JP5322935B2 - 血漿カリクレインの阻害薬 - Google Patents

血漿カリクレインの阻害薬 Download PDF

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JP5322935B2
JP5322935B2 JP2009522995A JP2009522995A JP5322935B2 JP 5322935 B2 JP5322935 B2 JP 5322935B2 JP 2009522995 A JP2009522995 A JP 2009522995A JP 2009522995 A JP2009522995 A JP 2009522995A JP 5322935 B2 JP5322935 B2 JP 5322935B2
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pharmaceutically acceptable
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JP2009545611A (ja
JP2009545611A5 (enExample
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スカント シンハ
タミー ジョー チルコッテ
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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
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2009522995A 2006-07-31 2007-07-30 血漿カリクレインの阻害薬 Active JP5322935B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US83437706P 2006-07-31 2006-07-31
US60/834,377 2006-07-31
US91903107P 2007-03-20 2007-03-20
US60/919,031 2007-03-20
PCT/US2007/074761 WO2008016883A2 (en) 2006-07-31 2007-07-30 Inhibitors of plasma kallikrein

Publications (3)

Publication Number Publication Date
JP2009545611A JP2009545611A (ja) 2009-12-24
JP2009545611A5 JP2009545611A5 (enExample) 2010-12-02
JP5322935B2 true JP5322935B2 (ja) 2013-10-23

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US (3) US7625944B2 (enExample)
EP (1) EP2051707B1 (enExample)
JP (1) JP5322935B2 (enExample)
AU (1) AU2007281220B2 (enExample)
CA (1) CA2658523C (enExample)
WO (1) WO2008016883A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2764680B2 (ja) 1993-07-20 1998-06-11 重良 長沼 フォーミングローラ装置

