JP2018515526A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018515526A5 JP2018515526A5 JP2017559026A JP2017559026A JP2018515526A5 JP 2018515526 A5 JP2018515526 A5 JP 2018515526A5 JP 2017559026 A JP2017559026 A JP 2017559026A JP 2017559026 A JP2017559026 A JP 2017559026A JP 2018515526 A5 JP2018515526 A5 JP 2018515526A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- compound
- pharmaceutical composition
- formula
- membered heterocyclyl
- 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
- 150000001875 compounds Chemical class 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 26
- 238000011282 treatment Methods 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 7
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- -1 homopiperidinyl Chemical group 0.000 claims description 6
- 206010061218 Inflammation Diseases 0.000 claims description 5
- 230000009286 beneficial effect Effects 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 208000015181 infectious disease Diseases 0.000 claims description 5
- 230000004054 inflammatory process Effects 0.000 claims description 5
- 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 4
- 239000000824 cytostatic agent Substances 0.000 claims description 4
- 230000001085 cytostatic effect Effects 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 231100000433 cytotoxic Toxicity 0.000 claims description 3
- 230000001472 cytotoxic effect Effects 0.000 claims description 3
- 102000004218 Insulin-Like Growth Factor I Human genes 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 230000006806 disease prevention Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 230000005959 oncogenic signaling Effects 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 201000010099 disease Diseases 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 4
- 239000003102 growth factor Substances 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 102000009465 Growth Factor Receptors Human genes 0.000 description 3
- 108010009202 Growth Factor Receptors Proteins 0.000 description 3
- 238000011321 prophylaxis Methods 0.000 description 3
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 description 2
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 description 2
- 102000018233 Fibroblast Growth Factor Human genes 0.000 description 2
- 108050007372 Fibroblast Growth Factor Proteins 0.000 description 2
- 102000003745 Hepatocyte Growth Factor Human genes 0.000 description 2
- 108090000100 Hepatocyte Growth Factor Proteins 0.000 description 2
- 102000014429 Insulin-like growth factor Human genes 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 239000012828 PI3K inhibitor Substances 0.000 description 2
- 108010038512 Platelet-Derived Growth Factor Proteins 0.000 description 2
- 102000010780 Platelet-Derived Growth Factor Human genes 0.000 description 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 description 2
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 description 2
- 230000004663 cell proliferation Effects 0.000 description 2
- 229940035811 conjugated estrogen Drugs 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 229940126864 fibroblast growth factor Drugs 0.000 description 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 description 1
- 102100037263 3-phosphoinositide-dependent protein kinase 1 Human genes 0.000 description 1
- 102100023990 60S ribosomal protein L17 Human genes 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 229940126638 Akt inhibitor Drugs 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 229940127512 Androgen Synthesis Inhibitors Drugs 0.000 description 1
- 102100032187 Androgen receptor Human genes 0.000 description 1
- 229940123877 Aurora kinase inhibitor Drugs 0.000 description 1
- 108091007065 BIRCs Proteins 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 208000020084 Bone disease Diseases 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 230000005778 DNA damage Effects 0.000 description 1
- 231100000277 DNA damage Toxicity 0.000 description 1
- 102000001301 EGF receptor Human genes 0.000 description 1
- 108060006698 EGF receptor Proteins 0.000 description 1
- 239000012824 ERK inhibitor Substances 0.000 description 1
- 108010041308 Endothelial Growth Factors Proteins 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- 206010018364 Glomerulonephritis Diseases 0.000 description 1
- 101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 description 1
- 101500025419 Homo sapiens Epidermal growth factor Proteins 0.000 description 1
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 description 1
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 description 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 1
- 101000701396 Homo sapiens Serine/threonine-protein kinase 33 Proteins 0.000 description 1
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 1
- 101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 229940124647 MEK inhibitor Drugs 0.000 description 1
- 102100021760 Magnesium transporter protein 1 Human genes 0.000 description 1
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 description 1
