AR051698A1 - Derivados de pirrolo[3,2-d]pirimidin-4-ona como inhibidores de mieloperoxidasa - Google Patents
Derivados de pirrolo[3,2-d]pirimidin-4-ona como inhibidores de mieloperoxidasaInfo
- Publication number
- AR051698A1 AR051698A1 ARP050105071A ARP050105071A AR051698A1 AR 051698 A1 AR051698 A1 AR 051698A1 AR P050105071 A ARP050105071 A AR P050105071A AR P050105071 A ARP050105071 A AR P050105071A AR 051698 A1 AR051698 A1 AR 051698A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- alkyl
- optionally substituted
- incorporates
- optionally
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/12—Mucolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
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- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Junto con procesos para su preparacion, composiciones que ,los contienen y su uso terapéutico. Los compuesto son inhibidores de la enzima MPO y, por ello, son particularmente utiles en el tratamiento o la prevencion de trastornos neuroinflamatorios, trastornos cardiovasculares. Reivindicacion 1: Un compuesto de la formula (1) donde al menos uno de X e Y representa S y el otro representa O o S; L representa un enlace directo o alquileno C1-7, donde dicho alquileno incorpora opcionalmente un heteroátomo seleccionado de O, S(O)n y NR6 y dicho alquileno incorpora opcionalmente 1 o 2 enlaces dobles C-C, y dicho alquileno está opcionalmente sustituido con uno o varios sustituyentes seleccionados, de modo independiente, de OH, halogeno, CN y NR4R5, alquilo C1-6 y alcoxi C1-6, donde dicho alcoxi incorpora opcionalmente un carbonilo adyacente al O; n representa un numero entero 0, 1, o 2; R1 representa H o i) un anillo saturado o parcialmente insaturado de 3 a 7 miembros que opcionalmente incorpora 1 o 2 heteroátomos seleccionados, de modo independiente, de O, N y S, y que opcionalmente incorpora un grupo carbonilo, opcionalmente sustituido con 1 o varios sustituyentes seleccionados de halogeno, SO2R9, SO2NR9R10, OH, alquilo C1-7, alcoxi C1-7, CN, CONR2R3, NR2COR3 y COE3, donde dicho alcoxi está también opcionalmente sustituido con alcoxi C1-6 y donde dicho alcoxi incorpora opcionalmente un carbonilo adyacente al O y dicho alquilo está también opcionalmente sustituido con hidroxi o alcoxi C1-6 y dicho alquilo o alcoxi incorpora opcionalmente un carbonilo adyacente al O o en cualquier posicion en el anillo o ii) un sistema de anillos aromáticos seleccionado de fenilo, bifenilo, naftilo o una estructura de anillo heteroaromática monocíclica o bicíclica que contiene 1 a 3 heteroátomos seleccionados, de modo independiente, de O, N y S, donde dicho sistema e anillo aromático está opcionalmente sustituido con 1 o varios sustituyentes seleccionados de halogeno, SO2R9, SO2NR9R10, OH, alquilo C1-7, alcoxi C1-7, CN, CONR2R3, NR2COR3 y COR3; donde dicho alcoxi está también opcionalmente sustituido con alcoxi C1-6 y donde dicho alcoxi incorpora opcionalmente un carbonilo adyacente al O y dicho alquilo está también opcionalmente sustituido con hidroxi o alcoxi C1-6 y dicho alquilo o alcoxi incorpora un carbonilo adyacente al O o en cualquier posicion en el alquilo; R12 representa H o halogeno o un C opcionalmente sustituido con 1 a 3 átomos de halogeno; en cada aparicion R2, R3, R4, R5, R6, R9 y R10 representan, de modo independiente, H, alquilo C1-6 o alcoxi C1-6 donde dicho alcoxi incorpora