-30 | 2004-01-02 | Smithkline Beecham Corporation | Pyrazolopyridines, process for their preparation and use as therapeutic compounds |
| EP1372642A1 (en) | 2001-03-30 | 2004-01-02 | SmithKline Beecham Corporation | Use of pyrazolopyridines as therapeutic compounds |
| EP1385847B1 (en) | 2001-04-27 | 2005-06-01 | SmithKline Beecham Corporation | Pyrazolo[1,5-a]pyridine derivatives |
| CZ294535B6 (cs) | 2001-08-02 | 2005-01-12 | Ústav Experimentální Botaniky Avčr | Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující |
| GB0121033D0 (en) | 2001-08-30 | 2001-10-24 | Novartis Ag | Organic compounds |
| US8124625B2 (en) | 2001-09-14 | 2012-02-28 | Shionogi & Co., Ltd. | Method of enhancing the expression of apolipoprotein AI using olefin derivatives |
| WO2003024967A2 (en) | 2001-09-19 | 2003-03-27 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| HRP20040309A2 (en) | 2001-09-26 | 2006-05-31 | Bayer Pharmaceuticals Corporation | 1,6-nafthyridine derivatives as antidiabetics |
| EP1432714B1 (en) | 2001-10-02 | 2008-08-06 | Smithkline Beecham Corporation | Chemical compounds |
| MXPA04004137A (es) | 2001-10-30 | 2005-01-25 | Novartis Ag | Derivados de estauroesporina como inhibidores de la actividad de cinasa de tirosina del receptor flt3. |
| JP4663233B2 (ja) | 2001-11-09 | 2011-04-06 | エンゾン，インコーポレーテッド | ベンジル脱離系を利用する高分子チオール結合プロドラッグ |
| EP1314733A1 (en) | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
| WO2003049678A2 (en) | 2001-12-06 | 2003-06-19 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| DE60222302T2 (de) | 2001-12-06 | 2008-05-29 | Merck & Co., Inc. | Inhibitoren von mitotischem kinesin |
| TW200301135A (en) | 2001-12-27 | 2003-07-01 | Otsuka Maryland Res Inst Inc | Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor |
| CA2476162A1 (en) | 2002-02-13 | 2003-08-21 | Takeda Chemical Industries, Ltd. | Jnk inhibitor |
| WO2003074497A1 (en) | 2002-03-01 | 2003-09-12 | Pintex Pharmaceutical, Inc. | Pin1-modulating compounds and methods of use thereof |
| EP1490371B1 (en) | 2002-04-03 | 2007-08-15 | Bristol-Myers Squibb Company | Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same |
| CN1653077A (zh) | 2002-05-06 | 2005-08-10 | 健亚生物科技公司 | 治疗c型肝炎病毒感染的核苷衍生物 |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| US7358249B2 (en) | 2002-08-13 | 2008-04-15 | Shionogi & Co., Ltd. | Heterocyclic compounds having inhibitory activity against HIV integrase |
| JP4190232B2 (ja) | 2002-08-26 | 2008-12-03 | 富士通株式会社 | 機械研磨を行う方法 |
| ES2387388T3 (es) | 2002-09-27 | 2012-09-21 | Dainippon Sumitomo Pharma Co., Ltd. | Compuesto de adenina y uso del mismo |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| EP2316831B1 (en) | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
| AU2003302416A1 (en) | 2002-11-25 | 2004-06-18 | Mochida Pharmaceutical Co., Ltd. | Therapeutic agent for respiratory disease containing 4-hydroxypiperidine derivative as active ingredient |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| CA2512000C (en) | 2002-12-26 | 2011-08-09 | Eisai Co., Ltd. | Selective estrogen receptor modulator |
| CZ294538B6 (cs) | 2002-12-30 | 2005-01-12 | Ústav Experimentální Botaniky Akademie Vědčeské Re | Substituční deriváty N6-benzyladenosinu, způsob jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující |
