JP2013519707A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013519707A5 JP2013519707A5 JP2012553318A JP2012553318A JP2013519707A5 JP 2013519707 A5 JP2013519707 A5 JP 2013519707A5 JP 2012553318 A JP2012553318 A JP 2012553318A JP 2012553318 A JP2012553318 A JP 2012553318A JP 2013519707 A5 JP2013519707 A5 JP 2013519707A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolo
- pyrimidine
- ylamino
- pyridin
- cyclopentyl
- 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
Links
- FJWYXWJQDPCIEZ-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,8-diazabicyclo[3.2.1]octane-3-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCC(N4)C3)N=C2N1C1CCCC1 FJWYXWJQDPCIEZ-UHFFFAOYSA-N 0.000 claims description 3
- PBGMYLLXSOFMTR-ZWKOTPCHSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(1s,6r)-3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@@]1(CC[C@](C2)(N1)[H])[H])C(=O)N2C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 PBGMYLLXSOFMTR-ZWKOTPCHSA-N 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 30
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 18
- -1 5- (9-hydroxy-1,5,7-trimethyl-3,7-diazabicyclo [3.3.1] nonane-3-carbonyl) pyridin-2-ylamino Chemical group 0.000 claims 15
- 206010028980 Neoplasm Diseases 0.000 claims 12
- 201000011510 cancer Diseases 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 9
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- ZDRGTMWWJMXNIG-JGAZGGJJSA-N O=C1C[C@@H]2[C@H](CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CNC2.CN(C2=CC=CC=C2)C Chemical compound O=C1C[C@@H]2[C@H](CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CNC2.CN(C2=CC=CC=C2)C ZDRGTMWWJMXNIG-JGAZGGJJSA-N 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 239000000654 additive Substances 0.000 claims 3
- 230000000996 additive effect Effects 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 210000003739 neck Anatomy 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 210000001685 thyroid gland Anatomy 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- JCRUSEOGJUANIE-UHFFFAOYSA-N 2-[[5-(3,4,6,7,8,8a-hexahydro-1h-pyrrolo[1,2-a]pyrazine-2-carbonyl)pyridin-2-yl]amino]-7-cyclopentyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCCN4CC3)N=C2N1C1CCCC1 JCRUSEOGJUANIE-UHFFFAOYSA-N 0.000 claims 1
- WBCAOAIDJLJRCZ-UHFFFAOYSA-N 7-(3-tert-butylphenyl)-2-[[5-(3,8-diazabicyclo[3.2.1]octane-3-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCC(N4)C3)N=C2N1C1=CC=CC(C(C)(C)C)=C1 WBCAOAIDJLJRCZ-UHFFFAOYSA-N 0.000 claims 1
- VTSDFHMWTKRCAL-UHFFFAOYSA-N 7-(4-tert-butylphenyl)-2-[[5-(3,8-diazabicyclo[3.2.1]octane-3-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCC(N4)C3)N=C2N1C1=CC=C(C(C)(C)C)C=C1 VTSDFHMWTKRCAL-UHFFFAOYSA-N 0.000 claims 1
- YYUJVQQJCJMRSG-UHFFFAOYSA-N 7-[4-(2-cyanopropan-2-yl)phenyl]-2-[[5-(3,8-diazabicyclo[3.2.1]octane-8-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3C4CCC3CNC4)N=C2N1C1=CC=C(C(C)(C)C#N)C=C1 YYUJVQQJCJMRSG-UHFFFAOYSA-N 0.000 claims 1
- HBBBOMMFSYNTJJ-SJORKVTESA-N 7-cyclobutyl-n,n-dimethyl-2-[[5-[(1r,6s)-3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@]1(CC[C@@](C2)(N1)[H])[H])C(=O)N2C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCC1 HBBBOMMFSYNTJJ-SJORKVTESA-N 0.000 claims 1
- QVFRZHXKIZTYEZ-UHFFFAOYSA-N 7-cycloheptyl-2-[[5-(2,5-diazabicyclo[2.2.1]heptane-2-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3C4CC(NC4)C3)N=C2N1C1CCCCCC1 QVFRZHXKIZTYEZ-UHFFFAOYSA-N 0.000 claims 1
- KSBSIXFKBIRVML-RBUKOAKNSA-N 7-cyclohexyl-n,n-dimethyl-2-[[5-[(1s,6r)-3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@@]1(CC[C@](C2)(N1)[H])[H])C(=O)N2C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCCC1 KSBSIXFKBIRVML-RBUKOAKNSA-N 0.000 claims 1
- VMHOCSPSLUBLHE-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,6-diazabicyclo[3.2.1]octane-3-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4NCC(C4)C3)N=C2N1C1CCCC1 VMHOCSPSLUBLHE-UHFFFAOYSA-N 0.000 claims 1
- MGVGOHXTHDTWHQ-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,8-diazabicyclo[3.2.1]octane-3-carbonyl)-4-methylpyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=C(C)C=3)C(=O)N3CC4CCC(N4)C3)N=C2N1C1CCCC1 MGVGOHXTHDTWHQ-UHFFFAOYSA-N 0.000 claims 1
- SOBQJDMKGXGEQA-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,8-diazabicyclo[3.2.1]octane-3-carbonyl)-6-methylpyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=C(C)C(C(=O)N4CC5CCC(N5)C4)=CC=3)N=C2N1C1CCCC1 SOBQJDMKGXGEQA-UHFFFAOYSA-N 0.000 claims 1
- QUGUCRTXIGFAAB-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,8-diazabicyclo[3.2.1]octane-8-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3C4CCC3CNC4)N=C2N1C1CCCC1 QUGUCRTXIGFAAB-UHFFFAOYSA-N 0.000 claims 1
- IUMNOHMCVRQIFR-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,9-diazabicyclo[3.3.1]nonane-3-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCCC(N4)C3)N=C2N1C1CCCC1 IUMNOHMCVRQIFR-UHFFFAOYSA-N 0.000 claims 1
