JP2017503813A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017503813A5 JP2017503813A5 JP2016546472A JP2016546472A JP2017503813A5 JP 2017503813 A5 JP2017503813 A5 JP 2017503813A5 JP 2016546472 A JP2016546472 A JP 2016546472A JP 2016546472 A JP2016546472 A JP 2016546472A JP 2017503813 A5 JP2017503813 A5 JP 2017503813A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- nitrogen
- optionally substituted
- 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 132
- 150000003839 salts Chemical class 0.000 claims description 130
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 123
- 229910052757 nitrogen Inorganic materials 0.000 claims description 74
- 229910052739 hydrogen Inorganic materials 0.000 claims description 71
- 239000001257 hydrogen Substances 0.000 claims description 71
- 125000001931 aliphatic group Chemical group 0.000 claims description 52
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 36
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 35
- 125000005842 heteroatom Chemical group 0.000 claims description 35
- 125000000623 heterocyclic group Chemical group 0.000 claims description 35
- 229910052760 oxygen Inorganic materials 0.000 claims description 35
- 239000001301 oxygen Substances 0.000 claims description 35
- 229910052799 carbon Inorganic materials 0.000 claims description 32
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 31
- 229910052717 sulfur Inorganic materials 0.000 claims description 30
- 239000011593 sulfur Substances 0.000 claims description 30
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 27
- 125000005843 halogen group Chemical group 0.000 claims description 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 25
- 150000002431 hydrogen Chemical group 0.000 claims description 21
- 125000001624 naphthyl group Chemical group 0.000 claims description 21
- 125000002947 alkylene group Chemical group 0.000 claims description 20
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 19
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 19
- 125000002723 alicyclic group Chemical group 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 125000001153 fluoro group Chemical group F* 0.000 claims description 16
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 14
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 11
- -1 chloro, methyl Chemical group 0.000 claims description 10
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 10
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 9
- 239000000203 mixture Substances 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 229940124597 therapeutic agent Drugs 0.000 claims description 8
- 239000003937 drug carrier Substances 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 claims description 4
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 0.000 claims description 4
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 230000002757 inflammatory effect Effects 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 206010002198 Anaphylactic reaction Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims description 2
