JP2018531982A5 - - Google Patents
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- JP2018531982A5 JP2018531982A5 JP2018522556A JP2018522556A JP2018531982A5 JP 2018531982 A5 JP2018531982 A5 JP 2018531982A5 JP 2018522556 A JP2018522556 A JP 2018522556A JP 2018522556 A JP2018522556 A JP 2018522556A JP 2018531982 A5 JP2018531982 A5 JP 2018531982A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- formula
- hydrogen
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims description 154
- 150000001875 compounds Chemical class 0.000 claims description 86
- 229910052739 hydrogen Inorganic materials 0.000 claims description 54
- 239000001257 hydrogen Substances 0.000 claims description 54
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 42
- 125000002947 alkylene group Chemical group 0.000 claims description 41
- 150000003839 salts Chemical class 0.000 claims description 35
- 125000005843 halogen group Chemical group 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 26
- 125000001424 substituent group Chemical group 0.000 claims description 26
- 208000023504 respiratory system disease Diseases 0.000 claims description 24
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 23
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 22
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000004432 carbon atom Chemical group C* 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 12
- 208000006673 asthma Diseases 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000003566 oxetanyl group Chemical group 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 10
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 10
- 206010006448 Bronchiolitis Diseases 0.000 claims description 9
- 230000000414 obstructive effect Effects 0.000 claims description 9
- YEGFDJOAFMPJSE-UHFFFAOYSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CCN(CC2)C)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CCN(CC2)C)N=1 YEGFDJOAFMPJSE-UHFFFAOYSA-N 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 8
- 241000124008 Mammalia Species 0.000 claims description 7
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 6
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 6
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 6
- 206010014561 Emphysema Diseases 0.000 claims description 6
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 206010035664 Pneumonia Diseases 0.000 claims description 6
- 206010035742 Pneumonitis Diseases 0.000 claims description 6
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 6
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims description 6
- 206010069351 acute lung injury Diseases 0.000 claims description 6
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 6
- 206010006451 bronchitis Diseases 0.000 claims description 6
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 6
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 6
- 239000002002 slurry Substances 0.000 claims description 6
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 5
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 125000006239 protecting group Chemical group 0.000 claims description 4
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims description 3
- HROWLWGDTOBEDM-UHFFFAOYSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CN(C2)C)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CN(C2)C)N=1 HROWLWGDTOBEDM-UHFFFAOYSA-N 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- PRNDBSRPZSZAPK-UHFFFAOYSA-N C(C)(CC)N(CCN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)C Chemical compound C(C)(CC)N(CCN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)C PRNDBSRPZSZAPK-UHFFFAOYSA-N 0.000 claims description 2
- VKFCLOVOQMXKJM-UHFFFAOYSA-N C(C)(CC)N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F Chemical compound C(C)(CC)N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F VKFCLOVOQMXKJM-UHFFFAOYSA-N 0.000 claims description 2