| RU2233842C1 (ru) | 2003-01-13 | 2004-08-10 | Петров Владимир Иванович | Производные пурина, обладающие противовирусной активностью |
| PE20050068A1 (es) | 2003-02-06 | 2005-03-11 | Novartis Ag | 2-cianopirrolopirimidinas como inhibidores de la catepsina s |
| GB0304640D0 (en) | 2003-02-28 | 2003-04-02 | Novartis Ag | Organic compounds |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| SE0300908D0 (sv) | 2003-03-31 | 2003-03-31 | Astrazeneca Ab | Azaindole derivatives, preparations thereof, uses thereof and compositions containing them |
| US7129264B2 (en) | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
| EP1619948A4 (en) | 2003-05-05 | 2007-02-14 | Neurogen Corp | SUBSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS |
| ES2339862T3 (es) | 2003-06-20 | 2010-05-26 | Novartis Vaccines And Diagnostics, Inc. | Compuestos de piridino 1,2-a-pirimidin-4-ona como agentes anticancerosos. |
| WO2005000309A2 (en) | 2003-06-27 | 2005-01-06 | Ionix Pharmaceuticals Limited | Chemical compounds |
| JP4570015B2 (ja) | 2003-07-14 | 2010-10-27 | クミアイ化学工業株式会社 | ２−イソオキサゾリン誘導体及びそれを有効成分として含有する除草剤 |
| JP2007502776A (ja) | 2003-08-15 | 2007-02-15 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Ｒｔｋ阻害剤としての６−置換アニリノプリン類 |
| KR20060070572A (ko) | 2003-09-18 | 2006-06-23 | 콘포마 세러퓨틱스 코포레이션 | Ｈｓｐ90-저해제로서의 신규 헤테로시클릭 화합물 |
| EP1667978B1 (en) | 2003-09-23 | 2013-09-04 | Merck Sharp & Dohme Corp. | Isoquinolinone potassium channel inhibitors |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| WO2005074603A2 (en) | 2004-02-03 | 2005-08-18 | Abbott Laboratories | Aminobenzoxazoles as therapeutic agents |
| EP1717238A4 (en) | 2004-02-16 | 2008-03-05 | Daiichi Seiyaku Co | FUNGICIDES HETEROCYCLIC COMPOUNDS |
| CN1560035A (zh) | 2004-03-12 | 2005-01-05 | 沈阳药科大学 | 5－羟基吲哚－3－羧酸脂类衍生物 |
| WO2005091857A2 (en) | 2004-03-12 | 2005-10-06 | Bayer Pharmaceuticals Corporation | 1,6-naphthyridine and 1,8-naphthyridine derivatives and their use to treat diabetes and related disorders |
| WO2005092892A1 (ja) | 2004-03-26 | 2005-10-06 | Dainippon Sumitomo Pharma Co., Ltd. | ８−オキソアデニン化合物 |
| WO2005097140A2 (en) | 2004-04-02 | 2005-10-20 | Adenosine Therapeutics, Llc | Selective antagonists of a2a adenosine receptors |
| PT2612862T (pt) | 2004-05-13 | 2016-12-15 | Icos Corp | Quinazolinonas como inibidores de fosfatidilinositol 3-quinase delta humana |
| EP1753428A4 (en) | 2004-05-14 | 2010-09-15 | Abbott Lab | INHIBITORS OF KINASES AS THERAPEUTIC AGENTS |
| US20070287703A1 (en) | 2004-07-22 | 2007-12-13 | Astrazeneca Ab | Fused Pyrimidones Useful in the Treatment and the Prevention of Cancer |
| RU2447077C2 (ru) | 2004-08-18 | 2012-04-10 | Астразенека Аб | Энантиомеры выбранных конденсированных пиримидинов и их применение для лечения и предотвращения злокачественного новообразования |
| DE102004044221A1 (de) | 2004-09-14 | 2006-03-16 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| US8008335B2 (en) | 2004-10-19 | 2011-08-30 | Novartis Vaccines And Diagnostics, Inc. | Indole and benzimidazole derivatives |
| WO2006052546A2 (en) | 2004-11-04 | 2006-05-18 | Neurogen Corporation | Pyrazolylmethyl heteroaryl derivatives |
| EP1831225A2 (en) | 2004-11-19 | 2007-09-12 | The Regents of the University of California | Anti-inflammatory pyrazolopyrimidines |