- 208000006029 Cardiomegaly Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims description 2
- 239000005977 Ethylene Substances 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 206010019280 Heart failures Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000007536 Thrombosis Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000038016 acute inflammation Diseases 0.000 claims description 2
- 230000006022 acute inflammation Effects 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 230000036783 anaphylactic response Effects 0.000 claims description 2
- 208000003455 anaphylaxis Diseases 0.000 claims description 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000037976 chronic inflammation Diseases 0.000 claims description 2
- 230000006020 chronic inflammation Effects 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 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 description 2
- 229940121647 egfr inhibitor Drugs 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 2
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 2
- 150000004917 tyrosine kinase inhibitor derivatives Chemical group 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 1
- 0 CClc(cc1)cc(*)c1Cl Chemical compound CClc(cc1)cc(*)c1Cl 0.000 description 29
- RNEMUWDQJSRDMQ-UHFFFAOYSA-N CC(C)c(cccc1)c1Cl Chemical compound CC(C)c(cccc1)c1Cl RNEMUWDQJSRDMQ-UHFFFAOYSA-N 0.000 description 4
- JTQKFJWXQHKANB-UHFFFAOYSA-N CCc(cc1)cc(F)c1F Chemical compound CCc(cc1)cc(F)c1F JTQKFJWXQHKANB-UHFFFAOYSA-N 0.000 description 4
- BLDNWXVISIXWKZ-UHFFFAOYSA-N CCc(cc1)ccc1F Chemical compound CCc(cc1)ccc1F BLDNWXVISIXWKZ-UHFFFAOYSA-N 0.000 description 4
- GGLWSLBFZLEDEF-UHFFFAOYSA-N CCc(ccc(F)c1)c1F Chemical compound CCc(ccc(F)c1)c1F GGLWSLBFZLEDEF-UHFFFAOYSA-N 0.000 description 4
- LMWWLNKVUIHGBR-UHFFFAOYSA-N CCc(cccc1)c1F Chemical compound CCc(cccc1)c1F LMWWLNKVUIHGBR-UHFFFAOYSA-N 0.000 description 4
- CSARJIQZOSVYHA-UHFFFAOYSA-N Cc(ccc(F)c1)c1Cl Chemical compound Cc(ccc(F)c1)c1Cl CSARJIQZOSVYHA-UHFFFAOYSA-N 0.000 description 4
- LRLRAYMYEXQKID-UHFFFAOYSA-N Cc1ccc(C(F)(F)F)cc1 Chemical compound Cc1ccc(C(F)(F)F)cc1 LRLRAYMYEXQKID-UHFFFAOYSA-N 0.000 description 4
- PMCOWOCKUQWYRL-UHFFFAOYSA-N Cc1nc(C)ncc1 Chemical compound Cc1nc(C)ncc1 PMCOWOCKUQWYRL-UHFFFAOYSA-N 0.000 description 3
- LVILGAOSPDLNRM-UHFFFAOYSA-N Cc1ncncc1 Chemical compound Cc1ncncc1 LVILGAOSPDLNRM-UHFFFAOYSA-N 0.000 description 3
- ZYBGAMKVRIXRDI-UHFFFAOYSA-N CC(C)N(C1)CC1(F)F Chemical compound CC(C)N(C1)CC1(F)F ZYBGAMKVRIXRDI-UHFFFAOYSA-N 0.000 description 2
- RZEAFTDKXQTDJE-UHFFFAOYSA-N CC(C)c(ccc(Cl)c1)c1Cl Chemical compound CC(C)c(ccc(Cl)c1)c1Cl RZEAFTDKXQTDJE-UHFFFAOYSA-N 0.000 description 2
- HIZIRPVSPJYCJR-UHFFFAOYSA-N CC1=NC(C(F)(F)F)NC=C1 Chemical compound CC1=NC(C(F)(F)F)NC=C1 HIZIRPVSPJYCJR-UHFFFAOYSA-N 0.000 description 2
- QWNYXDCVDPAVOO-UHFFFAOYSA-N CCN(C1)CC1(F)F Chemical compound CCN(C1)CC1(F)F QWNYXDCVDPAVOO-UHFFFAOYSA-N 0.000 description 2
- MNOFPJZMZIBMBK-UHFFFAOYSA-N CCc(cc(cc1)[F]C)c1F Chemical compound CCc(cc(cc1)[F]C)c1F MNOFPJZMZIBMBK-UHFFFAOYSA-N 0.000 description 2
