CN113387933A - 作为血浆激肽释放酶抑制剂的吡唑衍生物 - Google Patents

作为血浆激肽释放酶抑制剂的吡唑衍生物 Download PDF

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Publication number
CN113387933A
CN113387933A CN202110792609.7A CN202110792609A CN113387933A CN 113387933 A CN113387933 A CN 113387933A CN 202110792609 A CN202110792609 A CN 202110792609A CN 113387933 A CN113387933 A CN 113387933A
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China
Prior art keywords
methyl
phenyl
pyrazole
carboxamide
methoxymethyl
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Pending
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CN202110792609.7A
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Chinese (zh)
Inventor
丽贝卡·路易丝·戴维
汉娜·乔伊·爱德华兹
戴维·米歇尔·埃万斯
西蒙·泰亚比·霍奇森
斯蒂芬·约翰·派森
戴维·菲利普·鲁克
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Kalvista Pharmaceuticals Ltd
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Kalvista Pharmaceuticals Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60478506&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN113387933(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GBGB1609517.6A external-priority patent/GB201609517D0/en
Priority claimed from GBGB1702044.7A external-priority patent/GB201702044D0/en
Application filed by Kalvista Pharmaceuticals Ltd filed Critical Kalvista Pharmaceuticals Ltd
Publication of CN113387933A publication Critical patent/CN113387933A/zh
Pending legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
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    • A61K31/33Heterocyclic compounds
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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  • Heart & Thoracic Surgery (AREA)
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  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN202110792609.7A 2016-05-31 2017-05-31 作为血浆激肽释放酶抑制剂的吡唑衍生物 Pending CN113387933A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201662343363P 2016-05-31 2016-05-31
GBGB1609517.6A GB201609517D0 (en) 2016-05-31 2016-05-31 Enzyme inhibitors
GB1609517.6 2016-05-31
US62/343,363 2016-05-31
US201762456219P 2017-02-08 2017-02-08
GBGB1702044.7A GB201702044D0 (en) 2017-02-08 2017-02-08 Enzyme inhibitors
US62/456,219 2017-02-08
GB1702044.7 2017-02-08
CN201780034028.9A CN109311847B (zh) 2016-05-31 2017-05-31 作为血浆激肽释放酶抑制剂的吡唑衍生物

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CN113387933A true CN113387933A (zh) 2021-09-14

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CN202110792609.7A Pending CN113387933A (zh) 2016-05-31 2017-05-31 作为血浆激肽释放酶抑制剂的吡唑衍生物

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US (2) US11180484B2 (enExample)
EP (2) EP3760622A1 (enExample)
JP (2) JP6884801B2 (enExample)
KR (2) KR20220107319A (enExample)
CN (2) CN109311847B (enExample)
AU (2) AU2017275820B2 (enExample)
BR (1) BR112018074395A2 (enExample)
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CL (1) CL2018003213A1 (enExample)
CO (1) CO2018012894A2 (enExample)
CY (1) CY1123223T1 (enExample)
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ES (1) ES2805027T3 (enExample)
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ME (1) ME03794B (enExample)
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PH (2) PH12018502355A1 (enExample)
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PT (1) PT3464271T (enExample)
RS (1) RS60600B1 (enExample)
RU (2) RU2020140891A (enExample)
SG (2) SG11201809922YA (enExample)
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Families Citing this family (27)

* Cited by examiner, † Cited by third party
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
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
JP6884801B2 (ja) 2016-05-31 2021-06-09 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
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
MX2020005168A (es) 2017-11-29 2020-08-20 Kalvista Pharmaceuticals Ltd Formas de dosificacion que contienen un inhibidor calicreina de plasma.
TW201925188A (zh) * 2017-11-29 2019-07-01 英商卡爾維斯塔製藥有限公司 酶抑制劑
GB201719881D0 (en) * 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
GB201719882D0 (en) * 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of a plasma kallikrein inhibitor and salts thereof
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
CN112839711A (zh) * 2018-10-10 2021-05-25 勃林格殷格翰国际有限公司 作为血浆激肽释放酶抑制剂的苯基四唑衍生物
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
EP4010333A1 (en) * 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
JP7695232B2 (ja) 2019-09-18 2025-06-18 武田薬品工業株式会社 ヘテロアリール血漿カリクレインインヒビター
ES2987744T3 (es) 2019-09-18 2024-11-18 Takeda Pharmaceuticals Co Inhibidores de calicreína plasmática y usos de los mismos
TW202535863A (zh) 2020-02-13 2025-09-16 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
TW202144331A (zh) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
WO2021175290A1 (zh) * 2020-03-04 2021-09-10 南京明德新药研发有限公司 杂环类化合物
US12459927B2 (en) * 2020-06-16 2025-11-04 Merck Sharp & Dohme Llc Plasma kallikrein inhibitors
EP4210694B1 (en) * 2020-09-10 2025-10-15 Merck Sharp & Dohme LLC Plasma kallikrein inhibitors
WO2022079446A1 (en) 2020-10-15 2022-04-21 Kalvista Pharmaceuticals Limited Treatments of angioedema
WO2022172006A1 (en) 2021-02-09 2022-08-18 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
JP2024510503A (ja) 2021-03-17 2024-03-07 武田薬品工業株式会社 血漿カリクレイン阻害剤
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
CN116003386B (zh) * 2022-11-20 2024-03-26 药康众拓(北京)医药科技有限公司 一种氘代n-苄基吡啶酮吡唑甲酰胺类化合物、药物组合物和用途
WO2025153806A1 (en) 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity

