JP2016528245A5 - - Google Patents
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- Publication number
- JP2016528245A5 JP2016528245A5 JP2016533962A JP2016533962A JP2016528245A5 JP 2016528245 A5 JP2016528245 A5 JP 2016528245A5 JP 2016533962 A JP2016533962 A JP 2016533962A JP 2016533962 A JP2016533962 A JP 2016533962A JP 2016528245 A5 JP2016528245 A5 JP 2016528245A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- formula
- alkoxy
- 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 19
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 10
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 230000000694 effects Effects 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 201000011190 diabetic macular edema Diseases 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 4
- 206010019860 Hereditary angioedema Diseases 0.000 claims 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- MVXVYAKCVDQRLW-UHFFFAOYSA-N 1h-pyrrolo[2,3-b]pyridine Chemical compound C1=CN=C2NC=CC2=C1 MVXVYAKCVDQRLW-UHFFFAOYSA-N 0.000 claims 2
- 239000004215 Carbon black (E152) Substances 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 208000001953 Hypotension Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 206010040070 Septic Shock Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 235000010290 biphenyl Nutrition 0.000 claims 2
- 239000004305 biphenyl Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000002612 cardiopulmonary effect Effects 0.000 claims 2
- 150000004292 cyclic ethers Chemical class 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 150000002430 hydrocarbons Chemical class 0.000 claims 2
- 230000036543 hypotension Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 230000002207 retinal effect Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 230000036303 septic shock Effects 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 230000008728 vascular permeability Effects 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 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 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000000059 Dyspnea Diseases 0.000 claims 1
- 206010013975 Dyspnoeas Diseases 0.000 claims 1
- 208000032843 Hemorrhage Diseases 0.000 claims 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 claims 1
- 206010051077 Post procedural haemorrhage Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 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
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 208000034158 bleeding Diseases 0.000 claims 1
- 230000000740 bleeding effect Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- -1 methylenedioxy, ethylenedioxy Chemical group 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361865696P | 2013-08-14 | 2013-08-14 | |
| GB1314578.4 | 2013-08-14 | ||
| US61/865,696 | 2013-08-14 | ||
| GB1314578.4A GB2517908A (en) | 2013-08-14 | 2013-08-14 | Bicyclic inhibitors |
| PCT/GB2014/052511 WO2015022547A1 (en) | 2013-08-14 | 2014-08-14 | Bicyclic inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016528245A JP2016528245A (ja) | 2016-09-15 |
| JP2016528245A5 true JP2016528245A5 (https=) | 2017-09-21 |
| JP6527148B2 JP6527148B2 (ja) | 2019-06-05 |
Family
ID=49262178
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533962A Expired - Fee Related JP6527148B2 (ja) | 2013-08-14 | 2014-08-14 | 二環式阻害薬 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9738641B2 (https=) |
| EP (1) | EP3033332B8 (https=) |
| JP (1) | JP6527148B2 (https=) |
| CN (1) | CN105683175B (https=) |
| BR (1) | BR112016003040B1 (https=) |
| CA (1) | CA2920817C (https=) |
| ES (1) | ES2691084T3 (https=) |
| GB (1) | GB2517908A (https=) |
| MX (1) | MX362806B (https=) |
| PL (1) | PL3033332T3 (https=) |
| RU (1) | RU2672582C2 (https=) |
| WO (1) | WO2015022547A1 (https=) |
Families Citing this family (14)
| 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 |
| WO2015171527A1 (en) | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Pyrazolopyridine pyrazolopyrimidine and related compounds |
| 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 |