- GPOFSFLJOIAMSA-UHFFFAOYSA-N CCc(cc1)ccc1Cl Chemical compound CCc(cc1)ccc1Cl GPOFSFLJOIAMSA-UHFFFAOYSA-N 0.000 description 2
- MJTYPPBFTMKLGA-UHFFFAOYSA-N CCc(ccc(Cl)c1)c1Cl Chemical compound CCc(ccc(Cl)c1)c1Cl MJTYPPBFTMKLGA-UHFFFAOYSA-N 0.000 description 2
- CKQINTYJQOUAOQ-UHFFFAOYSA-N CCc1cc(C(F)(F)F)ccc1 Chemical compound CCc1cc(C(F)(F)F)ccc1 CKQINTYJQOUAOQ-UHFFFAOYSA-N 0.000 description 2
- YEZPWKIUIAEMDJ-UHFFFAOYSA-N Cc(cc(cc1)[F]C)c1F Chemical compound Cc(cc(cc1)[F]C)c1F YEZPWKIUIAEMDJ-UHFFFAOYSA-N 0.000 description 2
- WISXXOGOMDYNSN-UHFFFAOYSA-N Cc(cc1)nc(C)c1N Chemical compound Cc(cc1)nc(C)c1N WISXXOGOMDYNSN-UHFFFAOYSA-N 0.000 description 2
- FUNUTBJJKQIVSY-UHFFFAOYSA-N Cc(ccc(Cl)c1)c1Cl Chemical compound Cc(ccc(Cl)c1)c1Cl FUNUTBJJKQIVSY-UHFFFAOYSA-N 0.000 description 2
- MKFCYQTVSDCXAQ-UHFFFAOYSA-N Cc(ccc(Cl)c1)c1F Chemical compound Cc(ccc(Cl)c1)c1F MKFCYQTVSDCXAQ-UHFFFAOYSA-N 0.000 description 2
- IBSQPLPBRSHTTG-UHFFFAOYSA-N Cc(cccc1)c1Cl Chemical compound Cc(cccc1)c1Cl IBSQPLPBRSHTTG-UHFFFAOYSA-N 0.000 description 2
- VJYXZJGDFJJDGF-UHFFFAOYSA-N Cc1cc(C(F)(F)F)ccc1 Chemical compound Cc1cc(C(F)(F)F)ccc1 VJYXZJGDFJJDGF-UHFFFAOYSA-N 0.000 description 2
- BTQZKHUEUDPRST-UHFFFAOYSA-N Cc1cc(F)ccc1 Chemical compound Cc1cc(F)ccc1 BTQZKHUEUDPRST-UHFFFAOYSA-N 0.000 description 2
- GETTZEONDQJALK-UHFFFAOYSA-N FC(c1ccccc1)(F)F Chemical compound FC(c1ccccc1)(F)F GETTZEONDQJALK-UHFFFAOYSA-N 0.000 description 2
- 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
- CWTLCUOLPNLRQQ-UHFFFAOYSA-N CC(Nc1cc(-c2cnc(C)c(NS(c(ccc(F)c3)c3F)(=O)=O)c2)ccn1)=O Chemical compound CC(Nc1cc(-c2cnc(C)c(NS(c(ccc(F)c3)c3F)(=O)=O)c2)ccn1)=O CWTLCUOLPNLRQQ-UHFFFAOYSA-N 0.000 description 1
- WGCIAJRBTDMFIO-UHFFFAOYSA-N Cc(c(-c1ccnc(NC(C2CC2)=O)c1)cnc1Cl)c1N Chemical compound Cc(c(-c1ccnc(NC(C2CC2)=O)c1)cnc1Cl)c1N WGCIAJRBTDMFIO-UHFFFAOYSA-N 0.000 description 1
- QGXZAZZCEUKMGZ-UHFFFAOYSA-N Cc(cc1)nc(C)c1C#N Chemical compound Cc(cc1)nc(C)c1C#N QGXZAZZCEUKMGZ-UHFFFAOYSA-N 0.000 description 1
- XPENFJAKMNONFL-UHFFFAOYSA-N Cc1nc(-c2ccccc2)ncc1 Chemical compound Cc1nc(-c2ccccc2)ncc1 XPENFJAKMNONFL-UHFFFAOYSA-N 0.000 description 1
- JHOQVQSTUMAGNQ-UHFFFAOYSA-N Cc1nc(C(F)(F)F)ncc1 Chemical compound Cc1nc(C(F)(F)F)ncc1 JHOQVQSTUMAGNQ-UHFFFAOYSA-N 0.000 description 1
- WRMHJGFQWZQEFO-UHFFFAOYSA-N Cc1nc(C2CC2)ncc1 Chemical compound Cc1nc(C2CC2)ncc1 WRMHJGFQWZQEFO-UHFFFAOYSA-N 0.000 description 1
- BSKHPKMHTQYZBB-UHFFFAOYSA-N Cc1ncccc1 Chemical compound Cc1ncccc1 BSKHPKMHTQYZBB-UHFFFAOYSA-N 0.000 description 1
- CAWHJQAVHZEVTJ-UHFFFAOYSA-N Cc1nccnc1 Chemical compound Cc1nccnc1 CAWHJQAVHZEVTJ-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- YXBLVHLPXCTIQN-UHFFFAOYSA-N O=S(c(ccc(F)c1)c1F)=O Chemical compound O=S(c(ccc(F)c1)c1F)=O YXBLVHLPXCTIQN-UHFFFAOYSA-N 0.000 description 1
- QHWNQKHTDTYPTH-UHFFFAOYSA-N O=SC(C(F)=C1)=CCC1F Chemical compound O=SC(C(F)=C1)=CCC1F QHWNQKHTDTYPTH-UHFFFAOYSA-N 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000013375 chromatographic separation Methods 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 150000003463 sulfur Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461927055P | 2014-01-14 | 2014-01-14 | |