un carbonilo adyacente al O, y dicho alquilo está también opcionalmente sustituido con halogeno, alcoxi C1-6, CHO, alcanoílo C2-6, OH, CONR7R8 y NR7COR8; o los grupos NR2R3, NR4R5 y NR9R10 representan cada uno, de modo independiente, un anillo azacíclico saturado e 5 a 7 miembros que opcionalmente incorpora un heteroátomo adicional seleccionado de O, S y NR11, donde dicho anillo está también opcionalmente sustituido con halogeno, alcoxi C1-6, CHO, alcanoílo C2-6, OH, CONR7R8 y NR7COR8; en cada aparicion R7, R8 y R11 representan, de modo independiente, H o alquilo C1-6, o el grupo NR7R8 representa un anillo azacíclico saturado de 5 a 7 miembros que opcionalmente incorpora un heteroátomo adicional seleccionado de O, S y NR11; y sus sales farmacéuticamente aceptables; con la condicion de que se excluyan los compuestos 1-beta-D- ribofuranosil-2-oxopirrolo[3,2-d]pirimidin-4(3H,5H)-tiona, 1-(2,3,5-tri-O-benzoil-1-beta-D-ribofuranosil)-2-oxopirrolo[3,2-d]pirimidin-4(3H,5H)-tiona y 5,7-dimercapto-1,4,6-triazaindeno.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE0402972A SE0402972D0 (sv) | 2004-12-06 | 2004-12-06 | Novel compounds |
SE0501093 | 2005-05-13 |
Publications (1)
Publication Number | Publication Date |
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AR051698A1 true AR051698A1 (es) | 2007-01-31 |
Family
ID=36578191
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050105071A AR051698A1 (es) | 2004-12-06 | 2005-12-05 | Derivados de pirrolo[3,2-d]pirimidin-4-ona como inhibidores de mieloperoxidasa |
Country Status (30)
Country | Link |
---|---|
US (3) | US7829707B2 (es) |
EP (1) | EP1824855B1 (es) |
JP (1) | JP5028270B2 (es) |
KR (3) | KR101412786B1 (es) |
CN (1) | CN101072778B (es) |
AR (1) | AR051698A1 (es) |
AU (1) | AU2005312388B2 (es) |
BR (1) | BRPI0518846B1 (es) |
CA (1) | CA2591314C (es) |
CY (1) | CY1113209T1 (es) |
DK (1) | DK1824855T3 (es) |
ES (1) | ES2390888T3 (es) |
HK (1) | HK1110859A1 (es) |
HR (1) | HRP20120781T1 (es) |
IL (1) | IL183182A (es) |
ME (1) | ME01486B (es) |
MX (1) | MX2007006497A (es) |
MY (1) | MY140748A (es) |
NO (1) | NO20072399L (es) |
NZ (1) | NZ555046A (es) |
PL (1) | PL1824855T3 (es) |
PT (1) | PT1824855E (es) |
RS (1) | RS52490B (es) |
RU (2) | RU2409578C2 (es) |
SA (1) | SA05260385B1 (es) |
SI (1) | SI1824855T1 (es) |
TW (1) | TWI365189B (es) |
UA (1) | UA89968C2 (es) |
UY (1) | UY29246A1 (es) |
WO (1) | WO2006062465A1 (es) |
Families Citing this family (57)
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AR039385A1 (es) | 2002-04-19 | 2005-02-16 | Astrazeneca Ab | Derivados de tioxantina como inhibidores de la mieloperoxidasa |
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TW200806667A (en) * | 2006-04-13 | 2008-02-01 | Astrazeneca Ab | New compounds |
TW200804383A (en) | 2006-06-05 | 2008-01-16 | Astrazeneca Ab | New compounds |
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GB201021992D0 (en) | 2010-12-23 | 2011-02-02 | Astrazeneca Ab | Compound |
GB201021979D0 (en) | 2010-12-23 | 2011-02-02 | Astrazeneca Ab | New compound |
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US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
CN109912594A (zh) | 2013-04-19 | 2019-06-21 | 因赛特控股公司 | 作为fgfr抑制剂的双环杂环 |
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US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
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