JP2019517463A5 - - Google Patents
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- Publication number
- JP2019517463A5 JP2019517463A5 JP2018559929A JP2018559929A JP2019517463A5 JP 2019517463 A5 JP2019517463 A5 JP 2019517463A5 JP 2018559929 A JP2018559929 A JP 2018559929A JP 2018559929 A JP2018559929 A JP 2018559929A JP 2019517463 A5 JP2019517463 A5 JP 2019517463A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- oxopyridin
- methoxypyridin
- methoxymethyl
- pyrazole
- 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
- 239000013078 crystal Substances 0.000 claims 19
- -1 3-Fluoro-4-methoxypyridin-2-yl Chemical group 0.000 claims 17
- 238000000034 method Methods 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 12
- 239000002904 solvent Substances 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- ZVXKYWHJBYIYNI-UHFFFAOYSA-N 1h-pyrazole-4-carboxamide Chemical compound NC(=O)C=1C=NNC=1 ZVXKYWHJBYIYNI-UHFFFAOYSA-N 0.000 claims 10
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical group CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 9
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 7
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 230000001404 mediated effect Effects 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 5
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 4
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 4
- 230000001351 cycling effect Effects 0.000 claims 4
- 201000011190 diabetic macular edema Diseases 0.000 claims 4
- 206010019860 Hereditary angioedema Diseases 0.000 claims 3
- 230000002207 retinal effect Effects 0.000 claims 3
- 229910021653 sulphate ion Inorganic materials 0.000 claims 3
- 230000008728 vascular permeability Effects 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000001953 Hypotension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010051077 Post procedural haemorrhage Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010047571 Visual impairment Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000023555 blood coagulation Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002612 cardiopulmonary effect Effects 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 230000036543 hypotension Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000020658 intracerebral hemorrhage Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 238000000527 sonication Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000029257 vision disease Diseases 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021164519A JP7383676B2 (ja) | 2016-06-01 | 2021-10-06 | カリクレインインヒビターとしての、ｎ－［（３－フルオロ－４－メトキシピリジン－２－イル）メチル］－３－（メトキシメチル）－１－（｛４－［（２－オキソピリジン－１－イル）メチル］フェニル｝メチル）ピラゾール－４－カルボキサミドの多形体 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662344059P | 2016-06-01 | 2016-06-01 | |
| US62/344,059 | 2016-06-01 | ||
| GB1609607.5 | 2016-06-01 | ||
| GBGB1609607.5A GB201609607D0 (en) | 2016-06-01 | 2016-06-01 | 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 |
| PCT/GB2017/051579 WO2017208005A1 (en) | 2016-06-01 | 2017-06-01 | Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1 -({4-[2-oxopyridin-1 -yl)methyl]phenyl} methyl) pyrazole -4-carboxamide as kallikrein inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021164519A Division JP7383676B2 (ja) | 2016-06-01 | 2021-10-06 | カリクレインインヒビターとしての、ｎ－［（３－フルオロ－４－メトキシピリジン－２－イル）メチル］－３－（メトキシメチル）－１－（｛４－［（２－オキソピリジン－１－イル）メチル］フェニル｝メチル）ピラゾール－４－カルボキサミドの多形体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019517463A JP2019517463A (ja) | 2019-06-24 |
| JP2019517463A5 true JP2019517463A5 (enExample) | 2020-07-09 |
| JP6957516B2 JP6957516B2 (ja) | 2021-11-02 |
Family
ID=56410856
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018559929A Active JP6957516B2 (ja) | 2016-06-01 | 2017-06-01 | カリクレインインヒビターとしての、ｎ−［（３−フルオロ−４−メトキシピリジン−２−イル）メチル］−３−（メトキシメチル）−１−（｛４−［（２−オキソピリジン−１−イル）メチル］フェニル｝メチル）ピラゾール−４−カルボキサミドの多形体 |
| JP2021164519A Active JP7383676B2 (ja) | 2016-06-01 | 2021-10-06 | カリクレインインヒビターとしての、ｎ－［（３－フルオロ－４－メトキシピリジン－２－イル）メチル］－３－（メトキシメチル）－１－（｛４－［（２－オキソピリジン－１－イル）メチル］フェニル｝メチル）ピラゾール－４－カルボキサミドの多形体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021164519A Active JP7383676B2 (ja) | 2016-06-01 | 2021-10-06 | カリクレインインヒビターとしての、ｎ－［（３－フルオロ－４－メトキシピリジン－２－イル）メチル］－３－（メトキシメチル）－１－（｛４－［（２－オキソピリジン－１－イル）メチル］フェニル｝メチル）ピラゾール－４－カルボキサミドの多形体 |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US11230537B2 (enExample) |
| EP (2) | EP3464265B1 (enExample) |
| JP (2) | JP6957516B2 (enExample) |
| KR (1) | KR102425918B1 (enExample) |
| CN (1) | CN109379891B (enExample) |
| AU (1) | AU2017273136B2 (enExample) |
| BR (1) | BR112018073521B1 (enExample) |
| CA (1) | CA3025720A1 (enExample) |
| CY (1) | CY1125589T1 (enExample) |
| DK (1) | DK3464265T3 (enExample) |
| ES (1) | ES2927779T3 (enExample) |
| GB (1) | GB201609607D0 (enExample) |
| HR (1) | HRP20221019T1 (enExample) |
| HU (1) | HUE059165T2 (enExample) |
| IL (1) | IL263222B (enExample) |
| LT (1) | LT3464265T (enExample) |
| MA (1) | MA45130B1 (enExample) |
| MD (1) | MD3464265T2 (enExample) |
| MX (1) | MX386113B (enExample) |
| PL (1) | PL3464265T3 (enExample) |
| PT (1) | PT3464265T (enExample) |
| RS (1) | RS63604B1 (enExample) |
| RU (1) | RU2756273C2 (enExample) |
| SI (1) | SI3464265T1 (enExample) |
| SM (1) | SMT202200341T1 (enExample) |
| WO (1) | WO2017208005A1 (enExample) |
| ZA (1) | ZA201808638B (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| WO2017207983A1 (en) | 2016-05-31 | 2017-12-07 | Kalvista Pharmaceuticals Limited | Pyrazole derivatives as plasma kallikrein inhibitors |
| 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 |
| GB201609603D0 (en) * | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| JP7078722B2 (ja) | 2017-11-29 | 2022-05-31 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレイン阻害剤を含む剤形 |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
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| GB201910125D0 (en) * | 2019-07-15 | 2019-08-28 | Kalvista Pharmaceuticals Ltd | Treatments of angioedema |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| PT4031547T (pt) | 2019-09-18 | 2024-08-27 | Takeda Pharmaceuticals Co | Inibidores de calicreína plasmática e utilizações dos mesmos |
| US11370803B2 (en) | 2019-09-18 | 2022-06-28 | Takeda Pharmaceutical Company Limited | Heteroaryl plasma kallikrein inhibitors |
| CN111875557B (zh) * | 2020-08-19 | 2023-06-02 | 南通大学 | 一种噻唑类衍生物及其合成方法 |
| EP4232031A1 (en) * | 2020-10-23 | 2023-08-30 | Kalvista Pharmaceuticals Limited | Treatments of angioedema |
| US20240122909A1 (en) * | 2021-02-09 | 2024-04-18 | Kalvista Pharmaceuticals Limited | Treatments of hereditary angioedema |
| EP4673437A1 (en) | 2023-02-27 | 2026-01-07 | Kalvista Pharmaceuticals Limited | New solid form of a plasma kallikrein inhibitor |
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