| US61/927,055 | 2014-01-14 | ||
| US201462054742P | 2014-09-24 | 2014-09-24 | |
| US62/054,742 | 2014-09-24 | ||
| PCT/US2015/011191 WO2015108861A1 (en) | 2014-01-14 | 2015-01-13 | Heteroaryls and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017503813A JP2017503813A (ja) | 2017-02-02 |
| JP2017503813A5 true JP2017503813A5 (enExample) | 2018-02-22 |
| JP6609258B2 JP6609258B2 (ja) | 2019-11-20 |
Family
ID=53543363
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546472A Active JP6609258B2 (ja) | 2014-01-14 | 2015-01-13 | ヘテロアリール及びそれらの使用 |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US9802960B2 (enExample) |
| EP (1) | EP3094325B1 (enExample) |
| JP (1) | JP6609258B2 (enExample) |
| KR (1) | KR20160122736A (enExample) |
| CN (1) | CN105916503B (enExample) |
| AP (1) | AP2016009368A0 (enExample) |
| AU (1) | AU2015206652A1 (enExample) |
| BR (1) | BR112016016289B1 (enExample) |
| CA (1) | CA2935867C (enExample) |
| CL (1) | CL2016001805A1 (enExample) |
| CR (1) | CR20160363A (enExample) |
| DO (1) | DOP2016000173A (enExample) |
| EA (1) | EA032458B1 (enExample) |
| EC (1) | ECSP16067303A (enExample) |
| ES (1) | ES2908042T3 (enExample) |
| GE (1) | GEP20196983B (enExample) |
| IL (1) | IL246755A0 (enExample) |
| MX (1) | MX2016009135A (enExample) |
| MY (1) | MY182908A (enExample) |
| PE (1) | PE20161313A1 (enExample) |
| PH (1) | PH12016501388A1 (enExample) |
| SG (1) | SG11201604820XA (enExample) |
| TN (1) | TN2016000270A1 (enExample) |
| TW (1) | TWI662024B (enExample) |
| UY (1) | UY35951A (enExample) |
| WO (1) | WO2015108861A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104230922B (zh) * | 2013-06-19 | 2016-12-28 | 中国科学院上海药物研究所 | 一类五元杂环并吡啶类化合物及其制备方法和用途 |
| US10202373B2 (en) | 2014-01-14 | 2019-02-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9802960B2 (en) | 2014-01-14 | 2017-10-31 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| LT3365334T (lt) * | 2015-10-21 | 2024-09-10 | Otsuka Pharmaceutical Co., Ltd. | Benzolaktamo junginiai kaip baltymų kinazės inhibitoriai |
| US11179399B2 (en) | 2016-02-19 | 2021-11-23 | Sprint Bioscience Ab | 6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes |
| WO2017140841A1 (en) | 2016-02-19 | 2017-08-24 | Sprint Bioscience Ab | 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes |
| WO2018144791A1 (en) * | 2017-02-03 | 2018-08-09 | Millennium Pharmaceuticals, Inc. | Combination of vps34 inhibitors and mtor inhibitors |
| GB201706327D0 (en) * | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| WO2019038387A1 (en) * | 2017-08-23 | 2019-02-28 | Sprint Bioscience Ab | PYRIDYLPYRIDONE COMPOUNDS |
| TWI785102B (zh) | 2017-08-23 | 2022-12-01 | 瑞典商斯普林特生物科技公司 | 吡啶胺-吡啶酮及嘧啶胺-吡啶酮化合物 |
| PL3672967T3 (pl) | 2017-08-23 | 2022-01-31 | Sprint Bioscience Ab | Związki azaindolilopirydonu i diazaindolilopirydonu |
| HUE058661T2 (hu) | 2017-08-23 | 2022-09-28 | Sprint Bioscience Ab | Morfolinilpiridon vegyületek |
