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 comprendeInfo
- 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
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
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.
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)
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)
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 |
-
1999
- 1999-10-04 TW TW88117079A patent/TW575567B/zh not_active IP Right Cessation
- 1999-10-19 JP JP2000578288A patent/JP2002528438A/ja not_active Withdrawn
- 1999-10-19 CN CNB998124966A patent/CN1146543C/zh not_active Expired - Fee Related
- 1999-10-19 PL PL99347948A patent/PL347948A1/xx unknown
- 1999-10-19 ID IDW20010914A patent/ID29885A/id unknown
- 1999-10-19 US US09/830,227 patent/US6903107B1/en not_active Expired - Fee Related
- 1999-10-19 AU AU63413/99A patent/AU763667B2/en not_active Ceased
- 1999-10-19 CA CA002346990A patent/CA2346990A1/en not_active Abandoned
- 1999-10-19 BR BR9914694-0A patent/BR9914694A/pt not_active IP Right Cessation
- 1999-10-19 HU HU0103806A patent/HUP0103806A3/hu unknown
- 1999-10-19 TR TR2001/01120T patent/TR200101120T2/xx unknown
- 1999-10-19 EP EP99950761A patent/EP1123280A1/en not_active Withdrawn
- 1999-10-19 WO PCT/EP1999/007928 patent/WO2000024718A1/en not_active Application Discontinuation
- 1999-10-19 RU RU2001113734/04A patent/RU2232760C2/ru not_active IP Right Cessation
- 1999-10-19 IL IL14239899A patent/IL142398A0/xx unknown
- 1999-10-19 KR KR1020017004938A patent/KR20010075648A/ko not_active Application Discontinuation
- 1999-10-19 CZ CZ20011440A patent/CZ20011440A3/cs unknown
- 1999-10-19 SK SK537-2001A patent/SK5372001A3/sk unknown
- 1999-10-19 NZ NZ511067A patent/NZ511067A/xx unknown
- 1999-10-21 AR ARP990105310A patent/AR020922A1/es unknown
- 1999-10-21 PE PE1999001065A patent/PE20001283A1/es not_active Application Discontinuation
- 1999-10-22 CO CO99067058A patent/CO5140114A1/es unknown
-
2001
- 2001-04-10 ZA ZA200102970A patent/ZA200102970B/en unknown
- 2001-04-20 NO NO20011966A patent/NO20011966L/no not_active Application Discontinuation
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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Legal Events
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FB | Suspension of granting procedure |