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 description 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 description 1
- 239000012661 PARP inhibitor Substances 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 description 1
- 102100024028 Progonadoliberin-1 Human genes 0.000 description 1
- 101710089372 Programmed cell death protein 1 Proteins 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 description 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 1
- 101710100969 Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 description 1
- 102100029986 Receptor tyrosine-protein kinase erbB-3 Human genes 0.000 description 1
- 102100029981 Receptor tyrosine-protein kinase erbB-4 Human genes 0.000 description 1
- 101710100963 Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 description 1
- 108091007602 SLC58A1 Proteins 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 102100030515 Serine/threonine-protein kinase 33 Human genes 0.000 description 1
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 description 1
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 description 1
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 description 1
- 229940123237 Taxane Drugs 0.000 description 1
- 229940122803 Vinca alkaloid Drugs 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 150000003838 adenosines Chemical class 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 229940100198 alkylating agent Drugs 0.000 description 1
- 239000002168 alkylating agent Substances 0.000 description 1
- 108010080146 androgen receptors Proteins 0.000 description 1
- 230000002491 angiogenic effect Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940045799 anthracyclines and related substance Drugs 0.000 description 1
- 230000003432 anti-folate effect Effects 0.000 description 1
- 230000003388 anti-hormonal effect Effects 0.000 description 1
- 230000000340 anti-metabolite Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 229940127074 antifolate Drugs 0.000 description 1
- 229940100197 antimetabolite Drugs 0.000 description 1
- 239000002256 antimetabolite Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940045688 antineoplastic antimetabolites pyrimidine analogues Drugs 0.000 description 1
- 239000003886 aromatase inhibitor Substances 0.000 description 1
- 229940046844 aromatase inhibitors Drugs 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 239000003719 aurora kinase inhibitor Substances 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000000601 blood cell Anatomy 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 210000003321 cartilage cell Anatomy 0.000 description 1
- 206010009887 colitis Diseases 0.000 description 1
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 description 1
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 description 1
- 229940127089 cytotoxic agent Drugs 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 201000006828 endometrial hyperplasia Diseases 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 230000008472 epithelial growth Effects 0.000 description 1
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 239000004052 folic acid antagonist Substances 0.000 description 1
- 208000024386 fungal infectious disease Diseases 0.000 description 1
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 239000003668 hormone analog Substances 0.000 description 1
- 229940116978 human epidermal growth factor Drugs 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 206010020718 hyperplasia Diseases 0.000 description 1
- 230000001024 immunotherapeutic effect Effects 0.000 description 1
- 238000009169 immunotherapy Methods 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940124302 mTOR inhibitor Drugs 0.000 description 1
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 description 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 description 1
- 230000011278 mitosis Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- GVUGOAYIVIDWIO-UFWWTJHBSA-N nepidermin Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C(C)C)C(C)C)C1=CC=C(O)C=C1 GVUGOAYIVIDWIO-UFWWTJHBSA-N 0.000 description 1
- OSTGTTZJOCZWJG-UHFFFAOYSA-N nitrosourea Chemical compound NC(=O)N=NO OSTGTTZJOCZWJG-UHFFFAOYSA-N 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 150000003057 platinum Chemical class 0.000 description 1
- 108010056274 polo-like kinase 1 Proteins 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 239000003197 protein kinase B inhibitor Substances 0.000 description 1
- 230000004850 protein–protein interaction Effects 0.000 description 1
- 150000003212 purines Chemical class 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 229940121896 radiopharmaceutical Drugs 0.000 description 1
- 239000012217 radiopharmaceutical Substances 0.000 description 1
- 230000002799 radiopharmaceutical effect Effects 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 description 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 description 1
- 210000000130 stem cell Anatomy 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 description 1
