AR020922A1 - Inhibidor de proteasas de serina, su uso y una composicion farmaceutica que lo comprende - Google Patents

Inhibidor de proteasas de serina, su uso y una composicion farmaceutica que lo comprende

Info

Publication number
AR020922A1
AR020922A1 ARP990105310A ARP990105310A AR020922A1 AR 020922 A1 AR020922 A1 AR 020922A1 AR P990105310 A ARP990105310 A AR P990105310A AR P990105310 A ARP990105310 A AR P990105310A AR 020922 A1 AR020922 A1 AR 020922A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
alkyl
alkoxy
halogen
optionally substituted
Prior art date
Application number
ARP990105310A
Other languages
English (en)
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of AR020922A1 publication Critical patent/AR020922A1/es

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Classifications

    • 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • C07D237/34Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Un inhibidor de proteasas de serina que tiene la formula (1) donde: J es H, R1, R1-O-C(O)-, R1-C(O)-, R1-SO2-, R3OOC-(CHR2)p-, (R2a,R2b)N-CO-(CHR2)p- oHet-CO-(CHR2)p-; D es un amino-ácido de la formula -NH-CHR1-C(O)-, -NR4-CH[(CH2)qC(O)OR1]-C(O)-, -NR4-CH[(CH2)qC(O)N(R2a,R2b)]-C(O)-, -NR4-CH[(CH2)qC(O)Het]-C(O)-, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq o D-3-Piq; E es -NR2-CH2- o el fragmento (2), opcionalmente sustituido con alquilo C1-6, alcoxi C1-6 o benciloxi;R1 se selecciona entre alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-12 y cicloalquil C3-12-alquileno C1-6, cuyos grupos pueden estaropcionalmente sustituidos con cicloalquilo C3-12, alcoxi C1-6, oxo, OH, CF3 o halogeno, y entre arilo C6-14, aralquilo C7-15, aralquenilo C8-16 y(bisaril)alquilo C14-20, donde los grupo arilo pueden estar opcionalmente sustituidos con alquilo C1-6, cicloalquilo C3-12, alcoxi C1-6, OH, CF3 o halogeno;R2, R2a, y R2b son seleccionados cada uno independientemente entre H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8 y cicloalquil C3-6-alquileno C1-4, donde cada uno puede estar opcionalmente sustituido con cicloalquilo C3-6, alcoxi C1-6, CF3 o halogeno, y entre arilo C6-14 y aralquilo C7-15donde los grupos arilo pueden estar opcionalmente sustituidos con alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, CF3 o halogeno; R3 es como se definio para R2 oHet-alquilo C1-6; R4 es H o alquilo C1-3; X e Y son CH o N con la salvedad de que no sean ambos N; Het es un heterociclo de 4, 5 o 6 miembros que contiene unoo más heteroátomos seleccionados entre O, N y S; m es 1 o 2; p es 1, 2 o 3; q es 1, 2 o 3; t es 2, 3 o 4; o una prodroga; o una sal de adicion y/o solvatofarmacéuticamente aceptable del mismo y su uso enterapia; su uso para la fabricacion de un medicamento para tratar o prevenir enfermedades mediadas portrombina y asociadas con trombina; y una composicion farmacéutica que lo comprende.
ARP990105310A 1998-10-23 1999-10-21 Inhibidor de proteasas de serina, su uso y una composicion farmaceutica que lo comprende AR020922A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP98203559 1998-10-23

Publications (1)

Publication Number Publication Date
AR020922A1 true AR020922A1 (es) 2002-06-05

Family

ID=8234249

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990105310A AR020922A1 (es) 1998-10-23 1999-10-21 Inhibidor de proteasas de serina, su uso y una composicion farmaceutica que lo comprende

Country Status (24)