- JMYHPWJJCGPKPL-UXHICEINSA-N 7-cyclopentyl-2-[[5-[(1r,6s)-4,9-diazabicyclo[4.2.1]nonane-4-carbonyl]pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@@]1(CC[C@](CC2)(N1)[H])[H])N2C(=O)C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 JMYHPWJJCGPKPL-UXHICEINSA-N 0.000 claims 1
- LCQFIXPBRDGHGG-HKUYNNGSSA-N 7-cyclopentyl-2-[[5-[(1s,4s)-2,5-diazabicyclo[2.2.1]heptane-2-carbonyl]pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@]1(NC[C@]2([H])C1)[H])N2C(=O)C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 LCQFIXPBRDGHGG-HKUYNNGSSA-N 0.000 claims 1
- JMYHPWJJCGPKPL-VQTJNVASSA-N 7-cyclopentyl-2-[[5-[(1s,6r)-4,9-diazabicyclo[4.2.1]nonane-4-carbonyl]pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@]1(CC[C@@](CC2)(N1)[H])[H])N2C(=O)C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 JMYHPWJJCGPKPL-VQTJNVASSA-N 0.000 claims 1
- UHLMUTYUXRIVIZ-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(1-oxo-3,4,6,7,8,8a-hexahydropyrrolo[1,2-a]pyrazin-2-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(C4CCCN4CC3)=O)N=C2N1C1CCCC1 UHLMUTYUXRIVIZ-UHFFFAOYSA-N 0.000 claims 1
- PBGMYLLXSOFMTR-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(CC4CCC(N4)C3)=O)N=C2N1C1CCCC1 PBGMYLLXSOFMTR-UHFFFAOYSA-N 0.000 claims 1
- RGGRAERHROXLKH-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(8-methyl-3,8-diazabicyclo[3.2.1]octane-3-carbonyl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)C(=O)N3CC4CCC(N4C)C3)N=C2N1C1CCCC1 RGGRAERHROXLKH-UHFFFAOYSA-N 0.000 claims 1
- GAAOQIXOPLWYKD-AREMUKBSSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(5r)-2-oxo-1-oxa-3,9-diazaspiro[4.5]decan-3-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N(C(O1)=O)C[C@@]21CCCNC2 GAAOQIXOPLWYKD-AREMUKBSSA-N 0.000 claims 1
- GAAOQIXOPLWYKD-SANMLTNESA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(5s)-2-oxo-1-oxa-3,9-diazaspiro[4.5]decan-3-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N(C(O1)=O)C[C@]21CCCNC2 GAAOQIXOPLWYKD-SANMLTNESA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- KXGOPETVBIUYIZ-RDJZCZTQSA-N C1(CCCC1)N1C(=CC2=C1N=C(N=C2)NC1=NC=C(C=C1)C(=O)N1[C@@H]2CN[C@H](C1)C2)C(=O)O Chemical compound C1(CCCC1)N1C(=CC2=C1N=C(N=C2)NC1=NC=C(C=C1)C(=O)N1[C@@H]2CN[C@H](C1)C2)C(=O)O KXGOPETVBIUYIZ-RDJZCZTQSA-N 0.000 claims 1
- YFEWOOFDUZLOIC-KGLIPLIRSA-N CN(C)C(C(N1)=CC2=C1N=C(NC(C=C1)=NC=C1N(C[C@H](CC1)N[C@H]1C1)C1=O)N=C2)=O Chemical compound CN(C)C(C(N1)=CC2=C1N=C(NC(C=C1)=NC=C1N(C[C@H](CC1)N[C@H]1C1)C1=O)N=C2)=O YFEWOOFDUZLOIC-KGLIPLIRSA-N 0.000 claims 1
- HYBFEEHWCKOPDK-LOCPCMAASA-N CN1C[C@@H]2[C@H](C1)CN(C2=O)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C Chemical compound CN1C[C@@H]2[C@H](C1)CN(C2=O)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C HYBFEEHWCKOPDK-LOCPCMAASA-N 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010023347 Keratoacanthoma Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- DQLSKESTXRBFDP-UHFFFAOYSA-N N-methyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CNC(=O)C1=CC2=C(N=CN=C2)N1 DQLSKESTXRBFDP-UHFFFAOYSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- JBXOTMIKJBDPAN-UHFFFAOYSA-N O=C1CC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CC3CCC(C2)N3.CN(C3=CC=CC=C3)C Chemical compound O=C1CC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CC3CCC(C2)N3.CN(C3=CC=CC=C3)C JBXOTMIKJBDPAN-UHFFFAOYSA-N 0.000 claims 1
- HTYLRIVMHDTPTG-MHDYBILJSA-N O=C1N(C[C@@H]2[C@H]1CNC2)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C Chemical compound O=C1N(C[C@@H]2[C@H]1CNC2)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C HTYLRIVMHDTPTG-MHDYBILJSA-N 0.000 claims 1
- HTYLRIVMHDTPTG-JGAZGGJJSA-N O=C1N(C[C@H]2[C@@H]1CNC2)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C Chemical compound O=C1N(C[C@H]2[C@@H]1CNC2)C=2C=CC(=NC2)NC=2N=CC1=C(N2)NC(=C1)C(=O)N.CN(C1=CC=CC=C1)C HTYLRIVMHDTPTG-JGAZGGJJSA-N 0.000 claims 1
- IPDGOMUDPWXKHK-UHFFFAOYSA-N O=C1OC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CCNCC2.CN(C2=CC=CC=C2)C Chemical compound O=C1OC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CCNCC2.CN(C2=CC=CC=C2)C IPDGOMUDPWXKHK-UHFFFAOYSA-N 0.000 claims 1
- ZXNFGCLFKLHORU-UHFFFAOYSA-N O=C1OC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CNCCC2.CN(C2=CC=CC=C2)C Chemical compound O=C1OC2(CN1C=1C=CC(=NC1)NC=1N=CC3=C(N1)NC(=C3)C(=O)N)CNCCC2.CN(C2=CC=CC=C2)C ZXNFGCLFKLHORU-UHFFFAOYSA-N 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 201000000497 familial melanoma Diseases 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000003911 head and neck carcinoma Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- MGJXBDMLVWIYOQ-UHFFFAOYSA-N methylazanide Chemical compound [NH-]C MGJXBDMLVWIYOQ-UHFFFAOYSA-N 0.000 claims 1
