JP2016530262A5 - - Google Patents
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- Publication number
- JP2016530262A5 JP2016530262A5 JP2016533961A JP2016533961A JP2016530262A5 JP 2016530262 A5 JP2016530262 A5 JP 2016530262A5 JP 2016533961 A JP2016533961 A JP 2016533961A JP 2016533961 A JP2016533961 A JP 2016533961A JP 2016530262 A5 JP2016530262 A5 JP 2016530262A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- alkoxy
- independently
- 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 26
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 11
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 10
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 230000000694 effects Effects 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 10
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 4
- 206010019860 Hereditary angioedema Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 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
- 208000024891 symptom Diseases 0.000 claims 4
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 150000005258 1H-pyrrolo(2,3-b)pyridines Chemical class 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
- 206010020772 Hypertension 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
- 206010040070 Septic Shock Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- MVXVYAKCVDQRLW-UHFFFAOYSA-N azain Natural products C1=CN=C2NC=CC2=C1 MVXVYAKCVDQRLW-UHFFFAOYSA-N 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
- 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
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 150000002430 hydrocarbons Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 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
- 230000002265 prevention Effects 0.000 claims 2
- 230000002207 retinal effect Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 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
- 101100495913 Arabidopsis thaliana CHR17 gene Proteins 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
- 125000006615 aromatic heterocyclic group Chemical group 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
- 239000003814 drug Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- -1 methylenedioxy, ethylenedioxy Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical class O=* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361865756P | 2013-08-14 | 2013-08-14 | |
| US201361865732P | 2013-08-14 | 2013-08-14 | |
| US61/865,756 | 2013-08-14 | ||
| US61/865,732 | 2013-08-14 | ||
| PCT/GB2014/052510 WO2015022546A1 (en) | 2013-08-14 | 2014-08-14 | Inhibitors of plasma kallikrein |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016530262A JP2016530262A (ja) | 2016-09-29 |
| JP2016530262A5 true JP2016530262A5 (enExample) | 2017-09-28 |
| JP6527147B2 JP6527147B2 (ja) | 2019-06-05 |
Family
ID=51392282
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533961A Expired - Fee Related JP6527147B2 (ja) | 2013-08-14 | 2014-08-14 | 血漿カリクレインの阻害薬 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10221161B2 (enExample) |
| EP (1) | EP3033336B1 (enExample) |
| JP (1) | JP6527147B2 (enExample) |
| CN (1) | CN105683179B (enExample) |
| CA (1) | CA2920815C (enExample) |
| ES (1) | ES2674088T3 (enExample) |
| HU (1) | HUE14755117T2 (enExample) |
| MX (1) | MX366498B (enExample) |
| PL (1) | PL3033336T3 (enExample) |
| RU (1) | RU2674028C2 (enExample) |
| WO (1) | WO2015022546A1 (enExample) |
Families Citing this family (30)
| 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 |
| US9611252B2 (en) | 2013-12-30 | 2017-04-04 | Lifesci Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| KR20160106627A (ko) * | 2013-12-30 | 2016-09-12 | 라이프에스씨아이 파마슈티컬스, 인크. | 치료적 억제 화합물 |
| JP6951970B2 (ja) * | 2014-07-16 | 2021-10-20 | ライフサイ ファーマシューティカルズ，インク． | 治療用阻害化合物 |
| US9463201B2 (en) | 2014-10-19 | 2016-10-11 | M.G. Therapeutics Ltd | Compositions and methods for the treatment of meibomian gland dysfunction |
| 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 |
| US9815853B2 (en) | 2015-06-12 | 2017-11-14 | Global Blood Therapeutics, Inc. | Bridged bicyclic kallikrein inhibitors |
| US10981893B2 (en) | 2015-07-01 | 2021-04-20 | Attune Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| US20190263818A1 (en) * | 2015-07-01 | 2019-08-29 | Lifesci Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| CA3000088A1 (en) | 2015-09-28 | 2017-04-06 | Azura Ophthalmics Ltd. | Thiol and disulfide-containing agents for increasing meibomian gland lipid secretion |
| US11040062B2 (en) | 2016-04-14 | 2021-06-22 | Azura Ophthalmics Ltd. | Selenium disulfide compositions for use in treating meibomian gland dysfunction |
| RS60600B1 (sr) | 2016-05-31 | 2020-08-31 | Kalvista Pharmaceuticals Ltd | Derivati pirazola kao inhibitori kalikreina plazme |
| 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 |
| WO2018011628A1 (en) | 2016-07-11 | 2018-01-18 | Lifesci Pharmaceuticals, Inc. | Therapeutic inhibitory compounds |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| GB201721515D0 (en) * | 2017-12-21 | 2018-02-07 | Kalvista Pharmaceuticals Ltd | Dosage forms comprising a plasma kallikrein inhibtor |