Country Link
US (1) US6903107B1 (es)
EP (1) EP1123280A1 (es)
JP (1) JP2002528438A (es)
KR (1) KR20010075648A (es)
CN (1) CN1146543C (es)
AR (1) AR020922A1 (es)
AU (1) AU763667B2 (es)
BR (1) BR9914694A (es)
CA (1) CA2346990A1 (es)
CO (1) CO5140114A1 (es)
CZ (1) CZ20011440A3 (es)
HU (1) HUP0103806A3 (es)
ID (1) ID29885A (es)
IL (1) IL142398A0 (es)
NO (1) NO20011966L (es)
NZ (1) NZ511067A (es)
PE (1) PE20001283A1 (es)
PL (1) PL347948A1 (es)
RU (1) RU2232760C2 (es)
SK (1) SK5372001A3 (es)
TR (1) TR200101120T2 (es)
TW (1) TW575567B (es)
WO (1) WO2000024718A1 (es)
ZA (1) ZA200102970B (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10046272A1 (de) * 2000-09-19 2002-03-28 Merck Patent Gmbh Aminoheterocyclen (Faktor Xa Inhibitoren 14)
US6924285B2 (en) 2002-03-30 2005-08-02 Boehringer Ingelheim Pharma Gmbh & Co. Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
GB0309850D0 (en) 2003-04-30 2003-06-04 Astrazeneca Ab Quinazoline derivatives
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
GB0326459D0 (en) 2003-11-13 2003-12-17 Astrazeneca Ab Quinazoline derivatives
US7632840B2 (en) 2004-02-03 2009-12-15 Astrazeneca Ab Quinazoline compounds for the treatment of hyperproliferative disorders
CN101213187B (zh) * 2005-06-28 2012-06-06 塞诺菲-安万特股份有限公司 作为rho-激酶抑制剂的异喹啉衍生物
WO2007012422A1 (en) 2005-07-26 2007-02-01 Sanofi-Aventis Cyclohexylamin isoquinolone derivatives as rho-kinase inhibitors
KR101373535B1 (ko) 2005-07-26 2014-03-12 사노피 Rho-키나제 억제제로서의 피페리디닐-치환된 이소퀴놀론유도체
TWI389899B (zh) 2006-08-08 2013-03-21 Msd Oss Bv 具口服活性之凝血酶抑制劑
EP1921070A1 (de) 2006-11-10 2008-05-14 Boehringer Ingelheim Pharma GmbH & Co. KG Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstelllung
AU2007338408B2 (en) * 2006-12-27 2012-07-26 Sanofi-Aventis Substituted isoquinoline and isoquinolinone derivatives
JP5405314B2 (ja) 2006-12-27 2014-02-05 サノフイ シクロアルキルアミン置換イソキノロン誘導体
CA2673920C (en) * 2006-12-27 2015-03-24 Sanofi-Aventis Cycloalkylamine substituted isoquinoline derivatives
ATE505458T1 (de) * 2006-12-27 2011-04-15 Sanofi Aventis Cycloalkylaminsubstituierte isochinolon- und isochinolinonderivate
RU2009128690A (ru) * 2006-12-27 2011-02-10 Санофи-Авентис (Fr) Новые замещенные производные изохинолина и изохинолинона
JP5318779B2 (ja) * 2006-12-27 2013-10-16 サノフイ シクロアルキルアミン置換イソキノリン及びイソキノリノン誘導体
MX2009005825A (es) * 2006-12-27 2009-06-16 Sanofi Aventis Derivados de isoquinolina e isoquinolinona sustituidos en calidad de inhibidores de rho-quinasa.
WO2008095847A1 (de) 2007-02-06 2008-08-14 Boehringer Ingelheim International Gmbh Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
AU2009211523B2 (en) 2008-02-07 2014-03-13 Boehringer Ingelheim International Gmbh Spirocyclic heterocycles, medicaments containing said compounds, use thereof and method for their production
JP5739802B2 (ja) 2008-05-13 2015-06-24 アストラゼネカ アクチボラグ 4−(3−クロロ−2−フルオロアニリノ)−7−メトキシ−6−{[1−(n−メチルカルバモイルメチル)ピペリジン−4−イル]オキシ}キナゾリンのフマル酸塩
SI2303846T1 (sl) * 2008-06-24 2015-08-31 Sanofi Substituirani izokinolini in izokinolinoni kot inhibitorji RHOP kinaze
PL2313374T3 (pl) * 2008-06-24 2014-03-31 Sanofi Sa 6-podstawione izochinoliny i izochinolinony
US8524737B2 (en) * 2008-06-24 2013-09-03 Sanofi Bi- and polycyclic substituted isoquinoline and isoquinolinone derivatives
CA2733153C (en) 2008-08-08 2016-11-08 Boehringer Ingelheim International Gmbh Cyclohexyloxy substituted heterocycles, pharmaceutical compositions containing these compounds and processes for preparing them
CN103946388A (zh) * 2011-06-28 2014-07-23 英伊布里克斯有限责任公司 Wap结构域融合多肽及其使用方法
WO2013003641A2 (en) 2011-06-28 2013-01-03 Inhibrx Llc Serpin fusion polypeptides and methods of use thereof
US10400029B2 (en) 2011-06-28 2019-09-03 Inhibrx, Lp Serpin fusion polypeptides and methods of use thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4473501A (en) 1981-05-04 1984-09-25 G. D. Searle & Co. Dihydro azino isoquinolines
GB8908229D0 (en) * 1989-04-12 1989-05-24 Smithkline Beckman Intercredit Compounds
HUP9901739A3 (en) * 1996-04-13 2000-06-28 Astrazeneca Ab Aminoisoquinolines and aminothienopyridine derivatives, process for producing thereof and pharmaceutical compositions containing them
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
WO1999047503A1 (fr) * 1998-03-19 1999-09-23 Ajinomoto Co., Inc. Derives d'aminoisoquinoleine

Also Published As

Publication number Publication date
AU763667B2 (en) 2003-07-31
US6903107B1 (en) 2005-06-07
AU6341399A (en) 2000-05-15
RU2232760C2 (ru) 2004-07-20
HUP0103806A2 (hu) 2002-02-28
NZ511067A (en) 2003-03-28
ID29885A (id) 2001-10-18
PL347948A1 (en) 2002-04-22
NO20011966L (no) 2001-04-23
TW575567B (en) 2004-02-11
BR9914694A (pt) 2001-07-10
TR200101120T2 (tr) 2001-08-21
CA2346990A1 (en) 2000-05-04
CZ20011440A3 (cs) 2001-09-12
CN1146543C (zh) 2004-04-21
CN1348444A (zh) 2002-05-08
KR20010075648A (ko) 2001-08-09
HUP0103806A3 (en) 2002-03-28
ZA200102970B (en) 2002-07-10
EP1123280A1 (en) 2001-08-16
IL142398A0 (en) 2002-03-10
WO2000024718A1 (en) 2000-05-04
CO5140114A1 (es) 2002-03-22
SK5372001A3 (en) 2001-11-06
JP2002528438A (ja) 2002-09-03
PE20001283A1 (es) 2000-11-20
NO20011966D0 (no) 2001-04-20

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