- WXCGPYFNDWQWHG-UHFFFAOYSA-N n,n-dimethyl-2-[[5-(3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl)pyridin-2-yl]amino]-7-phenylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(CC4CCC(N4)C3)=O)N=C2N1C1=CC=CC=C1 WXCGPYFNDWQWHG-UHFFFAOYSA-N 0.000 claims 1
- JMQDHZLNGSNZEH-UHFFFAOYSA-N n,n-dimethyl-7h-pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=CN=C2NC(C(=O)N(C)C)=CC2=C1 JMQDHZLNGSNZEH-UHFFFAOYSA-N 0.000 claims 1
- QLGFTMMDEPUTTK-UHFFFAOYSA-N n,n-dimethylpyrimidine-4-carboxamide Chemical compound CN(C)C(=O)C1=CC=NC=N1 QLGFTMMDEPUTTK-UHFFFAOYSA-N 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 210000001331 nose Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000008261 skin carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 0 C*(C)N1CC(C)CC(C)C1 Chemical compound C*(C)N1CC(C)CC(C)C1 0.000 description 38
- IUFRXYVUJWLFFS-UHFFFAOYSA-N C(C1)C2CNCC1NC2 Chemical compound C(C1)C2CNCC1NC2 IUFRXYVUJWLFFS-UHFFFAOYSA-N 0.000 description 2
- XJKNACDCUAFDHD-UHFFFAOYSA-N C(C1)C2NCCN1CC2 Chemical compound C(C1)C2NCCN1CC2 XJKNACDCUAFDHD-UHFFFAOYSA-N 0.000 description 2
- GOHPSJHRPIJNOF-UHFFFAOYSA-N C1C(CCCNC2)C2NC1 Chemical compound C1C(CCCNC2)C2NC1 GOHPSJHRPIJNOF-UHFFFAOYSA-N 0.000 description 2
- WTQANOMSKOCPEK-UHFFFAOYSA-N CCC1N(C)C(CC)CC1 Chemical compound CCC1N(C)C(CC)CC1 WTQANOMSKOCPEK-UHFFFAOYSA-N 0.000 description 2
- FJLGTCMSJKWHKL-UHFFFAOYSA-N CN(CC1)CC2NCC1OC2 Chemical compound CN(CC1)CC2NCC1OC2 FJLGTCMSJKWHKL-UHFFFAOYSA-N 0.000 description 2
- OBAXRSXTJUNZRQ-UHFFFAOYSA-N CN1CC(C2)C2C1 Chemical compound CN1CC(C2)C2C1 OBAXRSXTJUNZRQ-UHFFFAOYSA-N 0.000 description 2
- LUKBRIBWOWNLRW-UHFFFAOYSA-N CN1CC(C2)NCC2C1 Chemical compound CN1CC(C2)NCC2C1 LUKBRIBWOWNLRW-UHFFFAOYSA-N 0.000 description 2
- OUPIODYKEDELNJ-UHFFFAOYSA-N CN1CC2(CC2)NCC1 Chemical compound CN1CC2(CC2)NCC1 OUPIODYKEDELNJ-UHFFFAOYSA-N 0.000 description 2
- OJDDWFBNQVXOPZ-UHFFFAOYSA-N O=C1NCC(CC2)NC2C1 Chemical compound O=C1NCC(CC2)NC2C1 OJDDWFBNQVXOPZ-UHFFFAOYSA-N 0.000 description 2
- DJRNDULKXIEIBM-UHFFFAOYSA-N C(C1)CN2C1CCCNC2 Chemical compound C(C1)CN2C1CCCNC2 DJRNDULKXIEIBM-UHFFFAOYSA-N 0.000 description 1
- ONHPOXROAPYCGT-UHFFFAOYSA-N C(CC1)CC2N1CCNC2 Chemical compound C(CC1)CC2N1CCNC2 ONHPOXROAPYCGT-UHFFFAOYSA-N 0.000 description 1
- LQVCUGATZFCLAS-UHFFFAOYSA-N C1NCC2NC1COC2 Chemical compound C1NCC2NC1COC2 LQVCUGATZFCLAS-UHFFFAOYSA-N 0.000 description 1
- ULXBVKGHRJABDW-UHFFFAOYSA-N CCN(C)C(CNC)COC Chemical compound CCN(C)C(CNC)COC ULXBVKGHRJABDW-UHFFFAOYSA-N 0.000 description 1
- GHMBMLVKVRKVFX-UHFFFAOYSA-N CN(C(CC1)CCN1C1)C1=O Chemical compound CN(C(CC1)CCN1C1)C1=O GHMBMLVKVRKVFX-UHFFFAOYSA-N 0.000 description 1
- FIMQVRFSGKERNW-PZJWPPBQSA-N CN(C)C(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N(C)[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O Chemical compound CN(C)C(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N(C)[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O FIMQVRFSGKERNW-PZJWPPBQSA-N 0.000 description 1
- ZHKNIMYEUNBVIB-UHFFFAOYSA-N CN(CC(CNC1)C1C1)C1=O Chemical compound CN(CC(CNC1)C1C1)C1=O ZHKNIMYEUNBVIB-UHFFFAOYSA-N 0.000 description 1
- SEXCXAIQIMWSBF-UHFFFAOYSA-N CN(CC1)CC11CCNCC1 Chemical compound CN(CC1)CC11CCNCC1 SEXCXAIQIMWSBF-UHFFFAOYSA-N 0.000 description 1
- VPEKVGLYMNBOLA-UHFFFAOYSA-N CN(CC1)CC11NCCC1 Chemical compound CN(CC1)CC11NCCC1 VPEKVGLYMNBOLA-UHFFFAOYSA-N 0.000 description 1
- BIEJYKKRBBVADH-UHFFFAOYSA-N CN(CCC1)CC11CCNCC1 Chemical compound CN(CCC1)CC11CCNCC1 BIEJYKKRBBVADH-UHFFFAOYSA-N 0.000 description 1
- WGXIYIFYMGDZJY-UHFFFAOYSA-N CN1CC(CCCC2)N2CC1 Chemical compound CN1CC(CCCC2)N2CC1 WGXIYIFYMGDZJY-UHFFFAOYSA-N 0.000 description 1
- YQURLNGUWNDBIR-UHFFFAOYSA-N CN1CC(CNC2)C2C1 Chemical compound CN1CC(CNC2)C2C1 YQURLNGUWNDBIR-UHFFFAOYSA-N 0.000 description 1
- BNLKJYVQFIOOTE-UHFFFAOYSA-N CN1CC(CNC2)C2CC1 Chemical compound CN1CC(CNC2)C2CC1 BNLKJYVQFIOOTE-UHFFFAOYSA-N 0.000 description 1
- YHFOXLSMPVGJLK-UHFFFAOYSA-N CN1CN(CCC2)C2CCC1 Chemical compound CN1CN(CCC2)C2CCC1 YHFOXLSMPVGJLK-UHFFFAOYSA-N 0.000 description 1
- GVALVDSUZAFNAA-AZUAARDMSA-N CNC(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N(C)[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O Chemical compound CNC(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N(C)[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O GVALVDSUZAFNAA-AZUAARDMSA-N 0.000 description 1
- UJVHIJSYEJNERA-DLBZAZTESA-N CNC(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O Chemical compound CNC(c1cc2cnc(Nc(cc3)ncc3N(C[C@@H](CC3)N[C@@H]3C3)C3=O)nc2[n]1C1CCCC1)=O UJVHIJSYEJNERA-DLBZAZTESA-N 0.000 description 1
- BWQNNQDFBRFNHC-MSZQBOFLSA-N C[C@](CNC1)(CN2I)C1C2=O Chemical compound C[C@](CNC1)(CN2I)C1C2=O BWQNNQDFBRFNHC-MSZQBOFLSA-N 0.000 description 1
- VUAWVYBEPDXPRO-UHFFFAOYSA-N IN1CC(CNC2)C2C1 Chemical compound IN1CC(CNC2)C2C1 VUAWVYBEPDXPRO-UHFFFAOYSA-N 0.000 description 1