Family Cites Families (97)

* Cited by examiner, † Cited by third party
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
US5786328A (en) 1995-06-05 1998-07-28 Genentech, Inc. Use of kunitz type plasma kallikrein inhibitors
US7101878B1 (en) 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
ID30460A (id) 1999-04-15 2001-12-06 Bristol Myers Squibb Co Inhibitor-inhibitor protein siklik tirosin kinase
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
WO2003037274A2 (en) 2001-11-01 2003-05-08 Icagen, Inc. Pyrazole-amides and-sulfonamides
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
ATE384053T1 (de) 2002-04-26 2008-02-15 Lilly Co Eli Triazolderivate als tachykininrezeptor- antagonisten
EP1426364A1 (en) 2002-12-04 2004-06-09 Aventis Pharma Deutschland GmbH Imidazole-derivatives as factor Xa inhibitors
DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
EP2308848A1 (en) 2003-02-03 2011-04-13 Janssen Pharmaceutica NV Quinoline-derived amide modulators of vanilloid VR1 receptor
EP2281885A1 (en) 2003-08-27 2011-02-09 Ophthotech Corporation Combination therapy for the treatment of ocular neovascular disorders
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
GB0403155D0 (en) 2004-02-12 2004-03-17 Vernalis Res Ltd Chemical compounds
EP1568698A1 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
WO2006025714A1 (en) 2004-09-03 2006-03-09 Yuhan Corporation PYRROLO[3,2-c]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
EP2500031A3 (en) 2005-02-24 2012-12-26 Joslin Diabetes Center, Inc. Compositions and Methods for Treating Vascular Permeability
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
KR101142363B1 (ko) 2005-06-27 2012-05-21 주식회사유한양행 피롤로피리딘 유도체를 포함하는 항암제 조성물
AU2006270322A1 (en) 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase 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
GB0606876D0 (en) 2006-04-05 2006-05-17 Glaxo Group Ltd Compounds
US20070258976A1 (en) 2006-05-04 2007-11-08 Ward Keith W Combination Therapy for Diseases Involving Angiogenesis
PL2049478T3 (pl) 2006-07-06 2012-09-28 Glaxo Group Ltd Podstawione N-fenylometylo 5-okso-prolino-2-amidy jako antagoniści receptora P2X7 oraz sposoby ich zastosowania
WO2008016883A2 (en) 2006-07-31 2008-02-07 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
NZ577719A (en) 2006-12-29 2012-06-29 Abbott Gmbh & Co Kg Pyrazol-1-yl-aryl amides and their analogues and their pharmaceutical uses
US20100119512A1 (en) 2007-01-25 2010-05-13 Joslin Diabetes Center Methods of diagnosing, treating, and preventing increased vascular permeability
MX2009009540A (es) 2007-03-07 2009-09-16 Alantos Pharm Holding Inhibidores de metaloproteasa que contienen una porcion heterociclica.
JP5427769B2 (ja) 2007-03-30 2014-02-26 サノフイ Pgds阻害剤としてのピリミジンヒドラジド化合物
WO2008119825A2 (en) 2007-04-03 2008-10-09 Glaxo Group Limited Imidazolidine carboxamide derivatives as p2x7 modulators
CL2008002172A1 (es) 2007-07-26 2008-11-21 Syngenta Participations Ag Compuestos derivados de pirazol-etiloxiamidas; compuestos intermediarios; metodo para controlar o prevenir la infestacion de plantas utiles por parte de microorganismos fitopatogenos; y composicion para controlar y proteger contra microorganismos fitopatogenos.
BRPI0815668A2 (pt) 2007-08-22 2017-05-23 Allergan Inc compostos pirrol tendo atividade biológica antagonista e agonista de receptor de esfingosina-1-fosfato.
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
WO2009083553A1 (en) 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
WO2009097141A1 (en) 2008-01-31 2009-08-06 Joslin Diabetes Center Methods for treatment of kallikrein-related disorders
WO2009106980A2 (en) 2008-02-29 2009-09-03 Pfizer Inc. Indazole derivatives
CN102026996B (zh) 2008-03-13 2015-01-07 百时美施贵宝公司 作为凝血因子xia抑制剂的哒嗪衍生物
WO2010004972A1 (ja) 2008-07-08 2010-01-14 第一三共株式会社 含窒素芳香族ヘテロシクリル化合物
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
MX2012006913A (es) 2009-12-18 2012-08-23 Activesite Pharmaceuticals Inc Profarmacos de inhibidores de calicreina plasmatica.
