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AR039868A1 - Inhibidores selectivos de la enzima kalikreina plasmatica - Google Patents

Inhibidores selectivos de la enzima kalikreina plasmatica

Info

Publication number
AR039868A1
AR039868A1 ARP030100772A ARP030100772A AR039868A1 AR 039868 A1 AR039868 A1 AR 039868A1 AR P030100772 A ARP030100772 A AR P030100772A AR P030100772 A ARP030100772 A AR P030100772A AR 039868 A1 AR039868 A1 AR 039868A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
optionally substituted
kalikreina
plasmatic
enzyme
Prior art date
Application number
ARP030100772A
Other languages
English (en)
Original Assignee
Ferring Bv
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 Ferring Bv filed Critical Ferring Bv
Publication of AR039868A1 publication Critical patent/AR039868A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00Antineoplastic 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
    • 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
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuestos de la fórmula general 1, o sales de los mismos aceptables para el uso farmacéutico, donde R1 se selecciona entre H, alquilo inferior, R4-CO, R4-O2CCH2, R5-OCO y R5-SO2; R2 se selecciona entre alquilo inferior, cicloalquilo opcionalmente sustituido con un grupo alquilo o alquiloxilo, (C5-12) cicloalquilalquilo opcionalmente sustituido con un grupo alquilo o alquiloxilo, aralquilo opcionalmente sustituido con hasta tres grupos seleccionados entre F, Cl, Br, I, OH, alquilo inferior y O-(alquilo inferior), O-bencilo, NH2, NO2, NH-acilo, CN y CF3, y aralquiloximetilo opcionalmente sustituido hasta tres grupos seleccionados entre F, Cl, Br, OH, alquilo inferior y O-(alquilo inferior); o R1 y R2 son juntos un grupo o-xilileno, opcionalmente sustituido en el anillo aromático con un grupo seleccionado entre F, Cl, Br, OH, alquilo inferior y O-(alquilo inferior); R3 se selecciona entre H, OH y O-alquilo inferior; R4 se selecciona entre H, alquilo inferior y fenilo; y R5 se selecciona entre alquilo inferior, fenilo y bencilo. Los compuestos son útiles como composiciones farmacéuticas.
ARP030100772A 2002-03-08 2003-03-06 Inhibidores selectivos de la enzima kalikreina plasmatica AR039868A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0205527.5A GB0205527D0 (en) 2002-03-08 2002-03-08 Inhibitors

Publications (1)

Publication Number Publication Date
AR039868A1 true AR039868A1 (es) 2005-03-09

Family

ID=9932619

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030100772A AR039868A1 (es) 2002-03-08 2003-03-06 Inhibidores selectivos de la enzima kalikreina plasmatica

Country Status (26)

Country Link
US (1) US7649000B2 (es)
EP (1) EP1483284B1 (es)
JP (1) JP4330450B2 (es)
KR (1) KR100974633B1 (es)
CN (1) CN1274713C (es)
AR (1) AR039868A1 (es)
AT (1) ATE333463T1 (es)
AU (1) AU2003208471B2 (es)
CA (1) CA2478099C (es)
DE (1) DE60306904T2 (es)
DK (1) DK1483284T3 (es)
EG (1) EG25482A (es)
ES (1) ES2264523T3 (es)
GB (1) GB0205527D0 (es)
IL (2) IL163710A0 (es)
MX (1) MXPA04008523A (es)
MY (1) MY130830A (es)
NO (1) NO332678B1 (es)
NZ (1) NZ534891A (es)
PL (1) PL209670B1 (es)
PT (1) PT1483284E (es)
RU (1) RU2301225C2 (es)
TW (1) TWI283685B (es)
UY (1) UY27699A1 (es)
WO (1) WO2003076458A2 (es)
ZA (1) ZA200406856B (es)

