AR102851A1 - Compuestos de n-((het)arilmetil)-heteroaril-carboxamidas como inhibidores de calicreína plasmática - Google Patents

Compuestos de n-((het)arilmetil)-heteroaril-carboxamidas como inhibidores de calicreína plasmática

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Publication number
AR102851A1
AR102851A1 ARP150103901A ARP150103901A AR102851A1 AR 102851 A1 AR102851 A1 AR 102851A1 AR P150103901 A ARP150103901 A AR P150103901A AR P150103901 A ARP150103901 A AR P150103901A AR 102851 A1 AR102851 A1 AR 102851A1
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Argentina
Prior art keywords
independently selected
alkoxy
alkyl
alkylb
optionally substituted
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ARP150103901A
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English (en)
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Teanby Hodgson Simon
Joy Edwards Hannah
Louise Davie Rebecca
Michael Evans David
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Kalvista Pharmaceuticals Ltd
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Publication of AR102851A1 publication Critical patent/AR102851A1/es

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Abstract

Composiciones que comprenden dichos compuestos; el uso de estos compuestos en una terapia (por ejemplo en el tratamiento o la prevención de una enfermedad o condición en la cual está implicada la actividad de la calicreína plasmática); y métodos de tratamiento de pacientes con dichos compuestos. Reivindicación 1: Un compuesto caracterizado porque de fórmula (1), donde B es (CH₂)ₙ-fenilo, donde n es 0 ó 1 y fenilo está sustituido con 1 a 3 sustituyentes seleccionados entre alquilo, alcoxi, OH, halo, CN, COOR⁸, CONR⁸R⁹, OCF₃, CF₃ y NR⁸R⁹; o B es anillo heterocíclico de 5 ó 6 miembros que contiene uno o dos heteroátomos seleccionados entre N, O y S; dicho anillo heterocíclico puede ser aromático o no aromático y está sustituido con 1 a 3 sustituyentes seleccionados entre alquilo, alcoxi, OH, oxo, halo, CN, COOR⁸, CONR⁸R⁹, OCF₃, CF₃ y NR⁸R⁹; D se selecciona entre CH₂, CH-alquiloᵇ, C(alquilᵇ)₂ y CO; y U se selecciona entre CH₂, CH-alquiloᵇ y C(alquilᵇ)₂; y E se selecciona entre NH, N-alquiloᵇ, CH₂ y O; o U es CH; y E es N; donde U, D y E juntos forman parte de un azacarbociclo; W, X, Y y Z se seleccionan en forma independiente entre C, N, O y S, de manera que el anillo que contiene W, X, Y y Z es un heterociclo aromático de cinco miembros; R⁵, R⁶ y R⁷ en forma independiente están ausentes o se seleccionan en forma independiente entre H, alquilo, alcoxi, halo, OH, arilo, heteroarilo, -NR⁸R⁹, CN, COOR⁸, CONR⁸R⁹, -NR⁸COR⁹, CF₃, y R¹⁶; A se selecciona entre arilo y heteroarilo; R⁸ y R⁹ se seleccionan en forma independiente entre H y alquilo; R¹⁶ es un sistema de anillos monocíclico de 3, 4, 5 ó 6 miembros que contiene carbono que puede ser aromático, saturado o insaturado no aromático y que opcionalmente puede contener 1, 2, 3 ó 4 heteroátomos seleccionados entre N, O y S, donde el sistema de anillos R¹⁶ a su vez está opcionalmente sustituido con sustituyentes seleccionados entre alquilo y oxo; alquilo es un