| EP3684761A1 (en) | 2017-09-18 | 2020-07-29 | Basf Se | Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi |
| UA126458C2 (uk) | 2018-02-13 | 2022-10-05 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| EP3820572B1 (en) | 2018-07-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| KR102328682B1 (ko) * | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020045941A1 (ko) * | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| CA3153531A1 (en) | 2019-09-11 | 2021-03-18 | Prelude Therapeutics Incorporated | Cdk inhibitors and their use as pharmaceuticals |
| CN112574207B (zh) * | 2019-09-30 | 2023-04-11 | 南京药石科技股份有限公司 | Erk1/2蛋白激酶抑制剂及其用途 |
| CN115135648B (zh) * | 2020-02-13 | 2024-02-09 | 劲方医药科技(上海)有限公司 | 二氢萘啶酮类化合物，其制法与医药上的用途 |
| US11801238B2 (en) | 2020-11-25 | 2023-10-31 | Deciphera Pharmaceuticals, Llc | Anti-viral activity of VPS34 inhibitors |
| TWI824626B (zh) * | 2021-08-02 | 2023-12-01 | 大陸商勁方醫藥科技(上海)有限公司 | Ripk1抑制劑的晶型及其酸式鹽和其酸式鹽的晶型 |
| EP4444429A1 (en) | 2021-12-09 | 2024-10-16 | Deciphera Pharmaceuticals, LLC | Raf kinase inhibitors and methods of use thereof |
| WO2024084360A1 (en) | 2022-10-18 | 2024-04-25 | Pfizer Inc. | Patatin-like phospholipase domain-containing protein 3 (pnpla3) modifiers |
| WO2024084363A1 (en) | 2022-10-18 | 2024-04-25 | Pfizer Inc. | Use of patatin-like phospholipase domain-containing protein 3 compounds |
| GB202216324D0 (en) * | 2022-11-02 | 2022-12-14 | Cerevance Ltd | Novel compounds |
| WO2025184010A1 (en) * | 2024-03-01 | 2025-09-04 | Merck Sharp & Dohme Llc | N-biaryl sulfonamides as modulators of the hippo pathway |
Family Cites Families (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003286876A1 (en) | 2002-11-01 | 2004-06-07 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of jak and other protein kinases |
| FR2850652B1 (fr) | 2003-01-31 | 2008-05-30 | Aventis Pharma Sa | Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| SE0402735D0 (sv) | 2004-11-09 | 2004-11-09 | Astrazeneca Ab | Novel compounds |
| WO2006051311A1 (en) | 2004-11-12 | 2006-05-18 | Galapagos Nv | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| GB0425026D0 (en) * | 2004-11-12 | 2004-12-15 | Biofocus Discovery Ltd | Compounds which bind to the active site of protein kinase enzymes |
| RU2423351C2 (ru) * | 2004-12-16 | 2011-07-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний |
| ZA200704971B (en) * | 2004-12-16 | 2008-09-25 | Vertex Pharma | Pyrid-2-ones useful as inhibitors of Tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
| JP2009537621A (ja) | 2006-05-22 | 2009-10-29 | アストラゼネカ アクチボラグ | インドール誘導体 |
| US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
| ES2549862T3 (es) | 2006-08-30 | 2015-11-02 | Cellzome Limited | Derivados de triazol como inhibidores de quinasa |
| RU2469034C2 (ru) | 2006-12-04 | 2012-12-10 | Астразенека Аб | Химические соединения |
| EP2094682A2 (en) | 2006-12-22 | 2009-09-02 | Novartis AG | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
| UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
| EA201000104A1 (ru) | 2007-07-26 | 2010-08-30 | Новартис Аг | Производные пиримидина, применимые для лечения воспалительных или аллергических патологических состояний |