- 239000003744 tubulin modulator Substances 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15167553.5 | 2015-05-13 | ||
| EP15167553 | 2015-05-13 | ||
| PCT/EP2016/060481 WO2016180843A1 (en) | 2015-05-13 | 2016-05-10 | New 5,8-dimethyl-9-phenyl-5,8-dihydro-6h-pyrazolo[3,4-h]quinazolin-2- yl)-(1 h-pyrazol-3-yl)-amines and derivatives as igf-1 r/ir inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018515526A JP2018515526A (ja) | 2018-06-14 |
| JP2018515526A5 true JP2018515526A5 (https=) | 2019-06-13 |
| JP6664414B2 JP6664414B2 (ja) | 2020-03-13 |
Family
ID=53181095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017559026A Active JP6664414B2 (ja) | 2015-05-13 | 2016-05-10 | ＩＧＦ−１Ｒ／ＩＲ阻害薬としての新規５，８−ジメチル−９−フェニル−５，８−ジヒドロ−６Ｈ−ピラゾロ［３，４−ｈ］キナゾリン−２−イル）−（１Ｈ−ピラゾール−３−イル）−アミン及び誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10414769B2 (https=) |
| EP (1) | EP3294742B1 (https=) |
| JP (1) | JP6664414B2 (https=) |
| WO (1) | WO2016180843A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3294742B1 (en) * | 2015-05-13 | 2020-01-08 | Boehringer Ingelheim International GmbH | New (5,8-dimethyl-9-phenyl-5,8-dihydro-6h-pyrazolo[3,4-h)quinazolin-2-yl)-(1h-pyrazol-5-yl)-amines and theri derivatives as igf-1r/1r inhibitors. |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| 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 |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| BR112022003663A2 (pt) | 2019-08-28 | 2022-05-24 | Horizon Therapeutics Ireland Dac | Método para tratar oftalmopatia tireoidiana (ted) em um indivíduo com ted; método para reduzir proptose em pelo menos 2 mm em um indivíduo com oftalmopatia tireoidiana (ted); método para tratar ou reduzir a gravidade de diplopia em um indivíduo com oftalmopatia tireoidiana (ted); método para tratar ou reduzir a gravidade de oftalmopatia tireoidiana (ted); método para reduzir proptose em um olho em um indivíduo com oftalmopatia tireoidiana (ted); método para reduzir pontuação de atividade clínica (cas) de oftalmopatia tireoidiana (ted); método para a) reduzir proptose em pelo menos 2 mm e b) reduzir a pontuação de atividade clínica (cas) em um indivíduo com oftalmopatia tireoidiana (ted); e método para melhorar a qualidade de vida em um indivíduo com oftalmopatia tireoidiana (ted) |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2025014774A1 (en) | 2023-07-07 | 2025-01-16 | Viridian Therapeutics, Inc. | Methods of treating active and chronic thyroid eye disease |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8735386B2 (en) * | 2010-07-23 | 2014-05-27 | Boehringer Ingelheim International Gmbh | Aminopyrazoloquinazolines |
| AR089776A1 (es) * | 2012-01-23 | 2014-09-17 | Boehringer Ingelheim Int | 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir |
| EP3294742B1 (en) * | 2015-05-13 | 2020-01-08 | Boehringer Ingelheim International GmbH | New (5,8-dimethyl-9-phenyl-5,8-dihydro-6h-pyrazolo[3,4-h)quinazolin-2-yl)-(1h-pyrazol-5-yl)-amines and theri derivatives as igf-1r/1r inhibitors. |
-
2016
- 2016-05-10 EP EP16722644.8A patent/EP3294742B1/en active Active
- 2016-05-10 JP JP2017559026A patent/JP6664414B2/ja active Active
- 2016-05-10 US US15/572,992 patent/US10414769B2/en active Active
- 2016-05-10 WO PCT/EP2016/060481 patent/WO2016180843A1/en not_active Ceased
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018515526A5 (https=) | ||
| CA3218237A1 (en) | Quinazoline derivatives useful as ras inhibitiors | |
| DK2017278T3 (en) | DIHYDROPYRAZOLOPYRIMIDINON DERIVATIVES | |
| JP5925808B2 (ja) | 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用 | |
| US9938264B2 (en) | Proteolysis targeting chimera compounds and methods of preparing and using same | |
| EP2788351B1 (en) | SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASE INHIBITORS | |
| CN111741954B (zh) | 用作egfr抑制剂的新型苯并咪唑化合物及衍生物 | |
| JP6118383B2 (ja) | 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 | |
| EP2101759B1 (en) | Methods of using mek inhibitors | |
| ES2558780T3 (es) | Imidazopiridazinas como inhibidores de la cinasa Akt | |
| KR102066297B1 (ko) | 헤테로사이클릭 화합물 및 이의 유형 3 수용체 티로신 키나아제의 조절인자로서의 용도 | |
| RU2006121337A (ru) | Производные пиразола и их применение в качестве ингибиторов рецепторных тирозинкиназ | |
| JP2019535672A (ja) | インダゾール−３−カルボキサミドの使用方法およびｗｎｔ／β−カテニンシグナル伝達経路阻害剤としてのそれらの使用 | |
| CA2683641A1 (en) | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha | |
| AU2004289672A1 (en) | Inhibition of FGFR3 and treatment of multiple myeloma | |
| EA036013B1 (ru) | Новые спиро[3h-индол-3,2'-пирролидин]-2(1h)-оновые соединения и производные в качестве ингибиторов mdm2-p53 | |
| JP2017508763A (ja) | ５−置換インダゾール−３−カルボキサミドならびにその調製および使用の方法 | |
| CN105960407A (zh) | 用于治疗炎症障碍的新盐类及其药物组合物 | |
| EP2935260A1 (de) | Bet-proteininhibitorische dihydropyridopyrazinone | |
| EP2616077A1 (en) | Anti-cancer activity of novel bicyclic heterocycles | |
| WO2010067886A1 (en) | Dihydropyrimidopyrimidine derivative | |
| TR201816387T4 (tr) | Bisiklik heterosikllerin antiviral aktivitesi. | |
| CN103608018A (zh) | 取代的2,3-二氢咪唑并[1,2-c]喹唑啉的用途 | |
| JPWO2021060453A5 (https=) | ||
| KR20240089275A (ko) | 피롤로[2,1-f][1,2,4]트리아진 및 그의 제조 및 용도 |