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* Cited by examiner, † Cited by third party
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EP1736465A4 (en) 2004-03-31 2009-06-17 Ajinomoto Kk ANILINE DERIVATIVES
JP2010536870A (ja) * 2007-08-21 2010-12-02 ジェンザイム・コーポレーション カリクレイン阻害剤を用いた治療
GB0918924D0 (en) * 2009-10-28 2009-12-16 Vantia Ltd Azaindole derivatives
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
WO2013111107A1 (en) 2012-01-27 2013-08-01 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
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
IL239682B (en) 2013-01-08 2018-10-31 Kalvista Pharmaceuticals Ltd History of benzylamine and 2-(aminomethyl)pyridine
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
CA2912285C (en) 2013-05-23 2021-07-13 Kalvista Pharmaceuticals Limited Fused 6,5 or 6,6-heteroaromatic bicyclic amide derivatives and pharmaceutical compositions thereof useful as plasma kallikrein inhibitor
PL3033336T3 (pl) 2013-08-14 2018-11-30 Kalvista Pharmaceuticals Limited Inhibitory kalikreiny w plaźmie
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
WO2015063465A2 (en) * 2013-10-28 2015-05-07 Bicycle Therapeutics Limited Novel polypeptides
CN108892661B (zh) 2014-02-07 2023-03-14 艾克赛特赫拉制药有限责任公司 治疗化合物和组合物
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme 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
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
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
HUE057912T2 (hu) 2017-11-29 2022-06-28 Kalvista Pharmaceuticals Ltd Plazma kallikrein inhibitort tartalmazó dózisformák
EP3873446A4 (en) 2018-10-30 2022-08-03 Exithera Pharmaceuticals Inc. THERAPEUTIC COMPOUNDS AND COMPOSITIONS
GB201910116D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of hereditary angioedema
GB201910125D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of angioedema
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited 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
WO2021198534A1 (en) 2020-04-04 2021-10-07 Oxurion NV Plasma kallikrein inhibitors for use in the treatment of coronaviral disease
WO2022079446A1 (en) 2020-10-15 2022-04-21 Kalvista Pharmaceuticals Limited Treatments of angioedema
US20230381162A1 (en) 2020-10-23 2023-11-30 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
WO2023144030A1 (en) 2022-01-31 2023-08-03 Oxurion NV Plasma kallikrein inhibitor therapy for anti-vegf sensitization
WO2023148016A1 (en) 2022-02-04 2023-08-10 Oxurion NV Biomarker for plasma kallikrein inhibitor therapy response
HRP20241160T1 (hr) 2022-04-27 2024-11-22 Kalvista Pharmaceuticals Limited Formulacije inhibitora kalikreina u plazmi
EP4673437A1 (en) 2023-02-27 2026-01-07 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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9019558D0 (en) * 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
AU2882792A (en) * 1991-10-23 1993-05-21 Procter & Gamble Company, The Tripeptide derivative anti-inflammatory agents
SE9301911D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptide derivatives
GB9318637D0 (en) * 1993-09-08 1993-10-27 Ferring Res Ltd Enzyme inhibitors

Also Published As

Publication number Publication date
CN1639186A (zh) 2005-07-13
EP1483284A2 (en) 2004-12-08
JP4330450B2 (ja) 2009-09-16
IL163710A0 (en) 2005-12-18
CA2478099A1 (en) 2003-09-18
TW200403255A (en) 2004-03-01
TWI283685B (en) 2007-07-11
PL209670B1 (pl) 2011-10-31
EP1483284B1 (en) 2006-07-19
KR100974633B1 (ko) 2010-08-06
ZA200406856B (en) 2005-11-30
NZ534891A (en) 2006-03-31
US7649000B2 (en) 2010-01-19
DE60306904D1 (de) 2006-08-31
CA2478099C (en) 2011-10-04
ES2264523T3 (es) 2007-01-01
IL163710A (en) 2010-12-30
US20060052313A1 (en) 2006-03-09
DK1483284T3 (da) 2006-10-16
AU2003208471B2 (en) 2006-09-28
HK1072265A1 (en) 2005-08-19
WO2003076458A3 (en) 2003-11-06
PT1483284E (pt) 2006-11-30
CN1274713C (zh) 2006-09-13
NO332678B1 (no) 2012-12-03
UY27699A1 (es) 2003-10-31
MXPA04008523A (es) 2004-12-06
NO20043695L (no) 2004-10-07
JP2005533750A (ja) 2005-11-10
PL372977A1 (en) 2005-08-08
DE60306904T2 (de) 2007-02-08
AU2003208471A1 (en) 2003-09-22
MY130830A (en) 2007-07-31
KR20040089705A (ko) 2004-10-21
EG25482A (en) 2012-01-15
RU2301225C2 (ru) 2007-06-20
GB0205527D0 (en) 2002-04-24
RU2004126610A (ru) 2005-05-27
WO2003076458A2 (en) 2003-09-18
ATE333463T1 (de) 2006-08-15

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