| JP5561702B2 (ja) | 2007-08-02 | 2014-07-30 | アムジエン・インコーポレーテツド | Ｐｉ３キナーゼ調節剤および使用方法 |
| WO2009039140A1 (en) | 2007-09-17 | 2009-03-26 | Smithkline Beecham Corporation | Pyridopyrimidine derivatives as pi3 kinase inhibitors |
| EP2211615A4 (en) | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| PE20091268A1 (es) | 2007-12-19 | 2009-09-19 | Amgen Inc | Derivados heterociclicos como inhibidores de pi3 quinasa |
| US8343966B2 (en) | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| US8309577B2 (en) | 2008-04-23 | 2012-11-13 | Bristol-Myers Squibb Company | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands |
| ES2474147T3 (es) | 2008-05-30 | 2014-07-08 | Amgen, Inc | Inhibidores de PI3 cinasa |
| JP5502858B2 (ja) | 2008-06-05 | 2014-05-28 | グラクソ グループ リミテッド | Ｐｉ３キナーゼの阻害剤として有用な４−カルボキサミドインダゾール誘導体 |
| WO2010008847A2 (en) | 2008-06-24 | 2010-01-21 | Takeda Pharmaceutical Company Limited | Pi3k/m tor inhibitors |
| WO2010007100A1 (en) | 2008-07-15 | 2010-01-21 | Cellzome Ltd | 7-substituted amino triazoles as pi3k inhibitors |
| RU2523448C2 (ru) | 2008-08-04 | 2014-07-20 | СиЭйчДиАй ФАУНДЕЙШН, Инк, | Ингибиторы кинуренин-3-монооксигеназы |
| JP2012508239A (ja) | 2008-11-11 | 2012-04-05 | イーライ リリー アンド カンパニー | Ｐ７０ｓ６キナーゼ阻害剤およびｍｔｏｒ阻害剤の併用療法 |
| WO2010057877A1 (en) * | 2008-11-18 | 2010-05-27 | Cellzome Limited | 7-pyridinyl- or phenyl- substituted triazolo [1, 5 -a] pyridines as pi3k inhibitors |
| TW201026695A (en) | 2008-12-12 | 2010-07-16 | Astrazeneca Ab | Piperidine compounds and uses thereof-596 |
| EP2432779A1 (en) | 2009-05-22 | 2012-03-28 | Exelixis, Inc. | Benzoxazepines based p13k/mt0r inhibitors against proliferative diseases |
| CN102471339A (zh) | 2009-07-15 | 2012-05-23 | 雅培制药有限公司 | 激酶的吡咯并吡啶抑制剂 |
| JP2011033670A (ja) * | 2009-07-30 | 2011-02-17 | Sony Corp | 光学ファインダユニットおよび撮像装置 |
| AU2010291206A1 (en) | 2009-09-04 | 2012-02-23 | Novartis Ag | Bipyridines useful for the treatment of proliferative diseases |
| JP5675850B2 (ja) * | 2010-02-05 | 2015-02-25 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ヘタリール−［１，８］ナフチリジン誘導体 |
| KR20130131293A (ko) | 2010-07-05 | 2013-12-03 | 메르크 파텐트 게엠베하 | 키나아제 - 유도된 질환의 치료에 유용한 바이피리딜 유도체 |
| DK2592934T3 (en) | 2010-07-16 | 2015-10-26 | Nivalis Therapeutics Inc | NOVEL dihydropyridin-2 (1H) -one compounds as S-NITROSOGLUTATHIONREDUKTASEINHIBITORER and neurokinin-3 receptor antagonists |
| US8916553B2 (en) | 2010-07-26 | 2014-12-23 | Bristol-Myers Squibb Company | Sulfonamide compounds useful as CYP17 inhibitors |
| US8478700B2 (en) | 2010-08-11 | 2013-07-02 | Brightedge Technologies, Inc. | Opportunity identification and forecasting for search engine optimization |
| WO2012021696A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP2603216A4 (en) | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| WO2012037108A1 (en) | 2010-09-13 | 2012-03-22 | Glaxosmithkline Llc | Aminoquinoline derivatives as antiviral agents |
| WO2012066065A1 (en) | 2010-11-17 | 2012-05-24 | Novartis Ag | Phenyl-heteroaryl amine compounds and their uses |
