ME02202B - Jedinjenja pirolopirimidina kao inhibitori cdk4/6 - Google Patents
Jedinjenja pirolopirimidina kao inhibitori cdk4/6Info
- Publication number
- ME02202B ME02202B MEP-2015-157A MEP15715A ME02202B ME 02202 B ME02202 B ME 02202B ME P15715 A MEP15715 A ME P15715A ME 02202 B ME02202 B ME 02202B
- Authority
- ME
- Montenegro
- Prior art keywords
- pyridin
- pyrrolo
- ylamino
- diaza
- cyclopentyl
- Prior art date
Links
- 101100005789 Caenorhabditis elegans cdk-4 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000004944 pyrrolopyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 20
- -1 dimethylamide 7-(4-tert-Butyl-phenyl)-2-[5-(3,8-diaza-bicyclo[3.2.1]octan-3-carbonyl)-pyridin-2-ylamino]-7H-pyrrolo[2 ,3-d]pyrimidine-6-carboxylic acids Chemical class 0.000 claims 15
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 7
- QKIUAMUSENSFQQ-UHFFFAOYSA-N dimethylazanide Chemical compound C[N-]C QKIUAMUSENSFQQ-UHFFFAOYSA-N 0.000 claims 6
- 238000012552 review Methods 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 230000007170 pathology Effects 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 108700020796 Oncogene Proteins 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 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
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([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
- 229940079593 drug Drugs 0.000 claims 2
- 210000003238 esophagus Anatomy 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- PUNCJUFFXSLLLA-LPHOPBHVSA-N 2-[[5-[(3ar,6as)-4-oxo-1,2,3,3a,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]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)N3C([C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCC1 PUNCJUFFXSLLLA-LPHOPBHVSA-N 0.000 claims 1
- NGJPQECPPQEKSH-YLJYHZDGSA-N 2-[[5-[(3as,6ar)-2-methyl-4-oxo-3,3a,6,6a-tetrahydro-1h-pyrrolo[3,4-c]pyrrol-5-yl]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)N3C([C@@H]4CN(C)C[C@@H]4C3)=O)N=C2N1C1CCCC1 NGJPQECPPQEKSH-YLJYHZDGSA-N 0.000 claims 1
- PUNCJUFFXSLLLA-VQIMIIECSA-N 2-[[5-[(3as,6ar)-4-oxo-1,2,3,3a,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]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)N3C([C@@H]4CNC[C@@H]4C3)=O)N=C2N1C1CCCC1 PUNCJUFFXSLLLA-VQIMIIECSA-N 0.000 claims 1
- BXALLQBVYDONPU-ICSRJNTNSA-N 2-[[5-[(3as,7ar)-6-oxo-2,3,3a,4,7,7a-hexahydro-1h-pyrrolo[3,4-c]pyridin-5-yl]pyridin-2-yl]amino]-7-cycloheptyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(C[C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCCCC1 BXALLQBVYDONPU-ICSRJNTNSA-N 0.000 claims 1
- PXFIUPLVBBAUKD-WMZOPIPTSA-N 2-[[5-[(3as,7ar)-6-oxo-2,3,3a,4,7,7a-hexahydro-1h-pyrrolo[3,4-c]pyridin-5-yl]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)N3C(C[C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCC1 PXFIUPLVBBAUKD-WMZOPIPTSA-N 0.000 claims 1
- JFBMZUGLNFOQBA-UHFFFAOYSA-N 7-cycloheptyl-2-[[5-(2,7-diazaspiro[3.5]nonane-7-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C(=O)N(CC1)CCC21CNC2 JFBMZUGLNFOQBA-UHFFFAOYSA-N 0.000 claims 1
- KSBSIXFKBIRVML-UHFFFAOYSA-N 7-cyclohexyl-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=C2N1C1CCCCC1 KSBSIXFKBIRVML-UHFFFAOYSA-N 0.000 claims 1
- HYLVNBXAOJUSTK-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(2,6-diazaspiro[3.3]heptane-2-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C(=O)N(C1)CC21CNC2 HYLVNBXAOJUSTK-UHFFFAOYSA-N 0.000 claims 1
- BWRSHZDVVSAUGM-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(2'-oxospiro[8-azabicyclo[3.2.1]octane-3,4'-pyrrolidine]-1'-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(CC4(C3)CC3CCC(N3)C4)=O)N=C2N1C1CCCC1 BWRSHZDVVSAUGM-UHFFFAOYSA-N 0.000 claims 1
- YCUZSIPULIEBBG-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(3-oxo-1,4-diazabicyclo[3.2.2]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(CN4CCC3CC4)=O)N=C2N1C1CCCC1 YCUZSIPULIEBBG-UHFFFAOYSA-N 0.000 claims 1
- OHOGKSHNJOSNJQ-BGYRXZFFSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(1r,5s)-3-oxa-7,9-diazabicyclo[3.3.1]nonane-9-carbonyl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1([C@]2([H])CNC[C@]1(COC2)[H])C(=O)C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 OHOGKSHNJOSNJQ-BGYRXZFFSA-N 0.000 claims 1