| KR20070085433A (ko) | 2004-11-24 | 2007-08-27 | 노파르티스 아게 | Ｊａｋ 저해제들과 ｂｃｒ-ａｂｌ, ｆｌｔ-3, ｆａｋ 또는ｒａｆ 키나제 저해제들 중 하나 이상의 조합물 |
| EP1885356A2 (en) | 2005-02-17 | 2008-02-13 | Icos Corporation | Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation |
| ATE474829T1 (de) | 2005-06-27 | 2010-08-15 | Amgen Inc | Entzündungshemmende arylnitrilverbindungen |
| FR2889192A1 (fr) | 2005-07-27 | 2007-02-02 | Cytomics Systems Sa | Composes antifongiques, compositions contenant ces composes et leurs utilisations |
| JP2009504769A (ja) | 2005-08-16 | 2009-02-05 | ジェンザイム・コーポレーション | ケモカイン受容体結合化合物 |
| US7642270B2 (en) | 2005-09-14 | 2010-01-05 | Janssen Pharmaceutica N.V. | 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase |
| US20090118263A1 (en) | 2005-09-22 | 2009-05-07 | Dainippon Sumitomo Pharma Co., Ltd. | Novel Adenine Compound |
| GB0520657D0 (en) * | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| BR122021011787B1 (pt) | 2005-11-01 | 2022-01-25 | Impact Biomedicines, Inc | Inibidores de biaril meta pirimidina de cinases, composição farmacêutica e processo para preparar uma composição farmacêutica |
| EP1783114A1 (en) | 2005-11-03 | 2007-05-09 | Novartis AG | N-(hetero)aryl indole derivatives as pesticides |
| EP1954274B8 (en) | 2005-11-10 | 2011-01-12 | ChemoCentryx, Inc. | Substituted quinolones and methods of use |
| EP3838903B1 (en) | 2005-12-13 | 2023-11-22 | Incyte Holdings Corporation | Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor |
| US7989461B2 (en) | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
| US20100227880A1 (en) | 2006-01-25 | 2010-09-09 | Kristjan Gudmundsson | Chemical compounds |
| UY30118A1 (es) | 2006-01-31 | 2007-06-29 | Tanabe Seiyaku Co | Compueto amina trisustituido |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| JPWO2007102392A1 (ja) | 2006-03-03 | 2009-07-23 | 塩野義製薬株式会社 | Ｍｍｐ−１３選択的阻害剤 |
| EA200870385A1 (ru) | 2006-03-29 | 2009-04-28 | Фолдркс Фармасьютикалз, Инк. | Ингибирование токсичности альфа-синуклеина |
| KR20130087054A (ko) * | 2006-04-04 | 2013-08-05 | 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 | 키나제 길항물질 |
| DE102006029074A1 (de) * | 2006-06-22 | 2007-12-27 | Friedrich-Schiller-Universität Jena | 4-Amino-3-arylamino-6-arylpyrazolo[3,4-d]pyrimidin-Derivate, Verfahren zu ihrer Herstellung und deren Verwendung als antivirale Wirkstoffe |
| US8933130B2 (en) | 2006-06-23 | 2015-01-13 | Radius Health, Inc. | Treatment of vasomotor symptoms with selective estrogen receptor modulators |
| WO2008005303A2 (en) | 2006-06-30 | 2008-01-10 | Janssen Pharmaceutica N.V. | Thiazolopyrimidine modulators of trpv1 |
| US20080009508A1 (en) | 2006-07-10 | 2008-01-10 | Lucie Szucova | 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin |
| CA2656855A1 (en) | 2006-07-12 | 2008-01-17 | Christoph Luthy | Triazolopyridine derivatives as herbicides |
| RU2448109C2 (ru) | 2006-08-08 | 2012-04-20 | Чугаи Сейяку Кабусики Кайся | Производное пиримидина в качестве ингибитора pi3k и его применение |
| SG174086A1 (en) | 2006-08-30 | 2011-09-29 | Cellzome Ltd | Triazole derivatives as kinase inhibitors |
| WO2008032033A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| EP1972631A1 (en) | 2007-03-23 | 2008-09-24 | Novartis AG | Imidazopyridazines as PI3K lipid kinase inhibitors |