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6057287A (en) 1994-01-11 2000-05-02 Dyax Corp. Kallikrein-binding "Kunitz domain" proteins and analogues thereof
ES2528254T3 (es) 2002-06-07 2015-02-05 Dyax Corp. Polipéptidos de dominio Kunitz modificado y su uso para reducir la isquemia o el inicio de una respuesta inflamatoria sistémica asociada con un procedimiento quirúrgico
US7153829B2 (en) 2002-06-07 2006-12-26 Dyax Corp. Kallikrein-inhibitor therapies
JP2005537006A (ja) 2002-08-28 2005-12-08 ダイアックス、コープ 臓器及び組織の保存方法
RU2007112688A (ru) * 2004-09-06 2008-10-20 Ф.Хоффманн-Ля Рош Аг (Ch) Производные 4-аминометилбензамина и их применение в качестве ингибиторов фактора viia
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
WO2006091459A2 (en) * 2005-02-24 2006-08-31 Joslin Diabetes Center, Inc. Compositions and methods for treating vascular permeability
US20070213275A1 (en) * 2006-03-10 2007-09-13 Dyax Corp. Formulations for ecallantide
SI1854477T1 (sl) 2006-03-16 2017-01-31 Dyax Corp. Peptidi, ki inhibirajo plazma kalikrein za uporabo pri zdravljenju očesnih motenj
EP2051707B1 (en) 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
US8524917B2 (en) * 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
WO2008091692A2 (en) * 2007-01-25 2008-07-31 Joslin Diabetes Center, Inc. Methods of diagnosing, treating, and preventing increased vascular permeability
US8563594B2 (en) 2007-05-08 2013-10-22 Allergan, Inc. S1P3 receptor inhibitors for treating pain
EP2259679A4 (en) * 2008-01-31 2011-09-14 Joslin Diabetes Ct METHODS OF TREATING KALLIKREIN RELATED DISORDERS
US20110318359A1 (en) * 2008-12-02 2011-12-29 Feener Edward P Method for reducing blood pressure using inhibitors of plasma kallikrein
EP2385843A4 (en) 2009-01-06 2013-02-27 Dyax Corp TREATMENT OF MUZOSITIS WITH CALLICINE INHIBITORS
CN102438648A (zh) * 2009-03-25 2012-05-02 代阿麦迪卡股份有限公司 用于治疗胰腺β细胞功能障碍的组织激肽释放酶
GB0918924D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Azaindole derivatives
GB0918923D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminothiazole derivatives
GB0918922D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminopyridine derivatives
SG181811A1 (en) * 2009-12-18 2012-07-30 Activesite Pharmaceuticals Inc Prodrugs of inhibitors of plasma kallikrein
US9206123B2 (en) 2009-12-18 2015-12-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
HRP20220107T1 (hr) 2010-01-06 2022-04-15 Takeda Pharmaceutical Company Limited Proteini koji vežu kalikrein plazme
CA2829790C (en) 2010-03-30 2018-06-05 Verseon Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
CN105713092B (zh) 2011-01-06 2019-09-10 戴埃克斯有限公司 血浆前激肽释放酶结合蛋白
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2012170945A2 (en) 2011-06-10 2012-12-13 Isis Pharmaceuticals, Inc. Methods for modulating kallikrein (klkb1) expression
US9322021B2 (en) 2011-06-29 2016-04-26 Ionis Pharmaceuticals, Inc. Methods for modulating kallikrein (KLKB1) expression
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
US10188302B2 (en) * 2011-12-31 2019-01-29 The University Of Vermont And State Agriculture College Methods for dynamic visualization of clinical parameters over time
EP2807157A1 (en) 2012-01-27 2014-12-03 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
US20130315891A1 (en) 2012-05-25 2013-11-28 Matthew Charles Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
PT2854841T (pt) 2012-06-04 2017-05-15 Diamedica Inc Isoformas de glicosilação da calicreína 1 em tecido humano
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
CA2893239A1 (en) * 2012-12-03 2014-06-12 F. Hoffmann-La Roche Ag Substituted triazole and imidazole compounds
IL239682B (en) 2013-01-08 2018-10-31 Kalvista Pharmaceuticals Ltd History of benzylamine and 2-(aminomethyl)pyridine
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
ES2692408T3 (es) * 2013-01-20 2018-12-03 Dyax Corp. Evaluación y tratamiento de trastornos mediados por bradiquinina
EP3421036B8 (en) 2013-03-15 2020-12-30 Verseon International Corporation Multisubstituted aromatic compounds as serine protease inhibitors
CA2902431A1 (en) 2013-03-15 2014-09-25 Kevin Michael Short Halogenopyrazoles as inhibitors of thrombin
RU2712621C2 (ru) 2013-05-23 2020-01-30 Калвиста Фармасьютикалз Лимитед Азотсодержащие гетероциклические производные, полезные в качестве ингибитора калликреина плазмы
HUE14755117T2 (hu) 2013-08-14 2018-12-28 Kalvista Pharmaceuticals Ltd Plazma-kallikrein inhibitorok
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
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
CN105517556B (zh) 2013-08-28 2021-02-02 Ionis制药公司 前激肽释放酶(pkk)表达的调节
ES2873204T3 (es) 2013-10-21 2021-11-03 Takeda Pharmaceuticals Co Diagnóstico y tratamiento de enfermedades autoinmunes
IL289514B2 (en) 2013-10-21 2024-01-01 Takeda Pharmaceuticals Co Assays for determining plasma kallikrein system biomarkers
PT3096798T (pt) 2014-01-21 2021-02-25 Dyax Corp Proteínas de ligação à calicreína plasmática e seus usos no tratamento de angioedema hereditário
LT3828173T (lt) 2014-03-07 2022-11-10 Biocryst Pharmaceuticals, Inc. Pakeistieji pirazolai kaip žmogaus plazmos kalikreino inhibitoriai
IL247942B (en) 2014-03-27 2022-09-01 Dyax Corp Compositions and methods for drops in macular edema as a result of diabetes
ES2849600T3 (es) 2014-05-01 2021-08-19 Ionis Pharmaceuticals Inc Conjugados de oligonucleótidos antisentido modificados y su uso para modular la expresión de PKK