- PMFZHENGJAEDPC-UHFFFAOYSA-N O=C(C(CNC1)C1C1)N1I Chemical compound O=C(C(CNC1)C1C1)N1I PMFZHENGJAEDPC-UHFFFAOYSA-N 0.000 description 1
- QEQOYWOBYRWYNB-UHFFFAOYSA-N O=C1NCC(CNC2)C2C1 Chemical compound O=C1NCC(CNC2)C2C1 QEQOYWOBYRWYNB-UHFFFAOYSA-N 0.000 description 1
- UHFYTRKXKDDMME-UHFFFAOYSA-N O=C1NCCCC11CCNCC1 Chemical compound O=C1NCCCC11CCNCC1 UHFYTRKXKDDMME-UHFFFAOYSA-N 0.000 description 1
- AGBUHYGWJRLISC-UHFFFAOYSA-N O=C1NCCN2C1CCCC2 Chemical compound O=C1NCCN2C1CCCC2 AGBUHYGWJRLISC-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30624810P | 2010-02-19 | 2010-02-19 | |
| US61/306,248 | 2010-02-19 | ||
| US201161429372P | 2011-01-03 | 2011-01-03 | |
| US61/429,372 | 2011-01-03 | ||
| US201161429997P | 2011-01-05 | 2011-01-05 | |
| US61/429,997 | 2011-01-05 | ||
| PCT/EP2011/052353 WO2011101409A1 (en) | 2010-02-19 | 2011-02-17 | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013519707A JP2013519707A (ja) | 2013-05-30 |
| JP2013519707A5 true JP2013519707A5 (OSRAM) | 2014-03-13 |
| JP5788415B2 JP5788415B2 (ja) | 2015-09-30 |
Family
ID=44201966
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012553318A Active JP5788415B2 (ja) | 2010-02-19 | 2011-02-17 | Cdk4/6阻害剤としてのピロロピリミジン化合物 |
Country Status (38)
Families Citing this family (158)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ME02461B (me) | 2005-05-10 | 2017-02-20 | Incyte Holdings Corp | Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih |
| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| SG10201805844QA (en) | 2008-07-08 | 2018-08-30 | Incyte Holdings Corp | 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase |
| CN102186856B (zh) | 2008-08-22 | 2014-09-24 | 诺华股份有限公司 | 作为cdk抑制剂的吡咯并嘧啶化合物 |
| NZ592338A (en) | 2008-09-26 | 2012-11-30 | Oncomed Pharm Inc | Frizzled-binding agents and uses thereof |
| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Wnt拮抗劑及治療和篩選方法 |
| AU2011235904B2 (en) | 2010-04-01 | 2015-10-08 | Oncomed Pharmaceuticals, Inc. | Frizzled-binding agents and uses thereof |
| US20130035336A1 (en) * | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| US8501768B2 (en) * | 2011-05-17 | 2013-08-06 | Hoffmann-La Roche Inc. | Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds |
| AU2012279117A1 (en) | 2011-07-01 | 2014-01-09 | Novartis Ag | Combination therapy comprising a CDK4/6 inhibitor and a PI3K inhibitor for use in the treatment of cancer |
| WO2013086260A2 (en) * | 2011-12-09 | 2013-06-13 | Oncomed Pharmaceuticals, Inc. | Combination therapy for treatment of cancer |
| EP2831080B1 (en) | 2012-03-29 | 2017-03-15 | Francis Xavier Tavares | Lactam kinase inhibitors |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| RU2019102203A (ru) | 2012-07-11 | 2019-03-05 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
| HK1213044A1 (zh) | 2012-08-03 | 2016-06-24 | Foundation Medicine, Inc. | 人乳头瘤病毒作为肿瘤预後的预测因子 |
| US9266959B2 (en) | 2012-10-23 | 2016-02-23 | Oncomed Pharmaceuticals, Inc. | Methods of treating neuroendocrine tumors using frizzled-binding agents |
| SI2951183T1 (sl) | 2013-01-29 | 2019-07-31 | Aptinyx Inc. | Spiro-laktam NMDA receptorski modulatorji in njihove uporabe |
| US9359444B2 (en) | 2013-02-04 | 2016-06-07 | Oncomed Pharmaceuticals Inc. | Methods and monitoring of treatment with a Wnt pathway inhibitor |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| EP2967050A4 (en) | 2013-03-15 | 2016-09-28 | G1 Therapeutics Inc | HIGH-ACTIVE ANTINEOPLASTIC AND ANTIPROLIFERATIVE AGENTS |
| EP2968291B1 (en) | 2013-03-15 | 2025-04-16 | Pharmacosmos Holding A/S | Hspc-sparing treatments for rb-positive abnormal cellular proliferation |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| ES2900829T3 (es) | 2013-08-14 | 2022-03-18 | Novartis Ag | Terapia combinada para el tratamiento del cáncer |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| EP3660050A1 (en) | 2014-03-14 | 2020-06-03 | Novartis AG | Antibody molecules to lag-3 and uses thereof |
| US20150320754A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| US9717735B2 (en) | 2014-04-17 | 2017-08-01 | G1 Therapeutics, Inc. | Tricyclic lactams for use in HSPC-sparing treatments for RB-positive abnormal cellular proliferation |
| AU2015266492B2 (en) * | 2014-05-28 | 2017-11-02 | Fochon Pharmaceuticals, Ltd. | Certain protein kinase inhibitors |
| CN105294737B (zh) * | 2014-07-26 | 2019-02-12 | 广东东阳光药业有限公司 | Cdk类小分子抑制剂的化合物及其用途 |
| MX2017003254A (es) * | 2014-09-11 | 2017-10-12 | Janssen Pharmaceutica Nv | 2-azabiciclos sustituidos y su uso como moduladores de receptores de orexina. |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| CN114920840A (zh) | 2014-10-14 | 2022-08-19 | 诺华股份有限公司 | 针对pd-l1的抗体分子及其用途 |
| CN105111201B (zh) * | 2014-10-16 | 2017-01-11 | 上海页岩科技有限公司 | 5-甲基-2-(吡啶-2-基氨基)-8H-吡啶并[2,3-d]嘧啶-7-酮化合物 |