- YKKSLFAFHDNXRX-UHFFFAOYSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CN(C2)C(C)C)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C2CN(C2)C(C)C)N=1 YKKSLFAFHDNXRX-UHFFFAOYSA-N 0.000 claims description 2
- AOGXHIHTHRCTPK-UHFFFAOYSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCN(C)CC)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCN(C)CC)N=1 AOGXHIHTHRCTPK-UHFFFAOYSA-N 0.000 claims description 2
- ZFFSYYHNBNAIRW-KRWDZBQOSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCN2[C@H](CCC2)C)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCN2[C@H](CCC2)C)N=1 ZFFSYYHNBNAIRW-KRWDZBQOSA-N 0.000 claims description 2
- SNPLAOHHBAWLMU-UHFFFAOYSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCNC2CC(C2)OC)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)CCNC2CC(C2)OC)N=1 SNPLAOHHBAWLMU-UHFFFAOYSA-N 0.000 claims description 2
- JBYYBYKZQWGOJL-KRWDZBQOSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C[C@@H]2NCCOC2)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C[C@@H]2NCCOC2)N=1 JBYYBYKZQWGOJL-KRWDZBQOSA-N 0.000 claims description 2
- JBYYBYKZQWGOJL-QGZVFWFLSA-N C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C[C@H]2NCCOC2)N=1 Chemical compound C(C)C=1C(=CC(=C(C=1)O)F)C1=CC=C2C(=NNC2=C1)C=1NC2=C(CN(CC2)C[C@H]2NCCOC2)N=1 JBYYBYKZQWGOJL-QGZVFWFLSA-N 0.000 claims description 2
- CUIBPLIFKMBESI-UHFFFAOYSA-N C1(CC1)N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F Chemical compound C1(CC1)N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F CUIBPLIFKMBESI-UHFFFAOYSA-N 0.000 claims description 2
- FLPXNQWEAODYRF-UHFFFAOYSA-N CN(CC(CN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)F)C Chemical compound CN(CC(CN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)F)C FLPXNQWEAODYRF-UHFFFAOYSA-N 0.000 claims description 2
- YXKUPJSJNAKRLQ-UHFFFAOYSA-N CN(CCN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)C Chemical compound CN(CCN1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F)C YXKUPJSJNAKRLQ-UHFFFAOYSA-N 0.000 claims description 2
- HGQQGQFLBDQYCO-UHFFFAOYSA-N N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F Chemical compound N1CC(C1)N1CC2=C(CC1)NC(=N2)C1=NNC2=CC(=CC=C12)C1=CC(=C(C=C1CC)O)F HGQQGQFLBDQYCO-UHFFFAOYSA-N 0.000 claims description 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims description 2
- 229940011051 isopropyl acetate Drugs 0.000 claims description 2
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 239000003960 organic solvent Substances 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 0 CCc(cc(c(F)c1)O)c1-c(cc1)cc2c1c(-c1nc(CN(*)CC3)c3[n]1)n[n]2 Chemical compound CCc(cc(c(F)c1)O)c1-c(cc1)cc2c1c(-c1nc(CN(*)CC3)c3[n]1)n[n]2 0.000 description 14
- UPJNSCOYLNAEKD-UHFFFAOYSA-N Brc(cc1)cc2c1c(-c1nc(CN(Cc3ccccc3)CC3)c3[nH]1)n[nH]2 Chemical compound Brc(cc1)cc2c1c(-c1nc(CN(Cc3ccccc3)CC3)c3[nH]1)n[nH]2 UPJNSCOYLNAEKD-UHFFFAOYSA-N 0.000 description 2
- ZTQVHAJNEIOLPB-UHFFFAOYSA-N CCc(cc(c(F)c1)O)c1-c(cc1)cc2c1c(-c1nc(CNCC3)c3[nH]1)n[nH]2 Chemical compound CCc(cc(c(F)c1)O)c1-c(cc1)cc2c1c(-c1nc(CNCC3)c3[nH]1)n[nH]2 ZTQVHAJNEIOLPB-UHFFFAOYSA-N 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- -1 tetrahydropyran-4-yl Chemical group 0.000 description 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
- DLABLFPCTXRQMY-UHFFFAOYSA-N CC1CSCC1 Chemical compound CC1CSCC1 DLABLFPCTXRQMY-UHFFFAOYSA-N 0.000 description 1
- XBSDJXNXYCRWDX-UHFFFAOYSA-N CNC(C1)CC1OC Chemical compound CNC(C1)CC1OC XBSDJXNXYCRWDX-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562250113P | 2015-11-03 | 2015-11-03 | |
| US62/250,113 | 2015-11-03 | ||
| PCT/US2016/059999 WO2017079205A1 (en) | 2015-11-03 | 2016-11-02 | Jak kinase inhibitor compounds for treatment of respiratory disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018531982A JP2018531982A (ja) | 2018-11-01 |
| JP2018531982A5 true JP2018531982A5 (enExample) | 2019-09-26 |
