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AR043190A1 - Derivados de quinoleina como inhibidores del factor inhibidor de la migracion de macrofagos y metodos para su identificacion. sintesis y composiciones farmaceuticas. - Google Patents

Derivados de quinoleina como inhibidores del factor inhibidor de la migracion de macrofagos y metodos para su identificacion. sintesis y composiciones farmaceuticas.

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Publication number
AR043190A1
AR043190A1 ARP040100472A ARP040100472A AR043190A1 AR 043190 A1 AR043190 A1 AR 043190A1 AR P040100472 A ARP040100472 A AR P040100472A AR P040100472 A ARP040100472 A AR P040100472A AR 043190 A1 AR043190 A1 AR 043190A1
Authority
AR
Argentina
Prior art keywords
substituted
heterocycloalkyl
aryl
heterocycle
acylalkyl
Prior art date
Application number
ARP040100472A
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English (en)
Inventor
Wenbin Ying
Jagadish Sircar
Kumar K C Sunil
Original Assignee
Avanir Pharmaceuticals
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Filing date
Publication date
Application filed by Avanir Pharmaceuticals filed Critical Avanir Pharmaceuticals
Publication of AR043190A1 publication Critical patent/AR043190A1/es

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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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
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  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
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  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

La presente se refiere a derivados de quinoleina como inhibidores de l factor inhibidor de la migración de macrófagos y métodos para su identificación, síntesis y composiciones farmacéuticas. También se incluyen compuestos que contienen un inhibidor de FIM en combinación con un vehículo farmacéuticamente adecuado, así, como también los métodos de uso de los mismos. Reivindicación 1: Un compuesto con la estructura (1) o un estereoisómero, prodroga o sal farmacéuticamente aceptable del mismo, en el cual: X es O o S; Z es -CH2- o -C(=O)-; n es 0, 1 o 2, con la salvedad de que cuyo n es 0, Z es -C(=O)-; R1 se selecciona del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilo, sustituido, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, dialquilo y R´R"N(CH2)x- donde x es 2 a 4 y donde R´ y R" son independientemente seleccionados del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo o heterocicloalquilo sustituido y dialquilo; R2 y R3 son independientemente seleccionados del grupo que consiste en halógeno, -R5, -OR5, -SR5 o -NR5R6; R4 es seleccionado del grupo que consiste en -CH2R7, -C(=O)NR5R6-, -C(=O)OR7, -C(=O)R7 y R8; C(=O)OR7; y como se muestra en los restos de fórmulas (2); R5 y R6 son seleccionados independientemente del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, arilo, arilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, dialquilo, y R´R"N(CH2)x-, donde x es 2 a 4, y donde R´ y R" se seleccionan independientemente del grupo compuesto por H, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, arilo, arilo sustituido, acilalquilo,. acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, dialquilo; o R5 y R6 tomados juntos con un átomo de N al cual están unidos forman un heterociclo o heterociclo sustituido; R7 se selecciona del grupo que consiste en alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, heterocicloaril, heterocicloaril sustituido, dialquilo, y R¨R"N(CH2)x-, donde x es 2 a 4, y donde R´ y R" son seleccionados independientemente del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, heterocicloarilo, heterocicloarilo sustituido y dialquilo; y R8 se selecciona del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, heterocicloaril, heterocicloaril sustituido, dialquilo, y R´R"N(CH2)x-, donde x es 2 a 4, y donde R´ y R" son seleccionados independientemente del grupo que consiste en H, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, acilalquilo, acilalquilo sustituido, acilarilo, acilarilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, heterocicloarilo, heterocicloarilo sustituido y dialquilo.
ARP040100472A 2003-02-14 2004-02-16 Derivados de quinoleina como inhibidores del factor inhibidor de la migracion de macrofagos y metodos para su identificacion. sintesis y composiciones farmaceuticas. AR043190A1 (es)

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US (7) US7173036B2 (es)
EP (1) EP1594501A4 (es)
JP (1) JP2006517977A (es)
KR (1) KR20050106430A (es)
CN (1) CN1750823A (es)
AR (1) AR043190A1 (es)
AU (1) AU2004213408A1 (es)
BR (1) BRPI0407424A (es)
CA (1) CA2514862A1 (es)
CL (1) CL2008001813A1 (es)
CO (1) CO5640090A2 (es)
EC (1) ECSP056020A (es)
HR (1) HRP20050733A2 (es)
MX (1) MXJL05000031A (es)
MY (1) MY142846A (es)
NO (1) NO20054218L (es)
PE (1) PE20050274A1 (es)
PL (1) PL378113A1 (es)
RU (1) RU2005128190A (es)
TW (1) TW200418829A (es)
UY (1) UY28187A1 (es)
WO (1) WO2004074218A2 (es)
ZA (1) ZA200507170B (es)

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