MX345259B - Inhibidores de serina proteasas similares a tripsina, y su preparación y uso. - Google Patents

Inhibidores de serina proteasas similares a tripsina, y su preparación y uso.

Info

Publication number
MX345259B
MX345259B MX2012008813A MX2012008813A MX345259B MX 345259 B MX345259 B MX 345259B MX 2012008813 A MX2012008813 A MX 2012008813A MX 2012008813 A MX2012008813 A MX 2012008813A MX 345259 B MX345259 B MX 345259B
Authority
MX
Mexico
Prior art keywords
trypsin
preparation
protease inhibitors
serine protease
compounds
Prior art date
Application number
MX2012008813A
Other languages
English (en)
Other versions
MX2012008813A (es
Inventor
Herold Peter
Daghish Mohammed
Jelakovic Stjepan
Ludwig Friedrich-Alexander
Reichelt Claudia
Schulze Alexander
Schweinitz Andrea
Original Assignee
The Medicines Company (Leipzig) Gmbh
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 The Medicines Company (Leipzig) Gmbh filed Critical The Medicines Company (Leipzig) Gmbh
Publication of MX2012008813A publication Critical patent/MX2012008813A/es
Publication of MX345259B publication Critical patent/MX345259B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

La invención proporciona compuestos que son efectivos como inhibidores de la plasmina y calicreína plasmática humanas, y que son útiles para la prevención de la pérdida de sangre y como componentes de adhesivos de fibrina. La invención además proporciona métodos para elaborar y utilizar los compuestos.
MX2012008813A 2010-01-28 2011-01-28 Inhibidores de serina proteasas similares a tripsina, y su preparación y uso. MX345259B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29905410P 2010-01-28 2010-01-28
PCT/US2011/022863 WO2011094496A2 (en) 2010-01-28 2011-01-28 Trypsin-like serine protease inhibitors, and their preparation and use

Publications (2)

Publication Number Publication Date
MX2012008813A MX2012008813A (es) 2012-11-23
MX345259B true MX345259B (es) 2017-01-23

Family

ID=44320136

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012008813A MX345259B (es) 2010-01-28 2011-01-28 Inhibidores de serina proteasas similares a tripsina, y su preparación y uso.

Country Status (12)

Country Link
US (2) US8598206B2 (es)
EP (1) EP2528895B1 (es)
JP (1) JP5709902B2 (es)
CN (1) CN102858744B (es)
AU (1) AU2011210802B2 (es)
BR (1) BR112012019042A8 (es)
CA (1) CA2788417C (es)
EA (1) EA022121B1 (es)
ES (1) ES2569983T3 (es)
MX (1) MX345259B (es)
NZ (1) NZ601521A (es)
WO (1) WO2011094496A2 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd 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
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
WO2015171527A1 (en) * 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
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
EP3383847B1 (en) * 2015-12-02 2022-08-24 Merck Sharp & Dohme LLC FACTOR XIa INHIBITORS
KR102424709B1 (ko) 2016-05-31 2022-07-22 칼비스타 파마슈티컬즈 리미티드 혈장 칼리크레인 저해제로서 피라졸 유도체
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
EP3541381B1 (en) 2016-11-18 2022-12-28 Merck Sharp & Dohme LLC Inhibitors of factor xiia
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
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
BR112022001054A2 (pt) * 2019-08-21 2022-03-15 Kalvista Pharmaceuticals Ltd Inibidores enzimáticos

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2806722B1 (fr) * 2000-03-23 2002-05-17 Sanofi Synthelabo Derives de n-(heterocyclylbutyl) benzene-ou pyridine sulfonamide, leur preparation et leur application en therapeutique
DE10210590A1 (de) * 2002-03-11 2003-10-02 Curacyte Ag Hemmstoffe des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
DE10342108A1 (de) * 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
DE102006050672A1 (de) * 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins

Also Published As

Publication number Publication date
WO2011094496A2 (en) 2011-08-04
US9611290B2 (en) 2017-04-04
US20110301196A1 (en) 2011-12-08
EP2528895A4 (en) 2014-10-15
ES2569983T3 (es) 2016-05-13
EP2528895A2 (en) 2012-12-05
US20140073573A1 (en) 2014-03-13
CN102858744B (zh) 2015-03-04
EA201270703A1 (ru) 2013-03-29
EA022121B1 (ru) 2015-11-30
AU2011210802B2 (en) 2014-10-16
US8598206B2 (en) 2013-12-03
JP5709902B2 (ja) 2015-04-30
CA2788417A1 (en) 2011-08-04
WO2011094496A3 (en) 2011-12-29
BR112012019042A2 (pt) 2016-09-13
CA2788417C (en) 2017-02-14
BR112012019042A8 (pt) 2017-12-26
CN102858744A (zh) 2013-01-02
AU2011210802A1 (en) 2012-08-23
JP2013518126A (ja) 2013-05-20
MX2012008813A (es) 2012-11-23
EP2528895B1 (en) 2016-03-30
NZ601521A (en) 2014-09-26

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