JP2018515526A5 - - Google Patents
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- 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
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- Prior art keywords
- salt
- compound
- pharmaceutical composition
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- 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.)
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- 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
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- 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
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- 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
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- 239000003886 aromatase inhibitor Substances 0.000 description 1
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- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 description 1
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 description 1
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- 239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
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- 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
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- 239000004052 folic acid antagonist Substances 0.000 description 1
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- 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
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- 229940124302 mTOR inhibitor Drugs 0.000 description 1
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- 230000011278 mitosis Effects 0.000 description 1
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- 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
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- 239000003197 protein kinase B inhibitor Substances 0.000 description 1
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- 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
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- 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
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- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3294742B1 (enExample) |
| JP (1) | JP6664414B2 (enExample) |
| WO (1) | WO2016180843A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016180843A1 (en) * | 2015-05-13 | 2016-11-17 | Boehringer Ingelheim International Gmbh | 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 |
| 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 |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | 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 |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| JP7693656B2 (ja) | 2019-10-11 | 2025-06-17 | インサイト・コーポレイション | Ｃｄｋ２阻害剤としての二環式アミン |
| 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 |
| US9150578B2 (en) * | 2012-01-23 | 2015-10-06 | Boehringer Ingelheim International Gmbh | 5,8-dihydro-6H-pyrazolo[3,4-h]quinazolines as IGF-1R/IR inhibitors |
| WO2016180843A1 (en) * | 2015-05-13 | 2016-11-17 | Boehringer Ingelheim International Gmbh | 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 |
-
2016
- 2016-05-10 WO PCT/EP2016/060481 patent/WO2016180843A1/en not_active Ceased
- 2016-05-10 US US15/572,992 patent/US10414769B2/en active Active
- 2016-05-10 EP EP16722644.8A patent/EP3294742B1/en active Active
- 2016-05-10 JP JP2017559026A patent/JP6664414B2/ja active Active
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