JP2011157349A (ja) 2010-01-07 2011-08-18 Daiichi Sankyo Co Ltd 含窒素芳香族ヘテロシクリル化合物を含有する医薬組成物
US8598206B2 (en) 2010-01-28 2013-12-03 The Medicines Company (Leipzig) Gmbh Trypsin-like serine protease inhibitors, and their preparation and use
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
WO2012009009A2 (en) 2010-07-14 2012-01-19 Addex Pharma S.A. Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
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
US9133128B2 (en) 2011-06-17 2015-09-15 Research Triangle Institute Pyrazole derivatives as cannabinoid receptor 1 antagonists
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
WO2013048982A1 (en) 2011-09-27 2013-04-04 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
EP2760828B1 (en) 2011-09-27 2015-10-21 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
EP2807156A1 (en) 2012-01-27 2014-12-03 Novartis AG Aminopyridine derivatives as plasma kallikrein inhibitors
US20140378474A1 (en) 2012-01-27 2014-12-25 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013130603A1 (en) 2012-02-27 2013-09-06 Board Of Regents, The University Of Texas System Ganglioside gd2 as a marker and target on cancer stem cells
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
GB201300304D0 (en) * 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
HK1211286A1 (en) 2013-01-08 2016-05-20 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
IL273688B2 (en) 2013-01-20 2024-12-01 Dyax Corp Evaluation and treatment of bradykinin-mediated disorders
MX373964B (es) 2013-03-15 2020-07-13 Verseon Corp Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.
CN105452240B (zh) 2013-05-23 2018-06-26 卡尔维斯塔制药有限公司 杂环衍生物
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
JP6527147B2 (ja) 2013-08-14 2019-06-05 カルヴィスタ ファーマシューティカルズ リミテッド 血漿カリクレインの阻害薬
US9611252B2 (en) 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
EA032713B1 (ru) 2013-12-30 2019-07-31 Лайфсай Фармасьютикалс, Инк. Терапевтические ингибирующие соединения
SG11201607267SA (en) 2014-03-07 2016-09-29 Biocryst Pharm Inc Human plasma kallikrein inhibitors
WO2015171526A2 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Tricyclic pyrazolopyridine compounds
WO2015171527A1 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
CN107072985B (zh) 2014-07-16 2020-02-07 莱福斯希医药公司 治疗性抑制化合物
JP6824876B2 (ja) 2014-08-22 2021-02-03 バイオクライスト ファーマシューティカルズ, インコーポレイテッド アミジン誘導体組成物及びそれらの使用
US10189810B2 (en) 2014-09-17 2019-01-29 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
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
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
SI3261639T1 (sl) 2015-02-27 2023-01-31 Verseon International Corporation Substituirane pirazolne spojine kot zaviralci serinskih proteaz
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
JP6917988B2 (ja) 2015-10-27 2021-08-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体
US10640486B2 (en) 2015-10-27 2020-05-05 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
GB201609519D0 (en) 2016-05-31 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of n-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyr idin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide
JP6884801B2 (ja) 2016-05-31 2021-06-09 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
GB201609602D0 (en) 2016-06-01 2016-07-13 Nucuna Biomed Ltd Chemical compounds
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
GB201609601D0 (en) 2016-06-01 2016-07-13 Nucana Biomed Ltd Phosphoramidate compounds
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
WO2018011628A1 (en) 2016-07-11 2018-01-18 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
TW201925188A (zh) 2017-11-29 2019-07-01 英商卡爾維斯塔製藥有限公司 酶抑制劑
GB201719882D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of a plasma kallikrein inhibitor and salts thereof
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof

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