hidrocarburo saturado lineal que tiene hasta 10 átomos de carbono (C₁₋₁₀) o un hidrocarburo saturado ramificado de entre 3 y 10 átomos de carbono (C₃₋₁₀); alquilo puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre C₁₋₆ alcoxi, OH, CN, CF₃, COOR¹⁰, CONR¹⁰R¹¹, fluoro y NR¹⁰R¹¹; alquiloᵇ es un hidrocarburo saturado lineal que tiene hasta 6 átomos de carbono (C₁₋₆) o un hidrocarburo saturado ramificado de entre 3 y 6 átomos de carbono (C₃₋₆); alquiloᵇ puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre C₁₋₆ alcoxi, OH, CN, CF₃ y fluoro; alcoxi es un hidrocarburo lineal unido por O de entre 1 y 6 átomos de carbono (C₁₋₆) o un hidrocarburo ramificado unido por O de entre 3 y 6 átomos de carbono (C₃₋₆); alcoxi puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre OH, CN, CF₃, COOR¹⁰, CONR¹⁰R¹¹, fluoro y NR¹⁰R¹¹; azacarbociclo es un anillo monocíclico de 5 ó 6 miembros que contiene carbono, que comprende uno o dos átomos de nitrógeno en el anillo, y que puede estar opcionalmente sustituido con oxo; arilo es fenilo, bifenilo o naftilo; arilo puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, metilendioxi, etilendioxi, OH, OCF₃, halo, CN, heteroarilo, -(CH₂)₀₋₃-O-heteroarilo, ariloᵇ, -O-ariloᵇ, -(CH₂)₁₋₃-ariloᵇ, -(CH₂)₁₋₃-heteroarilo, -COOR¹⁰, -CONR¹⁰R¹¹, -(CH₂)₀₋₃-NR¹⁰R¹¹ y CF₃; ariloᵇ es fenilo, bifenilo o naftilo, que puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, halo, CN, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y NR¹⁰R¹¹; heteroarilo es un anillo aromático monocíclico o bicíclico de 5, 6, 9 ó 10 miembros, que contiene, donde sea posible, 1, 2 ó 3 miembros del anillo seleccionados en forma independiente entre N, NR⁸, S y O; heteroarilo puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, OCF₃, halo, CN, arilo, -(CH₂)₁₋₃-arilo, heteroariloᵇ, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y -(CH₂)₀₋₃-NR¹⁰R¹¹; heteroariloᵇ es un anillo aromático monocíclico o bicíclico de 5, 6, 9 ó 10 miembros, que contiene, donde sea posible, 1, 2 ó 3 miembros del anillo seleccionados en forma independiente entre N, NR⁸, S y O; donde heteroariloᵇ puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, halo, CN, arilo, -(CH₂)₁₋₃-arilo, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y NR¹⁰R¹¹; R¹⁰ y R¹¹ se seleccionan en forma independiente entre H, alquiloᵇ, CONR¹⁴R¹⁵, COR¹⁷, ariloᵇ y heteroarilᵇ; o R¹⁰ y R¹¹ junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros que contiene carbono, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, S y O, que puede ser saturado o insaturado con 1 ó 2 enlaces dobles y que puede estar opcionalmente mono- o di-sustituido con sustituyentes seleccionados entre oxo, alquiloᵇ, alcoxi, OH, halo y CF₃; R¹⁴, R¹⁵ y R¹⁷ se seleccionan en forma independiente entre H o alquiloᵇ; y tautómeros, isómeros, estereoisómeros (incluyendo enantiómeros, diasteroisómeros y mezclas racémicas y escalémicas de los mismos), sales farmacéuticamente aceptables y solvatos del mismo; con la condición de que el compuesto de fórmula (1) no es un compuesto de fórmula (2).
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Families Citing this family (13)