| WO2008055013A2 (en) | 2006-10-31 | 2008-05-08 | Janssen Pharmaceutica N.V. | 5-oxo-5,8 - dihydro - pyrido - pyrimidines as inhibitors of c-fms kinase |
| SG178786A1 (en) | 2006-11-13 | 2012-03-29 | Lilly Co Eli | Thienopyrimidinones for treatment of inflammatory disorders and cancers |
| EP3443958A1 (en) | 2006-11-22 | 2019-02-20 | Incyte Holdings Corporation | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
| CN101631786A (zh) | 2006-12-20 | 2010-01-20 | 先灵公司 | 新颖的jnk抑制剂 |
| EP2125827B1 (en) | 2006-12-29 | 2010-11-03 | F. Hoffmann-La Roche AG | Azaspiro derivatives |
| CA2677493A1 (en) | 2007-02-05 | 2008-08-14 | Xenon Pharmaceuticals Inc. | Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions |
| WO2008100867A2 (en) | 2007-02-12 | 2008-08-21 | Intermune, Inc. | Novel inhibitors hepatitis c virus replication |
| AR065784A1 (es) | 2007-03-20 | 2009-07-01 | Dainippon Sumitomo Pharma Co | Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas. |
| US20080233127A1 (en) | 2007-03-21 | 2008-09-25 | Wyeth | Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors |
| JP2010522177A (ja) | 2007-03-23 | 2010-07-01 | アムジエン・インコーポレーテツド | 複素環化合物およびその使用 |
| UA98955C2 (ru) | 2007-03-23 | 2012-07-10 | Амген Инк. | Гетероциклические соединения и их применение |
| US8039505B2 (en) | 2007-04-11 | 2011-10-18 | University Of Utah Research Foundation | Compounds for modulating T-cells |
| US8633186B2 (en) | 2007-06-08 | 2014-01-21 | Senomyx Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| US9603848B2 (en) | 2007-06-08 | 2017-03-28 | Senomyx, Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| EP2167058B1 (en) | 2007-06-18 | 2015-08-12 | University Of Louisville Research Foundation, Inc. | Family of pfkfb3 inhibitors with anti-neoplastic activities |
| ES2541434T3 (es) | 2007-06-29 | 2015-07-20 | Gilead Sciences, Inc. | Derivados de purina y su uso como moduladores del receptor de tipo Toll 7 |
| EP2190466A4 (en) | 2007-08-10 | 2011-12-21 | Burnham Inst Medical Research | Tissue-specific alkaline phosphatase (TNAP) activators and their use |
| TW200916447A (en) | 2007-08-29 | 2009-04-16 | Methylgene Inc | Sirtuin inhibitors |
| JP2009076865A (ja) | 2007-08-29 | 2009-04-09 | Fujifilm Corp | 有機電界発光素子 |
| WO2009034386A1 (en) | 2007-09-13 | 2009-03-19 | Astrazeneca Ab | Derivatives of adenine and 8-aza-adenine and uses thereof-796 |
| JP2009080233A (ja) | 2007-09-26 | 2009-04-16 | Kyocera Mita Corp | 電子写真感光体 |
| CZ300774B6 (cs) | 2007-10-05 | 2009-08-05 | Univerzita Palackého | Substituované 6-(alkylbenzylamino)purinové deriváty pro použití jako antagonisté cytokininových receptoru a prípravky obsahující tyto slouceniny |
| EP2217239A2 (en) | 2007-11-07 | 2010-08-18 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
| WO2009063235A1 (en) | 2007-11-13 | 2009-05-22 | Astrazeneca Ab | Derivatives of 1,9-dihydro-6h-purin-6-one and uses thereof-018 |
| JP2009120686A (ja) | 2007-11-14 | 2009-06-04 | Toyo Ink Mfg Co Ltd | 光重合開始剤、重合性組成物、および重合物の製造方法。 |
| US7820665B2 (en) | 2007-12-19 | 2010-10-26 | Amgen Inc. | Imidazopyridazine inhibitors of PI3 kinase for cancer treatment |
| EP2231641B1 (en) | 2007-12-21 | 2016-06-01 | UCB Biopharma SPRL | Quinoxaline and quinoline derivatives as kinase inhibitors |