| JP6800969B2 JP6800969B2 (ja) | 2020-12-16 |
Family
ID=57442794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018522556A Expired - Fee Related JP6800969B2 (ja) | 2015-11-03 | 2016-11-02 | 呼吸器疾患の処置のためのｊａｋキナーゼ阻害剤化合物 |
Country Status (22)
| Country | Link |
|---|---|
| US (6) | US10100049B2 (enExample) |
| EP (1) | EP3371186A1 (enExample) |
| JP (1) | JP6800969B2 (enExample) |
| KR (1) | KR20180073687A (enExample) |
| CN (1) | CN108349972B (enExample) |
| AU (1) | AU2016350816B2 (enExample) |
| BR (1) | BR112018008966B1 (enExample) |
| CA (1) | CA3001542C (enExample) |
| CL (1) | CL2018001145A1 (enExample) |
| CO (1) | CO2018005640A2 (enExample) |
| EA (1) | EA034914B1 (enExample) |
| HK (1) | HK1252685A1 (enExample) |
| IL (1) | IL258772B (enExample) |
| MX (1) | MX374605B (enExample) |
| MY (1) | MY195427A (enExample) |
| NZ (1) | NZ741737A (enExample) |
| PH (1) | PH12018500828B1 (enExample) |
| SA (1) | SA518391470B1 (enExample) |
| TW (1) | TWI710560B (enExample) |
| UA (1) | UA123633C2 (enExample) |
| WO (1) | WO2017079205A1 (enExample) |
| ZA (1) | ZA201802496B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3712152T3 (pl) | 2015-11-03 | 2021-08-02 | Topivert Pharma Limited | Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych |
| US10100049B2 (en) | 2015-11-03 | 2018-10-16 | Theravance Biopharma R&D Ip, Llc | JAK kinase inhibitor compounds for treatment of respiratory disease |
| US10556901B2 (en) | 2015-11-03 | 2020-02-11 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as Janus kinase inhibitors |
| EP3592743A1 (en) | 2017-03-09 | 2020-01-15 | Theravance Biopharma R&D IP, LLC | Fused imidazo-piperidine jak inhibitors |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| WO2018204233A1 (en) * | 2017-05-01 | 2018-11-08 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a jak inhibitor compound |
| CN110603255B (zh) | 2017-05-01 | 2023-02-10 | 施万生物制药研发Ip有限责任公司 | Jak抑制剂化合物的结晶型式 |
| WO2019104225A1 (en) | 2017-11-22 | 2019-05-31 | Dauntless 2, Inc. | Therapeutic compound formulations |
| EP3810094A1 (en) | 2018-06-20 | 2021-04-28 | Progenity, Inc. | Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor |
| CN112638902A (zh) * | 2018-09-04 | 2021-04-09 | 施万生物制药研发Ip有限责任公司 | 用于制备jak抑制剂的方法及其中间体 |
| EA202190686A1 (ru) | 2018-09-04 | 2021-07-23 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи | 5-7-членные гетероциклические амиды в качестве ингибиторов jak |
| JP7324836B2 (ja) | 2018-09-04 | 2023-08-10 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのジメチルアミノアゼチジンアミド |
| CN112955451A (zh) | 2018-10-29 | 2021-06-11 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的2-氮杂双环已烷化合物 |
| EP3883932B1 (en) * | 2018-11-19 | 2023-03-29 | New York University | Inhibitors of gli1 as therapeutic agents |
| CN114075200A (zh) * | 2020-08-14 | 2022-02-22 | 河南迈英诺医药科技有限公司 | 用于治疗重症肺炎的jak抑制剂化合物 |
| JP7514025B2 (ja) * | 2019-02-25 | 2024-07-10 | ホーナン メディノ ファーマシューティカル テクノロジー カンパニー リミテッド | Ｊａｋ阻害剤化合物及びその使用 |
| SG11202109563WA (en) | 2019-03-05 | 2021-09-29 | Incyte Corp | Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction |
| MX2021009863A (es) | 2019-03-21 | 2021-11-12 | Onxeo | Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer. |
| WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| JP7580136B2 (ja) * | 2019-12-30 | 2024-11-11 | 路良 | Ｊａｋ阻害剤化合物及びその使用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202144343A (zh) | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| WO2022178215A1 (en) | 2021-02-19 | 2022-08-25 | Theravance Biopharma R&D Ip, Llc | Amino amide tetrahydro imidazo pyridines as jak inhibitors |
| WO2022204473A1 (en) | 2021-03-26 | 2022-09-29 | Theravance Biopharma R&D Ip, Llc | Crystalline form of a dihydrochloride salt of a jak inhibitor compound |
| EP4359402A1 (en) * | 2021-06-25 | 2024-05-01 | Theravance Biopharma R&D IP, LLC | Imidazolo indazole compounds as jak inhibitors |