RU2017112739A (ru) 2014-09-17 2018-10-17 Версеон Корпорейшн Пиразолил-замещенные пиридоновые соединения как ингибиторы сериновых протеаз
GB201421088D0 (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
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
SG11201706411YA (en) 2015-02-27 2017-09-28 Verseon Corp Substituted pyrazole compounds as serine protease inhibitors
MX2018004763A (es) 2015-10-19 2018-09-06 Dyax Corp Inmunoensayo para detectar quininogeno escindido de alto peso molecular.
KR20250139401A (ko) 2015-12-11 2025-09-23 다케다 파머수티컬 컴패니 리미티드 혈장 칼리크레인 저해제 및 유전성 혈관부종 발작을 치료하기 위한 이의 용도
SG10201913616UA (en) 2016-05-31 2020-03-30 Kalvista Pharmaceuticals Ltd 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
CN109716137B (zh) * 2016-09-16 2023-07-21 武田药品工业株式会社 用于与接触活化系统相关的疾病的代谢产物生物标记
CA3054962A1 (en) 2017-03-09 2018-09-13 Rick PAULS Dosage forms of tissue kallikrein 1
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
MX2020005168A (es) 2017-11-29 2020-08-20 Kalvista Pharmaceuticals Ltd Formas de dosificacion que contienen un inhibidor calicreina de plasma.
WO2019178129A1 (en) * 2018-03-13 2019-09-19 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
AR116951A1 (es) 2018-11-02 2021-06-30 Biocryst Pharm Inc Sales cristalinas de un inhibidor de calicreína plasmática
GB201910125D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of angioedema
GB201910116D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of hereditary angioedema
EP3996707A4 (en) * 2019-07-08 2023-02-22 Rezolute, Inc. CRYSTALLINE FORMS OF PLASMACALLICREIN INHIBITORS
BR112022000113A2 (pt) * 2019-07-08 2022-03-15 Activesite Pharmaceuticals Inc Processos para preparação de inibidores de calicreí-na de plasma
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
WO2021055589A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Heteroaryl plasma kallikrein inhibitors
PT4031547T (pt) 2019-09-18 2024-08-27 Takeda Pharmaceuticals Co Inibidores de calicreína plasmática e utilizações dos mesmos
GB2591730A (en) 2019-12-09 2021-08-11 Kalvista Pharmaceuticals Ltd New polymorphs
GB201918994D0 (en) 2019-12-20 2020-02-05 Kalvista Pharmaceuticals Ltd Treatments of diabetic macular edema and impaired visual acuity
JP7245397B2 (ja) 2020-03-04 2023-03-23 メッドシャイン ディスカバリー インコーポレイテッド 複素環化合物
WO2021217053A1 (en) * 2020-04-24 2021-10-28 Rezolute, Inc. Plasma kallikrein inhibitors for the treatment of ards and related conditions
TW202228686A (zh) 2020-10-15 2022-08-01 英商卡爾維斯塔製藥有限公司 血管性水腫之治療
EP4232031A1 (en) 2020-10-23 2023-08-30 Kalvista Pharmaceuticals Limited Treatments of angioedema
JP2024505596A (ja) 2021-02-09 2024-02-06 カルビスタ・ファーマシューティカルズ・リミテッド 遺伝性血管性浮腫の治療
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
DK4288036T3 (da) 2022-04-27 2024-08-26 Kalvista Pharmaceuticals Ltd Formuleringer af en plasmakallikreinhæmmer
WO2024180100A1 (en) 2023-02-27 2024-09-06 Kalvista Pharmaceuticals Limited New solid form of a plasma kallikrein inhibitor
WO2025153806A1 (en) 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity
WO2025172693A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema
WO2025172692A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
LU86084A1 (fr) 1985-09-20 1987-04-02 Faco Sa Apparei de massage electrique
US5102417A (en) 1985-11-07 1992-04-07 Expandable Grafts Partnership Expandable intraluminal graft, and method and apparatus for implanting an expandable intraluminal graft
US4800882A (en) 1987-03-13 1989-01-31 Cook Incorporated Endovascular stent and delivery system
US4886062A (en) 1987-10-19 1989-12-12 Medtronic, Inc. Intravascular radially expandable stent and method of implant
WO1990013332A1 (en) 1989-05-11 1990-11-15 Cedars-Sinai Medical Center Stent with sustained drug delivery
EP0470246B1 (en) 1990-02-28 1995-06-28 Medtronic, Inc. Intralumenal drug eluting prosthesis
US5419760A (en) 1993-01-08 1995-05-30 Pdt Systems, Inc. Medicament dispensing stent for prevention of restenosis of a blood vessel
US5429634A (en) 1993-09-09 1995-07-04 Pdt Systems Biogenic implant for drug delivery and method
US6774278B1 (en) 1995-06-07 2004-08-10 Cook Incorporated Coated implantable medical device
US5998424A (en) * 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group
HUP0003906A2 (hu) * 1997-06-19 2001-05-28 Du Pont Pharmaceuticals Co. Xa faktort gátló hatású heterociklusos vegyületek és ezeket tartalmazó gyógyszerkészítmények
DE19753522A1 (de) * 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
PL195682B1 (pl) * 1997-12-24 2007-10-31 Sanofi Aventis Deutschland Pochodne indolu, sposób ich wytwarzania, środek farmaceutyczny oraz zastosowanie pochodnych indolu
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6770729B2 (en) 2002-09-30 2004-08-03 Medtronic Minimed, Inc. Polymer compositions containing bioactive agents and methods for their use
RU2007112688A (ru) * 2004-09-06 2008-10-20 Ф.Хоффманн-Ля Рош Аг (Ch) Производные 4-аминометилбензамина и их применение в качестве ингибиторов фактора viia
EP1830924B1 (en) 2004-12-23 2013-02-27 CSL Behring GmbH Prevention of thrombus formation and/or stabilization
EP2051707B1 (en) * 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2764680B2 (ja) 1993-07-20 1998-06-11 重良 長沼 フォーミングローラ装置

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