CA2658523C - Inhibitors of plasma kallikrein - Google Patents

Inhibitors of plasma kallikrein Download PDF

Info

Publication number
CA2658523C
CA2658523C CA2658523A CA2658523A CA2658523C CA 2658523 C CA2658523 C CA 2658523C CA 2658523 A CA2658523 A CA 2658523A CA 2658523 A CA2658523 A CA 2658523A CA 2658523 C CA2658523 C CA 2658523C
Authority
CA
Canada
Prior art keywords
alkyl
compound
group
nhc
bond
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.)
Active
Application number
CA2658523A
Other languages
English (en)
French (fr)
Other versions
CA2658523A1 (en
Inventor
Sukanto Sinha
Tamie Jo Chilcote
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Activesite Pharmaceuticals Inc
Original Assignee
Activesite Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Activesite Pharmaceuticals Inc filed Critical Activesite Pharmaceuticals Inc
Publication of CA2658523A1 publication Critical patent/CA2658523A1/en
Application granted granted Critical
Publication of CA2658523C publication Critical patent/CA2658523C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/34—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; 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
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic 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
    • C07D307/56—Heterocyclic 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/26—Heterocyclic 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[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
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyrrole Compounds (AREA)
CA2658523A 2006-07-31 2007-07-30 Inhibitors of plasma kallikrein Active CA2658523C (en)

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 (2)

Publication Number Publication Date
CA2658523A1 CA2658523A1 (en) 2008-02-07
CA2658523C true CA2658523C (en) 2012-06-12

Family

ID=38997791

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2658523A Active CA2658523C (en) 2006-07-31 2007-07-30 Inhibitors of plasma kallikrein

Country Status (6)

Country Link
US (3) US7625944B2 (https=)
EP (1) EP2051707B1 (https=)
JP (1) JP5322935B2 (https=)
AU (1) AU2007281220B2 (https=)
CA (1) CA2658523C (https=)
WO (1) WO2008016883A2 (https=)

Families Citing this family (92)