| US20170340733A1 (en) | 2014-12-19 | 2017-11-30 | Novartis Ag | Combination therapies |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| EA038045B1 (ru) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| JO3746B1 (ar) | 2015-03-10 | 2021-01-31 | Aduro Biotech Inc | تركيبات وطرق لتنشيط الإشارات المعتمدة على "منبه أو تحفيز جين انترفيرون" |
| AU2016228660B2 (en) * | 2015-03-11 | 2020-05-07 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Substituted 2-hydrogen-pyrazole derivative serving as anticancer drug |
| EP3316902A1 (en) | 2015-07-29 | 2018-05-09 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| PL3317301T3 (pl) | 2015-07-29 | 2021-11-15 | Novartis Ag | Terapie skojarzone zawierające cząsteczki przeciwciał przeciw lag-3 |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| MY198562A (en) | 2015-11-03 | 2023-09-05 | Janssen Biotech Inc | Antibodies specifically binding pd-1 and their uses |
| CN106810536A (zh) | 2015-11-30 | 2017-06-09 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| WO2017096323A1 (en) * | 2015-12-02 | 2017-06-08 | Astraea Therapeutics, Llc | Piperidinyl nociceptin receptor compounds |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| JP2019503349A (ja) | 2015-12-17 | 2019-02-07 | ノバルティス アーゲー | Pd−1に対する抗体分子およびその使用 |
| WO2017161253A1 (en) | 2016-03-18 | 2017-09-21 | Tufts Medical Center | Compositions and methods for treating and preventing metabolic disorders |
| US10449195B2 (en) | 2016-03-29 | 2019-10-22 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
| WO2017193872A1 (en) * | 2016-05-07 | 2017-11-16 | Shanghai Fochon Pharmaceutical Co., Ltd. | Certain protein kinase inhibitors |
| WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| CA3028751A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| EP3507367A4 (en) | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
| WO2018026763A1 (en) | 2016-08-01 | 2018-02-08 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| MX383650B (es) * | 2016-08-01 | 2025-03-14 | Aptinyx Inc | Moduladores del receptor nmda espiro-lactam y uso de los mismos. |
| SG11201900554YA (en) | 2016-08-01 | 2019-02-27 | Aptinyx Inc | Spiro-lactam nmda modulators and methods of using same |
| US20190192522A1 (en) | 2016-09-08 | 2019-06-27 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors |
| BR112019005526A2 (pt) | 2016-10-20 | 2019-06-18 | Pfizer | agentes antiproliferativos para tratamento de pah |
| WO2018081211A1 (en) * | 2016-10-26 | 2018-05-03 | Li George Y | Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide |
| WO2018089518A1 (en) | 2016-11-08 | 2018-05-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods of modulating anti-tumor immunity |
| CN110382495B (zh) | 2016-12-16 | 2022-04-05 | 基石药业(苏州)有限公司 | Cdk4/6抑制剂 |
| AU2018205262A1 (en) | 2017-01-06 | 2019-07-11 | G1 Therapeutics, Inc. | Combination therapy for the treatment of cancer |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| CN108794452B (zh) | 2017-05-05 | 2021-05-28 | 上海时莱生物技术有限公司 | 具有激酶抑制活性的化合物、其制备方法和用途 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EP3642240A1 (en) | 2017-06-22 | 2020-04-29 | Novartis AG | Antibody molecules to cd73 and uses thereof |
| MX392531B (es) | 2017-06-29 | 2025-03-24 | G1 Therapeutics Inc | Formas morficas de g1t38 y metodos de preparacion de las mismas. |
| JP7569688B2 (ja) | 2017-12-22 | 2024-10-18 | ハイバーセル,インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| WO2019136451A1 (en) | 2018-01-08 | 2019-07-11 | G1 Therapeutics, Inc. | G1t38 superior dosage regimes |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
| CN112204031B (zh) | 2018-01-31 | 2024-05-24 | 元羿生物科技(香港)有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| MA51846A (fr) * | 2018-02-15 | 2021-04-21 | Nuvation Bio Inc | Composés hétérocycliques utilisés en tant qu'inhibiteurs de kinases |
| JP7474709B2 (ja) | 2018-02-27 | 2024-04-25 | インサイト・コーポレイション | A2a/a2b阻害剤としてのイミダゾピリミジン及びトリアゾロピリミジン |
| JP7698418B2 (ja) * | 2018-03-13 | 2025-06-25 | ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム | Egfr活性化変異を有するがんを治療するための方法 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| US11174257B2 (en) | 2018-05-04 | 2021-11-16 | Incyte Corporation | Salts of an FGFR inhibitor |
| MA52940A (fr) | 2018-05-18 | 2021-04-28 | Incyte Corp | Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b |
| TWI869346B (zh) | 2018-05-30 | 2025-01-11 | 瑞士商諾華公司 | Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法 |
| AU2019297361B2 (en) | 2018-07-05 | 2024-06-27 | Incyte Corporation | Fused pyrazine derivatives as A2A / A2B inhibitors |
| CN120817904A (zh) | 2018-08-24 | 2025-10-21 | 法码科思莫斯有限公司 | 1,4-二氮杂螺[5.5]十一烷-3-酮改进的合成 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| JP7598642B2 (ja) * | 2018-10-12 | 2024-12-12 | ボード オブ リージェンツ オブ ザ ユニヴァーシティー オブ ネブラスカ | ホスホジエステラーゼ阻害剤 |