| CA2816679A1 (en) * | 2010-11-17 | 2012-05-24 | Novartis Ag | 3-(aminoaryl)-pyridine compounds |
| BR112013015449A2 (pt) * | 2010-12-21 | 2016-09-20 | Novartis Ag | compostos de bi-heteroarila como inibidores de vps23 |
| PT2655375E (pt) | 2010-12-23 | 2015-03-02 | Sanofi Sa | Derivados de pirimidinona, sua preparação e sua utilização farmacêutica |
| US8669370B2 (en) * | 2011-01-26 | 2014-03-11 | Sanofi | Substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals |
| WO2012101066A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyridine biaryl amine compounds and their uses |
| CN103339110A (zh) | 2011-01-28 | 2013-10-02 | 诺瓦提斯公司 | 作为cdk9抑制剂的取代的杂-联芳基化合物及其用途 |
| WO2012101064A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| DE102011077104A1 (de) | 2011-06-07 | 2012-12-13 | Siemens Aktiengesellschaft | Verfahren zur Gewinnung von metallhaltigen Wertstoffen aus einem metallhaltige Wertstoffe enthaltenden suspensionsartigen Massestrom |
| KR101502500B1 (ko) | 2011-07-01 | 2015-03-16 | 주식회사 엘지화학 | 비수 전해액 및 이를 이용한 리튬 이차전지 |
| UA111382C2 (uk) * | 2011-10-10 | 2016-04-25 | Оріон Корпорейшн | Інгібітори протеїнкінази |
| JP2015503505A (ja) | 2011-12-23 | 2015-02-02 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | ヘテロアリールおよびその使用 |
| BR112014020773A2 (pt) | 2012-02-22 | 2020-10-27 | Sanford-Burnham Medical Research Institute | compostos de sulfonamida e seus usos como inibidores tnap |
| WO2013152063A1 (en) * | 2012-04-05 | 2013-10-10 | Boehringer Ingelheim International Gmbh | Naphthyridinone derivatives as inhibitors of cytomegalovirus dna polymerase |
| FR2992314B1 (fr) | 2012-06-22 | 2015-10-16 | Sanofi Sa | Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique |
| WO2014053533A1 (en) * | 2012-10-05 | 2014-04-10 | Sanofi | Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation |
| EP2903613B1 (en) | 2012-10-08 | 2017-11-22 | Merck Sharp & Dohme Corp. | Pyrazole derivatives useful as inhibitors of irak4 activity |
| WO2014083327A1 (en) | 2012-11-27 | 2014-06-05 | Md Pharma Ab | Adenine derivatives suitable for the treatment of (inter alia) muscular dystrophy |
| GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
| BR112015016580A2 (pt) * | 2013-01-11 | 2017-07-11 | Fujifilm Corp | composto heterocíclico contendo nitrogênio ou sal deste |
| CN105189481A (zh) | 2013-03-13 | 2015-12-23 | 艾伯维公司 | 吡啶cdk9激酶抑制剂 |
| US9242969B2 (en) * | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| US9802960B2 (en) | 2014-01-14 | 2017-10-31 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US10202373B2 (en) | 2014-01-14 | 2019-02-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP3191478B1 (en) * | 2014-09-12 | 2019-05-08 | Novartis AG | Compounds and compositions as raf kinase inhibitors |
| UY36294A (es) * | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
-
2015
- 2015-01-13 US US14/596,052 patent/US9802960B2/en active Active
- 2015-01-13 PE PE2016001225A patent/PE20161313A1/es unknown
- 2015-01-13 CA CA2935867A patent/CA2935867C/en active Active
- 2015-01-13 TN TN2016000270A patent/TN2016000270A1/en unknown
