PE20001283A1 - Inhibidor de la proteasa de serina - Google Patents

Inhibidor de la proteasa de serina

Info

Publication number
PE20001283A1
PE20001283A1 PE1999001065A PE00106599A PE20001283A1 PE 20001283 A1 PE20001283 A1 PE 20001283A1 PE 1999001065 A PE1999001065 A PE 1999001065A PE 00106599 A PE00106599 A PE 00106599A PE 20001283 A1 PE20001283 A1 PE 20001283A1
Authority
PE
Peru
Prior art keywords
cycloalkyl
alkyl
het
formula
chr2
Prior art date
Application number
PE1999001065A
Other languages
English (en)
Inventor
Cornelis Marius Timmers
Johannes Bernardus Maria Rewinkel
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 PE20001283A1 publication Critical patent/PE20001283A1/es

Links

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

SE REFIERE A DERIVADOS DE QUINOLINA DE FORMULA I, DONDE: J ES H, R1, R1-O-CO-, R1-CO-, R1-SO2, R3OOC-(CH2)p-, (R2a,R2b)N-CO-(CHR2)p-, HET-CO-(CHR2)p; D ES UN AMINOACIDO DE FORMULA -NH-CHR1-CO-, -NR4-CH[(CH2)qC(O)OR1]-CO, -NR4-CH[(CH2)qCON(NR2aR2b)]-CO-, ENTRE OTROS; E ES -NR2-CH2-, UN GRUPO a OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6, ALCOXI C1-C6, BENCILOXI; R1 ES ALQUILO C1-C12, ALQUENILO C2-C12, ALQUINILO C2-C12, CICLOALQUILO C3-C12, (CICLOALQUILO C3-C12)-(ALQUILENO C1-C6) OPCIONALMENTE SUSTITUIDOS CON CICLOALQUILO C3-C12, ALCOXI C1-C6, OXO, OH, ENTRE OTROS; R2, R2a Y R2b SON H, ALQUILO C1-C8, ALQUENILO C3-C8, ALQUINILO C3-C8, CICLOALQUILO C3-C6, (CICLOALQUILO C3-C6)(ALQUILENO C1-C4); R3 ES R2 O HET-ALQUILO C1-C6; R4 ES H, ALQUILO C1-C3; X e Y SON CH o N CON LA CONDICION QUE AMBOS NO SON N; HET ES UN HETEROCICLO DE 4-6 MIEMBROS CON O, N Y S; m ES 1-2; p ES 1-3; q ES 1-3; t ES 2-4. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS DE FORMULA I SON INHIBIDORES DE LAS PROTEASAS DE SERINA, EN PARTICULAR INHIBIDOR DE LA TROMBINA POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE TROMBOSIS VENOSA PROFUNDA, EMBOLIA PULMONAR, TROMBOFLEBITIS, OCLUSION ARTERIAL
PE1999001065A 1998-10-23 1999-10-21 Inhibidor de la proteasa de serina PE20001283A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20001283A1 true PE20001283A1 (es) 2000-11-20

Family

ID=8234249

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999001065A PE20001283A1 (es) 1998-10-23 1999-10-21 Inhibidor de la proteasa de serina

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
AR020922A1 (es) 2002-06-05
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
NO20011966D0 (no) 2001-04-20

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FD Application declared void or lapsed