- FIMQVRFSGKERNW-PZJWPPBQSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(1s,6r)-9-methyl-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)(N1C)[H])[H])C(=O)N2C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 FIMQVRFSGKERNW-PZJWPPBQSA-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
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 206010016935 Follicular thyroid cancer 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 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
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma 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
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 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
- 230000001413 cellular effect Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 238000012512 characterization method Methods 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 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 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 201000000497 familial melanoma Diseases 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 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
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- MGJXBDMLVWIYOQ-UHFFFAOYSA-N methylazanide Chemical compound [NH-]C MGJXBDMLVWIYOQ-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
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 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
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000001696 purinergic effect Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- HKSQZEGSMBFHGC-UHFFFAOYSA-N pyrimidine-4-carboxamide Chemical compound NC(=O)C1=CC=NC=N1 HKSQZEGSMBFHGC-UHFFFAOYSA-N 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| PCT/EP2011/052353 WO2011101409A1 (en) | 2010-02-19 | 2011-02-17 | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
| EP11707115.9A EP2536730B1 (en) | 2010-02-19 | 2011-02-17 | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
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Country Status (38)
Families Citing this family (158)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101212967A (zh) | 2005-05-10 | 2008-07-02 | 因塞特公司 | 吲哚胺2,3-双加氧酶调节剂及其用法 |
| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| CN104042611B (zh) | 2008-07-08 | 2019-05-14 | 因塞特控股公司 | 作为吲哚胺2，3-双加氧酶的抑制剂的1，2，5-噁二唑 |
| BRPI0917791B1 (pt) | 2008-08-22 | 2022-03-22 | Novartis Ag | Compostos de pirrolopirimidina como inibidores de cdk, bem como composição farmacêutica e combinação |
| US7982013B2 (en) | 2008-09-26 | 2011-07-19 | Oncomed Pharmaceuticals, 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 |
| AU2011240735B2 (en) * | 2010-04-13 | 2015-01-29 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (CDK4/6) inhibitor and an mTOR 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 |
| CN103635189B (zh) | 2011-07-01 | 2016-05-04 | 诺华股份有限公司 | 用于治疗癌症的含有cdk4/6抑制剂和pi3k抑制剂的联合治疗 |
| EP2788378A4 (en) * | 2011-12-09 | 2015-09-09 | Oncomed Pharm Inc | ASSOCIATION THERAPY FOR THE TREATMENT OF CANCER |
| CA2868966C (en) | 2012-03-29 | 2021-01-26 | Francis Xavier Tavares | Lactam kinase inhibitors |
| EP3495367B1 (en) | 2012-06-13 | 2020-09-30 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| EP4119676A1 (en) | 2012-08-03 | 2023-01-18 | Foundation Medicine, Inc. | Human papilloma virus as predictor of cancer prognosis |
| JP2015536933A (ja) | 2012-10-23 | 2015-12-24 | オンコメッド ファーマシューティカルズ インコーポレイテッド | Ｗｎｔ経路結合剤を用いて神経内分泌腫瘍を処置する方法 |
| ES2935352T3 (es) | 2013-01-29 | 2023-03-06 | Aptinyx Inc | Moduladores de receptores NMDA de espiro-lactama y sus usos |
| AU2014212081A1 (en) | 2013-02-04 | 2015-08-13 | Oncomed Pharmaceuticals, Inc. | Methods and monitoring of treatment with a Wnt pathway inhibitor |
| 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 |
| 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 |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| US20140271460A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Highly Active Anti-Neoplastic and Anti-Proliferative Agents |