| AU2008345681A1 (en) | 2007-12-21 | 2009-07-09 | Wyeth Llc | Imidazo [1,2-a] pyridine compounds |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US7960397B2 (en) | 2007-12-28 | 2011-06-14 | Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic | 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions |
| JP5411161B2 (ja) | 2007-12-28 | 2014-02-12 | 上海特化医薬科技有限公司 | Ｎ−｛１−［３−（２−エトキシ−５−（４−エチルピペラジニル）スルホニルフェニル）−４，５−ジヒドロ−５−オキソ−１，２，４−トリアジン−６−イル］エチル｝ブチルアミド、その調製方法及び用途 |
| US8193182B2 (en) * | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| EP2247596A2 (en) | 2008-01-11 | 2010-11-10 | Natco Pharma Limited | Novel pyrazolo [3, 4 -d] pyrimidine derivatives as anti -cancer agents |
| US9089572B2 (en) | 2008-01-17 | 2015-07-28 | California Institute Of Technology | Inhibitors of p97 |
| EP2252616B1 (en) | 2008-01-30 | 2014-07-23 | Genentech, Inc. | Pyrazolopyrimidine pi3k inhibitor compounds and methods of use |
| US20110105457A1 (en) | 2008-04-18 | 2011-05-05 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on pi3k |
| US8119647B2 (en) | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
| WO2009140215A2 (en) | 2008-05-11 | 2009-11-19 | Geraghty, Erin | Method for treating drug-resistant bacterial and other infections with clioquinol, phanquinone, and related compounds |
| EP2300005A4 (en) | 2008-05-28 | 2011-07-13 | Us Of America As Represented By The Secretary Of The Army On Behalf Of U S Army Medical Res And Mate | Small-molecule inhibitors of botulinum neurotoxins |
| RU2010151352A (ru) | 2008-06-20 | 2012-07-27 | Метаболекс, Инк. (Us) | Арильные агонисты grp119 и их применения |
| US8026271B2 (en) | 2008-07-11 | 2011-09-27 | National Health Research Institutes | Formulations of indol-3-yl-2-oxoacetamide compounds |
| WO2010018458A2 (en) | 2008-08-12 | 2010-02-18 | Crystalgenomics, Inc. | Phenol derivatives and methods of use thereof |
| CA2738429C (en) * | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| WO2010057048A1 (en) | 2008-11-13 | 2010-05-20 | Calistoga Pharmaceuticals Inc. | Therapies for hematologic malignancies |
| EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
| AR075111A1 (es) | 2008-12-24 | 2011-03-09 | Bial Portela & Ca Sa | Derivados heterociclicos de diazoles y triazoles, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de trastornos del metabolismo y del sistema nervioso, entre otros. |
| WO2010083444A1 (en) | 2009-01-15 | 2010-07-22 | Anvyl, Llc | Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof |
| WO2010092340A1 (en) | 2009-02-13 | 2010-08-19 | Ucb Pharma S.A. | Fused pyridine and pyrazine derivatives as kinase inhibitors |
| WO2010114900A1 (en) | 2009-03-31 | 2010-10-07 | Arqule, Inc. | Substituted indolo-piperidine compounds |
| WO2010118367A2 (en) | 2009-04-10 | 2010-10-14 | Progenics Pharmaceuticals, Inc. | Antiviral pyrimidines |
| AP2011005956A0 (en) | 2009-04-20 | 2011-10-31 | Gilead Calistoga Llc | Methods of treatment for solid tumors. |
| WO2010127208A1 (en) | 2009-04-30 | 2010-11-04 | Forest Laboratories Holdings Limited | Inhibitors of acetyl-coa carboxylase |
| CA2760791C (en) | 2009-05-07 | 2017-06-20 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| US8716303B2 (en) | 2009-05-22 | 2014-05-06 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| WO2010151735A2 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | Heterocyclic compounds and their uses |
