JPWO2021032937A5 - - Google Patents
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- Publication number
- JPWO2021032937A5 JPWO2021032937A5 JP2022503825A JP2022503825A JPWO2021032937A5 JP WO2021032937 A5 JPWO2021032937 A5 JP WO2021032937A5 JP 2022503825 A JP2022503825 A JP 2022503825A JP 2022503825 A JP2022503825 A JP 2022503825A JP WO2021032937 A5 JPWO2021032937 A5 JP WO2021032937A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- halo
- alkoxy
- pharmaceutically acceptable
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 11
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 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 claims 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 6
- -1 -OH Chemical group 0.000 claims 5
- 108010071241 Factor XIIa Proteins 0.000 claims 5
- 208000007536 Thrombosis Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 208000028185 Angioedema Diseases 0.000 claims 3
- 101800004538 Bradykinin Proteins 0.000 claims 3
- 239000004215 Carbon black (E152) Substances 0.000 claims 3
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 3
- 102100035792 Kininogen-1 Human genes 0.000 claims 3
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 3
- 229930195733 hydrocarbon Natural products 0.000 claims 3
- 150000002430 hydrocarbons Chemical class 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 206010014522 Embolism venous Diseases 0.000 claims 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 2
- 208000004043 venous thromboembolism Diseases 0.000 claims 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000007257 Budd-Chiari syndrome Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 208000032843 Hemorrhage Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000010183 Papilledema Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 206010038886 Retinal oedema Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000001435 Thromboembolism Diseases 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 238000011882 arthroplasty Methods 0.000 claims 1
- 201000005008 bacterial sepsis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 238000002618 extracorporeal membrane oxygenation Methods 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 210000003709 heart valve Anatomy 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 230000002314 neuroinflammatory effect Effects 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000003331 prothrombotic effect Effects 0.000 claims 1
- 201000011195 retinal edema Diseases 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 210000005166 vasculature Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2019/052359 WO2021032936A1 (en) | 2019-08-21 | 2019-08-21 | Enzyme inhibitors |
| GBPCT/GB2019/052359 | 2019-08-21 | ||
| PCT/GB2020/050332 WO2021032937A1 (en) | 2019-08-21 | 2020-02-13 | Enzyme inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022545158A JP2022545158A (ja) | 2022-10-26 |
| JP2022545158A5 JP2022545158A5 (https=) | 2023-02-20 |
| JPWO2021032937A5 true JPWO2021032937A5 (https=) | 2023-02-20 |
| JP7566870B2 JP7566870B2 (ja) | 2024-10-15 |
Family
ID=67777359
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022503825A Active JP7566870B2 (ja) | 2019-08-21 | 2020-02-13 | 酵素阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20220363668A1 (https=) |
| EP (1) | EP4017587A1 (https=) |
| JP (1) | JP7566870B2 (https=) |
| KR (1) | KR20220051207A (https=) |
| CN (1) | CN114269430A (https=) |
| AR (1) | AR118085A1 (https=) |
| AU (1) | AU2020333222A1 (https=) |
| BR (1) | BR112022000936A2 (https=) |
| CA (1) | CA3147228A1 (https=) |
| CO (1) | CO2022000266A2 (https=) |
| IL (1) | IL289783A (https=) |
| MX (1) | MX2022002069A (https=) |
| PH (1) | PH12022550078A1 (https=) |
| TW (1) | TW202115033A (https=) |
| WO (2) | WO2021032936A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| WO2021032935A1 (en) * | 2019-08-21 | 2021-02-25 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| WO2025153806A1 (en) * | 2024-01-15 | 2025-07-24 | Kalvista Pharmaceuticals Limited | Methods for determining amidolytic activity |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ592039A (en) | 2003-08-27 | 2013-03-28 | Ophthotech Corp | Combination therapy for the treatment of ocular neovascular disorders |
| CN103415301A (zh) * | 2011-03-09 | 2013-11-27 | 德国杰特贝林生物制品有限公司 | 用于与包括与人造表面接触的医疗操作一起施用的fxii抑制剂 |
| GB2517908A (en) * | 2013-08-14 | 2015-03-11 | Kalvista Pharmaceuticals Ltd | Bicyclic inhibitors |
| WO2015171527A1 (en) * | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Pyrazolopyridine pyrazolopyrimidine and related compounds |
| GB201421088D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| WO2017123518A1 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
| AU2017269256B2 (en) | 2016-05-23 | 2021-02-25 | The Rockefeller University | Aminoacylindazole immunomodulators for treatment of autoimmune diseases |
| WO2018093695A1 (en) | 2016-11-18 | 2018-05-24 | Merck Sharp & Dohme Corp. | FACTOR XIIa INHIBITORS |
| EP3541381B1 (en) | 2016-11-18 | 2022-12-28 | Merck Sharp & Dohme LLC | Inhibitors of factor xiia |
| JP2021504490A (ja) | 2017-11-29 | 2021-02-15 | ザ ロックフェラー ユニバーシティーＴｈｅ Ｒｏｃｋｅｆｅｌｌｅｒ Ｕｎｉｖｅｒｓｉｔｙ | 自己免疫疾患治療用ピラノピラゾールおよびピラゾロピリジン免疫調節薬 |
| WO2021032935A1 (en) * | 2019-08-21 | 2021-02-25 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
-
2019
- 2019-08-21 EP EP19759703.2A patent/EP4017587A1/en not_active Withdrawn
- 2019-08-21 CN CN201980099528.XA patent/CN114269430A/zh active Pending
- 2019-08-21 WO PCT/GB2019/052359 patent/WO2021032936A1/en not_active Ceased
-
2020
- 2020-02-13 CA CA3147228A patent/CA3147228A1/en active Pending
- 2020-02-13 BR BR112022000936A patent/BR112022000936A2/pt not_active Application Discontinuation
- 2020-02-13 AU AU2020333222A patent/AU2020333222A1/en active Pending
- 2020-02-13 JP JP2022503825A patent/JP7566870B2/ja active Active
- 2020-02-13 MX MX2022002069A patent/MX2022002069A/es unknown
- 2020-02-13 AR ARP200100399A patent/AR118085A1/es not_active Application Discontinuation
- 2020-02-13 US US17/634,367 patent/US20220363668A1/en not_active Abandoned
- 2020-02-13 PH PH1/2022/550078A patent/PH12022550078A1/en unknown
- 2020-02-13 KR KR1020227008821A patent/KR20220051207A/ko not_active Withdrawn
- 2020-02-13 TW TW109104437A patent/TW202115033A/zh unknown
- 2020-02-13 WO PCT/GB2020/050332 patent/WO2021032937A1/en not_active Ceased
-
2022
- 2022-01-12 IL IL289783A patent/IL289783A/en unknown
- 2022-01-17 CO CONC2022/0000266A patent/CO2022000266A2/es unknown
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