- 2015-01-13 MX MX2016009135A patent/MX2016009135A/es unknown
- 2015-01-13 WO PCT/US2015/011191 patent/WO2015108861A1/en not_active Ceased
- 2015-01-13 AP AP2016009368A patent/AP2016009368A0/en unknown
- 2015-01-13 EA EA201691421A patent/EA032458B1/ru not_active IP Right Cessation
- 2015-01-13 MY MYPI2016702312A patent/MY182908A/en unknown
- 2015-01-13 AU AU2015206652A patent/AU2015206652A1/en not_active Abandoned
- 2015-01-13 BR BR112016016289-7A patent/BR112016016289B1/pt active IP Right Grant
- 2015-01-13 CR CR20160363A patent/CR20160363A/es unknown
- 2015-01-13 GE GEAP201514237A patent/GEP20196983B/en unknown
- 2015-01-13 CN CN201580004591.2A patent/CN105916503B/zh active Active
- 2015-01-13 EP EP15737173.3A patent/EP3094325B1/en active Active
- 2015-01-13 ES ES15737173T patent/ES2908042T3/es active Active
- 2015-01-13 SG SG11201604820XA patent/SG11201604820XA/en unknown
- 2015-01-13 KR KR1020167022343A patent/KR20160122736A/ko not_active Withdrawn
- 2015-01-13 JP JP2016546472A patent/JP6609258B2/ja active Active
- 2015-01-14 UY UY0001035951A patent/UY35951A/es not_active Application Discontinuation
- 2015-01-14 TW TW104101242A patent/TWI662024B/zh not_active IP Right Cessation
-
2016
- 2016-07-12 DO DO2016000173A patent/DOP2016000173A/es unknown
- 2016-07-13 IL IL246755A patent/IL246755A0/en unknown
- 2016-07-13 PH PH12016501388A patent/PH12016501388A1/en unknown
- 2016-07-14 CL CL2016001805A patent/CL2016001805A1/es unknown
- 2016-08-11 EC ECIEPI201667303A patent/ECSP16067303A/es unknown
- 2016-11-09 US US15/347,334 patent/US9751854B2/en active Active
-
2017
- 2017-08-01 US US15/665,506 patent/US10538533B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017503813A5 (enExample) | ||
| JP7471232B2 (ja) | Ｐｏｌｙｂｒｏｍｏ－１（ｐｂｒｍ１）の小分子分解剤 | |
| JP2013536193A5 (enExample) | ||
| AU766081B2 (en) | Phthalazine derivatives for treating inflammatory diseases | |
| JP2017502092A5 (enExample) | ||
| EP3227280B1 (en) | Substituted pyridines as bromodomain inhibitors | |
| CN103402519B (zh) | 肿瘤治疗剂 | |
| JP2015503504A5 (enExample) | ||
| US10934274B2 (en) | Quinoline derivatives as TAM RTK inhibitors | |
| US10016408B2 (en) | Chemokine CXCR4 receptor modulators and uses related thereto | |
| JP2019517487A5 (enExample) | ||
| WO2014096965A2 (en) | Novel heterocyclic compounds as bromodomain inhibitors | |
| JP2015503505A5 (enExample) | ||
| IL237831A (en) | Inhibitors of histone demethylases | |
| WO2014080290A2 (en) | Cyclic amines as bromodomain inhibitors | |
| HK1246273A1 (en) | Substituted pyridines as bromodomain inhibitors | |
| JP2017518981A5 (enExample) | ||
| EP3227281A1 (en) | Substituted pyridinones as bromodomain inhibitors | |
| CA2966452A1 (en) | Substituted bicyclic compounds as bromodomain inhibitors | |
| CN105473581A (zh) | 作为溴结构域抑制剂的新取代的双环化合物 | |
| JP2019502763A5 (enExample) | ||
| JP2014513110A5 (enExample) | ||
| CA2905841A1 (en) | Quinazoline and naphthyridine derivatives useful in the treatment of fibrotic disorders | |
| JP2024540600A (ja) | 選択的ｐａｒｐ１阻害剤およびその用途 | |
| JP2016514688A5 (enExample) |