| PL3716952T3 (pl) | 2017-11-29 | 2022-05-02 | Kalvista Pharmaceuticals Limited | Postacie dawkowania zawierające inhibitor kalikreiny osoczowej |
| EP3758702A4 (en) * | 2018-02-28 | 2021-11-10 | Attune Pharmaceuticals, Inc. | TREATMENT OF HEREDITARY ANGIOEDEMA |
| CN112135825A (zh) | 2018-03-13 | 2020-12-25 | 夏尔人类遗传性治疗公司 | 血浆激肽释放酶抑制剂及其用途 |
| EP3837252B1 (en) * | 2018-08-16 | 2025-12-10 | Boehringer Ingelheim International GmbH | Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors |
| CN114206852A (zh) | 2019-08-09 | 2022-03-18 | 卡尔维斯塔制药有限公司 | 血浆激肽释放酶抑制剂 |
| DK4031547T3 (da) | 2019-09-18 | 2024-09-09 | Takeda Pharmaceuticals Co | Plasmakallikreininhibitorer og anvendelser deraf |
| CN114667289B (zh) | 2019-09-18 | 2025-08-26 | 武田药品工业有限公司 | 杂芳基血浆激肽释放酶抑制剂 |
| WO2021121396A1 (zh) * | 2019-12-20 | 2021-06-24 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的三环类化合物及其用途 |
| WO2021138540A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| CA3166357A1 (en) | 2020-01-10 | 2021-07-15 | Azura Ophthalmics Ltd. | Instructions for composition and sensitivity |
| TW202448473A (zh) * | 2023-02-16 | 2024-12-16 | 南韓商治納輔醫藥科技有限公司 | 包含ｓｏｓ１抑制劑及抗癌藥物的用於治療癌症之藥學組成物 |
| WO2025153806A1 (en) | 2024-01-15 | 2025-07-24 | Kalvista Pharmaceuticals Limited | Methods for determining amidolytic activity |
Family Cites Families (34)
| 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 |
| SI1441734T1 (sl) | 2001-10-26 | 2007-08-31 | Angeletti P Ist Richerche Bio | Dihidropirimidin karboksamidni inhibitorji HIV-integraze |
| GB0205527D0 (en) | 2002-03-08 | 2002-04-24 | Ferring Bv | Inhibitors |
| ATE551324T1 (de) * | 2003-02-03 | 2012-04-15 | Janssen Pharmaceutica Nv | Chinolin-amid-derivate als modulatoren von vanilloid-vr1-rezeptoren |
| KR101471732B1 (ko) | 2003-08-27 | 2014-12-16 | 옵쏘테크 코포레이션 | 안구의 혈관신생성 장애를 치료하기 위한 조합 치료법 |
| GB0403155D0 (en) * | 2004-02-12 | 2004-03-17 | Vernalis Res Ltd | Chemical compounds |
| US7417063B2 (en) * | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic heterocycles useful as serine protease inhibitors |
| US7429604B2 (en) * | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US20070254894A1 (en) * | 2006-01-10 | 2007-11-01 | Kane John L Jr | Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation |
| 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 |
| KR20150090281A (ko) | 2006-12-29 | 2015-08-05 | 아비에 도이치란트 게엠베하 운트 콤파니 카게 | 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도 |
| WO2008109180A2 (en) * | 2007-03-07 | 2008-09-12 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors containing a heterocyclic moiety |
| EP2142516B1 (en) * | 2007-03-30 | 2012-12-26 | Sanofi | Pyrimidine hydrazide compounds as pgds inhibitors |
| WO2009083553A1 (en) | 2007-12-31 | 2009-07-09 | Rheoscience A/S | Azine compounds as glucokinase activators |
| US8324385B2 (en) * | 2008-10-30 | 2012-12-04 | Madrigal Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
| GB0910003D0 (en) | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| SG10201408429UA (en) | 2009-12-18 | 2015-02-27 | Activesite Pharmaceuticals Inc | Prodrugs of inhibitors of plasma kallikrein |
| JP2013121919A (ja) | 2010-03-25 | 2013-06-20 | Astellas Pharma Inc | 血漿カリクレイン阻害剤 |
| WO2012004678A2 (en) | 2010-07-07 | 2012-01-12 | 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 |
| EP2458315B1 (de) | 2010-11-25 | 2017-01-04 | Balcke-Dürr GmbH | Regenerativer Wärmetauscher mit zwangsgeführter Rotordichtung |
| EP2697196A1 (en) | 2011-04-13 | 2014-02-19 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| US20140378474A1 (en) * | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| US20140350034A1 (en) | 2012-01-27 | 2014-11-27 | Novartis Ag | Aminopyridine derivatives as plasma kallikrein inhibitors |
| GB201300304D0 (en) * | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| EP3305778B1 (en) * | 2013-05-23 | 2022-01-19 | Kalvista Pharmaceuticals Limited | Inhibitors of plasma kallikrein |
| KR20160106627A (ko) | 2013-12-30 | 2016-09-12 | 라이프에스씨아이 파마슈티컬스, 인크. | 치료적 억제 화합물 |
| WO2015171526A2 (en) | 2014-05-05 | 2015-11-12 | Global Blood Therapeutics, Inc. | Tricyclic pyrazolopyridine compounds |
| US9695166B2 (en) | 2014-05-05 | 2017-07-04 | Global Blood Therapeutics, Inc. | Pyrazolopyridine pyrazolopyrimidine and related compounds |
| JP6951970B2 (ja) | 2014-07-16 | 2021-10-20 | ライフサイ ファーマシューティカルズ，インク． | 治療用阻害化合物 |
-
2014
- 2014-08-14 US US14/907,842 patent/US10221161B2/en active Active
- 2014-08-14 HU HUE14755117A patent/HUE14755117T2/hu unknown
- 2014-08-14 CN CN201480055925.4A patent/CN105683179B/zh not_active Expired - Fee Related
- 2014-08-14 MX MX2016001864A patent/MX366498B/es active IP Right Grant
- 2014-08-14 EP EP14755117.0A patent/EP3033336B1/en active Active
- 2014-08-14 PL PL14755117T patent/PL3033336T3/pl unknown
- 2014-08-14 RU RU2016108753A patent/RU2674028C2/ru active
- 2014-08-14 JP JP2016533961A patent/JP6527147B2/ja not_active Expired - Fee Related
- 2014-08-14 CA CA2920815A patent/CA2920815C/en active Active
- 2014-08-14 ES ES14755117.0T patent/ES2674088T3/es active Active
- 2014-08-14 WO PCT/GB2014/052510 patent/WO2015022546A1/en not_active Ceased
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