CO5140114A1 - Derivados de aminoisoquinolina - Google Patents

Derivados de aminoisoquinolina

Info

Publication number
CO5140114A1
CO5140114A1 CO99067058A CO99067058A CO5140114A1 CO 5140114 A1 CO5140114 A1 CO 5140114A1 CO 99067058 A CO99067058 A CO 99067058A CO 99067058 A CO99067058 A CO 99067058A CO 5140114 A1 CO5140114 A1 CO 5140114A1
Authority
CO
Colombia
Prior art keywords
cycloalkyl
alkyl
carboxylic acid
alkoxy
optionally substituted
Prior art date
Application number
CO99067058A
Other languages
English (en)
Inventor
Bernardus Maria Rewin Johannes
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 CO5140114A1 publication Critical patent/CO5140114A1/es

Links

Classifications

    • 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
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen 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

Inhibidor de proteasas de serina CARACTERIZADO porque tiene la fórmula (I),<EMI FILE="99067058_1" ID="1" IMF=JPEG >Donde J es H, R1, R1-O-C(O)-, R1-C(O)-, R1-SO2-, R3OOC-(CHR2)p-, (R2a, R2b)N-CO-(CHR2)p- ó Het-CO-(CHR2)p-;D es un amino-ácido de la fórmula -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)-, ácido 1,2,3,4-tetrahidroisoquinolina-l-carboxílico, ácido 1,2,3,4-tetrahidroisoquinolina-3-carboxílico, ácido 2-aminotetralina-2-carboxílico, ácido 2-aminoindan-2-carboxílico, ácido perhidroisoquinolil-3-carboxílico ó ácido perhidroisoquinolil-3-carboxílico;E es -NR2-CH2- ó el fragmento(CH2)t-N CH-, opcionalmente sustituido con (1-6C)alquilo, (1-6C)alcoxi o benciloxi;R1 se selecciona entre (1-12C)alquilo, (2-12C)alqueniIo, (2-12C)alquinilo, (3-12C)cicloalquilo y (3-12C)cicloalquil-(1-6C)alquileno, cuyos grupos pueden estar opcionalmente sustituidos con (3-12-C)cicloalquiIo, (1-6C)alcoxi, oxo, OH,CF3 ó halógeno, y entre (6-14C)arilo, (7-15C) aralquilo, (8-16C)aralquenilo y (14-20C)(bisaril)alquilo, donde los grupos arilo pueden estar opcionalmente sustituidos con (1-6C)alquilo, (3-12C)cicloalquilo, (1-6C)alcoxi, OH, CF3 ó halógeno;R2, R2a y R2b son seleccionados cada uno independientemente entre H, (1-8C)alquilo, (3-8C)alquenilo, (3-8C)alquinilo, (3-8C)cicloalquilo y (3-6C)cicloalquil (1-4C)alquileno, donde cada uno puede estar opcionalmente sustituido con (3-6C)cicloalquilo, (1-6C)alcoxi, CF3 ó halógeno, y entre (6-14C)arilo y (7-15C)aralquilo donde los grupos arilo pueden estar opcionalmente sustituidos con (1-6C)alquilo, (3-6C)cicloalquilo, (1-6C)alcoxi, CF3 ó halógeno; R3 es como se definió para R2 ó Het-(1-6C)alquilo;R4 es H ó ( 1-3C)alquilo;X e Y son CH ó N con la salvedad de que no sean ambos N;Het es un heterociclo de 4, 5 ó 6 miembros que contiene uno o más heteroátomos seleccionados entre O, N y S;m es 1 ó 2;p es 1, 2 ó 3;q es, 1, 2, ó 3; t es 2, 3 ó 4;o una prodroga;o una sal de adición y/o solvato farmacéuticcamente aceptable del mismo y su uso en terapia, y a la fabricación de un medicamento para tratar o prevenir enfermedades medidas por trombina y asociadas con trombina.
CO99067058A 1998-10-23 1999-10-22 Derivados de aminoisoquinolina CO5140114A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO5140114A1 true CO5140114A1 (es) 2002-03-22

Family

ID=8234249

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99067058A CO5140114A1 (es) 1998-10-23 1999-10-22 Derivados de aminoisoquinolina