| US20100331306A1 (en) * | 2009-06-25 | 2010-12-30 | Amgen Inc. | Heterocyclic compounds and their uses |
| FR2947269B1 (fr) | 2009-06-29 | 2013-01-18 | Sanofi Aventis | Nouveaux composes anticancereux |
| AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
| JP5856052B2 (ja) | 2009-06-29 | 2016-02-09 | アジオス ファーマシューティカルズ， インコーポレイテッド | 治療化合物および組成物 |
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
| AU2010276160A1 (en) | 2009-07-21 | 2012-02-09 | Gilead Calistoga Llc | Treatment of liver disorders with PI3K inhibitors |
| WO2011025889A1 (en) | 2009-08-28 | 2011-03-03 | Takeda Pharmaceutical Company Limited | HEXAHYDROOXAZINOPTERINE COMPOUNDS FOR USE AS mTOR INHIBITORS |
| 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 |
| KR20120102601A (ko) | 2009-10-20 | 2012-09-18 | 셀좀 리미티드 | Ｊａｋ 저해제로서의 헤테로시클릴 피라졸로피리미딘 유사체 |
| NO2491035T3 (cg-RX-API-DMAC10.html) | 2009-10-22 | 2018-01-27 | ||
| RS56432B1 (sr) | 2009-11-05 | 2018-01-31 | Rhizen Pharmaceuticals S A | Novi benzopiran modulatori kinaze |
| ES2444543T3 (es) | 2009-11-10 | 2014-02-25 | Pfizer Inc | Inhibidores de la N1-pirazoloespirocetona acetil-CoA carboxilasa |
| WO2011058111A1 (en) | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Aminopurine derivatives as kinase inhibitors |
| WO2011058113A1 (en) | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors |
| US10174033B2 (en) | 2009-12-10 | 2019-01-08 | Institute Of Materia Medica, Chinese Academy Of Medical Sciences | N6-substituted adenosine derivatives and N6-substituted adenine derivatives and uses thereof |
| JP2013514989A (ja) | 2009-12-18 | 2013-05-02 | アムジエン・インコーポレーテツド | 複素環式化合物およびその使用法 |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| AR079529A1 (es) | 2009-12-18 | 2012-02-01 | Incyte Corp | Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k |
| PE20121505A1 (es) * | 2009-12-23 | 2012-11-05 | Medicis Pharmaceutical Corp | Derivados de aminoalquilpirimidina como antagonistas del receptor h4 de histamina |
| JP2011136925A (ja) | 2009-12-28 | 2011-07-14 | Dainippon Sumitomo Pharma Co Ltd | 含窒素二環性化合物 |
| KR101814835B1 (ko) | 2010-01-07 | 2018-01-04 | 다우 아그로사이언시즈 엘엘씨 | 티아졸로［5,4-ｄ］피리미딘 및 그의 농약으로서의 용도 |
| UY33199A (es) | 2010-01-26 | 2011-08-31 | Boehringer Ingelheim Int | 5-alquinil-pirimidinas. |
| ME02386B (me) | 2010-03-10 | 2016-09-20 | Incyte Holdings Corp | Derivati piperidin-4-il azetidina kao inhibitori jak1 |
| EA201290888A1 (ru) | 2010-03-22 | 2013-04-30 | Гленмарк Фармасьютикалс С.А. | Фармацевтическая композиция, содержащая производное пиримидинона |
| UY33304A (es) | 2010-04-02 | 2011-10-31 | Amgen Inc | Compuestos heterocíclicos y sus usos |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| EP2571357B1 (en) | 2010-05-21 | 2016-07-06 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| NZ603686A (en) | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| EP2579878A1 (en) | 2010-06-11 | 2013-04-17 | Gilead Calistoga LLC | Methods of treating hematological disorders with quinazolinone compounds in selected patients |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| CA2803259A1 (en) | 2010-07-01 | 2012-01-05 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of pi3k activity |