* 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
UA123735C2 (uk) 2016-05-31 2021-05-26 Калвіста Фармасьютікалз Лімітед Похідні піразолу як інгібітори калікреїну
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
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
MD3716952T2 (ro) 2017-11-29 2022-06-30 Kalvista Pharmaceuticals Ltd Forme de dozare cuprizând un inhibitor de kalikreină al plasmatică
GB201721515D0 (en) * 2017-12-21 2018-02-07 Kalvista Pharmaceuticals Ltd Dosage forms comprising a plasma kallikrein inhibtor
GB201719881D0 (en) * 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
AU2019234670B2 (en) 2018-03-13 2023-11-23 Takeda Pharmaceutical Company Limited Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN114667289A (zh) 2019-09-18 2022-06-24 武田药品工业有限公司 杂芳基血浆激肽释放酶抑制剂
EP4031547B1 (en) 2019-09-18 2024-07-17 Takeda Pharmaceutical Company Limited Plasma kallikrein inhibitors and uses thereof

Family Cites Families (85)

* 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
US7101878B1 (en) 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
DK1169038T3 (da) 1999-04-15 2012-11-26 Bristol Myers Squibb Co Cykliske proteintyrosinkinaseinhibitorer
CA2463975A1 (en) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
EP1451160B1 (en) 2001-11-01 2010-01-13 Icagen, Inc. Pyrazole-amides for use in the treatment of pain
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
PE20040600A1 (es) 2002-04-26 2004-09-15 Lilly Co Eli Derivados de triazol como antagonistas del receptor de taquicinina
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
WO2004069792A2 (en) 2003-02-03 2004-08-19 Janssen Pharmaceutica N.V. Quinoline-derived amide modulators of vanilloid vr1 receptor
WO2005020972A2 (en) 2003-08-27 2005-03-10 (Osi) Eyetech, Inc. 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
EP1858542A4 (en) 2005-02-24 2009-08-19 Joslin Diabetes Center Inc COMPOSITIONS AND METHODS FOR TREATING VASCULAR PERMEABILITY
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
CN101263121A (zh) 2005-07-14 2008-09-10 塔克达圣地亚哥公司 组蛋白脱乙酰基酶抑制剂
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
EP2051707B1 (en) 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
AU2007341232B2 (en) 2006-12-29 2013-01-31 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors
US20100119512A1 (en) 2007-01-25 2010-05-13 Joslin Diabetes Center Methods of diagnosing, treating, and preventing increased vascular permeability
CA2680312A1 (en) 2007-03-07 2008-09-12 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors containing a heterocyclic moiety
NZ579892A (en) 2007-03-30 2012-03-30 Sanofi Aventis Pyrimidine hydrazide compounds as prostaglandin D synthase inhibitors
WO2009012998A1 (en) 2007-07-26 2009-01-29 Syngenta Participations Ag Novel microbiocides
JP2010536871A (ja) 2007-08-22 2010-12-02 アラーガン、インコーポレイテッド スフィンゴシン−１−リン酸受容体アゴニストまたはアンタゴニスト生物学的活性を有するピロール化合物
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009083553A1 (en) 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
EP2259679A4 (en) 2008-01-31 2011-09-14 Joslin Diabetes Ct METHOD FOR THE TREATMENT OF CALLIQUE CLEANING DISORDERS
WO2009106980A2 (en) 2008-02-29 2009-09-03 Pfizer Inc. Indazole derivatives
US8324199B2 (en) 2008-03-13 2012-12-04 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
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.
AU2011210802B2 (en) 2010-01-28 2014-10-16 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
EP2590945B1 (en) 2010-07-07 2014-04-30 The Medicines Company (Leipzig) GmbH Serine protease inhibitors
EP2595986A2 (en) 2010-07-14 2013-05-29 Addex Pharma SA 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
WO2012174362A1 (en) 2011-06-17 2012-12-20 Research Triangle Institute Pyrazole derivatives as cannabinoid receptor 1 antagonists
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
EP2760828B1 (en) 2011-09-27 2015-10-21 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
WO2013048982A1 (en) * 2011-09-27 2013-04-04 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
EP2807157A1 (en) 2012-01-27 2014-12-03 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
JP5989805B2 (ja) 2012-02-10 2016-09-07 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． メチル基変更酵素の調節物質、組成物及びその使用
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
JP2016518305A (ja) 2013-01-08 2016-06-23 ザヴィラ ファーマシューティカルズ ゲーエムベーハー ピリミドン誘導体及びウイルス性疾患の治療、改善又は予防におけるそれらの使用
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
CN105324117B (zh) 2013-03-15 2019-04-09 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物
PT3305778T (pt) 2013-05-23 2022-05-02 Kalvista Pharmaceuticals Ltd Inibidores de calicreína plasmática
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
PL3033336T3 (pl) 2013-08-14 2018-11-30 Kalvista Pharmaceuticals Limited Inhibitory kalikreiny w plaźmie
JP6759100B2 (ja) 2013-12-30 2020-09-23 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
US9611252B2 (en) 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
PT3828173T (pt) 2014-03-07 2022-12-05 Biocryst Pharm Inc Pirazois substituídos como inibidores de calicreína plasmática humana
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
EP3169325B1 (en) 2014-07-16 2021-04-28 Attune Pharmaceuticals, Inc. Therapeutic inhibitory compounds
US10905683B2 (en) 2014-08-22 2021-02-02 Biocryst Pharmaceuticals, Inc. Compositions and uses of amidine derivatives
RU2017112739A (ru) 2014-09-17 2018-10-17 Версеон Корпорейшн Пиразолил-замещенные пиридоновые соединения как ингибиторы сериновых протеаз
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
AU2016224974B2 (en) 2015-02-27 2019-09-26 Verseon Corporation Substituted pyrazole compounds as serine protease 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
US10640486B2 (en) 2015-10-27 2020-05-05 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
US10399961B2 (en) 2015-10-27 2019-09-03 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
UA123735C2 (uk) 2016-05-31 2021-05-26 Калвіста Фармасьютікалз Лімітед Похідні піразолу як інгібітори калікреїну
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
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
CN110022875A (zh) 2016-07-11 2019-07-16 莱福斯希医药公司 治疗性抑制化合物
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
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

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