* 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
US6057287A (en) 1994-01-11 2000-05-02 Dyax Corp. Kallikrein-binding "Kunitz domain" proteins and analogues thereof
ES2348230T3 (es) * 2002-06-07 2010-12-01 Dyax Corp. Prevención y reducción de la isquemia.
US7153829B2 (en) 2002-06-07 2006-12-26 Dyax Corp. Kallikrein-inhibitor therapies
EP2386310B1 (en) 2002-08-28 2018-11-07 Dyax Corp. Methods for preserving organs and tissues
BRPI0515140A (pt) * 2004-09-06 2008-07-08 Hoffmann La Roche derivados de benzamidina de 4-aminometila e seu emprego como inibidores do fator viia
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
EP1858542A4 (en) 2005-02-24 2009-08-19 Joslin Diabetes Center Inc COMPOSITIONS AND METHOD FOR THE TREATMENT OF VASPEREPERMABILITY
EP2001500A4 (en) * 2006-03-10 2010-07-28 Dyax Corp FORMULATIONS FOR ECALLANTIDE
PL2374472T3 (pl) 2006-03-16 2018-11-30 Dyax Corp. Kompozycje i sposoby leczenia zaburzeń okulistycznych
WO2008016883A2 (en) * 2006-07-31 2008-02-07 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
US20100119512A1 (en) * 2007-01-25 2010-05-13 Joslin Diabetes Center 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
EP2369930A4 (en) * 2008-12-02 2012-10-03 Joslin Diabetes Ct METHOD OF REDUCING BLOOD PRESSURE USING PLASMATIC KALLICREIN INHIBITORS
US8637454B2 (en) 2009-01-06 2014-01-28 Dyax Corp. Treatment of mucositis with kallikrein inhibitors
AU2010228068A1 (en) * 2009-03-25 2011-10-20 Diamedica Inc. Tissue kallikrein for the treatment of pancreatic beta-cell dysfunction
GB0918924D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Azaindole derivatives
GB0918922D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminopyridine derivatives
GB0918923D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminothiazole derivatives
US9206123B2 (en) 2009-12-18 2015-12-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
AU2010330743A1 (en) * 2009-12-18 2012-07-05 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
SMT201800552T1 (it) 2010-01-06 2018-11-09 Dyax Corp Proteine che legano la callicreina plasmatica
CN102918034B (zh) 2010-03-30 2015-06-03 维颂公司 多取代芳族化合物作为凝血酶的抑制剂
US9290485B2 (en) * 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
KR102320178B1 (ko) 2011-01-06 2021-11-02 다케다 파머수티컬 컴패니 리미티드 혈장 칼리크레인 결합 단백질
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
EP3320922A1 (en) 2011-06-10 2018-05-16 Ionis 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
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
US20130315891A1 (en) 2012-05-25 2013-11-28 Matthew Charles Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
US20130323222A1 (en) 2012-06-04 2013-12-05 Matthew Charles Human tissue kallikrein 1 glycosylation isoforms
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
EP2925746A1 (en) * 2012-12-03 2015-10-07 F. Hoffmann-La Roche AG Substituted triazole and imidazole compounds
PH12015501492B1 (en) 2013-01-08 2015-09-28 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
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
EP4234583A3 (en) 2013-01-20 2024-01-24 Takeda Pharmaceutical Company Limited Evaluation and treatment of bradykinin-mediated disorders
LT2968297T (lt) 2013-03-15 2019-01-10 Verseon Corporation Multipakeistieji aromatiniai junginiai kaip serino proteazės inhibitoriai
ES2791749T3 (es) 2013-03-15 2020-11-05 Verseon Corp Halogenopirazoles como inhibidores de la trombina
EP2999697B1 (en) 2013-05-23 2017-04-19 Kalvista Pharmaceuticals Limited Heterocyclic derivates
HUE14755117T2 (hu) * 2013-08-14 2018-12-28 Kalvista Pharmaceuticals Ltd Plazma-kallikrein inhibitorok
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
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
KR102365486B1 (ko) 2013-08-28 2022-02-18 아이오니스 파마수티컬즈, 인코포레이티드 프리칼리크레인 (pkk) 발현의 조절
WO2015061183A1 (en) 2013-10-21 2015-04-30 Dyax Corp. Assays for determining plasma kallikrein system biomarkers
CA2927695C (en) 2013-10-21 2022-03-01 Dyax Corp. Diagnosis and treatment of autoimmune diseases
EA038532B1 (ru) 2014-01-21 2021-09-10 Такеда Фармасьютикал Компани Лимитед Способ лечения наследственного ангионевротического отека (hae)
KR102736869B1 (ko) 2014-03-07 2024-12-02 바이오크리스트파마슈티컬즈,인코포레이티드 인간 혈장 칼리크레인 저해제
US10428158B2 (en) 2014-03-27 2019-10-01 Dyax Corp. Compositions and methods for treatment of diabetic macular edema
HUE052709T2 (hu) 2014-05-01 2021-05-28 Ionis Pharmaceuticals Inc Módosított antiszensz oligonukleotidok konjugátumai és azok alkalmazása PKK expressziójának módosítására
CN106687445A (zh) 2014-09-17 2017-05-17 维颂公司 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物
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
RU2017131562A (ru) 2015-02-27 2019-03-27 Версеон Корпорейшн Замещенные пиразольные соединения как ингибиторы сериновых протеаз
EP4354146B1 (en) 2015-10-19 2026-04-15 Takeda Pharmaceutical Company Limited Immunoassay for the detection of cleaved high molecular weight kininogen
EP3387018A1 (en) 2015-12-11 2018-10-17 Dyax Corp. Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack
DK3464271T3 (da) 2016-05-31 2020-06-15 Kalvista Pharmaceuticals Ltd Pyrazolderivater som plasma-kallikreininhibitorer
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
US11340237B2 (en) 2016-09-16 2022-05-24 Takeda Pharmaceutical Company Limited Metabolite biomarkers for diseases associated with the contact activation system
AU2018230478B2 (en) 2017-03-09 2025-01-23 Diamedica Inc. Dosage forms of tissue kallikrein 1
PT3716952T (pt) * 2017-11-29 2022-04-14 Kalvista Pharmaceuticals Ltd Formas de administração que incluem um inibidor de calicreína plasmática
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
EP3765459A1 (en) * 2018-03-13 2021-01-20 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
UY38438A (es) 2018-11-02 2020-05-29 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
JP2022539856A (ja) * 2019-07-08 2022-09-13 リゾルート，インコーポレイティド 血漿カリクレイン阻害薬の結晶形態
BR112022000113A2 (pt) * 2019-07-08 2022-03-15 Activesite Pharmaceuticals Inc Processos para preparação de inibidores de calicreí-na de plasma
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
DK4031547T3 (da) 2019-09-18 2024-09-09 Takeda Pharmaceuticals Co Plasmakallikreininhibitorer og anvendelser deraf
EP4031245A1 (en) 2019-09-18 2022-07-27 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
GB201918994D0 (en) 2019-12-20 2020-02-05 Kalvista Pharmaceuticals Ltd Treatments of diabetic macular edema and impaired visual acuity
GB2591730A (en) 2019-12-09 2021-08-11 Kalvista Pharmaceuticals Ltd New polymorphs
EP4090427A1 (en) 2020-01-13 2022-11-23 Takeda Pharmaceutical Company Limited Plasma kallikrein inhibitors and uses thereof for treating pediatric hereditary angioedema attack
CN115210230A (zh) 2020-03-04 2022-10-18 南京明德新药研发有限公司 杂环类化合物
WO2021217053A1 (en) * 2020-04-24 2021-10-28 Rezolute, Inc. Plasma kallikrein inhibitors for the treatment of ards and related conditions
WO2022079446A1 (en) 2020-10-15 2022-04-21 Kalvista Pharmaceuticals Limited Treatments of angioedema
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
EP4480545A3 (en) 2022-04-27 2025-02-26 Kalvista Pharmaceuticals Limited Formulations of a plasma kallikrein inhibitor
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
DE69110787T2 (de) 1990-02-28 1996-04-04 Medtronic, Inc., Minneapolis, Minn. Intraluminale prothese mit wirkstoffeluierung.
US5429634A (en) 1993-09-09 1995-07-04 Pdt Systems Biogenic implant for drug delivery and method
US5419760A (en) 1993-01-08 1995-05-30 Pdt Systems, Inc. Medicament dispensing stent for prevention of restenosis of a blood vessel
US6774278B1 (en) 1995-06-07 2004-08-10 Cook Incorporated Coated implantable medical device
SK174699A3 (en) * 1997-06-19 2000-08-14 Du Pont Pharm Co Inhibitors of factor xa with a neutral p1 specificity group
US5998424A (en) * 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group
DE19753522A1 (de) * 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
DK1042287T3 (da) * 1997-12-24 2005-08-15 Aventis Pharma Gmbh Indolderivater som inhibitorer af faktor Xa
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
BRPI0515140A (pt) * 2004-09-06 2008-07-08 Hoffmann La Roche derivados de benzamidina de 4-aminometila e seu emprego como inibidores do fator viia
CA2591786C (en) 2004-12-23 2013-07-16 Bernhard Nieswandt Prevention of thrombus formation and/or stabilization
WO2008016883A2 (en) 2006-07-31 2008-02-07 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein

Also Published As

Publication number Publication date
US20100130563A1 (en) 2010-05-27
JP2009545611A (ja) 2009-12-24
US7625944B2 (en) 2009-12-01
EP2051707A4 (en) 2011-04-27
CA2658523A1 (en) 2008-02-07
EP2051707A2 (en) 2009-04-29
US8258170B2 (en) 2012-09-04
WO2008016883A2 (en) 2008-02-07
EP2051707B1 (en) 2013-07-17
AU2007281220B2 (en) 2013-08-15
US7977380B2 (en) 2011-07-12
WO2008016883A3 (en) 2008-04-03
JP5322935B2 (ja) 2013-10-23
AU2007281220A1 (en) 2008-02-07
US20110301215A1 (en) 2011-12-08
US20080038276A1 (en) 2008-02-14

Similar Documents

Publication Publication Date Title
CA2658523C (en) Inhibitors of plasma kallikrein
US8691861B2 (en) Prodrugs of inhibitors of plasma kallikrein
US8609866B2 (en) Prodrugs of inhibitors of plasma kallikrein
CN101495468A (zh) 血浆激肽释放酶抑制剂
US6632815B2 (en) Inhibitors of factor Xa
JP2021119196A (ja) 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
US6720317B1 (en) Inhibitors of factor Xa
KR20080012304A (ko) 피라졸 화합물 및 이들 피라졸 화합물을 포함하여이루어지는 당뇨병 치료약
SK122398A3 (en) Substituted sulfonic acid n-[(aminoiminomethyl)phenylalkyl]- -azaheterocycloamide compounds
SI9620136A (sl) Substituirani N-/(aminoiminometil ali aminometil)fenil/-propil amidi
EP1666469A1 (en) Plasminogen activator inhibitor-1 inhibitor
US9206123B2 (en) Prodrugs of inhibitors of plasma kallikrein
RU2379288C2 (ru) Новые производные пирролидин-3,4-дикарбоксамида
US11267790B2 (en) Processes for preparing plasma kallikrein inhibitors
JP2005506299A (ja) 化合物および方法
JPH10287622A (ja) ブタジエン誘導体及びその製法
JPH11189530A (ja) 医薬組成物
LT4673B (lt) Azoto heteroaromatiniai junginiai kaip faktoriaus xa inhibitoriai

Legal Events

Date Code Title Description
EEER Examination request
MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 18TH ANNIV.) - STANDARD

Year of fee payment: 18

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250610

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250610