AR043528A1 - Inhibidores de citoquinas - Google Patents

Inhibidores de citoquinas

Info

Publication number
AR043528A1
AR043528A1 ARP040100759A ARP040100759A AR043528A1 AR 043528 A1 AR043528 A1 AR 043528A1 AR P040100759 A ARP040100759 A AR P040100759A AR P040100759 A ARP040100759 A AR P040100759A AR 043528 A1 AR043528 A1 AR 043528A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
acyl
heterocycle
alkoxy
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
ARP040100759A
Other languages
English (en)
Inventor
Neil Moss
Mark Stephen Ralph
Ming Hong Hao
Zhaoming Xiong
Pier Francesco Cirillo
Donghong A Gao
Daniel R Goldberg
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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 Boehringer Ingelheim Pharma GmbH Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR043528A1 publication Critical patent/AR043528A1/es
Pending legal-status Critical Current

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    • 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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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    • A61P25/16—Anti-Parkinson drugs
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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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    • A61P25/24—Antidepressants
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    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Toxicology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
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Abstract

La presente se refiere a compuestos que inhiben la producción de las citoquinas involucradas en procesos inflamatorios y, por ende, son útiles para el tratamiento de enfermedades y estados patológicos que comprenden inflamaciones tales como enfermedad inflamatoria crónica. También se describen procesos para preparar estos compuestos y composiciones farmacéuticas que comprenden estos compuestos. Reivindicación 1: Un compuesto de fórmula (1) en el cual: Ar1 es un carbociclo aromático sustituido con un R1, y en donde Ar1 está sustituido, de modo independiente, con dos grupos R2 y en donde un R1 y un R2 en átomos adyacentes del anillo forman opcionalmente un anillo carbocíclico o heterocíclico de 5 o 6 miembros; R1 es halógeno, NO2, NH2, J-N(Ra)-(CH2)m-, N(J)2-(CH2)m-, NH2C(O)-, J-N(Ra)-C(O)-, J-S(O)m-N(Ra)-, J-N(Ra)-S(O)m- o heterociclo-(CH2)m- en donde el grupo heterocíclico está opcionalmente sustituido con alquilo C1-5; Q es un N o CRp; Y es >CRpRv, -CRp=C(Rv)-, -O-, -N(Rx)- o >S(O)m; en donde Ra, Rp, Rv, Rx y Ry son cada uno, de modo independiente, H o alquilo C1-5; X es -CH2-, -N(Ra)-, -O- o -S-; W es N o CH; cada m es, de modo independiente, 0, 1 o 2; J se selecciona entre alquilo C1-10 y carbociclo cada uno opcionalmente sustituido con Rb; R2 se selecciona entre alquilo C1-6, cicloalquilo C3-7 opcionalmente sustituido con alquilo C1-5, acilo C1-4, aroilo, alcoxi C1-4, estando cada uno parcial o totalmente halogenado de forma opcional, halógeno, alcoxicarbonilo C1-6, carbociclosulfonilo y -SO2-CF3; cada R3, R4 y R5 se selecciona, de modo independiente, de H, alquilo C1-6 y halógeno; R6 está opcionalmente unido en una posición orto o meta al átomo de N del anillo indicado, y se selecciona de un enlace, -O-, -O-(CH2)1-5-, >C(O), -NH-, -C(O)-NH-, -S-, alquilo C1-5 ramificado o no ramificado, alquenilo C2-5, acilo C1-3, alquil C1-3(OH), heterociclo seleccionado de morfolinilo, piperazinilo, piperidinilo, pirrolidinilo y tetrahidrofuranilo, heteroarilo seleccionado de piridinilo, pirimidinilo, pirazinilo, piridazinilo, pirrolilo, imidazolilo, pirazolilo, tienilo, furilo, isoxazolilo, tiazolilo, oxazolilo e isotiazolilo o arilo cada alquilo, alquenilo, acilo, heterociclo, heteroarilo y arilo están opcionalmente sustituidos con uno a tres hidroxi, oxo, alquilo C1-3, alcoxi C1-3, alcoxicarbonilo C1-5, -NR7R8 o NR7R8-C(O)-; en donde cada R6 también está unido opcionalmente de modo covalente a grupos seleccionados de: H, -NR7R8, alquilo C1-3, cicloalquil-C3-6-alquilo C0-2, hidroxi, alcoxi C1-3, fenoxi, benciloxi, arilalquilo C0-4, heteroarilalquilo C0-4 y heterociclo-alquilo C0-4, cada grupo heterociclo, heteroarilo y arilo antes enumerado está opcionalmente sustituido con uno a tres hidroxi, oxo, alquilo C1-4, alcoxi C1-3, alcoxicarbonilo C1-5, NR7R8-C(O)- o acilo C1-4; cada R7 y R8 es, de modo independiente, H, fenilalquilo C0-3 opcionalmente sustituido con halógeno, alquilo C1-3 o dialquilamino C1-5, o R7 y R8 son acilo C1-2, benzoilo o alquilo C1-5 ramificado o no ramificado opcionalmente sustituido con alcoxi C1-4, hidroxi o mono o dialquilamino C1-3; y Rb se selecciona entre H, alquilo C1-5, hidroxialquilo C1-5, alquenilo C2-5, alquinilo C2-5,carbociclo, heterociclo, heteroarilo, alcoxi C1-5, alquiltio C1-5, amino, alquilamino C1-5, dialquilamino C1-5, acilo C1-5, alcoxicarbonilo C1-5, aciloxi C1-5, acilamino C1-5, cada uno de los antes mencionados están opcionalmente halogenados en forma parcial o total, o Rb se selecciona entre alquilsulfonilamino C1-5, hidroxi, oxo, halógeno, nitro y nitrilo; o sus sales, ácidos, ésteres o isómeros farmacéuticamente aceptables.
ARP040100759A 2003-03-10 2004-03-10 Inhibidores de citoquinas Pending AR043528A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US45336403P 2003-03-10 2003-03-10

Publications (1)

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AR043528A1 true AR043528A1 (es) 2005-08-03

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US (2) US7078419B2 (es)
EP (1) EP1631567A2 (es)
JP (1) JP4954701B2 (es)
KR (1) KR101084961B1 (es)
CN (2) CN101239972A (es)
AR (1) AR043528A1 (es)
AU (1) AU2004264409B2 (es)
BR (1) BRPI0408228A (es)
CA (1) CA2518774C (es)
CL (1) CL2004000469A1 (es)
IL (1) IL170740A (es)
MX (1) MXPA05009554A (es)
MY (2) MY149577A (es)
NZ (1) NZ542775A (es)
PE (1) PE20050308A1 (es)
RU (2) RU2394029C2 (es)
TW (1) TWI369354B (es)
UY (1) UY28222A1 (es)
WO (1) WO2005016918A2 (es)
ZA (1) ZA200506242B (es)

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US7335657B2 (en) 2008-02-26
US20040186114A1 (en) 2004-09-23
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US20060235017A1 (en) 2006-10-19
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CA2518774A1 (en) 2005-02-24
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