| JP2013530238A (ja) | 2010-07-01 | 2013-07-25 | アムジエン・インコーポレーテツド | Ｐｉ３ｋ活性の阻害剤としての複素環化合物及びその使用 |
| WO2012003271A1 (en) | 2010-07-02 | 2012-01-05 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of pi3k activity |
| EP2619209A1 (en) | 2010-09-24 | 2013-07-31 | Gilead Calistoga LLC | Atropisomers of pi3k-inhibiting compounds |
| EP2635565A1 (en) | 2010-11-04 | 2013-09-11 | Amgen Inc. | 5 -cyano-4, 6 -diaminopyrimidine or 6 -aminopurine derivatives as pi3k- delta inhibitors |
| CN103298474B (zh) | 2010-11-10 | 2016-06-29 | 无限药品股份有限公司 | 杂环化合物及其用途 |
| WO2012068343A1 (en) | 2010-11-17 | 2012-05-24 | Amgen Inc. | Quinoline derivatives as pik3 inhibitors |
| TW201249845A (en) | 2010-11-19 | 2012-12-16 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| CA2818903C (en) | 2010-12-14 | 2021-03-23 | Electrophoretics Limited | 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| JP2014501261A (ja) | 2010-12-23 | 2014-01-20 | アムジエン・インコーポレーテツド | 複素環化合物およびそれらの使用 |
| MX347708B (es) | 2011-01-10 | 2017-05-09 | Infinity Pharmaceuticals Inc | Proceso para preparar isoquinolinonas y formas solidas de isoquinolinonas. |
| CA2825599C (en) | 2011-02-01 | 2021-07-13 | The Board Of Trustees Of The University Of Illinois | 4-methyl-n-hydroxybenzamide compounds as histone deacetylase (hdac) inhibitors |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| AU2012284088B2 (en) | 2011-07-19 | 2015-10-08 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| 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 |
| AR087760A1 (es) * | 2011-09-02 | 2014-04-16 | Incyte Corp | Heterociclilaminas como inhibidores de pi3k |
| WO2013052699A2 (en) | 2011-10-04 | 2013-04-11 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of pi3k |
| 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 |
| SG11201503141TA (en) | 2012-11-01 | 2015-06-29 | Incyte Corp | Tricyclic fused thiophene derivatives as jak inhibitors |
| TW202214254A (zh) | 2013-03-01 | 2022-04-16 | 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 |
| CN105026400A (zh) | 2013-03-15 | 2015-11-04 | 詹森药业有限公司 | 用于制备药物的方法和中间体 |
| MX385187B (es) | 2013-05-17 | 2025-03-14 | Incyte Holdings Corp | Derivados del bipirazol como inhibidores de janus cinasa (jak) |
| EA202191009A1 (ru) | 2014-04-08 | 2021-08-31 | Инсайт Корпорейшн | Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k |
| US20170158699A1 (en) | 2014-05-27 | 2017-06-08 | Almirall, S.A. | Addition salts of (s)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3,4-dihydropyrrolo[1,2-f][1,2,4]triazine-5-carbonitrile |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| AR103297A1 (es) | 2014-12-30 | 2017-05-03 | Forma Therapeutics Inc | Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina |
| PT3831833T (pt) | 2015-02-27 | 2023-02-06 | Incyte Corp | Processos para a preparação de um inibidor pi3k |
| 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 |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| KR102884803B1 (ko) | 2018-06-01 | 2025-11-12 | 인사이트 코포레이션 | Pi3k 관련 장애의 치료를 위한 투여 요법 |
| WO2023114369A2 (en) | 2021-12-16 | 2023-06-22 | Incyte Corporation | Topical formulations of pi3k-delta inhibitors |
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