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
AU2003302238A1 (en) 2002-12-03 2004-06-23 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
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
CN1914182B (zh) 2004-02-03 2011-09-07 阿斯利康(瑞典)有限公司 喹唑啉衍生物
CA2611295C (en) 2005-06-28 2014-04-22 Sanofi-Aventis Isoquinoline derivatives as inhibitors of rho-kinase
AU2006274246B2 (en) * 2005-07-26 2012-07-12 Sanofi-Aventis Cyclohexylamin isoquinolone derivatives as Rho-kinase inhibitors
EP1910333B1 (en) 2005-07-26 2013-05-22 Sanofi Piperidinyl-substituted isoquinolone derivatives as rho-kinase inhibitors
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
DE602007013295D1 (de) 2006-12-27 2011-04-28 Sanofi Aventis Substituierte isochinoline und ihre verwendung als rho-kinase-inhibitoren
EP2125746B1 (en) 2006-12-27 2012-04-18 Sanofi Cycloalkylamine substituted isoquinoline derivatives
EP2125745B1 (en) * 2006-12-27 2017-02-22 Sanofi Cycloalkylamine substituted isoquinolone derivatives
BRPI0720986A2 (pt) * 2006-12-27 2014-03-11 Sanofi Aventis Derivados de isoquinolina e isoquinolinona substituídos
RS51655B (en) * 2006-12-27 2011-10-31 Sanofi-Aventis Isoquinoline derivatives and isoquinolinone derivatives substituted by cycloalkylamine
BRPI0720710A2 (pt) * 2006-12-27 2014-12-23 Sanofi Aventis Derivados de isoquinolona e isoquinolinona substituídos com cicloalquilamina
CA2673916C (en) * 2006-12-27 2015-02-17 Sanofi-Aventis Substituted isoquinolone and isoquinolinone derivatives as inhibitors of rho-kinase
EA200901041A1 (ru) 2007-02-06 2010-02-26 Бёрингер Ингельхайм Интернациональ Гмбх Бициклические гетероциклы, содержащие эти соединения лекарственные средства, их применение и способ их получения
WO2009098061A1 (de) 2008-02-07 2009-08-13 Boehringer Ingelheim International Gmbh Spirocyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2009138781A1 (en) 2008-05-13 2009-11-19 Astrazeneca Ab Fumarate salt of 4- (3-chloro-2-fluoroanilino) -7-methoxy-6- { [1- (n-methylcarbamoylmethyl) piperidin- 4-yl] oxy}quinazoline
JP5713893B2 (ja) * 2008-06-24 2015-05-07 サノフイ Ｒｈｏ−キナーゼ阻害剤としての置換イソキノリン類及びイソキノリノン類
MX2010013867A (es) * 2008-06-24 2011-02-24 Sanofi Aventis Derivados de isoquinolina e isoquinolinona bi- y policiclicos sustituidos.
JP5714485B2 (ja) * 2008-06-24 2015-05-07 サノフイ ６−置換イソキノリン類及びイソキノリノン類
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
IN2013MN02441A (es) * 2011-06-28 2015-06-12 Inhibrx Llc
KR20140068861A (ko) * 2011-06-28 2014-06-09 인히브릭스 엘엘씨 Wap 도메인 융합 폴리펩티드 및 이의 이용 방법
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
CN1221407A (zh) * 1996-04-13 1999-06-30 英国阿斯特拉药品有限公司 氨基异喹啉和氨基噻吩并吡啶衍生物及其作为抗炎剂的用途
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
ZA200102970B (en) 2002-07-10
AU763667B2 (en) 2003-07-31
NO20011966D0 (no) 2001-04-20
CN1348444A (zh) 2002-05-08
JP2002528438A (ja) 2002-09-03
HUP0103806A2 (hu) 2002-02-28
BR9914694A (pt) 2001-07-10
CA2346990A1 (en) 2000-05-04
KR20010075648A (ko) 2001-08-09
WO2000024718A1 (en) 2000-05-04
IL142398A0 (en) 2002-03-10
EP1123280A1 (en) 2001-08-16
TR200101120T2 (tr) 2001-08-21
HUP0103806A3 (en) 2002-03-28
AR020922A1 (es) 2002-06-05
RU2232760C2 (ru) 2004-07-20
ID29885A (id) 2001-10-18
PL347948A1 (en) 2002-04-22
TW575567B (en) 2004-02-11
PE20001283A1 (es) 2000-11-20
CZ20011440A3 (cs) 2001-09-12
US6903107B1 (en) 2005-06-07
CN1146543C (zh) 2004-04-21
SK5372001A3 (en) 2001-11-06
NO20011966L (no) 2001-04-23
AU6341399A (en) 2000-05-15
NZ511067A (en) 2003-03-28

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