| ES2761406T3 (es) | 2013-03-15 | 2020-05-19 | G1 Therapeutics Inc | Protección transitoria de células normales durante una quimioterapia |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| HRP20211879T1 (hr) | 2013-08-14 | 2022-03-04 | Novartis Ag | Kombinirana terapija za liječenje raka |
| PH12016500739B1 (en) | 2013-10-25 | 2022-04-29 | Blueprint Medicines Corp | Inhibitors of the fibrolast growth factor receptor |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| 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 |
| KR102442436B1 (ko) | 2014-03-14 | 2022-09-15 | 노파르티스 아게 | Lag-3에 대한 항체 분자 및 그의 용도 |
| WO2015160986A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2015161288A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use as anti-neoplastic and anti-proliferative agents |
| DK3149008T3 (en) | 2014-05-28 | 2019-04-01 | Shanghai Fochon Pharmaceutical Co Ltd | Specific 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. |
| EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| 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 |
| 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 |
| EA201790834A1 (ru) | 2014-10-14 | 2018-01-31 | Новартис Аг | Молекулы антител к pd-l1 и их применение |
| 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 |
| WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| EA035817B1 (ru) | 2015-03-10 | 2020-08-14 | Адуро Байотек, Инк. | Композиции и способы для активации сигналинга, зависимого от "гена стимулятора интерферона" |
| KR102615733B1 (ko) | 2015-03-11 | 2023-12-18 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 항암제로서의 치환 2-h-피라졸 유도체 |
| EP3316902A1 (en) | 2015-07-29 | 2018-05-09 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| ES2878188T3 (es) | 2015-07-29 | 2021-11-18 | Novartis Ag | Terapias de combinación que comprenden moléculas de anticuerpos contra LAG-3 |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| MA43186B1 (fr) | 2015-11-03 | 2022-03-31 | Janssen Biotech Inc | Anticorps se liant spécifiquement à pd-1 et leurs utilisations |
| 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 |
| US10112924B2 (en) * | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| CN121181546A (zh) * | 2015-12-02 | 2025-12-23 | 阿斯特来亚治疗有限责任公司 | 哌啶基痛敏肽受体化合物 |
| WO2017106656A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
| 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 |
| US10835535B2 (en) * | 2016-05-07 | 2020-11-17 | Shanghai Fochon Pharmaceutical Co., Ltd. | Certain protein kinase inhibitors |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| MX2019000200A (es) | 2016-07-01 | 2019-09-26 | G1 Therapeutics Inc | Agentes antiproliferativos basados en pirimidina. |
| WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| CA3031563C (en) | 2016-08-01 | 2023-12-05 | Aptinyx Inc. | Spiro-lactam nmda modulators and methods of using same |
| KR102503590B1 (ko) | 2016-08-01 | 2023-02-24 | 앱티닉스 인크. | 스피로-락탐 nmda 수용체 조정제 및 그의 용도 |
| EA201990424A1 (ru) * | 2016-08-01 | 2019-08-30 | Аптиникс Инк. | Спиролактамовые модуляторы nmda-рецептора и их применение |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| CA3040815C (en) | 2016-10-20 | 2021-07-20 | Steven Martin Evans | Anti-proliferative agents for treating 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 |
| EA201991622A1 (ru) | 2017-01-06 | 2020-01-23 | Г1 Терапьютикс, Инк. | Комплексная терапия для лечения рака |
| 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 |
| US20200172628A1 (en) | 2017-06-22 | 2020-06-04 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| KR102659211B1 (ko) | 2017-06-29 | 2024-04-18 | 쥐원 쎄라퓨틱스, 인크. | G1t38의 형체 형태 및 그의 제조 방법 |
| 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 |
| MY205589A (en) | 2018-01-08 | 2024-10-28 | 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 |
| SG11202007256PA (en) | 2018-01-31 | 2020-08-28 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| JP2021514359A (ja) | 2018-02-15 | 2021-06-10 | ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． | キナーゼ阻害剤としての複素環式化合物 |
| CA3092470A1 (en) | 2018-02-27 | 2019-09-06 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| KR20200132902A (ko) * | 2018-03-13 | 2020-11-25 | 보드 오브 리전츠, 더 유니버시티 오브 텍사스 시스템 | Egfr 활성화 돌연변이를 갖는 암의 치료 방법 |