| CN111100128B (zh) * | 2018-10-26 | 2022-09-06 | 广安凯特制药有限公司 | 一种瑞博西尼中间产品的合成方法及其中间体化合物 |
| EP3902805A4 (en) * | 2018-12-28 | 2023-03-01 | SPV Therapeutics Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| CN114040764A (zh) | 2019-02-15 | 2022-02-11 | 因赛特公司 | 细胞周期素依赖性激酶2生物标记物及其用途 |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US20220296595A1 (en) | 2019-05-05 | 2022-09-22 | Qilu Regor Therapeutics Inc. | Cdk inhibitors |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN112094272A (zh) | 2019-06-18 | 2020-12-18 | 北京睿熙生物科技有限公司 | Cdk激酶抑制剂 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP2022543062A (ja) | 2019-08-01 | 2022-10-07 | インサイト・コーポレイション | Ido阻害剤の投与レジメン |
| BR112022002698A2 (pt) | 2019-08-14 | 2022-07-19 | Incyte Corp | Compostos de imidazolil pirimidinilamina como inibidores de cdk2 |
| CN114502590A (zh) | 2019-09-18 | 2022-05-13 | 诺华股份有限公司 | Entpd2抗体、组合疗法、以及使用这些抗体和组合疗法的方法 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MX2022004390A (es) | 2019-10-11 | 2022-08-08 | Incyte Corp | Aminas biciclicas como inhibidores de la cinasa dependiente de ciclina 2 (cdk2). |
| PH12022550892A1 (en) | 2019-10-14 | 2023-05-03 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| MX2022012780A (es) | 2020-04-16 | 2023-01-18 | Incyte Corp | Inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras) triciclicos fusionados. |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| ES3048084T3 (en) | 2020-05-19 | 2025-12-09 | Pharmacosmos Holding As | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| CN114306245A (zh) | 2020-09-29 | 2022-04-12 | 深圳市药欣生物科技有限公司 | 无定形固体分散体的药物组合物及其制备方法 |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| CN112375081B (zh) * | 2020-11-23 | 2022-04-12 | 中国医学科学院医药生物技术研究所 | 具有抑制CDK4、6或9活性的吡咯[2,3-d]嘧啶衍生物及其制备方法和应用 |
| AR124154A1 (es) | 2020-11-27 | 2023-02-22 | Rhizen Pharmaceuticals Ag | Inhibidores de cdk |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022155941A1 (en) | 2021-01-25 | 2022-07-28 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors |
| WO2022206888A1 (en) | 2021-03-31 | 2022-10-06 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors and use thereof |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法 |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為fgfr抑制劑之三環雜環 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| WO2023283213A1 (en) | 2021-07-07 | 2023-01-12 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| EP4370515A1 (en) | 2021-07-14 | 2024-05-22 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| TW202320795A (zh) | 2021-07-26 | 2023-06-01 | 美商凱爾科迪股份有限公司 | 使用1-(4-{[4-(二甲胺基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二嗎啉-4-基-1,3,5-三-2-基)苯基]脲治療癌症之方法 |
| CA3229855A1 (en) | 2021-08-31 | 2023-03-09 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| WO2023036252A1 (zh) * | 2021-09-08 | 2023-03-16 | 希格生科(深圳)有限公司 | 吡咯并嘧啶类或吡咯并吡啶类衍生物及其医药用途 |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| MX2024004444A (es) | 2021-10-14 | 2024-05-08 | Incyte Corp | Compuestos de quinolina como inhibidores de la proteina del virus de sarcoma de rata kirsten (kras). |
| KR20240122783A (ko) | 2021-11-22 | 2024-08-13 | 인사이트 코포레이션 | Fgfr 저해제 및 kras 저해제를 포함하는 병용 요법 |
| WO2023102184A1 (en) | 2021-12-03 | 2023-06-08 | Incyte Corporation | Bicyclic amine compounds as cdk12 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| US20230192722A1 (en) | 2021-12-22 | 2023-06-22 | Incyte Corporation | Salts and solid forms of an fgfr inhibitor and processes of preparing thereof |
| WO2023168686A1 (en) | 2022-03-11 | 2023-09-14 | Qilu Regor Therapeutics Inc. | Substituted cyclopentanes as cdk2 inhibitors |
| WO2023116884A1 (en) | 2021-12-24 | 2023-06-29 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors and use thereof |
| JP2025512710A (ja) | 2022-03-07 | 2025-04-22 | インサイト・コーポレイション | Cdk2阻害剤の固体形態、塩、ならびに調製プロセス |
| WO2023213271A1 (en) * | 2022-05-05 | 2023-11-09 | Beigene , Ltd. | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
| TW202413359A (zh) | 2022-06-22 | 2024-04-01 | 美商英塞特公司 | 雙環胺cdk12抑制劑 |
| WO2024015731A1 (en) | 2022-07-11 | 2024-01-18 | Incyte Corporation | Fused tricyclic compounds as inhibitors of kras g12v mutants |
| EP4561991A1 (en) * | 2022-07-25 | 2025-06-04 | Cayman Chemical Company, Inc. | Novel heterocycles as spla2-x inhibitors |
| EP4561552A2 (en) * | 2022-07-29 | 2025-06-04 | Cedilla Therapeutics, Inc. | Cdk2 inhibitors and methods of using the same |
| WO2024220532A1 (en) | 2023-04-18 | 2024-10-24 | Incyte Corporation | Pyrrolidine kras inhibitors |
| US20240368156A1 (en) | 2023-04-18 | 2024-11-07 | Incyte Corporation | 2-azabicyclo[2.2.1]heptane kras inhibitors |
| WO2024254245A1 (en) | 2023-06-09 | 2024-12-12 | Incyte Corporation | Bicyclic amines as cdk2 inhibitors |