| CN114181055A (zh) * | 2021-12-21 | 2022-03-15 | 苏州楚凯药业有限公司 | 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法 |
| JP2025515078A (ja) | 2022-05-05 | 2025-05-13 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | 噴霧経口吸入による送達のためのネズルシチニブ |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| AU2004259012C1 (en) | 2003-07-23 | 2012-08-02 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US7884109B2 (en) | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| US8193197B2 (en) | 2006-10-19 | 2012-06-05 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| BRPI0910021A2 (pt) | 2008-06-20 | 2015-09-01 | Genentech Inc | "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinas em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase" |
| US20110184013A1 (en) | 2008-10-01 | 2011-07-28 | Shelley Allen | Imidazo[1,2-a]Pyridine Compounds As Receptor Tyrosine Kinase Inhibitors |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JP2010111624A (ja) | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| WO2010114971A1 (en) | 2009-04-03 | 2010-10-07 | Sepracor Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| US20110028503A1 (en) | 2009-07-28 | 2011-02-03 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| SMT201700581T1 (it) | 2009-12-21 | 2018-01-11 | Samumed Llc | 1h-pirazolo[3,4-b]piridine e loro usi terapeutici |
| EP2338888A1 (en) | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| EP2643314B1 (en) | 2010-11-25 | 2016-07-13 | ratiopharm GmbH | Novel salts and polymorphic forms of afatinib |
| US8575336B2 (en) * | 2011-07-27 | 2013-11-05 | Pfizer Limited | Indazoles |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| TW201513861A (zh) * | 2013-01-17 | 2015-04-16 | Galapagos Nv | 用於治療退化性及發炎疾病之新穎化合物 |
| EP3318565B1 (en) | 2013-12-05 | 2021-04-14 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
| CA2948587C (en) * | 2014-05-14 | 2018-07-17 | Pfizer Inc. | Pyrazolopyridines and pyrazolopyrimidines |
| WO2016026078A1 (en) | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
| KR101663277B1 (ko) | 2015-03-30 | 2016-10-06 | 주식회사 녹십자 | TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물 |
| US10556901B2 (en) | 2015-11-03 | 2020-02-11 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as Janus kinase inhibitors |
| US10100049B2 (en) | 2015-11-03 | 2018-10-16 | Theravance Biopharma R&D Ip, Llc | JAK kinase inhibitor compounds for treatment of respiratory disease |
| PL3712152T3 (pl) | 2015-11-03 | 2021-08-02 | Topivert Pharma Limited | Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych |
| EP3592743A1 (en) | 2017-03-09 | 2020-01-15 | Theravance Biopharma R&D IP, LLC | Fused imidazo-piperidine jak inhibitors |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| CN110603255B (zh) | 2017-05-01 | 2023-02-10 | 施万生物制药研发Ip有限责任公司 | Jak抑制剂化合物的结晶型式 |
| WO2018204233A1 (en) | 2017-05-01 | 2018-11-08 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a jak inhibitor compound |
| JP7324836B2 (ja) | 2018-09-04 | 2023-08-10 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのジメチルアミノアゼチジンアミド |
| EA202190686A1 (ru) | 2018-09-04 | 2021-07-23 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи | 5-7-членные гетероциклические амиды в качестве ингибиторов jak |
| CN112638902A (zh) | 2018-09-04 | 2021-04-09 | 施万生物制药研发Ip有限责任公司 | 用于制备jak抑制剂的方法及其中间体 |
| CN112955451A (zh) | 2018-10-29 | 2021-06-11 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的2-氮杂双环已烷化合物 |
| WO2022204473A1 (en) | 2021-03-26 | 2022-09-29 | Theravance Biopharma R&D Ip, Llc | Crystalline form of a dihydrochloride salt of a jak inhibitor compound |
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- 2016-11-02 WO PCT/US2016/059999 patent/WO2017079205A1/en not_active Ceased
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- 2016-11-02 KR KR1020187015680A patent/KR20180073687A/ko not_active Withdrawn
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