| IL263235B (en) | 2016-05-31 | 2022-07-01 | Kalvista Pharmaceuticals Ltd | History of pyrazoles 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 |
| US11554104B2 (en) * | 2017-08-18 | 2023-01-17 | The Schepens Eye Research Institute, Inc. | Compositions for the treatment of dry eye and methods of use thereof |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| HUE057912T2 (hu) | 2017-11-29 | 2022-06-28 | Kalvista Pharmaceuticals Ltd | Plazma kallikrein inhibitort tartalmazó dózisformák |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| EP4017587A1 (en) * | 2019-08-21 | 2022-06-29 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| CN116133660B (zh) | 2020-07-22 | 2025-05-02 | 詹森药业有限公司 | 可用作因子XIa抑制剂的化合物 |
| WO2025153806A1 (en) | 2024-01-15 | 2025-07-24 | Kalvista Pharmaceuticals Limited | Methods for determining amidolytic activity |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5187157A (en) | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| GB9019558D0 (en) | 1990-09-07 | 1990-10-24 | Szelke Michael | Enzyme inhibitors |
| SE9301911D0 (sv) | 1993-06-03 | 1993-06-03 | Ab Astra | New peptide derivatives |
| US5589467A (en) | 1993-09-17 | 1996-12-31 | Novo Nordisk A/S | 2,5',N6-trisubstituted adenosine derivatives |
| AU698911B2 (en) * | 1995-04-04 | 1998-11-12 | Merck & Co., Inc. | Thrombin inhibitors |
| US5786328A (en) | 1995-06-05 | 1998-07-28 | Genentech, Inc. | Use of kunitz type plasma kallikrein inhibitors |
| JP3957023B2 (ja) * | 1997-11-12 | 2007-08-08 | 三菱化学株式会社 | プリン誘導体及びそれを有効成分として含む医薬 |
| GB0205527D0 (en) * | 2002-03-08 | 2002-04-24 | Ferring Bv | Inhibitors |
| NZ592039A (en) | 2003-08-27 | 2013-03-28 | Ophthotech Corp | Combination therapy for the treatment of ocular neovascular disorders |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| MX2007002214A (es) * | 2004-09-03 | 2007-05-07 | Yuhan Corp | Derivados de pirrolo[3,2-c]piridina y procesos para su preparacion. |
| KR101142363B1 (ko) * | 2005-06-27 | 2012-05-21 | 주식회사유한양행 | 피롤로피리딘 유도체를 포함하는 항암제 조성물 |
| EP1981854B1 (en) * | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| JP5322935B2 (ja) * | 2006-07-31 | 2013-10-23 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬 |
| DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| GB0910003D0 (en) | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| JP2013121919A (ja) | 2010-03-25 | 2013-06-20 | Astellas Pharma Inc | 血漿カリクレイン阻害剤 |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | The Medicines Company (Leipzig) GmbH | Serine protease inhibitors |
| US9290485B2 (en) * | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| US20140378474A1 (en) * | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2807156A1 (en) * | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| CN106257976B (zh) | 2014-03-07 | 2021-02-02 | 拜奥克里斯特制药公司 | 人类血浆激肽释放酶抑制剂 |
| WO2015171527A1 (en) | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Pyrazolopyridine pyrazolopyrimidine and related compounds |
| WO2015171526A2 (en) | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Tricyclic pyrazolopyridine compounds |
| MX381342B (es) | 2014-07-16 | 2025-03-12 | Lifesci Pharmaceuticals Inc | Compuestos terapeuticos inhibidores. |
-
2013
- 2013-08-14 GB GB1314578.4A patent/GB2517908A/en not_active Withdrawn
-
2014
- 2014-08-14 JP JP2016533962A patent/JP6527148B2/ja not_active Expired - Fee Related
- 2014-08-14 CN CN201480055946.6A patent/CN105683175B/zh not_active Expired - Fee Related
- 2014-08-14 US US14/907,095 patent/US9738641B2/en not_active Expired - Fee Related
- 2014-08-14 CA CA2920817A patent/CA2920817C/en active Active
- 2014-08-14 EP EP14753140.4A patent/EP3033332B8/en active Active
- 2014-08-14 RU RU2016108762A patent/RU2672582C2/ru active
- 2014-08-14 WO PCT/GB2014/052511 patent/WO2015022547A1/en not_active Ceased
- 2014-08-14 ES ES14753140.4T patent/ES2691084T3/es active Active
- 2014-08-14 MX MX2016001865A patent/MX362806B/es active IP Right Grant
- 2014-08-14 PL PL14753140T patent/PL3033332T3/pl unknown
- 2014-08-14 BR BR112016003040-0A patent/BR112016003040B1/pt not_active IP Right Cessation
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