| US20250163079A1 (en) | 2023-11-01 | 2025-05-22 | Incyte Corporation | Kras inhibitors |
| US20250195536A1 (en) | 2023-12-13 | 2025-06-19 | Incyte Corporation | Bicyclooctane kras inhibitors |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| BR0308232A (pt) | 2002-03-07 | 2004-12-28 | Hoffmann La Roche | Inibidores de cinase p38 de piridina e pirimidina bicìclicas |
| JP2006516561A (ja) | 2003-01-17 | 2006-07-06 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 細胞増殖の阻害剤としての2−アミノピリジン置換ヘテロ環類 |
| CN101723891A (zh) | 2003-02-10 | 2010-06-09 | 沃泰克斯药物股份有限公司 | 通过使n-芳基氨基甲酸酯与卤代杂芳基反应制备n-杂芳基-n-芳基胺的方法和类似方法 |
| AP2006003559A0 (en) | 2003-09-05 | 2006-04-30 | Neurogen Corp Ventis Pharmaceuticals Inc | Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF 1 receptor ligands |
| WO2005023761A2 (en) | 2003-09-11 | 2005-03-17 | Kemia, Inc. | Cytokine inhibitors |
| MXPA06005578A (es) | 2003-11-17 | 2006-08-11 | Pfizer Prod Inc | Compuestos de pirrolopirimidina utiles en el tratamiento del cancer. |
| US7319102B1 (en) | 2003-12-09 | 2008-01-15 | The Procter & Gamble Company | Pyrrolo[2,3-d]pyrimidine cytokine inhibitors |
| AR049769A1 (es) * | 2004-01-22 | 2006-09-06 | Novartis Ag | Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina |
| EP1713806B1 (en) | 2004-02-14 | 2013-05-08 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| JP2007526906A (ja) | 2004-03-05 | 2007-09-20 | 大正製薬株式会社 | ピロロピリミジン誘導体 |
| RS52545B (sr) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| WO2005107760A1 (en) | 2004-04-30 | 2005-11-17 | Irm Llc | Compounds and compositions as inducers of keratinocyte differentiation |
| US20080167309A1 (en) | 2004-07-22 | 2008-07-10 | Astex Therapeutics, Ltd. | Pharmaceutical Compounds |
| WO2006042102A2 (en) | 2004-10-05 | 2006-04-20 | Neurogen Corporation | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| KR20070085286A (ko) | 2004-10-29 | 2007-08-27 | 티보텍 파마슈티칼즈 리미티드 | Hiv를 저해하는 바이사이클릭 피리미딘 유도체 |
| US7723340B2 (en) | 2005-01-13 | 2010-05-25 | Signal Pharmaceuticals, Llc | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith |
| US7521446B2 (en) | 2005-01-13 | 2009-04-21 | Signal Pharmaceuticals, Llc | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith |
| WO2006074985A1 (en) | 2005-01-14 | 2006-07-20 | Janssen Pharmaceutica N.V. | 5-membered annelated heterocyclic pyrimidines as kinase inhibitors |
| WO2006091737A1 (en) | 2005-02-24 | 2006-08-31 | Kemia, Inc. | Modulators of gsk-3 activity |
| JP2006241089A (ja) | 2005-03-04 | 2006-09-14 | Astellas Pharma Inc | ピロロピリミジン誘導体またはその塩 |
| WO2006137769A1 (en) | 2005-06-20 | 2006-12-28 | Astrazeneca Ab | Process for the preparation of 3,7-dihydroxy-1,5-diazacyclooctanes |
| DE102005030051A1 (de) | 2005-06-27 | 2006-12-28 | Grünenthal GmbH | Substituierte 1-Oxa-3,8-diazaspiro[4,5]-decan-2-on-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| US20070225304A1 (en) | 2005-09-06 | 2007-09-27 | Pharmacopeia Drug Discovery, Inc. | Aminopurine derivatives for treating neurodegenerative diseases |
| GB0520164D0 (en) | 2005-10-04 | 2005-11-09 | Novartis Ag | Organic compounds |
| WO2007040280A1 (ja) | 2005-10-06 | 2007-04-12 | Nippon Soda Co., Ltd. | 環状アミン化合物および有害生物防除剤 |
| WO2007058990A2 (en) | 2005-11-14 | 2007-05-24 | Kemia, Inc. | Therapy using cytokine inhibitors |
| GB0526246D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| BRPI0620151A2 (pt) | 2005-12-22 | 2010-06-29 | Wyeth Corp | composto; composição farmacêutica; método de tratar ou inibir o crescimento de células tumorais cancerosas em um mamìfero que deste necessita; método; e processo |
| BRPI0709007A2 (pt) | 2006-03-09 | 2011-06-21 | Pharmacopeia Inc | inibidores de 8-heteroarilpurina mnk2 para tratamento de distúrbios metabólicos |
| US7998978B2 (en) | 2006-05-01 | 2011-08-16 | Pfizer Inc. | Substituted 2-amino-fused heterocyclic compounds |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | Novartis Ag | 吡咯并嘧啶化合物及其用途 |
| WO2008135232A1 (en) | 2007-05-02 | 2008-11-13 | Riccardo Cortese | Use and compositions of purine derivatives for the treatment of proliferative disorders |
| WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
| ATE533771T1 (de) | 2007-11-20 | 2011-12-15 | Bristol Myers Squibb Co | Cyclopropylkondensierte indolobenzazepine als hcv-ns5b-inhibitoren |
| MX2010006457A (es) | 2007-12-19 | 2010-07-05 | Amgen Inc | Compuestos fusionados de piridina, pirimidina y triazina como inhibidores de ciclo celular. |
| CA2714177A1 (en) * | 2008-02-06 | 2009-08-13 | Novartis Ag | Pyrrolo [2,3-d] pyridines and use thereof as tyrosine kinase inhibitors |
| WO2009115084A2 (de) | 2008-03-20 | 2009-09-24 | Schebo Biotech Ag | Neue pyrrolopyrimidin-derivate und deren verwendungen |
| CN102186856B (zh) | 2008-08-22 | 2014-09-24 | 诺华股份有限公司 | 作为cdk抑制剂的吡咯并嘧啶化合物 |
| UY33226A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