| US11466004B2 (en) | 2018-05-04 | 2022-10-11 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
| CN112566912A (zh) | 2018-05-04 | 2021-03-26 | 因赛特公司 | Fgfr抑制剂的盐 |
| WO2019222677A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| AR126019A1 (es) | 2018-05-30 | 2023-09-06 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
| AU2019297361B2 (en) | 2018-07-05 | 2024-06-27 | Incyte Corporation | Fused pyrazine derivatives as A2A / A2B inhibitors |
| EP3840756B1 (en) | 2018-08-24 | 2025-11-05 | Pharmacosmos Holding A/S | Improved synthesis of 1,4-diazaspiro[5.5]undecan-3-one |
| 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 |
| US20230065740A1 (en) * | 2018-12-28 | 2023-03-02 | Spv Therapeutics Inc. | Cyclin-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 |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| MA54947A (fr) | 2019-02-15 | 2021-12-22 | Incyte Corp | Biomarqueurs de kinase 2 dépendant de la cycline et leurs utilisations |
| 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 |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| KR102898876B1 (ko) | 2019-05-05 | 2025-12-12 | 제넨테크, 인크. | Cdk 억제제 |
| 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 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN114502196A (zh) | 2019-08-01 | 2022-05-13 | 因赛特公司 | Ido抑制剂的给药方案 |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| JP2022548881A (ja) | 2019-09-18 | 2022-11-22 | ノバルティス アーゲー | Ｅｎｔｐｄ２抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法 |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | 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). |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| 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 |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| EP4135844A1 (en) | 2020-04-16 | 2023-02-22 | Incyte Corporation | Fused tricyclic kras inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| KR20230012547A (ko) | 2020-05-19 | 2023-01-26 | 쥐원 쎄라퓨틱스, 인크. | 의학적 장애의 치료를 위한 시클린-의존성 키나제 억제 화합물 |
| 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 |
| US11767320B2 (en) | 2020-10-02 | 2023-09-26 | 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 |
| TW202237585A (zh) | 2020-11-27 | 2022-10-01 | 瑞士商瑞森製藥公司 | Ｃｄｋ抑制劑 |
| 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 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US12441727B2 (en) | 2021-07-07 | 2025-10-14 | Incyte Corporation | Tricyclic compounds as inhibitors of KRAS |
| CA3224841A1 (en) | 2021-07-14 | 2023-01-19 | Zhenwu Li | Tricyclic compounds as inhibitors of kras |
| CA3227191A1 (en) | 2021-07-26 | 2023-02-02 | Celcuity Inc. | 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (gedatolisib) and its combinations for use in the treatment of cancer |
| 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 |
| US12030883B2 (en) | 2021-09-21 | 2024-07-09 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of KRAS |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| PE20242113A1 (es) | 2021-10-14 | 2024-10-28 | Incyte Corp | Compuestos de quinolina como inhibidores de kras |
| WO2023091746A1 (en) | 2021-11-22 | 2023-05-25 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a kras inhibitor |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2023122134A1 (en) | 2021-12-22 | 2023-06-29 | Incyte Corporation | Salts and solid forms of an fgfr inhibitor and processes of preparing thereof |
| TW202341982A (zh) | 2021-12-24 | 2023-11-01 | 大陸商上海齊魯銳格醫藥研發有限公司 | Ｃｄｋ２抑制劑及其用途 |
| WO2023168686A1 (en) | 2022-03-11 | 2023-09-14 | Qilu Regor Therapeutics Inc. | Substituted cyclopentanes as cdk2 inhibitors |
| AU2023232823A1 (en) | 2022-03-07 | 2024-09-12 | Incyte Corporation | Solid forms, salts, and processes of preparation of a cdk2 inhibitor |
| CN119156389A (zh) * | 2022-05-05 | 2024-12-17 | 百济神州有限公司 | 杂环化合物、其组合物和其治疗方法 |
| US20250353842A1 (en) | 2022-06-22 | 2025-11-20 | Incyte Corporation | Bicyclic amine cdk12 inhibitors |
| US20240101557A1 (en) | 2022-07-11 | 2024-03-28 | 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 |
| WO2024026484A2 (en) * | 2022-07-29 | 2024-02-01 | Cedilla Therapeutics, Inc. | Cdk2 inhibitors and methods of using the same |
| US20240368156A1 (en) | 2023-04-18 | 2024-11-07 | Incyte Corporation | 2-azabicyclo[2.2.1]heptane kras inhibitors |
| US20240390340A1 (en) | 2023-04-18 | 2024-11-28 | Incyte Corporation | Pyrrolidine 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 |
| WO2004065378A1 (en) | 2003-01-17 | 2004-08-05 | Warner-Lambert Company Llc | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| 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 |
| CA2537829A1 (en) | 2003-09-05 | 2005-03-17 | Neurogen Corporation | Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands |
| JP4895811B2 (ja) | 2003-09-11 | 2012-03-14 | ケミア，インコーポレイテッド | サイトカイン阻害剤 |
| JP2007511596A (ja) | 2003-11-17 | 2007-05-10 | ファイザー・プロダクツ・インク | 癌の治療において有用なピロロピリミジン化合物 |
| US7319102B1 (en) | 2003-12-09 | 2008-01-15 | The Procter & Gamble Company | Pyrrolo[2,3-d]pyrimidine cytokine inhibitors |
| PE20051089A1 (es) * | 2004-01-22 | 2006-01-25 | Novartis Ag | Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina |
| JP4989233B2 (ja) | 2004-02-14 | 2012-08-01 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| CN1926140A (zh) | 2004-03-05 | 2007-03-07 | 大正制药株式会社 | 吡咯并嘧啶衍生物 |
| DK2253614T3 (da) | 2004-04-07 | 2013-01-07 | Novartis Ag | IAP-inhibitorer |
| WO2005107760A1 (en) | 2004-04-30 | 2005-11-17 | Irm Llc | Compounds and compositions as inducers of keratinocyte differentiation |
| WO2006008545A2 (en) | 2004-07-22 | 2006-01-26 | Astex Therapeutics Limited | Thiazole and isothiazole derivatives as protein kinase inhibitors |
| WO2006042102A2 (en) | 2004-10-05 | 2006-04-20 | Neurogen Corporation | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| EP1807430B1 (en) | 2004-10-29 | 2014-07-23 | Janssen R&D Ireland | Hiv inhibiting bicyclic pyrimidine derivatives |
| US7521446B2 (en) | 2005-01-13 | 2009-04-21 | Signal Pharmaceuticals, Llc | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith |
| US7723340B2 (en) | 2005-01-13 | 2010-05-25 | 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 |
| AR054391A1 (es) | 2005-06-20 | 2007-06-20 | Astrazeneca Ab | Procedimiento para la preparacion de 3,7- dihidroxi-1,5-diazaciclooctanos |
| 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 |
| WO2007030438A2 (en) | 2005-09-06 | 2007-03-15 | Pharmacopeia, Inc. | Aminopurine derivatives for treating neurodegenerative diseases |
| GB0520164D0 (en) | 2005-10-04 | 2005-11-09 | Novartis Ag | Organic compounds |
| BRPI0616667B1 (pt) | 2005-10-06 | 2017-07-18 | Nippon Soda Co. , Ltd. | Compounds of cyclical amine or salts thereof or non-oxides thereof, and agents for control of fever |
| WO2007058990A2 (en) | 2005-11-14 | 2007-05-24 | Kemia, Inc. | Therapy using cytokine inhibitors |
| 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 |
| GB0526246D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| AU2007222982A1 (en) | 2006-03-09 | 2007-09-13 | Pharmacopeia, Inc. | 8-Heteroarylpurine Mnk2 inhibitors for treating metabolic disorders |
| CA2651072A1 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| JO3235B1 (ar) | 2006-05-26 | 2018-03-08 | Astex Therapeutics Ltd | مركبات بيررولوبيريميدين و استعمالاتها |
| 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 |
| MX2010005226A (es) | 2007-11-20 | 2010-05-27 | Bristol Myers Squibb Co | Inhibidores de ns5b de hcv de indolobenzazepina fusionados a ciclopropilo. |
| EP2231656A1 (en) * | 2007-12-19 | 2010-09-29 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| KR20130066703A (ko) | 2008-02-06 | 2013-06-20 | 노파르티스 아게 | 피롤로［２,３ｄ］피리미딘 및 티로신 키나제 억제제로서 그의 용도 |
| WO2009115084A2 (de) | 2008-03-20 | 2009-09-24 | Schebo Biotech Ag | Neue pyrrolopyrimidin-derivate und deren verwendungen |
| BRPI0917791B1 (pt) | 2008-08-22 | 2022-03-22 | Novartis Ag | Compostos de pirrolopirimidina como inibidores de cdk, bem como composição farmacêutica e combinação |
| UY33226A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
| AU2011240735B2 (en) | 2010-04-13 | 2015-01-29 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (CDK4/6) inhibitor and an mTOR inhibitor for treating cancer |
| US20120115878A1 (en) | 2010-11-10 | 2012-05-10 | John Vincent Calienni | Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof |
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