| US20130035336A1 (en) | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer |
| AR083797A1 (es) | 2010-11-10 | 2013-03-20 | Novartis Ag | Succinato de dimetil-amida del acido 7-ciclopentil-2-(5-piperazin-1-il-piridin-2-il-amino)-7h-pirrolo-[2,3-d]pirimidin-6-carboxilico, proceso para prepararla, intermediarios de dicha sintesis y proceso de preparacion de los mismos |
-
2011
- 2011-02-15 UY UY33227A patent/UY33227A/es not_active Application Discontinuation
- 2011-02-17 PL PL11707115T patent/PL2536730T3/pl unknown
- 2011-02-17 CA CA2790637A patent/CA2790637C/en active Active
- 2011-02-17 PH PH1/2012/501649A patent/PH12012501649A1/en unknown
- 2011-02-17 MX MX2012009613A patent/MX2012009613A/es active IP Right Grant
- 2011-02-17 MA MA35209A patent/MA34066B1/fr unknown
- 2011-02-17 ES ES11707115.9T patent/ES2548532T3/es active Active
- 2011-02-17 SG SG2012058566A patent/SG183218A1/en unknown
- 2011-02-17 PE PE2012001259A patent/PE20121815A1/es not_active Application Discontinuation
- 2011-02-17 PT PT117071159T patent/PT2536730E/pt unknown
- 2011-02-17 AR ARP110100478 patent/AR080198A1/es unknown
- 2011-02-17 DK DK11707115.9T patent/DK2536730T3/en active
- 2011-02-17 WO PCT/EP2011/052353 patent/WO2011101409A1/en not_active Ceased
- 2011-02-17 RS RS20150623A patent/RS54263B1/sr unknown
- 2011-02-17 US US13/579,359 patent/US8957074B2/en active Active
- 2011-02-17 ME MEP-2015-157A patent/ME02202B/me unknown
- 2011-02-17 CN CN201180021222.6A patent/CN102918043B/zh active Active
- 2011-02-17 KR KR1020127024329A patent/KR101812357B1/ko active Active
- 2011-02-17 SI SI201130591T patent/SI2536730T1/sl unknown
- 2011-02-17 NZ NZ60175411A patent/NZ601754A/en not_active IP Right Cessation
- 2011-02-17 JP JP2012553318A patent/JP5788415B2/ja active Active
- 2011-02-17 UA UAA201209879A patent/UA108369C2/uk unknown
- 2011-02-17 EA EA201201161A patent/EA022355B1/ru not_active IP Right Cessation
- 2011-02-17 EP EP11707115.9A patent/EP2536730B1/en active Active
- 2011-02-17 BR BR112012020922-1A patent/BR112012020922B1/pt active IP Right Grant
- 2011-02-17 GE GEAP201112834A patent/GEP20146146B/en unknown
- 2011-02-17 HR HRP20151071TT patent/HRP20151071T1/hr unknown
- 2011-02-17 AU AU2011217286A patent/AU2011217286B2/en active Active
- 2011-02-18 TW TW100105536A patent/TWI503322B/zh not_active IP Right Cessation
-
2012
- 2012-08-14 ZA ZA2012/06079A patent/ZA201206079B/en unknown
- 2012-08-15 TN TNP2012000413A patent/TN2012000413A1/en unknown
- 2012-08-16 IL IL221520A patent/IL221520A/en not_active IP Right Cessation
- 2012-08-17 CL CL2012002270A patent/CL2012002270A1/es unknown
- 2012-08-17 HN HN2012001744A patent/HN2012001744A/es unknown
- 2012-08-17 NI NI201200135A patent/NI201200135A/es unknown
- 2012-08-17 DO DO2012000225A patent/DOP2012000225A/es unknown
- 2012-08-20 EC ECSP12012111 patent/ECSP12012111A/es unknown
-
2014
- 2014-12-12 US US14/568,410 patent/US9309252B2/en active Active
-
2015
- 2015-10-28 SM SM201500265T patent/SMT201500265B/it unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013519707A5 (OSRAM) | ||
| HRP20151071T1 (hr) | Spojevi pirolopirimidina kao inhibitori za cdk4/6 | |
| AU2015296322B2 (en) | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as CDK inhibitors and uses thereof | |
| EP3645121B1 (en) | Methods for treating huntington's disease | |
| JP6263269B2 (ja) | キナーゼ阻害剤及びその使用 | |
| JP7654071B2 (ja) | 複素環スピロ化合物及び使用方法 | |
| RU2020133727A (ru) | Ингибиторы shp2 и их применение | |
| JP2014506929A5 (OSRAM) | ||
| JP2011500774A5 (OSRAM) | ||
| RU2019115115A (ru) | Производные пиперидина в качестве ингибиторов убиквитин-специфической протеазы 7 | |
| JP2019535664A5 (OSRAM) | ||
| JP2015521600A5 (OSRAM) | ||
| SI2945632T1 (en) | HETEROBICYL-SUBSTITUTED- (1,2,4) TRIAZOLO (1,5-C) KINAZOLIN-5-AMIN COMPOUNDS SUITABLE FOR TREATMENT AND PREVENTION OF THE EMISSION OF THE CENTRAL LIVING SYSTEM | |
| RU2019120986A (ru) | Фармацевтическая комбинация, содержащая ингибитор alk и ингибитор shp2 | |
| HRP20150235T1 (hr) | Derivati pirimidina, njihovo dobivanje i njihova farmaceutska upotreba | |
| JP2015511245A5 (OSRAM) | ||
| JPWO2020081848A5 (OSRAM) | ||
| NZ601128A (en) | Certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor | |
| JP2015508075A5 (OSRAM) | ||
| HRP20161319T1 (hr) | Derivati 8-karbamoil-2-(2,3-disupstituirani pirid-6-il)-1,2,3,4-tetrahidroizokinolina kao sredstva za izazivanje apoptoze za liječenje karcinoma i imunih i autoimunih bolesti | |
| JP2016504363A5 (OSRAM) | ||
| ME02635B (me) | Novi derivati pirola, postupak njihove priprave i farmaceutski pripravci koji ih sadrže | |
| JP2015504057A5 (OSRAM) | ||
| RU2013109776A (ru) | Замещенные пиразолхиназолиновые производные в качестве ингибиторов киназы | |
| WO2022093856A1 (en) | Heterocyclic spiro compounds and methods of use |